Technical Field [0001] The present invention relates to a novel isoxazoline-substituted benzamide compound and the salt thereof, and a pesticide characterized by containing the compound as an active ingredient. The pesticide in the present invention" means a pest controlling agent applied for harmful arthropodsln .. agricultural and horticultural field or livestock farming and hygienic field ¬(endo-parasiticides and ecto-parasiticides for mammals or birds as domesticfanimals or pets, or hygienic pest- or unpleasant pest-controlling agents for domestic or business use). In addition, agricultural chemicals in the present invention mean insecticides, acaricides (miticides), nematicides, herbicides and fungicides, and the like. Background Art [0002] Conventionally, as to isoxazoline-substituted benzoic acid amide compounds, the followings are known: a report of synthesis by use of solid phase synthesis of 4-(5-methy!-5-substituted pyrroiyl-4,5-dihydroisoxazole-3-yl) benzoic acid amide derivatives (see, Non-patent Document 1); 4-(5-pyrfdyl¬ 415-dihydroisoxazole-3-yi) benzoic acid amide derivatives have matrix metalloprotease and TNF-a inhibition activity, or the like, and can be used as an anti-inflammatory agent or a chondro-proteclive agent (see, Patent Document 1); 4-(5-substituted carbamoylmethyl-4,5-dihydroisoxazole-3-yl) benzoic acid amide derivatives, 3-(5-substituted carbamoylmethyl-5-substituted ajkyl¬ 4,5-dihydroisoxazole-3-yl) benzoic acid amide derivatives and 4-(5-substituted carbamoylmethy!-4,5-dihydroisoxazole-3-yl) benzamidine derivatives have platelet glycoprotein llb/Illa fibrinogen receptor complex competitive activity or factor Xa inhibition-activity or the like, and can be used as a thrombolysis agent or a therapeutic agent of thronbo-embolic disorder (see, for example Patent Documents 2-5), etc. In addition, it is known that other specific substituted isoxazoline compound can be used as a production intermediate of HIV protease inhibitors, or production intermediate of insecticides (see, for example'Patent Documents 6 and 7). However, there is no disclosure on 4-(5-substIFuted-5-substituted aryl¬ 1 4,5-dihydroisoxazole-3-yl)benzoic acid amide compounds according to the present invention, and further the usefulness thereof as a pesticide is not known at all. [0003] On the other hand, as, to 3-(4-substituted pheny!)-4,5-dihydroisoxazole derivatives, 5-substituted alkyl-3f,5-bis substituted phenyl-4,5-dihydroisoxazole derivatives (see, Patent Document 7), 3-alkoxyphenyl-5-substituted-5-phenyl¬4',5-dihydroisoxazole derivatives (see, Patent Document 8), 3-alkoxyphenyl¬5-substituted alkyl-5-substituted carbamoyl-4,5-dihydroisoxazole derivatives (see, Patent Document 9), 3-(4-halophenyl)-5-substituted-5-substituted phenyl¬4,5-dihydroisoxazole derivatives (see, Patent Documents 10 and Non-pafent Document 2), and 3-(4-nitrophenyl)-5-substituted -5-substituted phenyl¬4,5-dihydroisoxazole derivatives (see, patent Document 11 and Non-patent Document 3), etc. are known. However, 5-substituted alkyl-3,5-bis substituted phenyl-4,5-dihydroisoxazole derivatives that can be used as a production intermediate of the pesticides according to the present invention are not described in any documents and thus novel compounds. [0004] Further, as to 4-hydroxyiminomethyl benzoic acid amide derivatives, 4-hydroxyiminomethyl-N,N-dimethyl benzoic acid amide (see, Non-patent Document 4), 4-hydroxyiminomethyl benzoyl piperidine derivatives (see, Patent Documents 12 and 13), 4-hydroxyiminomethyl-N-bicycloalkyl benzoic acid amide derivatives (see, Patent Document 14), and 6-(hydroxyiminomethyl) pyridine-2-carboxamide derivatives (see, Non-patent Document 5), etc. are known. However, 4-hydroxyiminomethyl benzoic acid amide derivatives that can be used as a production intermediate of the pesticides according to the present invention are not described in any documents and thus novel compounds. [0005] In addition, as to haloalkenylbenzene derivatives, substituted 3,3,3-trifluoro-2-prope'nylbenzene derivatives (see, Non-patenf Documents 6-8), etc. are known. However, specific substituted haloalkenylbenzene derivatives that can be used as a production intermediate of the pesticides according to the present invention are not described in any documents and thus novel compounds. Patent Document 1: WO 01/070673 Pamphlet Patent Document 2: WO 96/038426 Pamphlet Patent Document 3: WO 97/023212 Pamphlet Patent Document 4: WO 95/014683 Pamphlet Patent Document 5: WO 97/048395 Pamphlet Patent Document 6: WO 99/014210 Pamphlet Patent Document 7: WO 04/018410 Pamphlet Patent Document 8: WO 95/024398 Pamphlet Patent Document 9: WO 98/057937 Pamphlet Patent Document 10: EP 0455052 A1 (1991) Patent Document 11: WO 2004/018410 Pamphlet Patent Document 12: WO 95/019773 Pamphlet Patent Document 13: WO 00/066558 Pamphlet Patent Document 14: WO 97/000853 Pamphlet Non-patent Document 1: J. Comb. Chem., vol. 6, p. 142 (2004) Non-patent Document 2: Synth. Commun, vol. 33, p. 4163 (2003) Non'-jpatent Document 3: Australian J. Chem., vol. 32, p. 1487 (1979) Non-patent Document 4: J. Chem. Soc. Perkin Trans, 1, p. 643 (1979) Non-patent Document 5: J. Org. Chem., vol. 35, p. 841 (1970) Non-patent Document 6: J. Org. Chem., vol. 24, p. 238 (1959) Non-patent Document 7: J. Am. Chem. Soc, vol. 101, p. 357 (1979) Non-patent Document 8: Bull. Chem. Soc. Jpn., vol. 69, p. 3273 (1996) Disclosure of Invention Problems to be solved by the invention [0006] Recently, pests acquire resistance by the use of pesticides such as insecticides or fungicides over long term, and thus control by the insecticides or fungicides that have been conventionally used becomes difficult. In addition, a part of known pesticides has a high toxicity, or some of them start to disturb native ecosystems due to long-term persistency. Under the circumstances, it is expected all the time to develop a novel pesticide having a low toxicity and a low persistency. Means for solving the problems [0007] The inventors have eagerly investigated in order to solve the above-mentioned problems, and as a result of it, they found that novel isoxazoline- substituted benzamide compounds of formula (I) are extremely useful compounds having excellent pest controlling activity, particularly insecticidal activity and acaricidal activity, and having little adverse affect on non-targeted beings such as mammals, fishes and useful insects, etc. Thus, the present invention has been accomplished. [0008] That is, the presentinvention relates to the following aspects (1) to (15): (1) An isoxazoline-substituted benzamide compound of formula (1) or a salt thereof: R3 0-N (Y)n ro7) \n ? (i) II W wherein A1, A2and A3 independently of one another are carbon atom or nitrogen atom, G isbenzene ring, nitrogen-containing 6-membered aromatic heterocyclic ring, furan ring, thiophene ring, or 5-membered aromatic heterocyclic ring containing two or more hetero atoms selected from oxygen atom, sulfur atom and nitrogen atom, W is oxygen atom or sulfur atom, X is halogen atom, cyano, nitro, azido, -SCN, -SF5, C.,-C6alkyl, Chalky ! arbitrarily substituted with R4, C3-C8cycloalkyl, C3-C8cycloalkyl arbitrarily substituted with R4, C2-C6alkenyi, C2-C6alkenyl arbitrarily substituted with R4, C3-C8cycloalkenyl, C3¬Cghalocycloalkenyl, C2-C6alkynyl, C2-C6alkynyl arbitrarily substituted with R4, -OH, -OR5, -OS02R5, -SH, -S(0)rR5, -N(R7)R6, -N=CHOR8, -N=C(R9)OR8, -CHO, -C(0)R9, -C(0)OR9, -C(0)SR9, -C(0)NHR10, -C(O)N(R10)R9, -C(S)OR9, -C(S)SR9, -C(S)NHR10, -C(S)N(R10)R9, -CH=NOR11, -C(R9)=NOR11, -S(0)2OR9, -S(0)2NHR1°, -S(O)2N(R10)R9, -Si(Ri3)(R14)R12, phenyl, phenyl substituted with (Z)p1, D-1 to D-60 or E-1 to E-49, when m is 2, 3, 4 or 5, each X may be identical with or different from each other, further, when two Xs are adjacent, the adjacent two Xs may form 5-membered or 6¬membered ring together with carbon atoms to which the two Xs are bonded by forming -CH2CH2CH2-, -CH2CH20-, -CH2OCH2-, -OCH20-s -CH2CH2S-, -CH2SCH2-, -CH2CH2N(R15)-, -CH2N(R15)CH2-, -CH2CH2CH2CH2-, -CH2CH2CH20-, -CH2CH20CH2-, -CH2OCH20-, -OCH2CH20-, -0CH2CH2S-, -CH2CH=CH-, -OCH=CH-, -SCH=CH-, -N(R15)CH=CH-, -OCH=N-, -SCH=N-, -N(R15)CH=N-, -N(R15)N=CH-, -CH=CHCH=CH-, -OCH2CH=CH-, -N=CHCH=CH-, -N=CHCH=N- or -N=CHN=CH-, in this case, hydrogen atoms bonded to each carbon atom forming the ring may be arbitrarily substituted with Z, further when the hydrogen atoms are substituted with two or more Zs at the same time, each Z may be identical with or different from each other, Y is halogen atom, cyano, nitro, kido, -SCN, -SF5f CrC6alkyl, Chalky! arbitrarily substituted with R4, C3-C8cycloaikyl, C3-C8cycloalkyl arbitrarily substituted with R4, -OH, -OR5, -OS02R5, -SH, -S(0)rR5| -NHR7, -N(R7)R6, -N=CHOR8, -N=C(R9)OR8, -C(0)NHR10, -C(O)N(R10)R9, -C(S)NHR10, -C(S)N(R10)R9, -Si(R13)(R14)R1'2, phenyl, phenyl substituted with (Z)p1) D-1 to D-60 or E-1 to E-49, when n is 2, 3 or 4, each Y may be identical with or different from each other, further, when two Ys are adjacent, the adjacent two Ys may form 5-membered or 6-¬membered ring together with carbon atoms to which the two Ys are bonded by forming -CH2CH2CH2-, -CH2CH20-, -CH2OCH2-, -OCH20-, -CH2CH2S-, -CH2SCH2-, -SCH2S-, -CH2CH2CH2CH2-, -CH2CH2CH20-, -CH2CH2OCH2-, -CH2OCH20-, -OCH2CH20-, -OCH2CH2S-, -SCH2CH2S-, -OCH=N- or -SCH=N-, in this case, hydrogen atoms bonded to each carbon atom forming the ring may be arbitrarily substituted with Z, further when the hydrogen atoms are substituted with two or more Zs at the same time, each Z may be identical with or different from each other, R1 and R2 independently of each other are hydrogen atom, cyano, 0,-C^alkyl, C r C12alkyl arbitrarily substituted with R16, C3-C12cycloalkyl, C3-C12cycloalkyl arbitrarily substituted with R16, C3-C12alkenyl, C3-C12aikenyl arbitrarily substituted with R16, C3¬C12cycloalkenyl, C3-C12halocycloalkenyl, C3-C12alkynyl, C3-C12alkynyl arbitrarily substituted with R16,-SR9, -S(0)2R9, -SN(R18)R17, -S(O)2N(R10)R9, -OH, -OR19, -NHR20, -N(R20)R19, -N=CHR19b, -N=C(R19b)R19a, -C(0)R9, -C(0)OR9, -C(0)SR9, ¬-C(O)N(R10)R9, -C(S)OR9, -C(S)SR9, -C(S)N(R10)R9, -C(=NR11)OR9, -C(=NR11)SR9, -C(=NR11)N(R10)R9, phenyl, phenyl substituted with (Z)p1, D-1 to D-4, D-6 to D-13, D¬15 to D-23, D-25 to D-37, D-39, D-40, D-42, D-45 to D-60, E-3 to E-9, E-23 to E-28, E-30, E-31, E-34 or E-45, or R1 and R2 together form =C(R2a)R1a, and further R1 and R2 together may form 3- to 8-membered ring together'with the nitrogen atom bonding them by forming C2-C7 alkylene chain, in. this case, the alkylene chain may contain one oxygen atom, sulfur atom or nitrogen atom, and may be arbitrarily substituted with halogen atom, C^C^Ikyl, CrC6haloalkyl, C^Cealkoxy (C1-C6)alkyl, CrC6alkoxy, formyl, CrC6alkylcarbonyl, CVCehaloalkylcarbonyl or C,-C6alkoxycarbonyl, R1a and R2a independently of each other are CrC12alkyl, C^C^haloalkyl, C3¬C12cycloalkyI, C3-C12alkenyl, C3-C12haloalkenyl, C3-C12alkynyi, C3-C12haloalkynyl, -SR9, -OR9, -N(R10)R9, phenyl, phenyl substituted with (Z)p1, or R1a and R2a together may form 5- or 6-membered ring together with the carbon atom bonding them by forming C4 or C5 alkylene chain or C4 or C5 alkenylene chain, in this case, the 5 alkylene chain and the alkenylene chain may contain one to three oxygen atoms, sulfur atoms or nitrogen atoms, -and may be arbitrarily substituted with halogen atom, CrC6alkyl, C.,-C6haloalkyl, C^Cealkoxy, CrC6haloalkoxy, CrC6alkylthio or C r Cghaloalkylthio, R3 is halogen atom, cyano, CrC6alkyl, CrC6alkyl arbitrarily substituted'with R4, C3¬CBcycloalkyl, C3-C6cycloalkyl arbitrarily substituted with R4, C3-C6alkenyl, C2¬C6alkenyl arbitrarily substituted with R4, C3-C6alkynyl, C2-C6alkynyl arbitrarily substituted with R4,-OR5, -S(0)rR5, -N(R10)R9, -CHO, -C(0)R9, -C(0)OR9, -C(0)SR9, ¬-C(0)NHR10, -C(O)N(R10)R9, -C(S)OR9, -C(S)SR9, -C(S)NHR10, -C(S)N(R10)R9, -CH=NOR11, -C(R9)=NOR11, -Si(R13)(R14)R12, -P(0)(OR21)2, phenyl, phenyl substituted with (Z)p1, D-1 to D-60 or E-1 to E-49, D-1jto D-60 are aromatic heterocyclic rings of the following formulae, respectively (Z)p3 (Z)p3 (Z)P3 (Z)P3 (Z)P2 N~i(Z)p5 ' N={ (Z)ps N~~i (Z)p5 J)D-l >&> U) D-2 D-3 ^> D-4 J3 D-5 R15^v>D-6 R15 X ^(Z)p3 D-7 (Z)p4 ^v° D-8 ^^N D-9 (Z)p4 ^V* D-10 ' (Z)p4/=K -^ysD-ll (Z)P4TT" ^^N D-12 (Z)p4 f h ^VN D-13 (Z)p3 H=\ ¬N V D-14 R15 J H ¬^ (Z)p4 D-15 R15 R15 (Z)p4 (Z)p4 /r-N' N-N N—^ ,7v yr-0 /7-N (Z)p4D-16 (Z)p4 'D-17 D-18 D-19 D-20 N->(Z)p4X SD-21 (Z)H /Ts x N D-22 (Z) -4 ^ S D-23 (Z)p3 /=K N ^ ¬ D-24 r Rj5 (Z)p 4 ?1\ N D-25 R15/7~ N ,™ Rj5 N "l \ m , (Z)P5 ?7~s (Z)p5 )T~N (Z)ps N={ D-26 D-27 D-28 D-29 D-30 7 -V* -^VS ' '^V D-31 D-32 D-33 (Z)ps (Z)p5 (Z)P4 >=N h=N ^—N ^ N N N D-36 D-37 D-38 '(Z)p4 R;5 (z)p5 (Z)p5 r--S N— / >=N ^ N N D-41 D-42 D-43 R15 N-N -V D-46 (Z)p5 A'°~iN D-34 R1S N-N N &V D-39 (z)p5 N=r{ N D-44 (Z)pS s ~^ ^VN D-35 R15 N-N N (Z>p5 D-40 R;S N-N N D-45 (Z)p2 (Z)p2 (Z)p3 (Z)P3 r^i (T% * ^N'(0)t N^, r^N (6). (Z)p2 D-47 D-48 D-49 D-50 D-51 (Z)p3 (Z)p3 (Z)p4 rT% ifN (*% a . - i° ^* ^ E-l E-2 E-3 E-4 E-5 , (0)r (0)r R23 R23 (R22)q2 'S—v /— S N—A r-N 0--A (R22)q3 (R22)q3 (R2)q3 (R^qS E-6 E-7 E-8 E-9 E-10 (R22)q2 (R22)q2 (R22)q2 (R°)q2 (* % r|-o o--v H-° r\~s o--v ^ ^ -0 A> A> R23 E-ll E-12 E-13 E-14 E-15 (R22)q2 (R22)q2 R23 (R )q2 (R22)q2 (R22)q2 /-•O r-N S-n r\-S S--A -v A> ^> A> -V R23 R23 E-16 JE-17 E-18 E-19 E-20 ^22, R23 (R )q4 ( I )q2 ' W /Ov ^\ r--S r--N ° /] ("^ ^ " f ° -V -V A^ A^ AN| R23 (R22)q4 (R22)q4 E-21 E-22 E-23 E-24 E-25 (0)r fX* f (0)rR» f% f XX XX X^ XX XX (R22)q4 (R22)q4 (R22)q4 E-26 E-27 E-28 E-29 E-30 10 M Ap -AV, A> A, J E-31 E-32 E-33 E-34 E-35 ^ R22)^ 3 (R22)q3 23 /A22 A^ A^22 AN0 A^a (R22)q3 (R )q3 R23 (R22)q3 E-36 E-37 E-38 E-39 E-40 A> ^ AP A\" Ail (R22)q3 (R22)q3 E-41 E-42 E-43 E-44 E-45 AN0 AVa A^ A^M . ¬ R23 (R2\3 (R2)q3 E-46 E-47 E-48 E-49 R4 is halogen atom, cyano, C3-C8cycloalkyl, C3-C8halocycloalkyl, -OH, -OR5, -SH, -S(0)rR5, -N(R10)R9, -N(R10)CHO, -N(R10)C(O)R9, -N(R10)C(O)OR9, -N(R10)C(O)SR9, -N(R10)C(S)OR9, -N(R10)C(S)SR9, -N(R10)S(O)2R9, -C(0)OR9, -C(O)N(R10)R9, -Si(R13)(R14)R12, phenyl, phenyl substituted with (Z)p1, Dr1 to D-60 or E-1 to E-49, R5 is CrC6alkyl, CrC6alkyl arbitrarily substituted with R24, C3-C8cycloalkyl, C3¬C8cycloalkyl arbitrarily substituted with R24, C2-C6alkenyl, C2-C6alkenyl arbitrarily substituted with R24, C3-C8cycloalkenyl, C3-C8halocycloaIkenyl, C3-C6alkynyl, C3¬C6alkynyl arbitrarily substituted with R24, phenyl, phenyl substituted with (Z)p1, D-1 to D-4, D-6 to D-13, D-15 to D-23, D-25 to D-35, D-39, D-40, D-42, D-45 to D-60, E-3 to E-9, E-23 to E-31, E-34 or E-45, R6 is CrC6alkyl, CrC6haloalkyl, C3-C6cycloalkyl C1-C4alkyl, CrC4alkoxy CrC4alkyl, CrC4alkylthio CrC4alkyl, phenythio C1-C4alkyl, phenylthio CrC4alkyl substituted with (Z)p1,cyano Chalky!, CrC6alkQxycarbonyl CrC4alkyl, C1-C6alkylaminocarbonyl C r C4alkyl, di(CrC6alkyl)aminocarbonyl CrC4alkyl, phenyl CrC4alkyl, phenyl CrC4alkyl substituted with (Z)p1, CrC4alkyj substituted with anyone of D-1 to D-60, CrC4alkyl substituted with any one of E-1 to E-49, C3-C6cycloalkyl, C3-C6alkenyl, C3¬C6haloalkenyl, C3-C6alkynyl, C3-C6haloalkynyl, -OH, CrC6alkylcarbonyloxy, C r C6alkylthio, C,-C6haloalkylthio, phenylthio, phenylthio substituted with (Z)p1, -SN(R18)R17, -S(0)2R9, -S(O)2N(R10)R9, -CHO, -C(0)R9, -C(0)0R9, -C(0)SR9, -C(0)NHR10, -C(O)N(R10)R9, -C(S)OR9, -C(S)SR9, -C(S)NHR10, -C(S)N(Rj°)R9, -C(0)C(0)R9, -C(0)C(0)OR9, -P(0)(OR21)2 or -P(S)(OR21)2, R7 is hydrogen atom, CrC6alkyl, CrC6haloalkyl, C3-C8cycloalkyl CrC6alkyl, C r C4alkoxy CrC4alkyl, CrC4 alkylthio CrC4alkyl, C3-C8cycloalkyl, C3-C6alkenyl, C3¬Cshaloalkenyl, C3-C6alkynyl, C3-C6haloalkynyl, -CHO, CrC6alkylcarbonyl, C r C6haloalkylcarbonyl or CVCgalkoxycarbonyl, or R7 together with R6 may form 3- to 7¬membered ring with the bonding nitrogen atom by forming C2-C6alkylene chain, in this case, the alkylene chain may contain one oxygen atom, sulfur atom or nitrogen atom, and may be arbitrarily substituted with halogen atom, CrC6alkyl or C r C6haloalkyl, R8 is CrC6alkyl, CrC6haloalkyl, C3-C6alkenyl, phenyl or phenyl substituted with (Z)p1, R9 is C,-C6alkyl, CrC6haloalkyl, C3-C6cycloalkyl CrC4alkyl, C,-C6alkoxy CrC4alkyl, C^Cghaloalkoxy CrC4alkyl, CrC6alkylthio CrC4alkyl, CrC6haloalkylthio CrC4alkyl, cyano C1-C6alkyl, phenyl CrC4alkyl, phenyl CrC4alkyl substituted with (Z)p1, Cf C4alkyl substituted with any one of D-1 to D-60, CrC4alkyl substituted with any one of E-1 to E-49, C3-C8cycloalkyl, C3-C8halocycloalkyl, C3-C6alkenyl, C3-C6haloalkenyl, C3-C6alkynyl, C3-C6haloalkynyl, phenyl, phenyl substituted with (Z)p1, D-1 to D-60 or E-1 to E-49, R10 is hydrogen atom, CrC6alkyi, CrC6haloalkyl, C3-C6cycloalkyl CrC4alkyl, C r C6alkoxy C^C^Ikyl, C^Cgalkylthio C^alkyl, cyano CrC6alkyl, C3-C6alkenyl or C3¬C6alkynyl, R10 together with R9 may form 3- to 7-membered ring with the atom bonding them by forming C2-C6alkylene chain, in this case, the alkylene chain may contain one oxygen atom, sulfur atom or nitrogen atom, and may be arbitrarily substituted with halogen atom, CrC6alkyl, C^Cealkoxy, formyl, CrC6alkylcarbonyl or CrC6alkoxycarbonyl, R11 is hydrogen atom, CrC6alkyl, CrC6haloalkyl, phenyl C^-C4alkyl, phenyl C r C4alkyl substituted with (Z)p1, C3-C6alker.yl, C3-C6haloalkenyl, C3-C6alkynyl, C3¬C6haloalkynyl, phenyl or phenyl that may be substituted with (Z)p1, R11 together with R3 may form 5- to 7-membered ring with the atom bonding them by forming C2¬C4alkylene chain, in this case, the alkylene chain may contain one oxygen atom, sulfur atom or nitrogen atom, and may be arbitrarily substituted with halogen atom or CrC6alkyl, R12 is CrC6alkyl, CrC6haloalkyI, phenyl or phenyl substituted with (Z)p1, R13 and R14 independently of each other are CrC6alkyl or CrC6haloalkyl, R15 is hydrogen atom, CrC6alkyl, CrC6haloalkyl, CrC6alkoxycarbonyl CrC4alkyl, C,-C6haloalkoxycarbonyl C^^alkyl, phenyl C^C^Ikyl, phenyl CrC4alkyl substituted-with (Z)p1, C3-C6alkenyl, C3-C6haloalkenyl, C3-C6alkynyl, C3-C6haIoalkynyl, C r C6alkoxy, CrC6alkoxycarbonyl, CrC6haloalkoxycarbonyl, phenyl or phenyl substituted with (Z)p1, further, in case where Z is present in an adjacent position of R15, the adjacent R15 and Z may form 6-membered ring together with the atom bonding them by forming -CH2CH2CH2CH2-, -CH=CH-CH=CH-, -N=CH-CH=CH-, -CH=N-CH=CH-, -CH=CH¬N=CH- or -CH=CH-CH=N-, in this case, hydrogen atoms bonded to each carbon atom forming the ring may be arbitrarily substituted with halogen atom, CrC4alkyl or C,-C4haloalkyl, R16 is halogen atom, cyano, nitro, C3-C8cycloalkyl, C3-C8halocycloalkyl, -OR25, -N(R26)R25, -SH, -S(0)rR27, -S02NHR29, -S02N(R29)R28, -CHO, -C(0)R28, -C(0)OH, -C(0)OR28, -C(0)SR28, -C(0)NHR29, -C(0)N(R29)R28, -C(S)NHR29, -C(S)N(R29)R28, -C(0)C(0)OR28, -C(R31)=NOH, -C(R31)=NOR30, -C(=NR31)OR30, -C(=NR31)SR30, -C(=NR31)N(R29)R30,rC(=NOR31)NHR29,-C(=NOR31)N(R29)R30,-Si(R13)(R14)R12, -P(0)(OR21)2, -P(S)(OR21)2, -P(phenyl)2,-P(0)(phenyl)2, phenyl, phenyl substituted with (Z)p1I D-1 to D-60, E-1 to E-49 or M-1 to M-22, M-1 to M-22 are partially saturated heterocyclic rings of the following formulae, respectively J^ ^> ^A> A\0 ^N (R22)q2 ~ -(R2 % CR22),! M-l M-2 M-3 M-4 M-5' (Z)p5 ^22, (Z)p5 (Z)p5 (Z)p5 (Z)p5 V=N ^ )qlr^( N=K 0_^ N=rf ^ON^ Ri5^>> ^l^O X\ N ^/^ST (R22)ql ^i5 (R22)qi (R22)qi (R22)qi M-6 M-7 M-8 M-9 M-10 i^ r> J7* J^ ft? --^\N A^N >/> -Ao-N ^ V (R22)ql (Z)p5 (R^ql (R22)q2 M-ll M-12 M-13 M-14 M-15 (Z)p5 (Z)p5 (Z)p5 >/i ^ AV >/J ^ ¬ (R22)q2 , (R^qZ (^ V (R22)q2 (R22)q2 M-16 M-17 M-18 M-19 M-20 (f)p5 O^Y(Z)p5 O^N (R22)ql (R22)ql M-21 M-22 R17 is CrC12alkyl, CrC12haloalkyl, CrC12alkoxy C.,-C12alkyl, cyano CrC12alkyl, Cn¬C12alkoxycarbonyl CrC12alkyl, phenyl CrC4alkyl, phenyl CrC4alkyl substituted with (Z)p1l C3-C12alkenyl, C3-C12haloalkenyl, C3-C12alkynyl, C3-C12haloalkynyl, C r C12alkylcarbonyl, C^C^alkoxycarbonyl, -C(0)ON=C(CH3)SCH3) ¬C(0)ON=C(SCH3)C(0)N(CH3)2, phenyl or phenyl substituted with (Z)p1, R18 is CrC12alkyl, CrC12haloalkyl, C^C^alkoxy CrC12alkyl, cyano C1-C12alkyl, CrC12alkoxycarbonyl CrC12alkyj, phenyl CrC4alkyl, phenyl CrC4alkyl substituted with (Z)p1l C3-C12a!keny!, C3-C12haloalkenyl, C3-C12alkynyl, C3-C12haloalkynyl, phenyl or phenyl substituted with (Z)^ or R1S together with R17 may form 5- to 8-membered ring with the nitrogen atom bonding them by forming C4-C7alkylene chain, in this case, the alkylene chain may contain one oxygen atom or sulfur atom, and may be arbitrarily substituted with CrC4alkyl or CrC4alkoxy, R19 is hydrogen atom, CrC6alkyl, CrC6alkyl arbitrarily substituted with R16, C3¬C8cycloalkyl, C3-C8halocycloalkyl, C3-C6alkenyl, C3-C6haloalkenyl, C3-Qalkynyl, C3¬C6haloalkynyl, -CHO, -C(0)R28, -C(0)OR28, -C(0)SR28, -C(0)NHR29, -C(0)N(R29)R28, -C(S)NHR29, -C(S)N(R29)R28, -S(0)2R28, -S(0)2NHR29, -S(0)2N(R29)R28, -P(0)(0R21)2, -P(S)(OR?1)2, phenyl, phenyl substituted with (Z)p1, D-1 to D-13, D-15 to D-25, D-30 to D-37, D-39, D-40, D-42, D-45 to D-60, E-5, E-7, E-9, E-24, E-25, E-27, E-28, E-30 orE-31, R19a is CrC6alkyl, C1-C6haloalkyl, CrC4alkoxy CrC4alkyl, CrC4alkylthio CrC4alkyl, CrC4alkylsulfonyl CrC4alkyl, CrC4alkoxycarbonyl CrC4alkyl, phenyl CrC4alkyl, phenyl CrC4alkyl substituted with (Z)p1, C3-C6cycloalkyl, phenyl, phenyl substituted with (Z)p1, D-1 to D-60 or E-1 to E-49, R19b is hydrogen atom or CrC6alkyl, or R19a together with R19b may form 4- to 6¬membered ring with the carbon atom bonding them by forming C3-C5alkylene chain, in this case, the alkylene chain may contain one oxygen atom, sulfur atom or nitrogen atom, and may be arbitrarily substituted with CrC6alkyl, formyl, Cr C6alkylcarbonyl or CvC6alkoxycarbonyl, R20 is hydrogen atom, C^Cgalkyl, C^Cghaloalkyl, CrC4alkoxy C1-C4alkyl, C r C4haloalkoxy CrC4alkyl, CrC4aIkylthio CrC4alkyl, CrC4haloalkylthio C^C.alkyl, C r C4alkylsulfonyl CrC4alkyl, CrC4haloalkylsulfonyl CrC4alkyl, cyano CrC6alkyl, C r C4alkoxycarbonyl CrC4alkyl, C2-C6alkenyl, C2-C6haloalkenyl, C3-C6alkynyl, C3¬C6haloalkynyl, -CHO, -C(0)R9, -C(0)OR9, -C(0)SR9, -C(S)OR9, -C(S)SR9, C r C6alkylsulfonyI or CrC6haloalkylsulfonyl, R21 is C^Cealkyl or CrC6haloalkyl, R22 is halogen atom, cyano, CrC6alkyl, CrC6ha!oalkyl, hydroxy C^Cealkyl, C r C4alkoxy CrC4alkyl, CrC4alkoxycarbonyl CrC4alkyl, CrC6alkoxy, CrC6alkylthio, C r , C6alkylamino, di(CrC4alkyf)amino, C^Cealkoxycarbonyl, phenyl or phenyl substituted with (Z)p1, when q1, q2, q3 or q4 is an integer of 2 or more, each R22 may be identical with or different from each other, further in case where two R22s are present on the same carbon atom, the two R22s together may form oxo, thioxo, imino, CrC6alkylimino, CrC6alkoxyimino or CrC6alkylidene, R23 is hydrogen atom, CrC6alk'yi, CrCBalkyl substituted with R32, C3-C6cycloalkyi, C3-C6alkenyl, C3-C6haloalkenyi,.C3-C6alkynyl, -OH, benzyloxy, -CHO, -C(0)R33, -C(0)OR33, -C(0)SR33, -C(0)NHR34, -C(0)N(R34)R33, -C(S)NHR34, -C(S)N(R34)R33, -S(0)2R33, -P(0)(OR21)2, -P(S)(OR21)2, phenyl, phenyl substituted with (Z)p1 or D-5, ' R24 is halogen atom, cyano, C3-C8cycioalkyl, C3-C8halocycloaJkyl, CrC6alkoxy, C r C6haloalkoxy, CrC6aikylthio, CrC6haloalkyIthio, C^Cealkylsulfonyl, C r C6haloalkylsulfonyl, C^Cealkylamino, di(C1-C6alkyl)amino, -CHO, CrC^alkylcarbonyi; CrC6haloalkyIcarbonyl, CrC5alkoxycarbonyl, CrC6haloaIkoxycarbonyl, -CH=NOR11, -C(R9)=NOR11, phenyl, phenyl substituted with (Z)p1, D-1 to D-60 or E-1 to E-49, R25 is hydrogen atom, CrC8alkyl, CrC8alkyl arbitrarily substituted with R32, C3¬C8cycloalkyl, C3-C8cycloalkyl arbitrarily substituted with R32, C3-C8alkenyl, C3¬C8alkenyl arbitrarily substituted with R32, C3-C8alkynyl, C3-C8alkynyl arbitrarily substituted with R32, -CHO, -C(0)R33, -C(0)OR33, -C(0)SR33, -C(0)NHR34, -C(0)N(R34)R33, -C(0)C(0)R33, -C(0)C(0)OR33, -C(S)R33, -C(S)OR33, -C(S)SR33, -C(S)NHR34, -C(S)N(R34)R33, -S(0)2R33, -S(0)2N(R34)R33, -Si(R13)(R14)R12, -P(0)(OR21)2l -P(S)(OR21)2, phenyl, phenyl substituted with (Z)p1, D-1 to D-4, D-6 to D-13, D-15 to D-23, D-25 to D-37, D-39, D-40, D-42, D-45 to D-60, E-3 to E-9, E-23 toE-31, E-34orE-45, R2S is hydrogen atom, C,-C6alkyl, C^-Cghaloalkyl, C^alkoxy GrC4alkyl, C r C4alkylthio CrC4alkyl, C3-C6cycloalkyl, C3-C6alkenyl, C3-C6alkynyl orC^Cgalkoxy, or R26 together with R2* may form 3- to 6-membered ring with the nitrogen atom bonding them by forming C2-C5alkylene chain, in this case, the alkylene chain may one contain oxygen atoni, sulfur atom or nitrogen atom, and may be substituted with halogen atom, CrC6alkyl, CrC6haloalkyl, CrC6alkoxy, phenyl,-phenyl substituted with (Z)p1, oxo or thioxo, R27 is CrC8alkyl, C1-C8alkyl arbitrarily substituted with R32, C3-C8cycloalkyl, C3¬C8cycloalkyl arbitrarily substituted with R32, C3-C8alkenyi; C3-C8alkenyl arbitrarily substituted with R32, C3-C8alkynyl, C3-C8alkynyl arbitrarily substituted with R32, -SH, C^Cgalkylthio, C^Cghaloalkylthio, phenylthio, phenylthio substituted with (Z)p1, -CHO, -C(0)R33, -C(0)OR33, -C(0)SR33, -C(0)NHR34, -C(6)N(R34)R33, -C(0)C{0)R33, -C(0)C(0)OR33, -C(S)R33, -C(S)OR33, -C(S)SR33, -C(S)NHR34, -C(S)N(R34)R33, -P(0)(OR21)2, -P(S)(OR21)2, phenyl, phenyl substituted with (Z)p1, D-18, D-21, D-25, D-30 to D-35, D-47, D-50, D-51, E-3 to E-9, E-23 to E-31, E-34 or E-45, R28 is CrC6alkyl, CrC6alkyl arbitrarily substituted with R32, C3-C8cycloalkyl, C3¬ Cgcycloalkyl arbitrarily substituted with R32, C2-C6alkenyl C3-C8cycloalkyl, C2¬C6haloalkenyl C3-C8cycloalkyl, C2-C8alkenyl, C2-C8alkenyl arbitrarily substituted with R32, C2-C8alkynyl, C2-C8alkynyl arbitrarily substituted with R32, phenyl, phenyl substituted with (Z)p1l D-1 to D-60"or E-1 to E-49, R29 is hydrogen atom, CrC6alkyl, CrC6alkyl arbitrarily substituted with R32, C3¬C6alkenyl, C3-C6haloalkenyl, C3-C6alkynyl, C3-C6haloalkynyl, phenyl or phenyl substituted with (Z)p1, or R29 together with R28 may form 3- to 6-membered ring with the nitrogen atom bonding them by forming C2-C5alkylene chain, in this"tase, the alkylene chain may contain one oxygen atom, sulfur atom or nitrogen atom, and may be arbitrarily substituted with halogen atom, CrC6alkyl, CrC6alkoxy, formyl, C,¬C6alkylcarbonyl, CrC6alkoxycarbonyl, phenyl or phenyl substituted with (Z)p1, R30 is: (VCealkyl, CrC8alkyl arbitrarily substituted with R32, C3-C8cycloalkyl, C3¬C8alkfenyl, C3-C8alkenyl arbitrarily substituted with R32, C3-C8alkynyl, C3-C8alkynyl arbitrarily substituted with R32, R31 is hydrogen atom, CrC6alkyl, C1-C6ha!oalkyl, C3-C6cycloalkyl CVC^alkyl, C,¬C6a!koxy CrC4alkyl, CrC6haloalkoxy CrC4alkyl, CrC6alkylthio CrC4alkyl, C r C6haloalkylthio CrC4alkyl, CrC6alkylsulfonyl C1-C4alkyl, CrC6haloalkylsulfonyl C r C4alkyl, phenyl C1-C4alkyl, phenyl CrC4alkyl substituted with (Z)p1 C3-C6cycloalkyl, phenyl or phenyl substituted with (Z)p1, or R31 together with R30 may form 5- to 7¬membered ring with the atom bonding them by forming C2-C4alkylene chain, in this case, the alkylene chain may contain one oxygen atom, sulfur atom or nitrogen atom, and may be arbitrarily substituted with halogen atom or (VCealkyl, R32 is halogen atom, cyano, nitro, C3-C8cycloalkyl, C3-C8halocycloalkyl, -OH, -OR33, -OC(0)R33, -OC(0)OR33, -OC(0)NHR33, -OC(0)N(R34)R33, -OC(S)NHR33, -0C(S)N(R34)R33, -SH, -S(0)rR33, -SC(0)R33, -SC(0)OR33, -SC(0)NHR33, -SC(0)N(R34)R33, -SC(S)NHR33, -SC(S)N(R34)R33, -NHR34, -N(R34)R33, -N(R34)CH0, -N(R34)C(0)R33, -N(R34)C(0)0R33, -N(R34)C(0)NHR33, -N(R34)C(0)N(R34)R33, -N(R34)C(S)NHR33, -N(R34)C(S)N(R34)R33, -CHO, -C(0)R33; -C(0)0R33, -C(0)SR33, -C(0)NHR34, -C(0)N(R34)R33, -C(0)C(0)0R33, -CH=NOR11, -C(R9)=NOR11, --Si(R13)(R14)R12, -P(0)(OR21)2, -P(S)(OR21)2, -P(phenyl)2, -P(0)(phenyl)2, phenyl, phenyl substituted with (Z)p1, D-1 to D-60 or E-1 to E-49, R33 is C1-C6alkyl, CrC6haloalkyl, C3-C6cycloalkyl CrC4alkyl, C3-C6halocycloalkyl C r C4alkyl, CrC4alkoxy C^C^Ikyl, CrC4haloalkoxy C1-C4alkyi, CrC4 alkylthio C r C4alkyl, CrC4haloalkylthio CrC4alkyl, CrC4alkylsulfonyl CrC4alkyl, C r C4haloalkylsufonyl C^^alkyl, cyano CrC6alkyl, CrC6 alkylcarbonyl CrC4alkyl, C,¬ C6haloalkylcarbonyl C1-C4alkyl, CrC6alkoxycarbonyl C^alkyl , di(Cn¬C6alkyl)aminocarbonyl Chalky!, tri(CrC4alkyl)silyl CrC4alkyl, phenyl O^alkyl, phenyl Chalky! substituted with (Z)p1) CrC4alkyl substituted with any one of D-1 to D-60, CrC4alkyl substituted with any one of E-1 to E-49, C3-C6cycloalkyl, C3¬C6halocycloalkyl, C2-C6alkenyl C3-CBcyc!oalkyl, C2-C6haloalkenyl C3-C8cycloalkyl, C2¬C8alkenyl, C2-C8haloalkenyl, C3-C8cycloalkenyl, C3-C8halocycloalkenyl, C2-C8alkynyl, C2-C8haloalkynyl, phenyl, phenyl substituted with (Z)p1, D-1 to D-60 or E-1 to E-49, R34 is hydrogen atom, CrC6alkyl, CrC6haloalkyl, C3-'C8cycloalkyl, C3-C t) CNN V^ x^ ' ^-^ V_N v_N N-N ^-N G-6 G-7 G-8 G-9 G-10 (X)m-^=\ Wm-^f W-Vff (X)m^P\ W-n^C^ v° v ^s V vN G-ll G-12 G-13 G-14 G-15 (X)m^K (X)»-0 ^^ Y W^-O CXkJ^K , R15 R15 G-16 G-17 G-18 G-19 G-20 R15 G-21 G-22 G-23 G - 24 G - 25 X is halogen atom, cyano, nitro, -SFS, CrC6alkyl, CrC6alkyl arbitrarily substituted with R4, C3-C8cycloalkyl, C3-C8cycloalkyl arbitrarily substituted with R4, C2-C6alkenyl, C2-C6alkenyl arbitrarily substituted with R4, C2-C6alkynyl, C,-C6alkynyl arbitrarily substituted with R4, -OH, -OR5, -OS02R5, -S(0)rR5, -N(R7)R6, -C(0)OR9, -C(0)SR9, -C(0)NHR10, -C(O)N(R,0)R9, -C(S)OR9, -C(S)SR9, -C(S)NHR10;-C(S)N(R10)R9, -CH=NOR^\ -C(R^)=NOR", -S(0)2NHR^°, -S(0)2N(R^°)R^ -Si(R'')(R'')R'', phenyl, phenyl substituted with (Z)p„ D-1 to D-60 or E-1 to E-49, when m is an integer of 2 or more, each X may be identical with or different from each other, further, when two Xs are adjacent, the adjacent two Xs may form 5-membered or 6¬membered ring together with carbon atoms to which the two Xs are bonded by forming -CH2CH2CH2-, -CHjCHjO-, -CHjOCHj-, -OCHjO-, -CH2CH2S-, -CH2SCH2-, -CH2CH2CH2CH2-, -CH2CH2CH2O-, -CH2CH2OCH2-, -CH2OCH2O-, -OCH^CHjO-, -OCH2CH2S- or -CH=CHCH=CH-, in this case, hydrogen atoms bonded to each carbon atom forming the ring may be arbitrarily substituted with halogen atom, C^¬C4alkyl or Ci-C4haloalkyl, Y is halogen atom, cyano, nitro, Ci-Cealkyl, Ci-Cgalkyl arbitrarily substituted with R", -0R^ -OSO2R', -S(0),R^ -NHR^ -N(R')R^ -N=CHOR^ -N=C(R')OR^ -C{0)NHR'°, -C(0)N(R^°)R^ -C(S)NHR^°, -C(S)N(R'°)R^ phenyl, phenyl substituted with {Z%„ D-1 to D-24, D-30 to D-38, D-43 to D-52 or D-53, when n is an integer of 2 or more, each Y may be identical with or different from each other, further, when two Ys are adjacent, the adjacent two Ys may form 5-membered or 6¬membered ring together with carbon atoms to which the two Ys are bonded by forming -CH2CH2CH2-, -CH2CH2O-, -CH2OCH2-, -OCH2O-, -CH2CH2CH2CH2-, -CH2CH2CH2O-, -CH2CH2OCH2-, -CH2OCH2O-, -OCH2CH2O-, -OCH=N- or -SCH=N-, in this case, hydrogen atoms bonded to each carbon atom forming the ring may be arbitrarily substituted,with halogen atom, Ci-C^aikyl or Ci-C4halba[kyl, R^ is Ci-Cgalkyl, Ci-CgalkyI arbitrarily substituted with R^^ Ca-CeCycloalkyI, C3¬Cghalocycloalkyl, Cg-Cgalkenyl, Cg-Cshaloalkenyl, phenyl Ca-Cgalkenyl, phenyl C3¬Cgalkenyl substituted with (Z)pi, Ca-Cgalkynyl, Ca-Cghaloalkynyl,^ phenyl Ca-Cgalkynyl, phenyl Cj-Cgalkynyl substituted with {Z\„ Ci-CeaJkoxy, -N(R2°)R^^ -N=CHR^'^ -N=C(R^''')R^'^ -C(0)N(R'°)R^ -C(S)N(R^°)R^ -C(=NR^OOR^ -C(=NR'')SR^ -C(=NR^^)N(R^°)R^ phenyl, phenyl substituted with {Z)^,, D-1 to D-4, D-6 to D-13, D¬15 to D-23, D-26, D-27, D-29 to D-37, D-39, D-40, D-42, D-45 to D-58, E-4 to E-9, E-23 to E-28, E-30, E-31, E-34 or E-45, R^is hydrogen atom, Ci-Cgalkyl, Ci-Cghaloalkyl, Ca-Cecycloalkyi Ci-C4alkyl, C^¬C4alkoxy Ci-C4alkyl, Ci-C4haloalkoxy Ci-C4alkyl, benzyloxy Ci-C4alkyl, Ci-C4alkylthio Ci-C4alkyl, Ci-C4haloalkylthio Ci-C4alkyl, Ci-C4alkylsulfonyl Ci-C4alkyl, C^¬C4haloa(kylsulfonyl Ci-C4alkyl, phenylfhio Ci-C4alkyl, phenyithio Ci-C4alkyl substituted with (Z)pi, cyano CrCgalkyl, nitro Ci-Cgalkyl, CrC4alkylcarbonyl C^¬ C4alkyl, Ci-C^alkoxycarbony Ci-C^alkyl, Ca-CeCycloalkyI, Cs-Cea^kenyl, C3¬ ' Cehaloalkenyl, Ca-Cealkynyl, -SR^ -S(0)2R^ -SN(R^')R^^ -0H,".-'5R^^ -NHR^", -N(R'°)R'', -N=CHR''^ -N=C(R^'-'')R'-^ -C(0)R^ -C(0)OR^ -cfo)SR^ -C(S)OR^ -C(S)SR^ phenyl, phenyl substituted with {Z)^^, or R^ and R^ together form =C(R^^)R^^ and further R^ and RMogether may form 3- to 7-membered ring together with the nitrogen atom bonding them by forming C2 to Cg alkylene chain, in this case, the alkylene chain may contain one oxygen atom, sulfur atom or nitrogen atom, and may be arbitrarily substituted with Ci-Cgaiky], formyl, C^-' Cgalkylcarbonyl or Ci-Cgalkoxycarbonyl, R^^ and R^^ together may form 5- or 6-membered ring together with the carbon atom bonding them by forming C4 or C5 alkylene chain or C4 or C5 alkenylene chain, in this case, the alkylene chain and the alkenylene chain may contain one to three oxygen atoms, sulfur atoms or nitrogen atoms, and may be arbitrarily substituted with halogen atom or Ci-Cgalkyl, R^ is cyano, C^-Cealkyl, Ci-Cgalkyl arbitrarily substituted with R^ Cs-Cacycloalkyj, C3¬Cghalocycloalkyl, Cs-Cgalkenyl, Ca-Cghaloalkenyi, Ca-Cealkynyl, Cg-Cehaloalkynyl, -0R^ -S(0),R^ -N(R^°)R', -C(0)OR^ -C(0)SR^ -C(0)NHR'°, -C(0)N(R'°)R^ -C(S)OR^ -C(S)SR^ -C{S)NHR'°, -C(S)N(R^°)R^ -CH=NOR'\ -C(R')=NOR'\ -Si(R'')(R'')R'', phenyl, phenyl substituted with (Z)pi,D-1 to D-4, D8¬ to D-13, D-15 to D-23, D-25 to D-37, D-39, D-40, D-42, D-45 to D-60 or E-4 to E-7, E-23 to E27 or E-28, R'' is halogen atom, .cyano, Cj-CeCycIoalkyI, Ca-CehalocycloalkyI, -OH, -OR^, ¬S{0\R\ -N(R^°)R^ -N{R^°)C(0)R^ -N(R'°)C(0)OR^ -N(R^°)C(0)SR^ -N(R^°)C(S)OR^ -N(R^°)C(S)SR^ -N(R^°)S(0)2R^ -Si(R^^)(R^^)R^^ phenyl, phenyl substituted with {Z\^, D-1 to D-5, D-8 to D-38, D-41, D-43, D-44-, D-47 to D-52 or D¬53, R^ is Ci-Cgalkyl, Ci-Cghaloalkyl, Ci-Cshaloalkoxy Ci-CahaloalkyI, Ca-CgcycloalkyI, C3¬Cghalocycloalkyl, Ca-Cgalkenyl, Cs-Cghaloalkenyl, Ca-Cgaikynyl, Cg-Cehaloalkynyl, phenyl, phenyl substituted with {Z\^, D-1 to D-4, D-7, D-9, D-15 to D-23, D-30 to D¬35, D-47 to D-53, E-3 to E-9, E-23 to E-27 or E-28, R^ is CrCgalkyl, Ci-Cghaloalkyl, Cs-Cecycjoalkyl CrC4alkyl, CrC4alkoxy CrC4alkyl, C,-C4alkylthio CrC4alkyl, -S(0)2R^ -CHO, -C(0)R^ -C(0)OR^ -C(0)SR^ -C(S)0R^ . or -C(S)SR^ R^ is hydrogen atom, Ci-Cgalkyl, Ci-CehaloalkyI, C3-C6alkenyi or C3-C6alkynyl, R' is Ci-Csaikyl, R' is Ci-Cealkyl, Ci-CghaloalkyI, Cj-CeCycloalkyl Ci-C^alkyl, Ci-Cgalkoxy CrC4alkyl, Ci-Csalkylthio Ci-C4a!ky!, cyano Ci-Cealkyl, phenyl Ci-C^alkyl, phenyl C,-C4alky! substituted with (Z)pi, Cs-Cscydbalkyl, Ca-Cghalocycloalkyl, Cg-Cgalkenyl, C3¬Cehaloalkenyl, Cj-Cealkynyl, Ca-Cghaloalkynyl, phenyl, phenyl substituted with (Z)pi, D-1 to D-4, D-6 to D-35, 0-38, D-47 to D-54 or D-55, R^° is hydrogen atom or CrCealkyI, or R''" together with R^ may .form 5- to 7¬membered ring with the nitrogen atom bonding them by forming C^-Cgaikylene chain, in this case, the alkylene chain may contain one oxygen atom or sulfur atom, R^^ is C^-Cealkyl, Ci-Cghaloalkyl, phenyl Ci-C4alkyl, phenyl Ci-C4alkyl substituted with (Z)pi, phenyl or phenyl substituted with (Z)pi, or R^'' together with R^ may form 5¬or 6-membered ring with the atom bonding them by forming Cj-Cgalkylene chain, in this Gase, the alkylene chain may be arbitrarily substituted with Ci-Cgalkyl, R''^ is Ci-CealkyI, phenyl or phenyl substituted with (Z)pi, R^^ and R^"* independently of each other are Ci-CeBlkyl, R^^ is Ci-Cgalkyl, Ci-Cghaloalkyl, phenyl Ci-C4alkyl, phenyl Ci-C4alkyl substituted with (Z)pi, phenyl or phenyl substituted with (Z)pi, R^^ is halogen atom, cyano, Ca-CeCycloalkyI, Ca-Cghalocycloalkyl, -0R^^ -N(R^^)R^^ -SH, -S(0),R'^ -S02NHR'^ -S02N(R2')R2^ -CHO, -C(0)R'^ -C(0)OR2«, -C(0)NHR'^ -C(0)N(R2')R'^ -C(0)N(R2')0R'^ -C(S)NHR'^ -C(S)N(R'')R2^ -C(R'')=NOH, -C(R'')=NOR'°, -C(=NR'0OR'°, -C(=NR'')SR'°, -C(=NR'')N(R2^)R'°, -C(=N0R=^)NHR2^ -C(=NOR'^)N(R^^)R^°, -Si(R^^)(R^^)R^^ phenyl, phenyl substituted with (Z)p„ D-1 to D-6Q, E-1 to E-49 or M-1 to M-22, R^^ is Ci-Cgalkyl, Ci-C4a!koxy Ci-C4alkyl, Ci-Cgalkoxycarbonyl Ci-C4alkyl, phenyl C^¬C4alkyl, phenyl Ci-C4alkyl substituted with (Z)pi or Ci-Cgalkoxycarbonyl, R'^ is Ci-CealkyI, phenyl Ci-C4alkyl or phenyl CrC4alkylsubstituted with (Z)pi, or R'^ together with R^^ may form 5- or 6-membered ring with the nitrogen atom bonding them by forming C4-C5alkylene chain, in this case, the alkylene chain may contain one oxygen atom or sulfur atom, and may be arbitrarily substituted with methyl or methoxy, R^^ is C^-Cealkyl, Ci-Cgalkyl arbitrarily substituted with R^^ Cg-Cecycloalkyl, C3¬Cehalocycloalkyi, Ca-Cgalkenyl, Cs-Cghaloaikenyl, Ca-Cealkynyl, -CHO, -C(0)R'^ -C(0)0R2^ -C(0)NHR2^ -C(0)N(R2^)R2^ -C(S)NHR2^ -C(S)N(R^^)R2^ -S(0)2R^^ -S(0)2NHR'^ -S(0)2N(R'')R'', phenyl, phenyl substituted with (Z)pi, D-1 to D-13, D¬15 to D-25, D-30 to D-37, D-39, D-40, D-42, D-45 to D-60, E-5, E-7, E-9, E-24, E-25, E-27, E-28, E-30orE-31, R^®^ is Ci-Cealkyi, Ci-CehaloalkyI, Cj-CgCycloalkyI, phenyl, phenyl substituted with (Z)pi, D-1 to D-4, D-8 to D-10, D-'15 to D-23, D-47 to D-55, E-4 to E-7, E-23 to E-27 or E-28, R^^'^ is hydrogen atom or Ci-Cealkyl, or R^^^ together with R^^^may form 5- or 6¬membered ring with the carbon atom bonding them by forming C^-Cjalkylene chain, in this case, the alkylene chain may contain one oxygen atom or sulfur atom, R^° is hydrogen atom, CrCgaikyl, Ci-Cghaloalkyl, Ci-C4alkoxy Ci-C^alkyl, C^¬C^alkylthio Ci-C4a!kyl, cyano Ci-CealkyI, Ci-C^alkoxycarbonyl Ci-C4alkyt;j32¬Cealkenyl, Cj-Cgalkynyl, -CHO, -C(0)R^ -C(0)OR^ -C(0)SR^ -C(S)OR^ -C(S)SR' or CrCealkylsulfonyl, R^^ is halogen atom, cyano, Ci-Cgalkyl, Ci-CghaloalkyI, Ci-Cgalkoxy, C^-Cealkoxycarbonyl, -C(0)NH2 or -C(S)NH2, when q1, q2, q3 or q4 is an integer of 2 or more, each R^^ may be identical with or different from each other, further in case where two R^^s are present on the same carbon atom, the two R^^s together may form 0X0, thioxo, imino, Ci-Cealkylimino, Ci-Cealkoxyimino or C^-Ceaikyildene, R^^ is hydrogen atom, Ci-Cgalkyl, C^-Cealkyl arbitrarily substituted with R^^ C3¬Cecycioalkyl, Cg-Cealkenyl, Cs-Cgalkynyl, -OH, benzyloxy, -CHO, -C(0)R^^ -C(0)0R^^ -C(0)SR'^ -C(0)NHR^^ -C(0)N(R'')R'^ -S(0)2R'', phenyl, phenyl substituted with (Z)pi or D-5, R2^ is hydrogen atom, Ci-Cealkyi, CrCehaloalkyi, Ci-C4alkoxy Ci-C4alkyl, C^¬C4alkylthio C,-C4alkyl, cyano Ci-Cgaikyl, phenyl Ci-C4alkyl, phenyl Ci-C4alkyl substituted with (Z)p„.C3-C6aIkenyl, Ca-Ceaikynyl, -CHO, -C(0)R'^ -C(0)0R'^ -C(0)SR'^ -C(0)NHR'^ -C(0)N(R'')R'^ -C(S)R", -C(S)OR^^ -C(S)SR'^ -C(S)NHR^^ -C(S)N(R^')R", -S(0)2R", -S(0)2N(R^)R^^ di(CrC6alkyl)phosphoryl, di(Ci-C6alkyl)thiophosphoryl, tri(Ci-C4alkyl)silyl, phenyl or pheriyl substituted with (Z)pi, R^^is hydrogen atom, CrCgalkyl, Cj-Ceaikenyl, Cg-Cealkynyl or C^-Cgalkoxy, or R^® together with R^^ may form 4- to 6-membered ring with the nitrogen atom bonding them by forming Ca-Csalkylene chain, in this case, the alkylene chain may contain one oxygen atom, sulfur atom or nitrogen atom, and may substituted with Ci-CgalkyI, 0x0 or thioxo, R'^ is Ci-Cgalklyl, C^-Cghaloalkyi, hydroxy C^-Cgalkyl, Ci-C4alkoxy ei-C4alkyl, C,¬C4alkylthio Ci-C4alkyl, Ci-C4alkylcarbonyl Ci-C4alkyl, Ci-C4a!koxycarbonyl C^¬C4alkyl, di(Ci-C4alkyl)aminocarbonyl Ci-C4alkyl, tri(Ci-C4alkyl)silyI Ci-C4alkyl, phenyl Ci-C4alkyl, phenyl Ci-C4alkyi substituted with (Z)pi, Ca-Cgalkenyl, Ca-Cgalkyny!, C^ Cgalkylcarbonyl, Ci-Cealkylthio, phenylthio, phenylthio substituted with (Z)pi, -C(0)NHR'^ -C(0)N(R'')R'^,-C'(S)NHR'^ -C(S)N(R^^)R'^ phenyl, phenyl substituted with {Z%„ D-21, D-35,, D-47 or D-50, R^^ is Ci-CgalkyI, Ci-Cgalkyl arbitrarily substituted with R^^ Cg-CeCycloalkyI, C3¬Cehalocycloalkyl, Cj-Csalkenyl, Ca-Cghaloalkenyl, Ca-Csalkynyl, Ca-Cshaloalkynyl, phenyl, phenyl substituted with {Z)p„ D-1 to D-60 or E-1 to E-49, R2^ is hydrogen atom, Ci-CealkyI, Ci-C4alkoxy Ci-C4alkyl, Ci-C^alkylthio Ci-C^alkyl, cyano Ci-Cealkyl, Ca-Cgalkenyl or Ca-Cgalkynyl, or R^^ together with R^^Tnay form 3-' to 6-membered ring with the nitrogen atom bonding them by forming Cj-Cgalkylene chain, in this case, the alkylene chain may contain one oxygen atom or sulfur atom, R'° is Ci-Cgalkyl, CrC^alkoxy C^-C^alkyl, Ci-C^alkylthio C^-C^alkyl, Ca-Cgcycloalkyl Ci-G^alkyl, triCCi-CgalkyOsilyl Ci-C4alkyl, phenyl Ci-C4alkyl, phenyl CrC4alkyl substituted with (2)pi, Cs-Cgalkenyl, Cg-Cshaloalkenyl, Ca-Cgalkynyl or C3¬Cehaloalkynyl, R^^ is hydrogen atom, Ci-Cgalkyl, Ci-Cghaloalkyl or Ca-Cgcycloalkyl, or R^^ together with R^° may form 5- or 6-membered ring with the atom bonding them by forming Cz-Cgalkylene chain, in this case, the alkylene chain may be arbitrarily substituted with Ci-Cgalkyl, R^^ is halogen atom, cyano, Ca-CgCycloalkyl, Ca-Cghalocycloalkyl, -OR", -OC(0)R", -OC(0)NHR'^ -OC(0)N(R'')R'', -S(0),R", -SC(0)R", -SC(0)NHR", -SC(0)N(R'')R", -N(R'')CHO, -N(R'')C(0)R'^ -N(R'')C(0)OR", -C(0)0R", ' -C(0)NHR'', -C(0)H(R'')R'^ phenyl, phenyl substituted with {Z\„ D-1 to D-60 or E¬1 to E-49, R" is CrCgalky!, CrCghaloalkyl, Cs-CeCycloalkyI CrC4alkyl, Ci-C4alkoxy Ci-C4alkyl, Ci-C4ha!oalkoxy Ci-C4alkyl, Ci-C4alkylthio Ci-C4alkyl, CrC4haloalkylthio Ci-C4alkyl, Ci-C4alkylsulfonyl Ci-C4alkyl, CrC4haloalkylsulfonyl Ci-C4alkyl, cyano Ci-Cgalkyl, phenyl Ci-C4alkyl, phenyl Ci-C4alkyl substituted with (Z)pi, Ca-Cgcycloalkyl, C3¬Cghalocycloalkyl, C3-C6alkenyl, Ca-Cghaloalkenyl, C3-C6afkynyl, phenyl, phenyl substituted with (Z)p„ D-1 to D-4, D-8 to D-13, D-15 to D-18, D-21, D-29 to D-37, D¬47 to D-55, E-5, E-7, E-9, E-24, E-25, E-27, E-28, E-30, E-31or E-34, R^"* is hydrogen atom, Ci-Cgalkyl, Ci-CghaloalkyI, Ca-Cgalkenyl or Cj-Cealkynyl, or R^^ together with R" may form 3- to 6-membered ring with the nitrogen atom bonding them by forming Cj-Cjalkylene chain, in this case, the alkylene chain may contain one oxygen atom or sulfur atom. (3) The isoxazoline-substituted benzamide compound or the salt thereof as set forth in (2), wherein G is G-1, G-3, G-4, G-13, G-14, G-17, G-18, G-20, G-21 or G-22, X is halogen atom, cyano, nitro, -SF5, Ci-Cgalkyl, CrCealky! arbitrarily substituted with R^ Ca-CBcycioalkyI, Cj-Cghalocycloalkyi, Cj-Cgalkenyl, Cj-Cehaloaikenyl, C2¬Cgalkynyl, C^-Cghaloalkynyl, -0R^ -0S02R^ -S(0),R^ -C(0)OR^ -C(d)SR^ -C(S)OR^ -C(S)SR^ -C(S)NHR^°, -C(S)N(R^°)R^ -CH=NOR^\ -C(R')=NOR^\ -Si(R'')(R^')R^', E-10, E-12, E-18, E-32, E-35 or E-43, when m is 2 or 3, each X may be identical with or different from each other, further, when two Xs are adjacent, the adjacent two Xs may form 5-membered or 6¬membered ring together with carbon atoms to which the two Xs are bonded by forming -CF2OCF2-, -OCFgO-, -CF2OCF2O- or -OCF2CF2O-, Y is l!ialogen atom, cyano, nitro, Ci-Ceaikyl, C^-Cealkyl arbitrarily substituted with R"*, -OR^ -OSO2R', -S(0),R^ -NHR^ -N(R')R^ -N=C(R')OR^ -C(0)NH2 or -C(S)NH2, . when n is 2 or 3, each Y may be identical with or different from each other, R^ is Ci-Csalkyi, Ci-CealkyI arbitrarily substituted with R^^ Ca-CeCycloaikyl, C3¬Cahalocycloalkyl, Cj-Cgalkenyl, Cs-Cehaloalkenyl, Cg-Cgalkynyl, Ca-Cghaioalkynyl, -N(R'°)R'^ -C(0)N(R'°)R^ -C(S)N(R'°)R^ phenyl substituted with (Z)p„ D-8 to D-13, D-15 to D-18, D-21 to D-23, D-26, D-27, D-29 to D-37, D-39, D-40, D-42, D-45 to D¬58, E-5, E-7, E-8, E-9, E-24, E-25, E-27, E-28, E-30, E-31 or E-34, R^ is hydrogen atom, Ci-Cgalkyl, Ci-Cghaloalkyl, Ci-C4alkoxy Ci-C4alkyl, C,¬C^alkylthio Ci-C4alkyl, cyano Ci-Cgalkyl, Ca-CgCycloalkyl, Cj-Ceaikenyi, Cg-Cgalkynyl, -OH, Ci-Cgalkoxy, CiTCeaikylcarbonyloxy, Ci-Cgalkoxycarbonyloxy, C,-Cealkylsuifonyloxy, Ci-Cghaloalkylthio, phenylthio, phenylthio substituted with (Z)pi, Ci-Cgalkylsulfonyl, -SN(R'')R^^ -NHR'°, -N=CHR^^ -N=C(R^''')R^'^ -C(0)R^ -C(0)OR^ -C(0)SR^ -C(S)OR' or -C(S)SR^ or R' together with'R^ may form 3- to 7-membered ring with the nitrogen atom bonding them by forming Cj-Cgalkylene chain, in this case, the alkylene chain may contain one oxygen atom or sulfur atom, R' is CrCgalkyl, Ci-CehaloalkyI, Cg-CeCycloalkyl Ci-C4alky"l, Ca-CehalocycloalkyI C^¬ C4alkyl, Ci-C4alkoxy Ci-C4alkyl, Ci-C4haloalkoxy Ci-C4alkyl, Ci-C4alkylthio C^¬C4alkyl, CrC4aIkylsulfinyl CrC4alkyl, Ci-C4alkylsulfonyl Ci-C4alkyl, Ci-G4haloalkylthio Ci-C4alkyl, Ci-C4haloalkylsulfinyl Ci-G4alkyl, Ci-C4haloalkylsulfonyl Ci-C4alkyl, cyano C^-Cgalkyl, Ci-C4alkoxy Ci-C4haloalkyl, Ci-G4haloalkoxy Ci-G4halocilkyl, G^¬G4alkylthio Gi-G4haloalkyl, Ci-G4alkylsulfinyl Gi-C4haloalkyl, Gi-C4alkylsulfonyl G,¬G4haloalkyl, Gi-C4haloalkylthio Gi-C4haIoalkyl, Gi-G4haloalkylsulfinyI Gi-G4haloalkyl, Ci-G4haloalkylsulfony! Gi-G4haloaIkyl, cyano Gi-CehaloalkyI, Ga-Ggcycloalkyl, G3¬CehalocycioalkyI, E-4 to E-7, E-23 to E-27 or E-28, R" is haiogen atom, cyano, -OH \ Ci-Cgalkoxy, Ci-Cehaloalkoxy, Ci-Cgalkylthio, C,-Cghaloalkylthio, Ci-Cealkylsulfifiyl, C^-Cehaloalkylsulfinyl, Ci-Cgalkylsulfonyl, C^-Cshaloalkyisulfonyl or tri(Ci-C6alkyl)silyl, R^ is CrCgalkyI, Ci-CetialoaikyI, Ci-Cshaloalkoxy Ci-Cghaloalkyl, Cg-CgCycloalkyl, C3¬ ' CghalocycloalkyI, Cs-Cealkenyl, Cj-Cghaloalkenyl, Ca-Cgalkynyl, Cg-Cehaloalkyny), E-4 to E-9, E-23 to E-27 or E-28, R^ is CrCealkyi, CrCshaloaikyI, -S(0)2R', -CHO, -C(0)R^ -C(0)OR^ -•e(0)SR^ -C(S)OR'or-C(S)SR^ R^ is liydrogen atom, Ci-Cgalkyl or Ci-Cghaloalkyl, R^ is Ci-CgalkyI, Ci-CehaloalkyI, Ca-CeCycloalkyi Ci-C^aikyi, Ci-Cgalkoxy C^-C^alkyl, Ci-€ealkyltiiio Ci-C^alkyl, cyano Ci-Csalkyi, phenyl Ci-C4alkyl, Ca-CgCycloalkyI, C3¬Cghalocycloalkyl, Cj-Cgalkenyl or Ca-Cgalkynyl, R^° is liydrogen atom or Ci-Cealkyi, or R^° together with R® may form 5- or 6¬membered ring with the nitrogen atom bonding them by forming C4 or Cgalkylene chain, in this case, the aikylene chain may contain one oxygen atom or sulfur atom, R^^ is Ci-Cgalkyl or C^-Cghaloalkyl, or R" together with R^ may form 5- or 6¬membered ring with the atom bonding them by forming C2 or Cgalkyiene chain, in this case, the aikylene chain may be arbitrarily substituted with Ci-Cgalkyl, R^^ is Ci-Cgalkyl or Ci-Cghaloalkyl, R^^ is halogen atom, cyano, Ca-CeCycloalkyI, Ca-CehalocycloalkyI, -0R^^ -N(R^^)R^^ -S(0),R'^ -SOjNHRf, -S02N(R2^)R2^ -CHO, -C(0)R2^ -C(0)0R2^ -C(0)NHR2^ -C(0)N(R'')R'^ -C(0)N(R2^)OR'^ -C(S)NHR'', -C(S)N(R'')R2^ -C(R'^)=NOH, -C(R'>NOR'°, -C(=NR'^)OR'°, -C(=NR'^)SR'°, -C(=NR'0N(R2^)R'°, ¬C(=NOR'')NHR'^ -C(=NOR'^)N(R'')R'°, phenyl, phenyl substituted with (Z)pi, D-1 to D-4, D-8 to D-42, D-47 to D-55, E-4 to E-12, E-14, E-16 to E-19, E-21 to E-23, E-26 to E-35, E-40 to E-45, E-48, M-2, M-3, M-5, M-8 to M-1Q, M-14, M-15 or M-16, R^^ is Ci-CealkyI, Ci-Cgalkoxycarbonyl Ci-C4alkyl or Ci-C'ealkoxycarbonyl, R^^ is Ci-Cgalkyl or benzyl, R^' is Ci-Cgalkyl, Ci-Cghaloalkyl, Cg-CgCyclaolakyl Ci-Cgalkyl, phenyl Ci-CealkyI, phenyl Ci-CealkyI substituted with {Z\^, Cg-Cgcycloalkyl, Ca-Cgalkenyl, C3¬Cehaloalkenyl, Cg-Csalkynyl, -C(0)R'^ -C(0)OR2^ -C(0)NHR2^ -C(0)N(R'')R'^ -C(S)NHR'^ -C(S)N(R'')R'^ C-rCealkylsulfonyl, C.-Cghaloalkylsulfonyl, phenylsulfonyl, phenylsulfonyl substituted with (Z)pi, phenyl, phenyl substituted with (Z)pi, D-1 to D-4, D-18, D-21, D-25, D-3G to D-35, D-47 to D-55 or D-56, R^^^ is C,-C,a\ky\, R'^^ is hydrogen atom or Ci-CsaikyI, R2° is hydrogen atom, Ci-C5alkyl,,Ci-C4alkoxy Ci-C^alkyl, Ci-C4alkylthio Ci-C4alkyl, cyano Ci-Cgalkyi, Cs-Cealkenyl," Cj-Cealkynyl, -CHO, Ci-Cgalkylcarbonyl, C^-Cghaloalkylcarbonyl, Ci-Cealkoxycarbonyi, Ci-Cghaloalkoxycarbonyl or C^-Cgalkylsulfonyl, R^^ is Ci-C4alkyl or Ci-C4haloalkyl, or two R^^s present on the same carbon atom may together form oxo, or thioxo, '"•^ R^^ is hydrogen atom, Ci-Cgalkyi, -CHO, Ci-Ceaikylcarbonyl, Ci-Cehaloalkyicarbonyi, Ci-Cealkoxycarbonyi, Ci-Cgalkyisulfonyl or Ci-Cehaloalkyisulfonyl, R^' is hydrogen atom, CrCgalkyl, CrCehaloaikyI, -C(0)R^^ -C(0)OR'^ -C(0)SR'^ -C(G,)NHR'\ -C(0)N(R'')R", -C(S)R'^ -C(S)OR'^ -C(S)SR^^ -C(S)NHR'^ -C(S)N(R'')R'^ -S(0)2R'^ -S(0)2N(R'')R'^ di(C,-C6aikyl)thiophosphoryI, phenyl or phenyl substituted with (Z)pi, R^^ is hydrogen atom or Ci-Cgalkyl, or R^^ together with R^^ may form 4- to 6¬membered ring with the nitrogen atom bonding them by forming Cg-Cgalkylene chain, in this case, the aikylene chain may contain one oxygen atom, sulfur atom or nitrogen atom, and may be substituted with Ci-Cgalkyl, oxo or thioxo, R2^ is Ci-Cgalkyl, Ci-Cghaloalkyl, tri(Ci-C4alkyl)silyl CrC4alkyl, CrCealkylthio, -C(0)NHR'\ -C(0)N(R'')R'^ -C(S)^lHR'^ -C(S)N(R'')R^^ phenyl, phenyl substituted with (Z)pi, D-47 or D-50, R^^ is Ci-CealkyI, CrQeSlkyl arbitrarily substituted with R^^ Ca-C'eCycloalkyl, C3¬Cehaiocycioalkyl, Ca-Cealkenyi, Ca-Cghaloalkenyl, Ca-Cgalkynyl, Ca-Cghaloalkynyl, phenyl or phenyl substituted with (Z)pi, R^^ is hydrogen atom, Ci-Cgalkyl, Ca-Cgalkenyl or Ca-CgalkynyL^^or R^^ together with R^^ may form 3- to 6-membered ring with the nitrogen atom bonding them by forming Cj-Cgalkylene chain, in this case, the aikylene chain may-contain one oxygen atom or sulfur atom, R^° is Ci-CeaJkyl, Ca-CeCycloalkyI Ci-C4alkyl, phenyl Ci-C4alkyl, phenyl Ci-C4alkyl substituted with (Z)pi, Cg-Cgalkenyi or Cg-Cgalkynyl, R^^ is hydrogen atom or Ci-Cgalkyl, or R^^ together with R^° may form 5- or 6¬membered ring with the atom bonding them by forming C2 or Csalkyiene chain, in this case, the aikylene chain may be arbitrarily substituted with Ci-Cgalkyl, R^^ is halogen atom, cyano, Cj-Cecycloalkyi, Ca-Cghalocycloalkyl, Ci-C4alkoxy, C^¬C4haloalkoxy, Ci-C4alkylthio, Ci-C4haloalkylthio, Ci-C4alkoxycarbonyl, -C(0)NH2, C^¬ 27 C^alkylaminocarbonyl, di(Ci-C4alkyl)aminocarbonyl, phenyl or phenyl substituted with (Z)pi, R"' is Ci-Cgalkyl, CrCshaloalkyl, CrC^alkoxy Ci-C^alkyi, C,-C4alkylthio CrC^aikyl, Ci-C4aikylsulfonyl Ci-C4aikyl, phenyl Ci-C4alkyl, phenyl Ci-C4alkyl substituted with (Z)pi, Cs-Cgcycloalkyl, Ca-Cghalocycloalkyl, Ca-Cealkenyl, Cj-Cealkynyl, phenyl or phenyl substituted with (Z)pi, R^'' is hydrogen atom or Ci-Cgalkyl, m is an integer of 1 to 3, ""_ n is an integer of 0 to 2, q2 is an integer of 0 to 3, q3 is an integer of 0 to 2, and q4 i!s an integer of 0 to 2. (4) The isoxazoline-substituted benzamide compound or the salt thereof as set forth in (3), wherein A- is carbon atom or nitrogen atom, A^ and A^ are carbon atom, GisG-1, X is halogen atom, cyano, nitro, -SFg, Ci-CealkyI, Ci-Cgalkyl arbitrarily substituted with R", Cj-Cgcycloalkyl, Cs-Cghalocycloalkyi, Cj-Cgalkenyl, Cz-Cghaloalkenyl, Cj-Cgalkynyl, Cs-Cghaloalkynyl, -0R^ -OSOjR', -S(0),R' or tri(Ci-C6alkyl)silyl, when m is 2 or 3, each X may be identical with or different from each other, further, when two Xs, are adjacent, the adjacent two Xs may form 5-membered or 6¬membered ring together with carbon atoms to which the two Xs are bonded by forming -CF2OCF2-, -OCFjO-, -CF2OCF2O- or -OCF2CF2O-, Y is halogen atom, cyano, nitro, Ci-Cgalkyl, Ci-Cgaikyl arbitraqly substituted with R^ -0R^ -0S02R^ -S(0),R^ -NHR^ -N(R')R^ -C(0)NH2 or -C(S)NH2, when n is 2 or 3, each Y may be identical with or different from each other, R^ is Ci-Cgalkyl, Ci-Cgalkyl arbitrarily substituted with R^^ Ca-Cecycloalkyi, C3¬Cghalocycloalkyl, Ca-Cgalkenyl, Cs-Cehaloalkenyl, Ca-Cgalkynyl, Cg-Cghaloalkynyl, .N(R2°)R19, -C(0)N(R^°)R^ -C(S)N(R^°)R^ phenyl substituted with (Z)p„ D-8, D-10, D-11, D-13, D-15, D-17, D-18, D-21 to D-23, D-26, D-27, 0-29 to D-37, D-39, D-40, D-42, D-45, D-47, D-48, D-50, D-51, D-53, D-54, D-56, D-58, E-5, E-7 or E-9, R^ is hydrogen atom, Ci-Cgaikyl, CTC4alkoxy Ci-C4alkyl, Gi-C4alkylthio C,-C4alkyl, cyano Ci-Cgalkyl, Cg-CeCycloaJkyl, Cg-Cealkenyl, Cg-Cealkynyi, -OH, C^-Cgalkylcarbonyloxy, CrCealkylsulfonyioxy, -NH2, -C(0)R^ -C(0)OR', -C(0)SR^ -C(S)OR' or -C(S)SR^ R^ is Ci-Cghaloalkyl, C,-C4alkoxy Ci-C4haloalkyl, Ci-C^haloalkoxy Ci-C4haloalkyI, Ci-C4a!kylthio CrC^haloalkyl, Ci-Qhaloalkylthio CrC^haloalkyl, cyano Cr Cghaioalkyl or Cs-Cghalocycloalkyl, R^ is halogen atom, cyano, -OH, Ci-Cgalkoxy, Ci-Cghaloalkoxy, Ci-Cealkylthio, C^-Cehaloalkylthio, Ci-Cealkylsulfinyl, Ci-Cghaloalkylsulfinyl, Ci-Cgalkylsulfonyl, C^-Cghaloalkyisulfonyl or tri(Ci-C6alkyl)silyl, R^ is Ci-CealkyI, Ci-Cghaloalkyl, Ci-Cghaloalkoxy Ci-CghaloalkyI, Ca-CgCycloaikyl, C3-' CehalocycloaikyI, Cs-Cgalkenyl, Cz-Cehaloalkenyl, Ca-Cgalkynyl or Ca-Cghaloalkynyl, R^ is Ci-CeaikyI, Ci-Cghaloalkyl, -CHO, Ci-Cealkylcarbonyl, Ci-Cehaloalkylcarbonyl, Ca-Cecycloalkylcarbonyl, Ca-Cehalocycloalkylcarbonyl, Ci-Ceaikoxycarbonyl, C^-Cehaloalkoxycarbonyl, Ci-Cealkylthiocarbonyl, Ci-Cgalkoxythiocarbonyl, C^-Cealkyldithiocarbonyl, Ci-Cgaikylsulfonyl or Ci-Cehaloalkylsulfonyl, R^ is hydrogen atom or C^-Cealkyl, R^ is CrCeaikyI, Ci-Cehaioalkyl, Cj-CeCycloalkyI CrC^alkyi, C^-Cealkoxy Ci-C^alkyi, Ci-Cgalkylthio Ci-C^aikyl, cyano Ci-Cgalkyi, Cj-CgCycIoalkyI, Ca-Cealkenyl or C3¬Cgalkynyl, R^^ is halogen atom, cyano, Cg-Cecycloalkyi, Ca-Cghalocycloalkyl, -0R^^ -N(R^^)R^^ -S(OXR'^ -S02NHR2^ -S02N(R'')R'^ -C(0)R2^ -C(0)OR'^ -C(0)NHR2^ -C(0)N(R'')R2^ -C(0)N(R'')OR'^ -C(S)NHR2^ -C(S)N(R'')R2^ -C(R^^)=NOH, -C(R'^)=NOR'°, -C(=NR'^)OR'°, -C(=NR'^)SR'°, phenyl, phenyl substituted with (Z)p„ D-1 to D-4, D-8 to Dr.38, D-47 to D-55, E-4 to E-12, E-18, E-19, E-32, E-35, E-43, M-2, M-3, M-5, M-8, M-9 or M-10, R^^ is Ci-Cghaloalkyi; Cs-CgCycloalkyi, -C(0)R'^ -C(0)OR'^ -C(0)NHR2^ -C(0)N(R'')R'^ -C(S)NHR'^ -C(S)N(R'')R^^ phenyl, phenyl substituted with (Z)p„ D-3, D-4, D-21, D-47, D-50, D-51, D-53 or D-54, R^° is hydrogen atom, Ci-Cgalkyl, Ci-C^alkoxy Ci-C4alky], Ci-C4alkylthio Ci-C4alkyl, cyano Ci-Cgalkyl, Ca-Cealkenyi, Ca-Cgalkynyl, -CHO, Ci-Cealkylcarbonyl, C^-Cgalkoxycarbonyl or Ci-Cgalkylsulfonyl, R^^ is Ci-CgalkyI, Ci-CghaloalkyI, Ci-Cgaikylcarbonyi, Ci-Cgalkoxycarbonyl, C^-Cgalkylaminocarbonyl, di(Ci-C6aIkyl)aminocarbonyl or Ci-Cgalkylsulfonyl, R^^ is hydrogen atom or Ci-Cgalkyi, R'' is Ci-Cgalkyl, C,-Cghaloalkyi or tri(Ci-C4alkyl)silyl Ci-C4alkyl, R^' is Ci-CgalkyI, Ci-Cgha!oalkyl, Ca-Cgcycloaikyl Ci-C4alky!, Ci-C4alkoxy C,-C4alkyl, Ci-C4alkylthio Ci-C4alky, cyano C^-Cgalkyl, phenyl Ci-C4alkyl, phenyl Ci-C4alkyl 29 substituted with (Z)pi, Cj-CecycloalkyI, Cs-Cgalkenyl, Ca-Cehaloalkenyl, Ca-Cgalkynyl, phenyl or phenyl substituted with (Z)p,, R^^ is hydrogen atom, Ci-Cealkyl., Ca-Cgalkenyl or Ca-Cgalkynyl, R^° is C.-CealkyI or Ca-Cecycloalkyl Ci-C^alkyl, R^^ is hydrogen atom or Ci-Cgalkyl, or R^^ together with R^° may form 5- or 6¬membered ring with the atom bonding them by forming C^ or Caalkylene chain. (5) The isoxazoline-substituted benzamide compound or the salt thereof as set forth in (4), wherein '^^ X is halogen atom, cyano, nitro, -SF5, Ci-Cgalkyl, Ci-Cehaloaikyl, hydroxy C^-Cehaloalkyl, Ci-Cgalkoxy Ci-Cehaloaikyl, Ci-Cehaloalkoxy Ci-Cghaioalkyl, C3¬Cghalocycloalkyl, -OR', -OSO2R' or -S{0)rR^ when m is 2 or 3, each X may be iderltical with or different from each other, Y is halogen atom, cyano, nitro, Ci-C4alkyl, Ci-C^haloalkyl, Ci-C^alkoxy, C^¬C4haloalkoxy, Ci-Cgaikylthio, Ci-Cehaloalkylthio, Ci-Cealkylsulfonyi, C,-Cehaloalkylsulfonyl, -NHR' or -N(R0R' , R^ is Ci-Cgalkyl, Ci-Cgalkyl arbitrarily substituted with R^^ Cj-Cecycioaikyl, C3¬Ceaikenyl, Ca-Cehaloalkenyl, Cj-Cealkynyj, -N(R^°)R'^ D-8, D-10, D-13, D-15, D-18, D-21, D-34, D-35, D-50 or D-51, R^ is hydrogen atom, Ci-Cgalkyl, Ci-C4alkoxy Ci-C4alkyl, cyano C^-Cgalkyl, C3¬Cgalkynyl, -C(0)R' or -C(0)OR^ R^ is Ci-CehaloalkyI or Cg-CehalocycloalkyI, R^ is Ci-Cealkyl, Ci-Qehaloalkyi or Ci-Cghaloalkoxy Ci-CshaloalkyI, R^ is CrCeaikyl, -CHO, Ci-Cgalkylcarbonyl, Ci-Cehaioalkyicarbonyj, d -Cgaikoxycarbonyl, Ci-Cealkyithiocarbonyl, Ci-Ceaikoxythiocarbonyl, C^ Cgaikyldithiocarbonyl, Ci-Cgalkylsulfonyl or Ci-C6haloalkylsulfq.nyl, R' is Ci-Cgalkyl, Ci-Cgalkoxy Ci-C4alkyl, Ci-Cealkylth'io Ci-C4alkyl, Cg-CgCycloalkyl, Ca-Cgalkenyl or Cj-Cealkynyl, R^^ is halogen atom, cyano, Ca-Cgcycloalkyl, Ca-Cehalocybloalkyi, CrCeaikoxy, C^-Cehaloalkoxy, Ci-Cgalkylthio, Ci-CehaloaJkylthio, Ci-Cealkylsuifinyl, C^-Cghaioalkylsulfinyl, CrCgalkylsulfonyl, Ci-Cghaloalkylsulfonyl, Ci-Cealkyicarbonyl, -C(0)0R2^ -C(0)NHR2^ -C(0)N(R'')R2^ -C(S)NH2, -C(R^>NOH, -C(R=^)=NOR=°, phenyl, phenyl substituted with (Z)pi, D-1 to D-4, D-8 to D-38, D-47 to D-55, E-4 to E-7, E-10, E-11orE-32, R^' is CrCehaloaikyl, -C(0)R'^ -C(0)OR2«, phenyl, phenyl substituted with {Z\„ D-3, D-4, D-21, D-47, D-50, D-51, D-53 or D-54, R^° is hydrogen atom or Ci-CeaikyI, R^^ is Ci-Cgalkyl, Ci-CehaioalkylJ Cj-Cgcycloalkyl Ci-C4alkyl, Ca-CeCycloalkyI, C3¬Cgalkenyl or Ca-Cgalkynyl, R^^ is hydrogen atom or Ci-Cgalkyl, R^° is CrCeaikyI, R^^ is hydrogen atom or Ci-Cgalkyl, and n is an integer of 0 or 1. (6) 3,5-Bis (substituted aryl) substituted isoxazoline compound of foTmula (2) or a' salt thereof: R'P-N (Y)„ wherein A^ is carbon atom or nitrogen atom, X^ is halogen atom, -SF5, Ci-Cghaloalkyl, hydroxy Ci-Cehaloaikyi, Ci-Cgalkoxy C^-Cehaloalkyl, Ci-Cehaloalkoxy Ci-Cghaloaikyl, Cs-Cahaiocycloaikyl, Ci-Cehaloalkoxy, Ci-Cahaloalkoxy Ci-Cjhaloalkoxy, Ci-Cghaloalkylthio, Ci-Cehaloalkylsulfinyl or C,-Cghaloalkylsulfonyl, X^ is halogen atom, r-yano, nitro, Ci-Cgalkyl, Ci-CehaioalkyI, -OR^, -0S02R^ or ¬S(0)rR^ when m1 is 2, each X^ may be identical with or different from each other, Y is halogen atom, cyano, nitro, Ci-C4alkyl, Ci-C4haloalkyl, Ci-C4alkoxy, C^¬C4haloalkoxy, Ci-Cgalkylthio, Ci-Cehaloalkylthio, Ci-Cealkylsulfonyl, C^-Cghaloalkylsulfonyl, -NHR' or -N(R')R^ R^ is Ci-Cghaloalkyl or Ca-CghalocycloalkyI, R^ is Ci-Cgalkyl or Ci-Cghaloalkyl, R' is Ci-Cgalkyl, -CHO, C^-Cealkylcarbonyl, CrCehaloalkylcarbonyl, C,-Cgalkoxycarbonyl, Ci-Cgalkylthiocarbonyl, Ci-Cgalkoxythiocarbonyl, Ci-Cealkyldithiocarbonyl, Ci-Cgalkylsulfonyl or Ci-Cehaloalkyisulfonyi, R^ is hydrogen atom or Ci-Cgalkyl, R is halogen atom, cyano, nitro, -NH2, halosulfonyloxy, Ci-Cgalkylsulfonyloxy, Ci-Cghaloalkylsulfonyloxy, phenylsuifonyloxy, phenylsulfonyloxy substituted with (Z)pi or -C(0)R^ R^ is halogen atom, -OH, Ci-Cealkoxy, 1-pyrazolyl, 1-imidazolyl or 1-triazolyl, Z is iialogen atom, Ci-Cgalkyl or'-Ci-Cehaioalkyl, when p1 is an integer of 2 or more, each Z may be identical with ordifferent from each other, m1 is an integer of 0 to 2, n is an integer of 0 or 1, 'p1 is an integer of 1 or 5, and r is an integer of 0 to 2. (7) 3,5-Bis (substituted aryl) substituted isoxazoline compound or the-salt thereof ¬as set forth in (6), wherein (a) in case where R is halosulfonyloxy, Ci-Cehaloaikylsulfonyloxy, phenylsulfonyloxy or phenylsulfonyloxy substituted with (Z)pi, Y is halogen atom, cyano, nitro, C^-Cgalkyl, Ci-C4haIoaIkyl, Ci-C4alkoxy, Ci-C4haloalkoxy, Ci-Cealkyjthio, C^-Cehaloalkylthio, Ci-Cealkyisuifonyl or Ci-Cehaloalkyisuifonyl, (b) in case where R is -C(0)R^ Y is cyano, nitro, Ci-Cgalkyi, Ci-C4haloalkyl, C^-Cghaloalkylthio or Ci-Cghaloalkylsulfonyl,, (c) in case where, R is halogen atom, cyano, nitro or -NHj, Y is cyano, Ci-CealkyI, C^-Cehaloalkyl, Ci-Cghaloalkylthio or Ci-Cghaloalkylsulfonyl. (8) 4-Hydroxyiminomethyl substituted benzamide compound of formula (3) or a salt thereof: ^^f ^' (3) II . w wherein A^ is carbon atom or nitrogen atom, J is hydrogen atom or halogen atom, W is oxygen atom or sulfur atom, Y is halogen atom, cyano, nitro, Ci-C4alkyl, Ci-C4haloalkyl, Ci-C4alkoxy, C^¬C4haloalkoxy, Ci-Cealkylsulfonyl, Ci-Cehaloalkylsuifonyl o^'-N(R'')R^ R^ is Ci-CgalkyI, Ci-Cealkyl arbitrarily substituted with R^^ Ca-CeCycloalkyl, C3¬Cgalkenyl, Ca-Cghaloalkenyl, Cs-Cgalkynyl, -N(R'°)R'^ D-8,D-10, D-13, D-15, D-18, D-21, D-34, D-35, D-50 or D-51, R^ is hydrogen atom, Ci-Ceaikyi, Ci-C4alkoxy Ci-C4alkyl, cyano Ci-Cgalkyl, C3¬ Csalkynyl, -C(0)R^ or -C(0)OR^^ R^ is -CHO, Ci-Ceaikyicarbonyl, Ci-Cehaloalkyicarbonyi, Ci-Cealkoxycarbonyl, C^- Ceaikylthfocarbonyl, C^-C^alkoxythiocarbonyl, C^-CeBlkyldithiocarhonyl, C^- Cgalkylsulfonyl or Ci-Cehaloalkylsulfonyl, R^ is hydrogen atom or C^-Cealkyl, R' is Ci-CealkyI, C^-Csalkoxy Ci-C^alkyi, Ci-Ceaikylthio CrC4alkyl, Cs-Cgcycloalkyl, Ca-Cgalkenyl or Cj-Cgalkynyl, R^^ is halogen atom, cyano, Cg-CecycloalkyI, Cg-CshaJocycloalkyl, Ci-C^lkoxy, C^-' Cehaloafkoxy, C^-Cgalkylsuifonyl, Ci-Cehaloalkylsulfonyl, Ci-Cealkylcarbonyl, -C(0)0R2^ -C(0)NHR'^ -C(0)N(R'')R'', -C(S)NH2, -C(R'>NOH, -C(R^']=N0R'°, phenyl, phenyl substituted with (Z)pi, D-1 to D-4, D-8 to D-38, D-47 to D-55, E-4 to E-7;!E-10, E-11 orE-32, D-1 to D-4, D-8 to D-38, D-47 to D-54 and D-55 are aromatic heterocyclic rings of the following formulae, respectively, (Z)p3 D-l D-2 (Z)p4 (Z)p4 ^N -^i^ D-9 D-10 •I (Z)p3 R' ^ ^N /) ^A ^ ^ (Z)p4 D-14 D-15 (Z)p4 (Z)p4 D-19 'I)-20 (Z)p3 R; ' \ / N D-24 D-25 (Z)p5 (Z)p5 ^S'^ -^^N'« D-29 D-30 D-3 (Z)p4 ^^ D-11 R'^ .^N D-16 D-21 R'' N D-26 (Z)p5 ^O'^ D-31 (Z)p3 (Z)p4 D-4 (2:)p4 ^ k D-12 R' ' ,A^) (Z)p4 D-17 (Z)p4 D-8 (Z)p4 j}). D-13 ^ > D-18 (Z)p4 • D-22 RJ ' ^ ^ ¬ D-27 (Z)p5 A' ^ D-32 , D-23 (Z)p5 N D-28 (Z)p5 A' ^ D-33 (Z)p5 (Z)p5 (Z)p3 (Z)p5 ^^0), > ^ >-N^ >-N^ (6), (^)p2 D-47 D-48 D-49 D-50 D-51 (Z)p3 (Z)p3 -"^^^ ^ N /^ N /"\/ D-52 D-53 D-54 D-55 Z is halogen atom, cyano, nitro, Ci-C-galkyl, Ci-Cghaloalkyl, Ci-Cgalkoxy, C,-Cghaloalkoxy, Ci-Cgalkylsulfonyl, Ci-Cehaloalkylsulfonyl, Ci-Cealkoxycarbonyl, -C(0)NH2,Ci-C6alkylaminocarbony(, di(Ci-C6alkyl)aminocarbonyl,-C(S)NH2, -S(0)2NH2, Ci-Cealkylaminosulfonyl or di(Ci-C6alky!)aminosulfonyl, when p1, p2, p3 or p4 is an integer of 2 or more, each Z may be identical with or different from each other, R^^ is Ci-Cealky!, phenyl or phenyl substituted with (Z)pi, E-4, E-5, E-10, E-11 or E-32 is a saturated heterocyclic ring of the following formulae, respectively o-^ trgii-, /—o o-h r\o o /'^ ^^"•'^^^ X]) ^J AoO (R'')q3 E-4 E-5 E-10 E-11 E-32 R^' is Ci-Cghaloalkyl, -C(0)R'', -C(0)OR^', phenyl, phenyl substituted with (Z)pi, D-3, D-4, D-21, D-47, D-50, D-51, D-53 or D-54, R^° is hydrogen atom or Ci-Cgaikyl, R22 is Ci-C^alkyl, R^' is Ci-Cgalkyl, Ci-Cghaloalkyl, Cs-CgCycloalkyl Ci-C4alkyl, Ca-CeCycloalkyI, C3¬ Cgalkenyl or Ca-Cgalkynyl, R^^ is hydrogen atom or Ci-Cgalky!, R^° is CrCeaikyl, R^' is CrCgalkyl, n is an integer of 0 or 1, with a proviso that n is 1 when R^ and R^ are methyl at the same time, p1 is an integer of 1 to 5, p2 is an integer of 0 to 4, ^_ p3 is an integer of 0 to 3, p4 is an integer of 0 to 2, p5 is an integer of 0 or 1, q2 is an integer of 0 to 3, and q3 is an integer of 0 to 2 (9) 4-Hydroxyiminomethyl substituted benzamide compound or the salt thereof as set forth in (8), wherein R^ is Ci-Cgaikyl arbitrarily substituted with R^^ Cg-CeCycloalkyI, Cg-Cgalkenyl, Cg-Cghaloalkenyl, Ca-Cgalkynyl, -N(R'°)R'^ D-8, D-10, D-13, D-15, D-18, D-21, D-34, D¬35, D-50orD-51, R"*^ is halogen atom, cyano, Ca-Cecycloalkyi, Cj-Cehalocycloalkyi, Ci-Cealkoxy, C^-Cghaloalkoxy, Ci-Cgalkylsulfonyl, Ci-Cghaloalkylsulfonyl, -C(0)GR^^ -C(0)NHR2^ -C(0)N(R'')R'^ -C(S)NH2, -C(R'>NOH, -C(R'0=NOR'°, D-1 to D-4, D-8 to D-38, D-47 to D-55, E-4, ErS, E-10, E-11 or E-32. (10) Substituted alkenyibenzene compound of formula (4); T J ^' (4) ' x^ wherein X^ is halogen atom, -SFg, Ci-Cghaloalkyl, hydroxy CrCghaloalkyl, Ci-Cealkoxy Ci-Cghaloalkyl, Ci-Cghaloalkoxy Ci-Cghaloalkyl, Cg-CghalocycloalkyI, Ci-Cghaloalkoxy, Ci-Cahaloalkoxy Ci-Cghaioalkoxy, Ci-Cehaloalkylthio, Ci-Cghaloalkylsulfinyl or C^- Cghaloalkyisulfonyl, X^ is hydrogen atom, halogen atom, cyano, nitro, Ci-Cgalkyl, Ci-Cghaloaikyl, -0R^ -OSOjR' or -S(0),R^ X"* is hydrogen atom, halogen atom, cyano, nitro, Ci-Cgalkyl, -OH, Ci-Cealkoxy or Ci-Cghaloalkoxy, R^ is Ci-Cgalkyl that is arbitrarily substituted with two or more arbitrarily halogen atoms, or Cj-Cghalocycloalky! with a proviso that in case where X"" is fluorine atom, chlorine atom or -CF3 and both X^ and X" are hydrogen atom, in case where both X^ and X^ are fluorine atom, and X" is hydrogen atom, and in case where both X^ and X^ are -CF3, and X' is hydrogen atom, R' is -CHF2, -CHFCI, -CHFBr, -CHCIj, -CFjCI, -CFaBr, -CFjl, -CFCI2, -CFCIBr, -CFBrs, -CCI3, Cz-Cghaloalkyl or Cs-CghalpcycloaJkyl, " R^ is Ci-Cgalkyl or CrCehaloalkyl, r is an integer of 0 to 2. (11) The substituted alkenylbenzene compound as set forth in (10), wherein X'' isi halogen atom, -SF5, Ci-CehaloalkyI, Ci-Cghaioalkoxy, Ci-Cehaloaikyjthio, C^-Cghaloalkylsulfinyl or Ci-CehaloalkylsuIfonyl, X^ is hydrogen atom, halogen atom, cyano, nitro, Ci-CealkyI, Ci-Cehaloalkyi, C^-Cgalkoxy, Ci-Cghaloalkoxy, Ci-Cgaikylthio or Ci-Cehaloaikyithio, X'' is hydrogen atom, halogen atom, cyano, nitro, methyl, -OH, C^-G^aikoxy or C^¬C4haloalkoxy, R^ is -GHF2, -CF3, -CF2CI, -CFzBr or -GF2CF3, with a proviso that in case where X^ is fluorine atom, chlorine atom or -GF3 and both X^ and X'' are hydrogen atom, in case where both X'' and X^ are fluorine atom, and X"* is hydrogen atom, and in case where both X^ and X^ are -CF3, and X^ is hydrogen atom, R^ is -CHF2, -GFjGI, -GFzBr or -GF2CF3. ii (12) A pesticide containing as an active ingredient one or more selected from isoxazoline-substituted benzamide compound and the salt thereof as set forth in (1) to (5). . '• (13) An agrochemical containing as an active ingredient one or more selected from isoxazoline-substituted benzamide compound and the salt thereof as set forth in (1) to (5). (14) An endo- or ecto-parasiticide for mammals or birds containing as an active ingredient one or more selected from isoxazoline-substituted benzamide compound and the salt thereof as set forth in (1) to (5). (15) An insecticide or acaricide containing as an active ingredientone or more selected from isoxazoline-substituted benzamide compound and the salt thereof as set forth in (1) to (5). Effect of the Invention [0009] The compound according to the present invention has an excellent insecticidal and acaricidal activity for many agricultural insect pests, spider mites, endo- or ecto-parasiticide for mammals or birds, and exerts a control effect sufficient for pest insects that acquire resistance against exiting insecticides. Further, the compound has little adverse affect on mammals, fishes and beneficial insects, and has a low persistency and a low impact on the environment. Therefore, the present invention can provide a useful and novel pesticide. "1 Best Mode for carrying out the Invention [0010] Active compounds used as the pesticide in the present invention are generally the compounds of formulae (1) to (5) mentioned above, and the compounds of formulae (6) to (11) mentioned above are novel production intermediates used for the production of these active compounds. These intermediates contain specific compounds themselves having control activity against specific pests that can be used as a control agent for the pest. [0011] In the compounds included in the present invention, some compounds have geometrical isomers of E-form and Z-form depending on the kind of substituents. The present invention includes these E-forms, Z-forms and mixtures containing E-form and Z-form in an arbitrary proportion. In addition, the compounds included in the present invention have optically active forms resulting from the presence of 1 or more asymmetric carbon atoms, and the present invention includes all optically active forms or racemates. Further, in the compounds of formula (1) according to the present invention, some compounds wherein R^ is hydrogen atom are present in tautonier, and the present invention includes these structures, II I w w. H [0012] The compounds included in the present invention can be converted to acid addition salts for example salts of hydrohalide acid such as hydrofluoric acid, hydrochloric acid, hydrobromic acid, hydriodic acid or the like, salts of inorganic adds such as nitric acid, sulfuric acid, phosphoric acid, chloric acid, perchloric acid or the like, salts of sulfonic acid such as methansulfonic acid, ethansulfonic acid, trufluoromethansulfonic acid, benzene sulfonic acid, p-toluene sulfonic acid or the like, salts of carboxylic acid suchfas formic acid, acetic acid, propionic acid, trifluoroacetic acid, fumaric acid, tartaric acid, oxalic acid, maleic acid, malic acid, succinic acid, benzoic acid, mandelic acid, ascorbic acid, lactic acid, gluconic acid, citric acid or the like, or salts of amino acid such as glutamic acid, aspartic acid or the like, according to a conventional method. [0013] The compounds included in the present invention can be converted to matal salts for example salts of alkali metal such as lithium, sodium, potassium, salts ' of alkaline earth metal such as calcium, barium, magnesium, or salts of aluminum, according to a conventional method. [0014] Hereinafter, concrete examples of each substituent shown in the specification are described. In the specification, "n-" means normal, "i-" means iso, "s-" nheans secondary, and "t-" means tertiary, and "Ph" means phenyl. , [0015] Halogen atom in the compounds of the present invention includes fiurorine atom, chlorine atom, bromine atom and iodine atom, in the interim, the indication of "halo" in the specification also means these halogen atoms. [0016] In the specification, the indication of "Ca-CbalkyI" means straight-chain or branched-chain hydrocarbon groups having carbon atom number of a to b, and includes for example methyl, ethyl, n-propyl, i-propyl, n-butyl, s-butyl, i-butyl, t-butyl, n-pentyl, 1-methylbutyl, 2-methylbutyl, 3-methyIbutyl, 1-ethylpropyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, neopentyl, n-hexyl, 1-methyIpentyl, 2-methylpentyl, 3-melhylpentyl, 4-methylpentyl, 1-ethylbutyl, 2-ethyIbutyl, 1,1-dimethylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl, 2,2-dimethylbutyl, 2,3-dimethylbutyl, 3,3'-dimethylbutyl, 1,1,2-trimethylpropyl, 1,2,2-trimethylpropyl, 1-ethyl-1-methylpropyI, 1-ethyl-2-methylpropyl, heptyl, 5-methyjhexyl, 2-ethylpentyl, octyl, 2-ethylhexyl, nonyl, 2-methyloctyl, decyl, 2-methyInonyl, undecyl, 2-methyldecyl, dodecyl and the like. It is selected from the scope of the indicated carbon atom number. [0017] In the specification, the indication of "Ca-Cbhaloalkyl" means straight-chain or branched-chain hydrocarbon groups having carbon atom number of a to b that a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted with a halogen atom (halogen atoms). In this case, if it is substituted with two or more halogen atoms, these halogen atoms may be identical with or different from each other. Concrete examples thereof are for example fluoromethyl, chloromethyi, difluoromethyl, dichloromethyl, trifluoromethyl, chlorodifluoromethyl, trichloromethyl, bromodifluoromethyl, 2-fluoroethyl, 2-chloroethyl, 2-bronnoethyi, 2,2-difluoroethyi, 2-chloro-2-fluorbethyl, 2,2-dichloroethyl, 2-bromo-2-fluoroethyl, 2-bromo-2-chloroethyl, 2,2,2-trifluoroethyl, 2-chloro-2,2-difluoroethyl, 2,2-dichloro¬2-fluoroethyl, 2,2,2-trichloroethyl, 2-bromo-2,2-difluoroethyl, 2-bromo-2-chloro¬2-fluoroethyl, 2-bromo-2,2-dichloroethyl, pentafluoroethyl, 2-fluoropropyl, 2-chloropropyl, 2-bromopropyl, 2,3-dichloropropyl, 2,3-dibromopropyl, 3,3,3-trifluoropropyl, 3-bromo-3,3-difluoropropyl, 2,2,3,3-tetrafluoropropyI, 2¬chloro-3,3,3-trifluoropropyl, 2,2,3,3,3-pentafluoropropyl, 2,2,2-trifluoro-¬1-trifluoromethyIethyl, heptafiuoropropyl, 1,2,2,2-tetrafluoro-1-trifluoromethy!ethyl, 2,2,3,3,4,4-hexafluorobutyl, 2,2,3,4,4,4-hexafluorobutyl, 2,2,3,3,4,4,4-heptafluorobutyl, nonafluorobutyl, 5-chloro¬2,2,3,4,4,5,5-heptafluoropentyl, and the like. It is selected from the scope of the indicated carbon atom number. [0018] In the specification, the indication of "hydroxy Ca-Cbalkyi" means straight-chain or branched-chain alkyl groups having carbon atom number of a to b that a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted with a hydroxy group (hydroxy groups). Concrete examples thereof are for example hydroxymethyl, 1-hydroxyethyi, 2-hydroxyethyl, 2-hydroxypropyl, 3-hydroxypropyl, 2-hydroxybutyl, and the like. It is selected from the scope of the indicated carbon atom number. [0019] In the specification, the indication of "cyano Ca-Cbalkyi" means straight-chain or branphed-chain alkyl groups having carbon atom number of a to b that a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted with a cyano group (cyano groups). Concrete examples thereof are for example cyanomethyl, 1-cyanoethyl, 2-cyanoethyl, 2-cyanopropyl, 3-cyanopropyl, 2-cyanobutyl, and the like, it is selected from the scope of the indicated carbon atom number. [0020] In the specification, the indication of "Ca-CbCydoalkyl" means cyclic hydrocarbon groups having carbon atom number of a to b, and can form 3-membered to 6-membered single ring or conjugated ring structure. In addition, each ring may be arbitrarily substituted alkyl group in the scope of the indicated carbon atom number. Concrete examples thereof are for example cyclopropyl, 1-methylcyclopropyI, 2-methylcyclopropyl, 2,2-dimethylcyclopropyl, 2,2,3,3-tetramethylcyclopropyl, cyclobutyl, cyclopentyl, 2-methyIcyclopentyl, 3-methylcycIopentyl, cyclohexyl, 2-methylcyclohexyl, 3-methylcyclohexyl, 4-methylcyclohexyl, bicyclo[2.2.1]heptan-2-yl and the like. It is selected from the scope of the indicated carbon atom number. [0021] In the specification, the indication of "Ca-Cbhalocycloalkyl" means cyclic hydrocarbon groups having carbon atom number of a to b that a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted with a halogen atom (halogen atoms), and can form 3-membered to 6-membered single ring or conjugated ring structure. In addition, each ring may be arbitrarily substituted alkyl group in the scope of the indicated carbon atom number. The substitution for halogen atom may be in the ring structure moiety, the side chain moiety or both of them. Further, if it is substituted with two or more halogen atoms, these halogen atoms may be identical with or different from each other. Concrete examples thereof are for example 2,2-dichlorocyclopropyl, 2,2-dibromocyclopropyl, 2,2-difluoro-1-methylcyclopropyl, 2,2-dichIoro-1-methylcyclopropyl, 2,2-dibromo¬1-methylcyclopropyl, 2,2-dichloro-3,3-dimethylcyclopropyl, 2,2,3,3-tetrafluorocycIobutyl, 2-trifluoromethylcyclohexyl, 3-trifluoromethylcyclohexyl, 4-trifluoromethylcyclohexyl and the like. It is selected from the scope of the indicated carbon atom number. [0022] In the specification, the indication of "Ca-Cbalkenyl" means straight-chain or branched-chain unsaturated hydrocarbon groups having carbon atom number of a to b and having 1 or more double bonds. Concrete examples thereof are for example vinyl, 1-propenyl, 1-methylethenyl, 2-propenyl, 2-butenyl, 1-methyl¬2-propenyl, 2-methyJr2-propenyl, 2-methyl-2-butenyl, 3-methyI-2-butenyl, 2-hexenyl, 2-methyl~2-pentenyl, 2,4-dimethyI-2,6-heptadienyI, 3,7-dimethyl-2,6-octadienyl, and the like. It is selected from the scope of the indicated carbon atom number. [0023] In the specification, the indication of "Ca-Cuhalolkenyl" means straight-chain or branched-chain unsaturated hydrocarbon groups having carbon atom number of a to b and having 1 or more double bonds, which a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted with a halogen atom (halogen atoms). In this case, if it is substituted with two or more halogen atoms, these halogen atoms may be identical with or different from each other. Concrete examples thereof are for example 2,2-dichlorovinyl, 2-fluoro¬2-propenyl, 2-chioro-2-propenyl, 2-bromo-2-propenyl, 3-bromo-2-propenyl, 3,3-difluoro-2-propenyl, 2,3-dichloro-2-propenyl, 3,3-dichloro-2-propenyl, 2,3-dibromo-2-propenyl, 2,3,3-trifluoro-2-propenyl, 1-trifluoromethylvinyl, 2,3,3-trichloro-2-propenyl, 2-bromo-2-butenyI, 3-bromo-2-methyl-2-propenyl, 4,4-difluoro-3-butenyl, 3,4,4-trifluoro-3-butenyl, 3-chioro-4,4,4-trifluoro-2-butenyl, and the like. It is selected from'the scope of the indicated carbon atom ..number. [0024] In the specification, -the indication of "Ca-CbCycloalkenyl" means cyclic unsaturated hydrocarbon groups having carbon atom number of a to b and having 1 or more double bonds, and can form 3-membered to 6-membered single ring or conjugated ring structure. In addition, each ring may be arbitr3rily substituted alkyl group in the scope of the indicated carbon atom number, and further the double bond may be either endo- or exo-form. Concrete examples thereof are for example 2-cyclopenten-1-yl, 3-cyclopenten-1-yl, 2-cyclohexen-1-yl, 3-cyclohexen-1-yl, bicycio [2.2.1]-5-hepten-2-yl and the like. It is selected from the scope of the indicated carbon atom number. [002)5] In the specification, the indication of "Ca-Cbhaloycloalkenyl" means cyclic unsaturated hydrocarbon groups having carbon atom number of a to b and having 1 or more double bonds, which a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted with a halogen atom (halogen atoms), and can form 3-membered to 6-membered single ring or conjugated ring structure. In addition, each ring may be arbitrarily substituted alkyl group in the scope of the indicated carbon atom number, and further the double bond may be either endo- or exo-form. The substitution for halogen atom may be in the ring structure moiety, the side chain moiety or both of them. Further, if it is substituted with two or more halogen atoms, these halogen atoms may be identical with or different from each other. Concrete exa^mples thereof are for example 2-chlorobicyclo [2.2.1]¬5-hepten-2-yl and the like. It is selected from the scope of the indicated carbon atom number. [0026] In the specification, the indication of "Ca-Cbalkynyl" means straight-chain or branched-chain unsaturated hydrocarbon groups having carbon atom number of a to b and having 1 or more triple bonds. Concrete examples thereof are for example ethynyl, 1-propynyl, 2-propynyl, 1-methyl-2-propynyI, 2-butynyl, 2-pentynyl, 1-methyl-2-butynyl, 2-hexynyl, and the like. It is selected from the scope of the indicated carbon atom number. [0027] In the specification, the indication of "Ca-Ct,halolkynyl" means straight-chain or branched-chain unsaturated hydrocarbon groups having carbon atom number of a to b and having 1 or more triple bonds, which a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted with a halogen atom (halogen atoms). In this case, if it is substituted with two or more halogen atoms, these halogen atoms may be Identical with or different from each other. Concrete examples thereof are for example 2-chloroethynyl, 2-bromoethynyl, 2-iodoethynyl, 3-chloro-2-propYnyl, 3-bromo-2-propynyl, 3-iodo-2-propynyl, and the like. It is selected from the scope of the indicated carbon atom number. [0028] In the specification, the indication of "Cg-Cbalkoxy" means alkyl-0- groups wherein the alkyl has carbon atom number of a to b, and includes for example methoxy, ethoxy, n-propyloxy, i-propyloxy, n-butyloxy, s-butyloxy, i-butyloxy, t-butyloxy, n-pentyloxy, n-hexyioxy and the like. It is selected from the"scope of the indicated carbon atom number. [0029] In the specification, the indication of "Ca-Cbhaloaikoxy" means haloalkyl-0- groups wherein the haloalkyI has carbon atom number of a to b, and incliides for example difluoromethoxy, trifluoromethoxy, chlorodifluoromethoxy, broniodifluoromethoxy, 2-fluoroethoxy, 2-chloroethoxy, 2,2,2-trifluoroethoxy, 1,1,2,2-tetrafluoroethoxy, 2-chloro-1,1,2-trifluoroethoxy, 2-bromo¬1,1,2-trifluoroethoxy, 2,2-dichloro-1,1,2-trifiuoroethoxy, pentafluoroethoxy, 2,2,2-trichloro-1,1-difluoroethoxy, 2-bromo-1,1,2,2-tetrafluoroethoxy, 2,2,3,3-tetrafluoropropyloxy, 1,1,2,3,3,3-hexafluoropropyloxy, 2,2,2-trifluoro¬1-trifluoromethylethoxy, heptafluoropropyloxy, 2-bromo¬1,1,2,3,3,3-hexafluoropropyloxy, and the like. It is selected from the scope of the indicated carbon atom number. [0030] In the specification, the indication of "Cg-Cbalkenyloxy" means alkenyl- O- groups wherein the alkenyl has carbon atom number of a to b, and includes for example 2-propenyloxy, 2-butenyloxy, 2-methyl-2-peopenyloxy, 3-methyl¬2-butenyIoxy, and the like. It is selected from the scope of the indicated carbon atom number. [0031] In the specification, the indication of "Ca-Cbhaloalkenyloxy" means haloalkenyl-0- groups wherein the halbalkenyl has carbon atom number of a to b, and includes for example 2-chloro-2-propenyl, 3-chloro-2-propenyl, 3,3-difluoro¬2-propenyl, 3,3-dichloro-2-propenyl, 2,3,3-trifluoro-2-propenyl, and the like. It is selected from the scope of the indicated carbon atom number. [0032] In the specification, the indication of "Ca-Cbalkylthio" means alkyl-S- groups wherein the alkyl has carbon atom number of a to b, and includes for example methylthio, ethylthio, n-propylthio, i-propylthio, n-butylthio, s-butylthio, i-butylthio, t-butylthio, n-pentyjthio, n-hexylthio and the like. It is selected from the scope of the indicated carbon atom number. [0033] In the specification, the indication of "Ca-Ct,haioalkylthio" means f haloalkyl-S- groups wherein the fialoalkyi has carbon atom number of a to b, and includes for example difluoromethylthio, trifluoromethylthio, bromodifluoromethylthio, 2,2,2-trifluoroethylthio, 1,1,2,2-tetrafiuoroethylthio, 1,1,2-trifluoro-2-chloroethylthio, pentafluoroethylthio, 2-bromo-1,1,2,2-tetrafluoroethylthio, heptafiuoropropylthio, 1,2,2,2-tetrafluoro-1-trifluoromethylthio, 1,2,2,2-tetrafluoro-1-trifluoroethylthio, nonafluorobutylthio, and the like. It is selected from the scope of the indicated carbon atom number. "-^ [0034] In the specification, the indication of "Cg-Cbalkylsulfinyl" means alkyl-S(O)- groups wherein the alkyl has carbon atom number of a to b, and includes for example methylsulfinyl, ethylsulfinyl, n-propylsulfinyl, i-propylsulfinyl, n-butylsulfinyl, s-butylsulfinyl, i-butylsulfinyl, t-butylsulfinyl, and the like. It is selected from the scope of the indicated carbon atom number. . [0035] In the specification, the indication of "Ca-Cbhaloalkylsulfinyl" means haloalkyl-S(O)- groups wherein the haloalkyi has carbon atom number of a to b, and includes for example difluoromethylsulfinyl, trifluoromethylsulfinyl, bromodifluoromethyisulfinyl, 2,2,2-trifluoroethylsulfinyl, 2-bromo¬1,1,2,2-tetrafluoroethylsulfinyl, 1,2,2,2-tetrafluoro-1-trifluoromethylethylsulfinyl, nonafluorobutylsulfinyl, and the like. It is selected from the scope of the indicated carbon atom number. [0036] In the specification, the indication of "Ca-Cbalkylsulfonyl" means alkyl-S02- groups wherein the alkyl has carbon atom number of a to b, and includes for example methanesulfonyl, ethanesulfonyl, n-propylsulfonyl, i-propylsulfonyl, n-butylsulfonyl, s-butylsulfonyl, i-butylsulfonyl, t-butylsulfonyl, n-pentylsulfonyl, n-hexylsulfonyl, and the like. It is selected from the scope of the indicated carbon atom number. [0037] In the specification, the indication of "Ca-Cbhaloalkylsulfonyl" means haloalkyl-SOj- groups wherein the haloalkyi has carbon atom number of a to b, and includes for example difluoromethanesulfonyl, trifluoromethanesulfonyl, chlorodifluoromethanesulfonyl, bromodifluoromethanesulfonyl, 2,2,2-trifluoroethanesulfonyl, 1,1,2,2-tetrafluoroethanesuIfonyl, 1,1,2-trifluoro¬2-chloroethanesulfonyi, and the like. It is selected from the scope of the indicated carbon atom number. [0038] In the specification, the indication of "Cg-Cbalkylamino" means amino groups, which either hydrogen atom is substituted with the above-mentioned alkyl 44 group having carbon atonn number of a to b, and includes for example methylamino, ethylamino, n-propyiamino, i-prdpylamino, n-butylamino, i-butylamino, t-butylamino, and the like. It is selected from.the scope of the indicated carbon atom number. [0039] In the specification, the indication of "di(Ca-Cbaikyl)amino" means amino groups, which both hydrogen atoms are substituted with the above-nientioned alkyl groups having carbon atom number of a to b that may be identical with or different from each other, and includes for example dimethylamino, ethyl(methyl)amino, diethylamino, h-propyl(methyl)amino, i-propyl(methyl)amino, di(n-propyt2amino, n-butyl(methyI)amino, i-butyl(methyl)amino, t-butyl(methyl)amino, and the like. It is selected from the scope of the indicated carbon atom number. [0040] In the specification, the indication of "Ca-Cbalkylcarbonyl" means alkyl-C(Q)- groups wherein the alkyl has carbon atom number of a to b, and includes for example CH,C(0}-, CH^CHfiiO)-, CH3CH2CH2C(0)-, (CH,)fiHC(0)-, . CH3(CH2)3C(0)-, (CH3)2CHCH2C(0)-, CH3CH2CH(CH3)C(0)-, (CH3)3CC(0)-, CH3(CH2)4C(0)-, CH3(CH2)5C(0)-, and the like. It is selected from the scope of the indicated carbon atom number. [0041] In the specification, the indication of "Ca-Cbhaloalkyicarbonyl" means haloalkyl-C(O)- groups wherein the haloalkyi has carbon atom number of a to b, and includes for example FCHsCCO)-, CICHjCCO)-, FsCHCCO)-, Cl2CHC(0)-, CFgCCO)-, CICF2C(0)-, BrCF2C(0)-, CCIsCCO)-, CF3CF2C(0)-, CICH2CH2CH2C(0)-, CF3CF2CF2C(0)-, CICH2C(CH3)2C(0)-, and the like. It is selected from the scope of the indicated carboni.atom number. [0042] In the specification, the indication of "Ca-CbCycloalkylcarbonyl" means cycloalkyl-C(O)- groups wherein the cycloalkyi has carbon atom number of a to b, and includes for example cyclopropyl-C(O)-, l-methylcyclopropyl-C(O)-, 2¬methycyclopropyl-C(O)-, 2,2-dimethycycIopropyl-C(6)-, 2,2,3,3¬tetramethycyclopropyl-C(O)-, cyclobutyl-C(O)-, cyclopentyl-C(O)-, cycIohexyl-C(O)-, and the like. It is selected from the scope of the indicated carbon atom number. [0043] In the specification, the indication of "Ca-Cbhalocycloalkylcarbonyl" means halocycloalkyl-C(O)- groups wherein the halocycloalkyi has carbon atom number of a to b, and includes for example 2,2-dichlorocyclopropyI-C(0)-, 2,2¬dibromocyclopropyl-C(O)-, 2,2-difluoro-1-methylcyclopropyl-C(0)-, 2,2-dichloro-1¬methylcyclopropyl-C(O)-, 2,2-d;bromo-1-methyIcyclopropytC(0)-, 2,2-dichloro-3,3¬dimethylcyclopropyl-C(O)-, and the like. It is selected from the scope of the indicated carbon atom number. [0044] In the specification, the indication of "Ca-Cbalkoxycarbonyi" means alkyl-O-C(O)- groups wherein the alkyl'has carbon atom number of a to b, and includes for example CHaOCCO)-, CHsCHsObiO)-, CHsCHzCHjOCCO)-, (CH3)2CHOC(0)-, CH3(CH2)30C(0)-, (CH3)2CHCH20C(0)-, (CH3)3COC(0)-, and the like. It is selected from the scope of the indicated carbon atom number. [0045] In the specification, the indication of "Ca-Cbhaloalkoxycarbonyl" means haloalkyl-O-C(O)- groups wherein the haloalkyi has carbon atom number of a to b, and includes for example CICHsCHjOCCO)-, CF3CH20C(0)-, and the like. It is selected from the scope of the indicated carbon atom number. [0046] In the specification, the indication of "Ca-Ct,alkylthiocarbonyl" means alkyl-S-C(O)- groups wherein the alkyl has carbon atom number of a to b, and includes for example CH3SC(0)-, CH3CH2SC(0)-, CHaCHjCHsSCCO)-, (CH3)2CHSC(0)-, CH3(CH2)3SC(0)-, (CH3)2CHCH2SC(0)-, (CH3)3CSC(0)-, and the like. It is selected from the scope of the indicated carbon atom number. [0047] In the specification, the indication of "Ca-Cbalkoxythiocarbonyl" means alkyl-O-C(S)- groups wherein the alkyl has carbon atom number of a to b, and includes for example CHgOCfS)-, CH3CH20C(S)-, and the like. It is selected from the scope of the indicated carbon atom number. [0048] In the specification, the indication of "Ca-Cbalkyldithiocarbonyl" means alkyl-S-C(S)- groups wherein the alkyl has carbon atom numberof a to b, and includes for example CH3SC(S)-, CH3CH2SC(S)-, and the like. It is selected from the scope of the indicated carbon atom number. [0049] In the specification, the indication of "Ca-Cbalkylaminocarbonyl" means carbamoyl groups, which either hydrogen atom is substituted with the above-mentioned alkyl group having carbon atom number of a to b, and includes for example CHaNHCCO)-, CHaCHsNHCCO)-, CH3CH2CH2NHC(0)-, (CH3)2CHNHC(0)-, CH3(CH2)3NHC(0)-, (CH3)2CHCH2NHC(0)-, CH3CH2CH(eH3)NHC(0)-, (CH3)3CNHC(0)-, and the like. It is selected from the scope of the indicated carbon atom number. [0050] In the specification, the indication of "Ca-CbCycloalkylaminocarbonyl" means carbamoyl groups, which either hydrogen atom is substituted with the above-mentioned cycloalkyi group having carbon atom number of a to b, and includes for example cyclopropyl-NHC(O)-, cyclobutyl-NHC(O)-, cyclopentyl-NHC(O)-, cyclohexyl-NHC(O)-, and the like. It is selected from the scope of the indicated carbon atom number. [0051] In the specification, the indication of "di(Ca-Cbalkyl)aminocarbonyi" means carbamoyl groups, which both hydrogen atoms are substituted with the above-mentioned alkyl group having carbon atom number of a to b that may be identical with or different from each other, and includes for example (CH3)2NC(0)-, CH3CH2N(CH3)C(0)-, (CH3CH2)2NC(0)-, (CH3CH2CH2)2NC(0)-, (CH3CH2CH2CH2)2NC(0)-, and the like. It is selected from the scope of the indicated carbon atom number. [0052] In the specification, the indication of "Ca-CbalkylaminothiocarB'onyl" means ' thiocarbamoyi groups, which either hydrogen atom is substituted with the above-mentioned alkyl group having carbon atom number of a to b, and includes for example CH3NHC(S)-, CH3CH2NHC(S)-, CH3CH2CH2NHC(S)-, (CH3)2CHNHC(S)-, CH3(tH2)3NHC(S)-, (CH3)2CHCH2NHC(S)-, CH3CH2CH(CH3)NHC(S)-, (CH3)3CNHC(S)-, and the like. It is selected from the scope of the Indicated carbon atom number. [0053] In the specification, the indication of "di(Ca-Cbalkyl)aminothiocarbonyl" means thiocarbamoyi groups, which both hydrogen atoms are substituted with the above-mentioned alkyl group having carbon atom number of a to b that may be identical with or different from each other, and includes for example (CH3)2NC(S)-, CH3CH2N(CH3)C(S)-, (CH3CH2)2NC(S)-, (CH3CH2CH2)2NC(S)-, (CH3CH2CH2CH2)2NC(S)-, and the like. It is selected from the scope of the indicated carbon atom number. [0054] In the specification, the indication of "Ca-Cbalkylaminosulfonyl" means sulfamoyi groups, which either hydrogen atom is substituted with the above-mentioned alkyl group having carbon atom number of a to b, and includes for example CH3NHSO2-, CH3CH2NHSO2-, CH3CH2CH2NHSO2-, (CH3)2CHNHS02-, CH3(CH2)3NHS02-, (CH3)2CHCH2NHS02-, CH3CH2CH(CH3)NHS02-, (CH3)3CNHS02, and the like. It is selected from the scbpe of the indicated carbon atom number. [0055] In the specification, the indication of "di(Ca-Cbalkyl)aminosulfonyl" means sulfamoyi groups, which both hydrogen atoms are substituted with the above-mentioned alkyl group having carbon atom number of a to b that may be identical with or different from each other, and includes for example (CH3)2NS02-, CH3CH2N(CH3)S02-, (CH3CH2)2NS02-, (CH3CH2CH2)2NS02-, (CH3CH2CH2CH2)2NS02-, and the like. It is selected from the scope of the indicated carbon atom number. [0056] In the specification, the indication of "di(Ca-Cbalkyl)phosphoryl" means phosphoryl groups, which both hydrogen atoms are substituted with the above-mentioned alky! group having carbon atom number of a to b that may be identical with or different from each other, and includes for example (CH30)2P(0)-, (CH3CH20)2P(0)-, and the like, it is selected from the scope of the indicated carbon atom number. [0057] In the specification, the indication of "di(Ca-Cbalkyl)thiophosphoryl" means thiophosphoryl groups, which both hydrogen atoms are substituted with the above-mentioned alkyl group having carbon atom number of a to b that may be identical with or different from each other, and includes for example (CH30)2P(S)-, (CH3CH20)2P(S)-, and the like. It is selected from the scope of the indicated carbon atom number. [00^8] In the specification, the indication of "tri(Ca-Cbalkyl)silyl" means silyl groups substituted with the above-mentioned alkyl group having carbon atom number of a to b that may be identical with or different from each other, and includes for example trimethylsilyl, triethylsilyl, tri(n-propyl)silyl, ethyldimethyisilyl, n¬propyldimethylsiiyl, n-butyldimethylsilyl, i-butyldimethylsilyl, t-butyldimethylsilyl, and the like. It is selected from the scope of the indicated carbon atom number. [0059] In the specification, the indication of "Cg-Cbalkylcarbonyloxy" means alkyicarbonyl-0- groups wherein the alkyl has carbon atom number of a to b, and includes for example CH3C(0)-0-, CH3CH2C(0)-0-, GH3CH2CH2C(0)-0-, (CH3)2CHC(0)-0-, CH3(CH2)3C(0)-0-, (CH3)2CHCH2C(0)-0-, CH3CH2CH(CH3)C(0)¬0-, (CH3)3CC(0)-0-,'and the like. It is selected from the scope of the indicated carbon atom number. [0060] In the specification, the indication of "Cg-Cbalkylsulfonyloxy" means alkylsulfonyl-0- groups wherein the alkyl has carbon atom number of a to b, and includes for example CH3SO2-O-, CH3CH2SO2-O-, CH3CH2CH2SO2-O-, (CH3)2CHS02-0-, and the like. It is selected from the scope of the indicated carbon atom number. [0061] In the specification, the indication of "Cg-Cbhaloalkylsulfonyloxy" means haloalkylsulfonyl-0- groups wherein the haloalkyI has carbon atom number of a to b, and includes for example difluoromethanesulfonyl-0-, trifluoromethanesulfonyl-0-, chlorodifluoromethanesulfonyl-O-, bromodifluoromethanesulfonyl-O-, and the like. It is selected from the scope of the indicated carbon atoni number. [0062] In the specification, the indication of "Ca-Ct,cycloalkyl Cd-CealkyI", "Cg-Cbhalocycioalkyl C,-Cealkyl", "Cg-Cbalkoxy C^-Cealkyl", "C^-Cbhaloalkoxy Cd-CealkyI", "benzyloxy Cd-Cealkyl", "Cg-Cbalk^/lthio Cd-CealkyI", "C^-Cbhaloalkylthio Cd-CealkyI", "phenylthio Cd-CealkyI", "phenylth'io C^-Cealkyl substituted with {Z)^;', "C3¬ Cbalkylsulfinyl C,-Cealkyl", "Cg-ghaloalkylsulfinyl Cd-Cealkyl", "Cg-Cbaikylsulfonyl C^¬ C^alkyl", "Cg-Cbhaioalkylsulfonyl Cd-Cealkyl", "C3-Ct,alkylcarbonyl C^-Cealkyi", "C3¬ Cbhaloalkylcarbonyl Cd-C,alkyl", "Cg-Cbalkoxycarbonyl Cd-Cealkyl", "Cg- Cbinaloalkoxycarbonyl Cd-Cgalkyl", "Ca-Cbalkylaminocarbonyl Cd-Ceaikyi", "cli(Ca- Cbalkyl) aminocarbonyl Cd-CealkyI", "tri(Ca-Cbaikyi) silyl Cd-CealkyI", "phenyl C^- Cealkyl", "phenyl C^-Cealkyl substituted with {Z^^', "Cd-CealkyI substitute^__with any one of D-1 to D-60" or "Cd-CealkyI substituted with any one of E-1 to E-49" means straight-chain or branched-chain hydrocarbon groups having carbon atom number of d to e, which a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrlarily substituted with the Cg-CbCycloalkyl, Cg-Cbhalocycloalkyl, Cg-Cbalkoxy, Cg- Cbhaloalkoxy, benzyloxy, Cg-Cbaikylthio, Ca-Cbhaloalkyithio, phenylthio, phenylthio substituted with (Z)pi, Cg-Cbalkylsulfinyl, Cg-Cbhaloalkylsulfinyl, Cg-Cbalkylsulfonyl, Ca-Cbhaloalkylsulfonyl, Cg-Cbalkylcarbonyl, Cg-Cbhaloalkylcarbonyl, Cg¬'"t^bl'tkoxycarbonyl, Ca-Cbhaloalkoxycarbonyl, Ca-Cbalkylaminocarbonyl, di(Ca-Cbalkyl) aminocarbonyl, tri(Ca-Cbalkyl) silyl, phenyl, phenyl substituted with (Z)pi, D-1 to D-60 or E-1 to E-49 that has the meaning mentioned above, respectively. It is selected from the scope of the indicated carbon atom number. [0063] In the specification, the indication of "Cg-Cbalkyl arbitrarily substituted with R'", "Ca-CbalkyI arbitrarily substituted with R^'", "Ca-CbalkyI arbitrarily substituted with R^'*" or "Cg-Cbalkyl arbitrarily substituted with R^^" means straight-chain or branched- chain hydrocarbon groups having carbon atom number of d to e, which a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted with R^ R^^, R^'' or R^^. It is selected from the scope of the indicated carbon atom number. In this case, when two or more substituents R^ R''®, R^'' or R^^are present on the Ca- Cbalkyl, respective R^ R^^ R^"* or R^^may be identical with or different from each other. [0064] In the specification, the indication of "Ca-Cbhaloalkoxy Cd-CehaloalkyI" means the haloalkyi having carbon atom number of d to e, which a hydrogen atom (hydrogen atoms) or a halogen atom (halogen atoms) bonded to carbon atom is (are) arbitrarily substituted with the Cg-Cbhaloalkoxy, and includes for example 2,2,2¬ trifluoro-1 -(2,2,2-trifluoroethoxy)-1 -(trifluoromethyl)ethyl, 3(1,2-dichloro-1,2,2¬ trifluoroethoxy)-1,1,2,2,3,3-hexafluoropropyl, and the like. It is selected from the scope of the indicated carbon atom number. [0065] In the specification, the indication of "Cg-Cbalkenyl Cd-CeCycioalkyI" or "Ca-Cbhaloallalkyl groups having carbon atom number of a to b, which a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted with R\ R•'^ R2^ or R^l The substitution for R^ R^^ R^^ or R^^ may be in the ring structure moiety, the side chain moiety or both of them. In this case, when two or more substituents R^ R^^ R^^ or R^^are present on the Ca-CbCycloalkyI, respective R^ R^^ R^"* or R^^may be identical with or different from each other. [0067] In the specification, the indication of "phenyl Ca-Cbalkenyl" or "phenyl Cg-Cbaikenyl substituted with (Z)pi" means the alkenyl having carbon atom number of a to b, which a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted phenyl or phenyl substituted with (Z)pi. It is selected from the scope of the indicatefl carbon atom number. [0068] In the specification, the indication of "Cg-Cbalkenyl arbitrarily substituted with R'", "Cg-Cbalkenyl arbitrarily substituted with R^'", "Ca-Cbalkenyl arbitrarily substituted with R^^" or "Cg-Cbalkenyl arbitrarily substituted with R^^" means the alkenyl groups having carbon atom number of a to b, which a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted with R"*, R''^ R^'' or R^l It is selected from the scope of the indicated' carbon atom number. In this case, when two or more substituents R"*, R^^, R^'' or R^^ are present on the Cg-Cbalkenyl, respective R\ R^^ R^'' or R^^may be identical with or different from each other. [0069] In the specification, the indication of "phenyl Cg-Cbalkynyl" or "phenyl Cg-Cbalkynyl substituted with (Z)pi" means the alkynyl having carbon atom number of a to b, which a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted phenyl or phenyl substituted with {Z)^^. It is selected from the scope of the indicated carbon atqm number. [0070] In the specification,^thg indication of "Ca-Cbalkynyl arbitrarily substituted with R'", "Cs-Cbalkynyl arbitrarily substituted with R'^", "Ca-Cbalkyny! arbitrarily substituted with R^""' or "Cg-Cbalkynyl arbitrarily substituted with R^^" means the alkynyl groups having carbon atom number of a to b, which a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted with R^ R^^ R^** or R^^ It is selected from the scope of the indicated carbon atom number. In this case, when two or more substituents R^ R''^ R^'' or R^^ are present cm the Cg-Cfcalkenyl, respective R^ R''^ R^"* or R^^may be identical with or different from each other. [0071] In the specification, the indication of "phenyl Cg-Cbalkoxy" or "phenyl Ca-C't|alkoxy substituted with (Z)pi" means the Ca-Ctalkoxy, which a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted phenyl or phenyl substituted with (Z)pi. The concrete examples of Ca-Cbalkoxy are for example -CH2O-, -CH(CH3)0-, -C(CH3)20--, -CH2CH2O-, -CH(CH3)CH20-, -C(CH3)2CH20-, and the like, it is selected from the scope of the indicated carbon atom number. [0072] In the specification, the indication of "phenyl Ca-Cbalkylcarbonyl" or "phenyl Cg-Cbalkylcarbonyl substituted with (Z)pi" means the Cg-Cbalkylcarbonyl, which a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted phenyl or phenyl substituted with (Z)pi. The concrete examples of Cg-Cbalkylcarbonyl are for example -CH2C(0)-, -CH(CH3)C(0)-, -C(CH3)2C(0)-, -CH2CH2C(0)-, -CH(CH3)CH2C(0)-, -C(CH3)2CH2C(0)-, -CH2CH(CH3)C(0)-, -CH2C(CH3)2C(0)-, -CH2CH2CH2C(0)-, and the like. It is selected from the scope of the indicated carbon atom number. [0073] In the specification, the indication of "phenyl Ca-Cbalkoxycarbonyl" or "phenyl Ca-Cbaikoxycarbonyl substituted with (Z)pi" means the Ca-Cbaikoxycarbonyl, which a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted phenyl or phenyl substituted with {Z)^^. The concrete examples of Cg-Cbalkoxycarbonyl are for example -CH20-C(0)-, -CH(CH3)0-C(0)-, ¬C(CH3)20-G(0)-, -CH2CH20-C(0)-, -CH(CH3)CH20-C(0)-, -C(CH3)2CH20-C(0)-, and the like. It is selected from the scope of the indicated carbon atom number. [0074] In the specification, the indication of "phenyl Ca-Cbalkylaminocarbonyl" or "phenyl Ca-Cbalkylaminocarbonyi substituted with (Z)p/' means the Cg-Cbalkylaminocarbonyl, which a hydrogen atom (hydrogen atoms) bonded to carbon atom is (are) arbitrarily substituted phenyl or phenyl substituted with {Z)^^. The concrete examples of Ca-Cbalkylaminocarbonyl are for example -CHjNH-CCO)-, -CH(GH3)NH-C(0)-, -C(CH3)2NH-C(0)-, -CH2CH2NH-C(0)-, -CH(CH3)CH2NH-C(0)-, C(CH3)2CH2NH-C(0)-, and the like, (t is selected from the scope of the indicated carbon atom number. [0075] In the specification, concrete examples of the indication of "R'' and R^ together may form 3- to 8-membered ring together with the nitrogen atom bonding them by forming Cj to C7 alkylene chain, in this case, the alkyiene chaimnay contain ' one oxygen atom, sulfur atom or nitrogen atom", "R^° together with R^ may form 3- to 7-membered ring with the nitrogen atom bonding them by forming Cj-Cgalkyiene chain, in this case, the alkylene chain may contain one dxygen atom, sulfur atom or nitrogen atom", "R^^ together with R" may form 5- to 8-membered ring with the nitrogen atom . bonding them by forming C4-C7alkylene chain, in this case, the alkylene chain may contain one ox7gen atom or sulfur atom", "R^^ together with R^^ may form 3- to 6-membered ring with the nitrogen atom bonding them by forming Cz-Cgalkylene chain, in this case, the alkylene chain may contain one oxygen atom or sulfur atom", "R^^ together with R^® may form 3- to 6-membered ring with the nitrogen atom bonding them by forming Ca-Cgalkylene chain, in this case, the alkylene chain may contain one oxygen atom, sulfur atom or nitrogen atom", "R^"* together with R^^may form 3- to 6-membered ring with the nitrogen atom bonding them by forming Ca-CgaJkylene chain, in this case, the alkylene chain may contain one oxygen atom or sulfur atom", are for example aziridine, azetidine, pyrrolidine, oxazoiidine, thjazoridine, imidazolidine, piperidine, morphoiine, thiomorpholine, piperazine, homopiperidine, heptamethyleneimine, and the like. It is selected from the scope of the indicated carbon atom number. [0076] In the specification, concrete examples of the indication of "R^ together with R® may form 3- to 7-membered ring with the nitrogen atom bonding them by forming Cs-Cgalkylene chain, in this case, the alkylene chain may contain one oxygen atom, sulfur atom or nitrogen atom" are for example aziridine, azetidine, azetidin-2-one, pyrrolidine, pyrrrolidin-2-one, oxazoiidine, oxazoIidin-2-one, thiazoridine, thiazoridin-2-one, imidazolidine, imidazolidin-2-one, piperidine, piperidin-2-one, morphoiine, tetrahydro-1,3-oxadin-2-one, thiomorpholine, tetrahyciro-1,3-thiazin-2-one, piperazine, tetrahyclropyrimiciin-2-one, homopiperidine, homopiperidin-2-one, and the life. It is selected from the scope of the indicated carbon atom number. [0077] In the specification, concrete examples of the indication of "R'''' together with R^ may form 5- to 7-membered ring with the nitrogen atom bonding them by forming C2-C4alkylene chain, in this case, the alkylene chain may contain one oxygen atom, sulfur atom or nitrogen atom" are for example isoxazoline, oxazoline, thiazoline, imidazoline, 1,4,2-dioxazoline, 1,4,2-oxathiazorme, 1,2,4-oxadiazoline, dihydro-1,2-oxadine, dihydro-1,3-oxadine, dihydro-1,3-thiazine, 3,4,5,6-tetrahydropyrimidine, dihydro-1,4,2-dioxadine, dihydro-1,4,2-oxathiazine, dihydro-4H-1,2,4-oxadiazine, tetrahydro-1,2-oxazepine, and the like. It is selected frorri the scope of the indicated carbon atom number. [0078] In the specification, concrete examples of the indication of "R^^ together with R^° may form 5- to 7-membered ring with the nitrogen atom bonding them by forming C2-C4alkylene chain, in this case, the alkylene chain may contain one oxygen atom, sulfur atom or nitrogen atom" are for example oxazoline, thiazoline, imidazoline, dihydro-1,3-oxazine, dihydro-1,3-thiazine, 3,4,5,6-tetrahydropyrimidine, dihydro-1,4,2-dioxadine, and the like. It is selected from the scope of the indicated carbon atom number. [0079] In the compounds included in the present invention, the combination of the atoms of A\ A^ and A^ includes for example the following groups. That is, A-l: A\ A^ and A^ are carbon atoms. A-li: A^ is nitrogen atom, A^ and A^ are carbon atoms. A-I!l: A^ is nitrogen atom, A^ and A^ are carbon atoms. A-IV: A^ and A^ are nitrogen atonn, A^ is carbon atom. A-V: A^ and A^ are nitrogen atom, A^ is carbon atom. [0080] In the compounds included in the present invention, the substituent G includes for example aronnatic 6-membered rings shown in any one of G-1 to G-10 and aromatic 5-membered rings shown in any one of G-11 to G-25. Among them, aromatic 6-membered rings shown in G-1, G-3 and G-4 and aromatic 5-membered rings shown in any one of G-13, G-14, G-17, G-18, G-20, G-21 and G-22 are preferable, and aromatic 6-membered ring shown in G-1 is particularly preferable. [0081] In the compounds included in the present invention, the substituent W includes for example oxygen atom or sulfur atom. [0082] In the compounds included in the present invention, the substituent X includes for example the following groups, in eacli case mentioned below, wlien m is an integer of 2 or more, Xs ma) be identical with or different from each other. That is, X-l: halogen atom and C'l.Cehaloalkyl. X-ll: halogen atom, Ci-Cgalkyl, Ci-Cghaloalkyl, Ci-Cealkoxy, Ci-Cealkylsulfonyloxy, Ci-Cgalkylthio, Ci-Cgalkylsulfinyl and Ci-Cealkylsulfonyl. X-Ill: halogen atom, Ci-Cghaloalkyl, Ci-Cghaloalkoxy, C^-Cahaloalkoxy C^-Cahaloalkoxy, Ci-Cghaloalkylsulfonyloxy, Ci-Cghaloalklylthio, Ci-Cehaloaikylsulfinyl and Ci-Cehaloalkylsulfonyl. '"^ , X-IV: halogen atom, Ci-Cghaloalkyl, cyano, nitro, -SF5 and -Si(R^^)(R^^)R^2 wherein R^^ is C^-Cealkyl, phenyl or phenyl substituted with (Z)pi, R^^ and R^'' independently of each other are C^-Cealkyl. X-V:'.halogen atom and Ci-Cgalkyl arbitrarily substituted with R" wherein R"* is halegen atom, cyano, -OH, Ci-Cealkoxy, Ci-Cghaloalkoxy, Ci-Cgalkylthio, C^-Cghaloalkylthio, Ci-Cgalkylsulfinyl, Ci-Cehaloalkylsulfinyl, Ci-Cgalkylsulfonyl, C^-Cghaloalkylsulfonyl ortri(Ci-C6alkyl)silyl. X-VI: halogen atom, Ci-Cghaloalkyl, Ca-CaCycloalkyl, Cj-CshalocycloalkyI, Cj-Cealkenyl, Cj-Cehaloalkenyl, Cj-Cgalkynyl, Cj-Cghaloalkynyl, E-10, E-12, E-18, E-32, E-35 andE-43. X-VIl: halogen atom, Ci-CehaloalkyI, -0R^ -OSOjR^ and -S(0)rR^ wherein R^ is C^-Cgalkyl, Ci-Cghaloalkyl, Ci-Cghaloalkoxy Ci-CahaloalkyI, Cs-CaCycloalkyl, C3¬Cghalocycloalkyl, C2-Cealkenyl, Cj-Cehaloalkenyl, Ca-Cgalkynyl, Ca-Cehaioalkynyi, E-4 to E-9, E-23 to E-27 or E-28, r is an integer of 0 to 2. X-VIII: halogen atom, Ci-CehaloalkyI, -C(0)OR^ -C(0)SR^ -C(S)OR^ -C(S)SR^ ¬C(S)NHR^°, -C(S)N(R^°)R^ -CH=NOR'' and -C(R')=NOR'^ wherein R' is Ci-CealkyI, Ci-CehaloalkyI, Cg-Cgcycloaikyl or Ca-Cghalocycioalkyi, R^° is hydrogen atom or C^-Ceaikyl, or R^° together with R^ may form 5- or 6-membered ring with the nitrogen atom bonding them by forming C^-Cgalkylene chain, in this case, the alkylene chain may contain one oxygen atom or sulfur atom, R^^ is Ci-Cgalkyl or Ci-Cghaloalkyl, or R^^ together with R^may form 5- or 6-membered ring with the atom bonding them by forming Cj-Caalkylene chain, in this case, the alkylene chain may be arbitrarily substituted with Ci-Cgaikyl. X-IX: m is 2, two adjacent Xs form 5- or 6-membered ring with the carbon atom bonding them by forming -CF2OCF2-, -OCF2O-, -CF2OCF2O- or -OCF2CF2O-. [0083] In the compounds included in the present invention, m indicating the number of substituent X is an integer of 0 to 5. Among them, m is preferably 1, 2 and 3. [0084] In the compounds included in the present invention, the substituent Y includes for example the following groups. In each case mentioned below, when n is an integer of 2 or more, Ys may be identical with or different from each other. That is, Y-l: halogen atom, Ci-Cgalkyl and C^-Cehaloalkyl. Y-[l: halogen atom, C.-Cealkyl, cyano, nitro, -C(0)NH2 and -C(S)NH2. Y-lll: halogen atom, Ci-Cgalkyl and C^-Cgalkyl arbitrarily substututed with C^-Cealkyl and R" wherein R'' is halogen atom, cyano, -OH, Ci-Cgalkoxy, Ci-Cehalqalkoxy, C^-' Cgalkylthio, Ci-Cehaloalkylthio, Ci-Cgalkylsuifinyl, Ci-Cehaloalkylsulfinyl, C^-Cealkylsulfonyl, Ci-Cghaloalkylsuifonyl or tri(Ci-C6alkyl)silyl. Y-IV: halogen atom, Ci-Cgalkyl, -OR', -OSO2R' and -S(0)rR' wherein R^ is Cr Cealkyl, CrCehaloalkyi, Ci-Cahaloalkoxy Ci-Cahaioaikyl, Ca-CsCycloalkyi, C3¬Cghalocycloalkyl, Cz-Cgalkenyl, Cs-Cghaloalkenyl, Ca-Cealkynyl, Cg-Cehaloalkynyl, E-4 to E-9, E-23 to E-27 or E-28, r is an integer of 0 to 2. Y-V: halogen atom, Ci-Cgalkyl, -NHR^ -N(R^)R^ wherein R' is Ci-CealkyI, Cr Cehaloalkyl, -S(0)2R^ -CHO, -C(0)R^ -C(0)OR^ -C(0)SR^ -C(S)OR^ or -G(S)SR^ R^ is hydrogen atom, Ci-Cgalkyl or Ci-CehaloalkyI, R^ is Ci-Cgalkyl, Ci-Cehaloaikyl, Ca-Cgcycloalkyi or Cg-Cghalocycloalkyl and -N=C(R^)OR^ wherein R^ is Ci-Cgalkyl, R^ is Ci-CgalkyI or Ci-Cghaloalkyl. Y-VI: halogen atom, nitro, Ci-Ceaikyi, Ci-Cehaioalkyl, Ci-Cealkyilhio, Ci-Cealkylamino and di(Ci-C6alkyl)amino. [0085] In the compounds included in the present invention, n indicating the number of substituent Y is an integer of 0 to 4. Among them, n is preferably 0 and 1. [0086] In the conipounds included in the present invention., the substituent R'' includes for example the following groups. That is, R^-l: Ci-Cgalkyl, C,-C6alkyl arbitrarily substitutedwith R^^ (wherein R^^ is halogen atom, Ca-Cecycloaikyl, Ca-Cehalocycloalkyl, phenyl, phenyl substituted with (Z)p„ D-1 to D-4, D-8 to D-38, D-47 to D-55, E-4 to E-12, E-18, E-19, E-32, E-35, E-43, M-2, M-3, M-5, M-8, M-9 or M-10), Cg-Cgcycloalkyi and Ca-Cehalocycioalkyi. R^-ll: Ci-Cgalkyl arbitrarily substituted with -OR^^ wherein R^^ is Ci-Cgalkyl, Ci-CehaloalkyI, Ci-Cealkyicarbonyl, Ci-Cealkoxycarbonyl, Ci-Cgalkylaminocarbonyl, di(Ci-Cealkyl)aminocarbonyl or Ci-Cealkylsulfonyl. R'-lll: Ci-Cgalkyl arbitrarily substituted with -N(R2^)R2S wherein R^' is Ci-Cgalkyl, Ci-Cghaioalky!, Ci-Cgalkylcarbonyl, Ci-Cgalkoxycarbonyl, Ci-Cealkylaminocarbonyl, diCCrCgalkyOaminocarbonyl or C^-Cealkylsulfonyl, R^^is hydrogen or.Ci-Cealkyl. R^-IV: Ci-CealkyI arbitrarily substituted with -S(0)rR2^ wherein R^^ is Ci-CealkyI, Ci-Cghaioalkyl or tri(Ci-C4aIkyi)silyl Ci-C^aikyl, r is an integer of 0 to 2. R'-V: Ci-Cealkyl arbitrarily substituted with R'^ wherein R^^ is cyano, -C(0)R^^ -C(0)OR^^ -C(0)NHR2^ -C(0)N(R^')R2«, -C(0)N(R^')OR'^ -C(S)NHR^^ -C(S)N(R'')R'^ -S02NHR^^ -SOMP^^')^^\ -C(R^^)=NOH, -C(R.^^)=NOR'°. -C(=NR'^)OR'° or -C(=NR'^)SR'°, R"' is CrCealkyI, Ci-Cehaioaikyl, Cs-Cgcycloaikyl CrC4alky(, Ci-Ceaikoxy C^-C^alkyl, Ci-Cgalkylthio Ci-C4alkyl, cyano Ci-(\alkyl, phenyl Ci-C4alkyl, phenyl Ci-C4alkyl substituted with (Z)pi, Ca-CeCycJoaikyl, Ca-Ceaikenyl, Ca-Cehaioalkenyl, Cs-Cgalkynyl, phenyl or phenyl substituted with (Z)pi, R^® is hydrogen atom, Ci-Cgalkyl, Ca-Cealkenyl or Cg-Cgalkynyl, R^° is Ci-Cgalkyl or Cg-CicycloalkyI Ci-C4alkyl, R^^is hydrogen atom or Ci-Cgalkyl, or R^'' together with R^° may for 5- or 6-membered ring with the atom bonding them by forming . Cz-Cgalkylene chain. R^-VI: Cg-Cealkenyl, Ca-Cehaioalkenyl, Ca-Ceaikynyl, Ca-Cehaioalkynyl, phenyl substituted with (Z)pi, D-8, D-10, D-11, D-13, D-15, D-17, D-18, D-21 to D-23, D-26, D-27, D-29to D-37, D-39, D-40, D-42; D-45, D-47, D-48, D-50, D-51, D-53, D-54, D-56, D-58, E-5, E-7 and E-9. R^-VII: -N(R'°)R''wherein R^' is CrCghaloalkyl, Cj-CeCycloalkyl, -C(0)R2^ -C(0)OR'^ -C{0)NHR2^ -C(0)N(R2^)R'^ -C(S)NHR'^ -C(S)N(R^')R'^ phenyl, phenyl substituted with (Z)pi, D-3, D-4, D-21, D-47, D-50, D-51,,D-53 or D-54, R'° is hydrogen atom, Ci-C^alkyl, Ci-C4alkoxy Ci-C4alkyl, Ci-C4aikylthio Ci-C4a[kyl, cyano Ci-Cgalkyl, Cg-Cealkenyi, Cg-Cealkynyl, -CHO, Ci-Cealkylcarbonyi, Ci-Cealkoxycarbonyl or Ci-Cgalkylsuifonyi, R^^ is Ci-Cgalkyl, Ci-Cehaioalkyl, Cs-CgCycloaikyl Ci-C4alkyl, CrCgalkoxy Ci-C4alkyl, Ci-Cealkylthjo Ci-C4alkyl, cyano Ci-Cgalkyl, phenyl Ci-C4alkyl, phenyl Ci-C4alkyl substituted with (Z)pi, Ca-CeCycloalkyl, Ca-Ceaikenyl, Cj-Cehaloalkenyl, Ca-Cgalkynyl, phenyl or phenyl substituted with (Z)pi, R^® is hydrogen atom, Ci-Cgalkyl, Ca-Cgalkenyl or Ca-Cgalkynyl. R'-VIII: Ci-Cgalkyl, Ci-Cghaloalkyl, C^-Cealkyl arbitrarily substituted with R^'(wherein R^^ is cyano, Ca-CsCycloalkyI, Cg-Cghalocycloalkyl, Ci-Cgalkoxy, Ci-Cehaloalkoxy, C^-Cgalkylthio, Ci-Cghaloalkylthio, Ci-Cgalkyisulfinyl, Ci-Cghaloalkylsulfinyl, C^-Cealkylsulfonyl, Ci-Cghaloalkylsulfonyl, Ci-Cgalkylcarbonyl, -C(0)0R2^ -C(0)NHR'', -C(0)N(R2^)R^^ -C(S)NH2, -C(R'^)=NOH, -C(R^^)=NOR'°, phenyl, phenyl substituted with (Z)pi, D-1 to D-4, D-8 to D-38, D-47 to D-55, E-4 to E-7, E-10, E-11 or E-32, R'' is Ci-CealkyI, C.-Cehaloalkyl, Cj-Cecycloalkyi Ci-C4alkyl, Ca-Cgcycloalkyl, C3¬ Cgalkenyl or Cs-Cgalkynyl, R^^ is hydrogen atom or Ci-CealkyI, R^° is Ci-CeBlkyl, R^^is hydrogen or Ci-CealkyI), Cg-CeCycloalkyI, Cs-Cealkenyl, Ca-CehaloaJkenyi', C3¬Cgalkynyl, -N(R'°)R^' (whereinRl' is Ci-CehaloalkyI, -C(0)R2^ -C(0)0R2s, phenyl, phenyl substituted with (Z)p,, D-3, D-4, D-21, D-47, D-50, D-51, D-53 or D-54, R'° is hydrogen atom or Ci-CealkyI, R^^ is C^-Cealkyl, Ci-Cghaloaikyl, Ca-CeCycioalkyl C^¬C^alkyl, Ca-Cecycloalkyi, Cj-Csalkenyi or Ca-Cgalkynyl), phenyl substituted with (Z)pi, D-8, D-10, D-13, D-15, D-18, D-21, D-34, D-35, D-50 and D-51. R^-IX: Ci-Cghaioalkyl, Ci-Cgalkyl arbitrarily substituted with R^^(whereirrR^^ is cyano,' Cg-Cgcycloalkyl, Ca-CehalocycloalkyI, Ci-Cgalkoxy, Ci-Cghaloalkoxy, Ci-Cgalkylthio, Ci-Cghaloalkylthio, Ci-Cgalkylsulfinyl, Ci-CghaJoalkylsulfinyl, Ci-Cealkyisulfonyl, C^-Cehaloalkylsulfonyl, C.-Cgalkylcarbonyl, -C(0)OR'^ -C(0)NHR'^ -C(0)N(R'')R'', ¬C(S)NH2, -C(R'0=NOH, -C(R2^)=N0R'°, phenyl substituted with (Z)p„ D-1 to D-4, D¬8 to D-38, D-47 to D-55, E-4 to E-7, E-10, E-11 or E-32, R^' is Ci-Cealkyi, C^-Cghaloalkyl, Ca-CeCycloalkyl Ci-C4alkyl, Cg-CeCycloalkyl, Cg-Cgalkenyl or C3¬Cgalkynyl, R^^ is hydrogen atom or Ci-Cgalkyl, R^° is Ci-Ceaikyl, R^^is hydrogen or Ci-Cgalkyl), Ca-Cgcycloalkyl, Cs-Cealkenyl, Ca-Cehaloalkenyl, Cs-CeaJkynyl, -N(R^°)R'' (wherein R^' is Ci-CehaloalkyI, -CiO)R^\ -C(0)OR'', phenyl, phenyl substituted with (Z)pi, D-3, D-4, D-21, D-47, D-50, D-51, D-53 or D-54, R^° is hydrogen atom or C^-Cgalkyl, R^^ is Ci-Cgalkyl, Ci-Cghaloalkyl, Ca-Cgcycloalkyi Ci-C4alkyl, Ca-CeCycloalkyl, Cs-Csalkenyl or Ca-Ceaikynyl), phenyl substituted with (Z)pi, D-8,, D-10, D-13, D-15, D-18, D-21, D-34, D-35, D-50 and D-51. R^-X: Ci-Cshaloalkyl.'CrCealkyl arbitrarily substituted with R^^(wherein R^^ is Ca-Cgcycloalkyl, Ci-Cgalkoxy, Ci-Cgalkylthio, Ci-Cealkylsulfinyl, Ci-Cealkylsulfonyl, -C(0)NH2, -C(0)NHR^^ -C(S)NH2, -C(R'^)=NOH, -CiR'')=NOR'°, D-1 to D-4, D-8 to D-38, D-47 to D-54, E-4 to E-7, E-10, E-11 or E-32, R^' is Ci-Qealkyl, C.-Cghaloalkyl, Ca-CeCycloalkyI, Cj-Cgalkenyl or Ca-Cgalkynyl, R^° is CrCgalkyl, R^^ is hydrogen or Ci-Cgalkyl), Ca-Cecycioalkyl, Ca-Cgalkenyl, Cs-Cshaioalkenyl, Cg-Cgaikynyl, -N(R^°)R^' (wherein R^^ is Ci-Cghaloalkyl, -C(0)R2^ ^C(0)0R2^ phenyl, D-3, D-4, D-21, D-47, D-50, D-51, D-53 or D-54, R^" is hydrogen atom or Ci-Cgalkyl, R^^ is Ci-Cgalkyl, Ci-Cghaloalkyl, Cs-CeCycloalkyI C^-C^alkyl, Cg-CsCycloalkyI, Cg-Cgalkenyl or Cg-Cgalkynyl), D-8, D-10, D-13, D-15, D-18, D-21, D-34, D-35, D-50 and D-51. R'-XI: Ci-Cgalkyl and phenyl Ci-Cgalkyl. R^-XII: Ci-Cgalkyl, Ci-CgalkyI arbitrarily substituted with R^^ (wherein R^^ is halogen atom, Ca-CecycloalkyI, Ca-CghalocycloalkyI, phenyl, phenyl substituted with (Z)pi, D-1 to D-4, D-8 to D-42, D-47 to D-55, E-4 to E-12, E-14, E-16 to E-19, E-21 to E-23, E¬ 26 to E-35, E-40 to E-45, E-48, M-2, M-3, M-5, M-8 to M-10, M-14, M-15 or M-16), Cg-CgCycloalkyl and Cj-Cghalocycioalkyl. R^-Xlll: Ci-Cgalkyl arbitrarily subvStituted witii -OR^^ wherein R^^ is hydrogen atom, C.-Cealkyl, C-Cehaloalkyl, -C(6)R'^ -C(0)OR''. -C(0)NHR^^ -C(0)N(R^^)R=^^ -C(S)NHR'^ -C(S)N(R'')R", -S(0)2R", -S(0)2N(R'')R'^ di(CrC6alkyl)thiophosphoryl, phenyl or phenyl substituted with (Z)pi, R^^ is Ci-CealkyI, Ci-Cehaioalkyl, Cs-Cecycloalkyl, Ca-Cehaiocycloalkyl, phenyl Ci-C4alkyl, phenyl Ci-C4alkyl substituted with (Z)pi, Cs-Cgalkeny!, Cg-Cealkynyl, phenyl or phenyl substituted with^(Z)pi, R^^is ¬hydrogen atom or Ci-Cealkyl. R^-XIV : CrCsalkyl arbitrarily substituted with -N(R'')R'' wherein R^' is Ci-Cgalkyl, Ci-Cehaloalkyl, -C{0)R'^ -C(0)OR", -C(0)SR'', -C(0)NHR'^ -C(0)N(R^OR'^ -C(vS)R'^ -C(S)OR'^ -C(S)SR'^ -C(S)NHR'\ -C(S)N(R'')R'^ -S(0)2R'' or -S(0)2N(R^'')R", R^^ is hydrogen atom or Ci-Cgalkyl, or R^^ together with R^'may form 4- to 6-membered ring with the nitrogen atom bonding them by forming Ca-Cjalkylene chain, in this case, the alkylene chain may contain one oxygen atom, sulfur atom or nitrogen atom, and may be substituted with Ci-Cgalkyl, oxo or thioxo, R^^ is Ci-Cgalkyl, Ci-Cghaloalkyl, Cs-CecycloalkyI, Cg-CehalocycloalkyI, phenyl Ci-C4alkyl, phenyl Ci-C4alkyl substituted with (Z)pi, Cg-Cealkenyi, Ca-Cealkynyl, phenyl or phenyl substituted with (Z)pi, R^" is hydrogen atom or Ci-Cgalkyl. R^-XV: Ci-Csalkyl arbitrarily substituted with -S(0)rR^^ wherein R^^ is Ci-Cgalkyl, Ci-Cghaloalkyl, tri(Ci-C4alky()si!yl CrC4alkyl, Ci-Cealkyithio, -C(0)NHR'^ -C{0)N(R'')R=^ -C(S)NHR=^ -C(S)N(R=^)R^^ phenyl, phenyl substituted with {Z\„ D-47 or D-50, R" is Ci-Cgalkyl, CrCehaloalkyI, Cj-Cgcycloalkyl, Ca-Cghalocycloalkyl, phenyl Ci-C4alkyl, phenyl Ci-C4alkyl substituted with (Z)pi, Cg-Cgalkenyl, Ca-Cgalkynyl, phenyl or phenyl substituted with {Z\^, R^^\s hydrogen atom or Ci-Cgalkyl, r is an integer of 0 to 2. R^-XVI : CrCsalkyl arbitrarily substituted with R^^ wherein R^^ is cyano, -S02NHR2^ -S02N(R'')R'', -CHO, -C(0)R'^ -C(0)OR'^ -C(0)NHR'^ -C(0)N(R2^)R2«, -C(S)NHR2^ -C(S)N(R2')R2«, -C(R^^)=NOH, -C(R'>NOR'°, -C(=NR=^)OR^°, -C(=NR'^)SR'°, -C(=NR'^)N(R'°)R^^ -C(=N0R'^)NHR2 ^ or-C(=NOR^^)N(R^°)R2^ R^« is Ci-Cgalkyl, Ci-Cgalkyl arbitrarily substituted with R^^ Cg-Cgcycloalkyl, Cg-CshalocycloalkyI, Ca-Cealkenyl, Cg-Cehaioalkenyl, Ca-Cgalkynyl,' Cj-Cghaloalkenyl, . phenyl or phenyl substituted with (Z)pi, R^^ is hydrogen atom, Ci-Cgalkyl, Cj-Cealkenyl or Cj-Cgalkynyl, or R^^ together with R^^ may form 3- to 6-membered ring with the nitrogen atom bonding them by forming C2-C5alkylene chain, in this case, the alkylene chain may contain one oxygen atom or sulfur atom, R^° is Ci-Cgall^yi, Ca-Cgcycloaikyl Ci-C43.ikyl, phenyl Ci-C4aikyl, phenyl CrC^alkyl substituted with (Z)pi, Cs-Cgalkenylor Cj-Cgalkynyl, R^^ is hydrogen atom or C^-Cealky!, or R^^ together with R^° may form 5- or 6-membered ring with the atom bonding them by forming Cj-Cgalkylene chain, in this case, the alkylene chain may be arbitrarily substituted with Ci-Cgalkyl, R^^ is halogen atom, cyano, Ca-CgCycloalkyl, , Cj-Cghalocycloalkyl, Ci-C4alkoxy, Ci-C^haloalkoxy, Ci-C4alkylthio, Ci-C^haloalkylthio, Ci-C^alkoxycarbonyl, -C(0)NH2, Ci-C^alkylaminocarbonyl, di(CTC4alkyl)aminocarbonyl, phenyl or phenyl substituted with (Z)pi. R'-XVll: Cs-Cgalkenyl, Ca-Cghaloalkenyl, Ca-Csalkynyl. Ca-Cghaloalkynyl, phenyl substituted with {Z)^„ D-8 to D-13, D-15 to D-18, D-21 to D-23, D-26, D-27, D-29 to D-37j D-39, D-40, D-42, D-45 to D-58, E-5, E-7, E-9, E-24, E-25, E-27, E-28, E-30, E-31 and E-34. R'-XVlll: -N(R'°)R'' wherein R" is Ci-Cgalkyl, Ci-Cghaloalkyl, Ca-Cecycioalkyl C^-Cgalkyl, phenyl Ci-CgalkyI, phenyl Ci-Cgalkyl substituted with (Z)pi, Ca-Cecycioalkyl, Ca-Cgalkenyl, Cs-Cghaloalkenyl, Cg-Cealkynyl, -C(0)R'^ -C(0)OR'^ -C(0)NHR'', ¬C(0)N(R'')R'^ -C(S)NHR2', -C(S)N(R'')R'^ Ci-Cealkylsuifonyi, C^-Cghaloalkylsulfonyl, phenylsulfonyl, phenylsulfonyl substituted with (Z)pi, phenyl, phenyl substituted with (Z)pi, D-1 to D-4, D-18, D-21, D-25, D-30 to D-35, D-47 to D¬55 or D-56, R^° is hydrogen atom, Ci-Cealkyi, Ci-C4alkoxy Ci-C4alkyl, Ci-C4alkylthio Ci-C4alkyl, cyano Ci-CgalkyI, Ca-Cealkenyl, Ca-Cgalkynyl, -CHO; Ci-Cealkylcarbonyl, Ci-Cehaioaikylcarbonyi, Ci-Cealkoxycarbonyl, Ci-Cehaloalkoxycarbonyl or C^-Cealkyisufonyl, R'^ is Ci-Cgalkyl, Ci-CgalkyI arbitrarily substituted with R'^, Cg-CeCycloalkyi, Cj-Cehalbcycioalkyl, Cj-Cgalkenyl, Cg-Cehaioalkenyl, Ca-Csalkynyl, C3¬ Cghaloalkynyi, phenyl or phenyl substituted with (Z)pi, R^^ is hydrogen atom, C^-Cgalkyl, Cj-Cgalkenyl or Cj-Cealkynyl, R^^ together with R^^ may form 3- to 6¬membered ring with the nitrogen atom bonding them by forming C2-C5alkylene chain, in this case, the alkylene chain may contain one oxygen atom or sulfur atom, R^^ is hydrogen atom, cyano, Ca-CgCycloalkyI, Ca-Cghalocycloalkyl, Ci-C4alkoxy, C^¬C4haloalkoxy, Ci-C4alkylthio, Ci-C4haloalkylthio, Ci-C4alkoxycarbonyl, -C(0)NH2, C^¬C4alkylaminocarbonyl, di(Ci-C4alkyl)aminocarbonyl, phenyl or phenyl substituted with (Z)p,. [0087] In the compounds included in the present invention, the substituent R^ includes for example the following groups. That is, R^-l: hydrogen atom. R^-ll: Ci-CealkyI, Ci-Cghaloaikyl and Ca-CeCycloalkyl. R^-lil: CrC4alkoxy Ci-C4alkyl, C^l-C^alkylthio Ci-C^alkyl and cyano Ci-Cgalkyl. R^-IV: Cs-Cgalkenyl and Ca-Cgalkynyl. R^-V: -OH, Ci-Cealkoxy, Ci-Cealkylcarbonyloxy, Ci-Cgalkoxycarbonyloxy and C^-Cgalkylsulfonyloxy. 'R^-VI: Ci-Cghaloalkylthio, phenylthio, phenylthio substituted with {Z\^ and -SN(R^®)R" wherein R" is Ci-Cgalkyl, Ci-Cgalkoxycarbonyl Ci-C4alkyl or Ci-Cgalkoxycarbony, R^^ is Ci-Cgalkyl or benzyl. R2-VII: -NHR'° (wherein R^° is hydrogen atom, C^-Cealkyl, -CHO, Ci-Cealkyicarbonyl, Ci-Cealkoxycarbonyl or C.-Cealkylsulfonyj), -N=CHR^"' and -N=C(R'^'')R^'' wherein R^'" is Ci-Cealkyi, R^"' is hydrogen atom or Ci-Cealkyl. R'-yill: -C(0)R^ -C(0)OR^ -C(0)SR^ -C(S)0R^ -C(S)SR' (wherein R' is CrCgalkyl, Ci-Cghaloalkyl, Ca-CgCycloalkyl CrC4alkyl, CrCealkoxy CrC4alkyl, Ci-Cgalkylthio C^¬C4alkyl, cyano Ci-Cealkyi, phenyl Ci-C4alkyl, Cj-CaCycloalkyI, Ca-Cghalocycloalkyl, Cs-Cgalkenyl or Cs-Cgalkynyl) and Ci-Cealkylsulfonyl. R^-IX: 3- to 7-membered ring that R^ forms together with R^ is aziridine, azetidine, pyrrolidine, oxazolidine, thiazoridine,.piperidine, morpholine, thiomorpholine and homopiperidine. R^-X: hydrogen atom, Ci-Cgalkyl, Ci-C4alkoxy Ci-C4alkyl, Ci-C4alkylthio Ci-C4alkyl, cyano Ci-Cgalkyl, Ca-CgCycloalkyl, Ca-Cealkenyl, Cg-Cgalkynyl, -OH, Ci-Cealkylcarbonyloxy, Ci-Cealkylsulfonyloxy, -NH2, -C(0)R^ -C(0)OR', -C(0)SR', -C(S)OR' and -C(S)SR' wherein R^ is Ci-Cgalkyl, Ci-CehaloalkyI, Ca-CeCycloalkyl Ci-C4alkyl, Ci-Cgalkoxy Ci-C4alkyl, Ci-Cealkyithio Ci-C4alkyl, cyano C^-Cealkyl, Cs-CgCycloalkyI, Cs-Cgalkenyl or Cg-Cealkynyl. R^-XI: hydrogen atom, Ci-Cgalkyl, Ci-C4alkoxy Ci-C4alkyl, cyano Ci-Cgalkyl, C3¬Cgalkynyl, -C(0)R' arid -C(0)OR' wherein R' is Ci-Cgalkyl, CrCgalkoxy Ci-C4alkyl, Ci-Cgalkylthio Ci-C4alkyl, Ca-CscycloalkyI, Ca-Cgalkenyl or Cg-Cealkynyl. [0088] In the compounds included in the present invention, the substituent R^ includes for example the following groups. That is, R^-l: Ci-CehaloalkyI and Ca-Cghalocycloalkyl. R'-ll: Ci-Cgalkyl, Cj-CgCycloalkyl, E-4 to E-7, E-23 to E-27 and E-28. R'-lll: Ci-C4a!koxy Ci-C4haloalkyl, Ci-C4haIoalkoxy Ci-C4haIoalkyl; Ci-C4aIkylthio C,¬C4haloalkyl, Ci-C4alkylsulfinyl Ci-C4haloalkyl, Ci-C4alkyIsulfonyl C,-C4haloalkyl, C^¬C4haloalkylthio Ci-C4haloalkyl, Ci-C4haloalkylsulfinyl Ci-C4haloalkyl, C^¬C4haloalkylsulfonyl Ci-C4haloalkyl and cyano Ci-Cehaloaikyl. R'-IV: Cs-Cecycloalkyi Ci-C4alkyl, Ca-Cehalocycloalkyi Ci-C4alkyl, Ci-C^alkoxy C^ C4a!kyi, Ci-C4haloalkoxy Ci-C^alkyl, C,-C4alkylthio Ci-C4alkyl, CrC4alkylsulfinyI C^ C4alkyl, Ci-C4alkylsuifonyl Ci-C4alkyl, CrC4haloalkylthio Ci-C4a!kyl, C,¬C4haloalkyIsuIfinyl Ci-C4alkyl, Ci-C4haloalkylsulfonyl Ci-C4aikyl and cyano Ci-Cgalkyl. R^-V: Ci-Cghaloalkyl, Ci-C4alkoxy CrC4haloalkyl, Ci-C4haloalkoxy Ci-C4haloa!kyl, Ci-C4alkylthio Ci-C4haloalkyl, Ci-C4haloalkylthio Ci-C4haloalkyl, cyano Ci-Cghaloalkyl and Ca-Cghalocycloalkyl. '^^ . R'-VI: Ci-Cghaloalkyl. R^-VII: Ci-CgBlkyl arbitrarily substituted with two or more arbitrary halogen atoms. [0089] Each group showing the scope of each substituent in the compounds inclucled in the present invention can be arbitrarily combined one another, and all combination thereof falls within the scope of the present invention. Examples of the . combination of the scope of X, Y and R^ include for example the combination showin in Table 1. In the meantime, the combination of Table 1 is for illustrative purposes, and the present invention is not limited thereto. Table 1 Table 1 (continued) X Y R' X Y R^ X-l Y-l R'-l X-lll Y-VI R^-ll X-l Y-l R'-ll X-lll Y-Vl R^-lll X-l Y-l ••' R'-lll X-lll Y-Vi R^-IV X-l Y-l R'-IV X-lll Y-VI Ri-V X-l Y-l R'-V X-ill Y-VI R^-VI X-l Y-l R'-VI X-lll Y-VI R^-VII X-l Y-l R'-VII X-lll Y-VI R^-VIII X-l Y-l ' R'-VIII X-lll Y-VI R^-JX X-l Y-l R'-IX X-lll Y-VI Ri-X X-l Y-l R'-X X-lll • Y-Vl R^-XI X-l Y-l R'-XI X-IV Y-l R^-l X-l Y-l I R'-l X-IV Y-l Ri-ll XM Y-ll R'-ll X-IV Y-l R^-lil X-l Y-ll R'-lll X-IV Y-l • R^-IV X-l Y-ll R'-IV X-IV Y-l R^-V X-l Y-ll R'-V X-IV Y-l R^-VI X-l Y-ll R'-VI X-IV Y-l Ri-VII X-l Y-ll R'-VIl X-IV Y-l R^-VIII X-l Y-ll R'-Vlll X-IV Y-l R^-IX X-l Y-ll R'-IX X-IV Y-l R^-X X-t Y-ll R'-X X-IV Y-l R^-Xl X-1 Y-ll R'-XI X-IV Y-l! R^-X X-I Y-l!l R M X-IV Y-lll R'-X X-1 Y-!II R'-Vil X-IV Y-IV R^-X X-[ Y-lll R'"-Vill X-IV Y-V Ri-X X-1 Y-lll R'-IX X-IV Y-Vl R^-l X-1 Y-lll R^-X X-IV Y-Vl R^-U X-1 Y-IV R'-I X-IV Y-Vl R^-III X-1 Y-IV R'-!l X-IV Y-Vl R^-IV X-1 Y-iV R'-m X-IV Y-Vl R^-V X-1 Y-IV R'-IV X-IV Y-VI Ri-VI X-1 Y-IV R'-V X-IV Y-Vl R^-VII X-1 Y-IV R'-VI X-IV Y-Vl R^-Vlll X-1 Y-IV R'-Vll X-IV Y-Vl R^-IX X-1 Y-IV R^-VIII X-IV Y-Vl R^-X X-l Y-IV R'-IX X-IV Y-Vl Ri-XI X-I Y-IV R'-X X-V Y-l R^-1 X-I Y-IV R'-XI X-V Y-l R^-VII X-I Y-V R'-l X-V Y-l R^-IX X-1 Y-V R'-ll X-V Y-l R^-X X-I Y-V R'-lll X-V Y-ll R^-X X-I Y-V R'-IV X-V Y-l II R^-X X-I Y-V R'-V X-V Y-IV R^-X X-1 Y-V R'-Vl X-V Y-V R^-X X-I Y-V R'-Vli X-V Y-Vl R^-l X-I Y-V R^-VIII X-V Y-Vl R^-VIl X-1 Y-V R'-IX X-V Y-Vl R^-IX X-I Y-V R'-X X-V Y-Vl Ri-X X-I Y-V R'-XI X-VI Y-l R^-l X-I Y-Vf R'-l X-VI Y-l R^-ll X-1 Y-Vl R'-ll X-VI Y-l R^-lll X-I Y-Vl" R'-III X-VI Y-l R^-IV X-I Y-Vl R'-IV X-VI Y-I R^-V X-1 Y-Vl R^-V X-Vl Y-i R^-Vl X-I Y-Vl R'-VI X-VI Y-l R^-Vll X-I Y-Vl R'-VII X-VI Y-l R^-VIII X-I Y-Vl R^-VIII X-VI Y-l R^-IX X-I Y-Vl R^-IX X-Vl Y-l Ri-X X-I Y-Vl R^-X X-VI Y-ll R^-X X-i Y-Vl R^-XI X-Vl Y-l 11 R^-X X-11 Y-i R'-l X-Vl Y-IV R^-X X-ll Y-I R'-II X-Vl Y-V R^-X X-I I Y-l R'-lll X-VI Y-Vl R^-l X-I I Y-I R'-!V X-VI Y-Vl R^-ll X-ll Y-l R'-V X-V! Y-Vl R^-Ill X-ll Y-l R'-VI X-VI Y-Vl R^-IV X-ll Y-1 R'-Vli X-V! Y-VI R^-V X-il Y-l R'-VIN X-VI Y-VI R^-VI X-ll Y-l R^-IX X-VI Y-Vl R^-V!l X-ll Y-l R^-X X-VI Y-Vi R^-VIII X-ll Y-il R^-X • X-VI Y-VI R^-IX X-ll Y-lll R^-X X-VI Y-VI R^--X X-ll Y-IV R'-X X-VI I Y-l R^-I X-Il Y-V R^-X X-Vll Y-! R^-11 X-!I Y-VI R'-l X-V!l Y-l R^-lll X-ll Y-VI R^-II X-VIl Y-l RL-IV X-ll Y-VI R^-lil X-VII Y-l R^-V X-ll Y-VI R'-IV X-VII Y-l R'-Vl X-ll Y-V! R'-V X-VIl Y-l R'-VII X-ll Y-VI R'-VI X-VII Y-l R^-Vlll X-ll Y-VI R'-VI! X-VII Y-l R'-IX X-ll Y-VI R'-Vlll X-Vll Y-l R^-X X-ll Y-VI R'-IX X-VII Y-ll R^-X X-ll Y-VI R'-X X-Vl! Y-lll R^-X X-lll Y-l R'-l X-Vll Y-IV R^-X X-lll Y-l R^-ll X-VII Y-V R^-X X-lll Y-l R'-lll X-VII Y-VI R'-l X-MI Y-l R'-IV X-VII Y-VI R'-li X-lll Y-! R^-V X-VII Y-VI R^-lll X-il I Y-l R^-VI X-VII Y-VI R^-IV X-lll Y-l R'-VII X-Vl! Y-Vl R'-V X-lll Y-l R'-VIII X-Vll Y-VI R^-VI X-lll Y-l R'-IX X-VII Y-Vl R'-VI! X-lll Y-l R'-X X-VII Y-VI R^-Vlll X-lll Y-l R'-Xl X-Vll Y-Vl R^-IX X-IIl Y-ll R'-X X-Vll Y-VI R^-X X-lll Y-lll R'-X X-Vlil Y-I R^-X X-lll Y-iV R'-X X-Vl 11 Y-Vl R^-X X-lll Y-V R^-X X-IX Y-l R^-X X-lll Y-V! R'-l X-IX Y-VI R^-X X-l Y-l R'-Xll X-l Y-Vl R^-XIl X-l Y-l R^-XIII X-l Y-VI R^-XIll X-l Y-l R^-XIV X-l Y-VI R^-XIV X-l Y-l R'-XV X-l Y-VI R^-XV X-l Y-l R^-XVI X-l Y-VI R^-XVI X-l Y-I R'-XV!1 X-l Y-Vl R^-XVIl X-l Y-l R'-XVllI X-l Y-VI R^-XVllI X-lll Y-l R^-Xll X-lll Y-Vi R^-Xll X-lll Y-l R^-XIII X-lll Y-VI R^-Xlll X-lll Y-l R'-XIV X-lll Y-VI R^-XIV X-lll Y-l R^-XV X-lll Y-VI R^-XV X-ll! Y-l R'-XVi X-lll Y-VI R^-XVI X-lll Y-l R'-XVII X-lll Y-VI R^-XVII X-lll Y-! R'-XVIH X-lll Y-Vl R^-XVlll [0090] The compounds of the present invention can be produced for example according to the methods mentioned below. Production Method A H~N ^ ^ R^ P"^N (Y) D^ R P~N (Y) ~ Wm A ^ / //c\ '-'''".-—>X 11 / ( G I II / I ^ (C I II / I , ^A^ X V C R^ j II II (5) ^ (1-1) ^ \ / ^' R^ .o~N m /H-N 11 (7) ° [0091] The compound of formula (1-1) wherein A\ A', A^ G, X, Y, R\ R^ R^ m and n are as defined-above that is the compound of formula (1) wherein W is oxygen atom can be obtained by reacting the compound of formula (5) wherein A\ A^, A^ G, X, Y, R^ m and n are as defined above with the compound of formula (6) wherein R'' and R^ are as defined above by use of a condensation agent^optionally by using a solvent inactive for the reaction, optionally in the presence of a base. [0092] The reaction substrates can be used in an amount of 1 to 100 equivalents of the compound of formula (6) based on 1 equivalent of the compound of formula (5). [0093] The condensation agent is not specifically limited if it is a compound used for ordinary amide synthesis, but it is for example Mukaiyama agent (2-chloro-N¬methylpyridinium iodide), DCC (1,3-dicyclohexyl carbodiimide), WSC (1-ethyl-3-(3¬dimethylaminopropyi)-carbodiimide hydrochloride), GDI (carbonyl diimidazole), dimethylpropynyl sulfonium bromide, propagyl triphenyi phosphonium bromide, DEPC (diethyl phosphorocyanidate) or the like, and can be used in an annount of 1 to 4 equivalents based on the compound of formula (5). [0094] In case where a solvent is used, the solvent is not specifically limited if it dose not inhibit the progress of the reaction, but it includes for example aromatic hydrocarbons such as benzene, toluene, xylene or the like, aliphatic hydrocarbons such as hexane, heptane or the like, alicyclic hydrocarbons su9h as cyclohexane or the like, aromatic halogenated hydrocarbons such as chlorobenzene, dichlorobenzene or the like, aliphatic halogenated hydrocarbons such as dichloro methane, chloroform, carbon tetrachloride, 1,2-dichloroethane, 1,1,1-trichloroethane, trichloroethylene, tetrachloroethylene or the like, ethers such as diethyl ether, 1,2-dimethoxyethane, tetrahydrofuran, 1,4-dioxane or the like, esters such as ethyl acetate, ethyl propionate or the like, amides such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyroIidone or the like, amines such as triethyl amine, tributyl amine, N,N-dimethyl aniline or the like, pyridines such as pyridine, picoline or the like, acetonitrile and dimethyl sulfoxide, and the like. These solvents may be used alone or in a mixture of two or more. [0095] The addition of a base is not necessarily required. However, when the base is used, alkali metal hydroxides such as sodium hydroxide, potassium hydroxide or the like, alkali metal carbonates such as sodium carbonate, potassium carbonate or the like, alkali metal bicarbonates such as sodium hydrogen carbonate, potassium hydrogen carbonate or the like, organic bases such as triethyamine; tributylamine, N,N-dicpethylaniline, pyridine, 4-(dimethyIamino)pyridine, imidazole, 1,8-diazabicyclo[5.4.0]-7-undecene, and the like can be used in an amount of 1 to 4 equivalents based on the compound of formula (5). [0096] The reaction temperature may be an arbitrary temperature ranging from -60°C to the reflux temperature of a reaction mixture, and the reaction time may be an arbitrary time ranging from 5 minutes to 100 hours although it varies depending on the concentration of the reaction substrates or the reaction temperature. [0097] Generally, it is preferable to carry out the reaction by using 1 to 20 equivalents of the compound of formula (6) and 1 to 4 equivalent of the condensation agent such as WSC (1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide hydrochloride), GDI (carbonyl diimidazole) or the like based on 1 equivalent of the compound of formula (5), optionally in the presence of 1 to 4 equivalents of a base such as potassium carbonate, triethylamine, pyridine, 4-(dimethylamino)pyridine or the like, without solvent or in a solvent such as dichloromethane, chloroform, diethyl ether, tetrahydrofurane, 1,4-dioxane or the like, at a temperature ranging from 0°C to the 1. reflux temperature of these solvents for 10 minutes to 24 hours. [0098] In addition, the compound of formula (1-1) according to the present invention can be also synthesized"by reacting the compound of formula (7) wherein A\ A^ A^ G, X, Y, R\ m and n are as defined above, J^ is chlorine atom, bromine atom, Ci-C4alkylcarbonyloxy (for example pivaloyloxy), Ci-C4all<:oxycarbonyloxy (for example isobutyloxycarbonyloxy) or azolyl (for example imidazol-1-yl) that can be synthesized according to a known method disclosed in documents from-the compound of formula (5), for example a method by reacting with a chlorinating agent such as thionyl chloride, phosphorus pentachloride or oxalyl chloride, a method by reacting with a organic acid halide such as pivaloyi chloride or isobutyl chlorformate, etc. optionally in the presence of a base, or a method by reacting with carbonyl diimidazole or sulfonyl diimidazole, etc., with the compound of formula (6), optionally by using a solvent inactive for the reaction, optionally in the presence of a base. [0099] The reaction substrates can be used in an amount of 1 to 50 equivalents of the compound of formula (6) based on 1 equivalent of the compound of formula (7). [0100] In case where a solvent is used, the solvent is not specifically limited if it dose not inhibit the progress of the reaction, but it includes for example aromatic hydrocarbons such as benzene, toluene, xylene or the like, aliphatic hydrocarbons such as hexane, heptane or the like, alicyclic hydrocarbons such as cyclohexane or the like, aromatic halpgenated hydrocarbons such as chloroberizene, dichlorobenzene or the like, aliphatic halogenated hydrocarbons such as dichloro methane, chloroform, carbon tetrachloride, 1,2-dichloroethane, 1,1,1-trichloroethane, trichloroethylene, tetrachloroethylene or the like, ethers such as diethyl ether, 1,2-dimethoxyethane, tetrahydrofuran, 1,4-dioxane or the like, esters such as ethyl acetate, ethyl propionate or the like, .amides such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyI-2-pyrolidone or the like, amines such as triethyl amine, tributyi amine, N,N-dimethyl aniline or the like, pyridines such as pyridine, picoline or the like, acetonitriie and water, and the like. These solvents may be used alone or in a mixture of two or more. [0101] The addition of a base is not necessarily required. Hov/ever, when the base is used, alkali metal hydroxides such as sodium hydroxide, potassium hydroxide or the like, alkali metal carbonates such as sodium carbonate, potassium carbonate or the like, alkali metal bicarbonates such as sodium hydrogen carbonate, potassium hydrogen carbonate or the like, organic bases such as triethyamine, tributylamine, N.N-dimethyianiline, pyridine, 4-(dimethylamino)pyridine, imidazole, 1,8-diazabicyclo[5.4.0]-7-undecene, and the like can be used in an amount of 1 to 4 equivalents based on the compound of formula (7). [0102] The reaction temperature may be an arbitrary temperature ranging from -60°C to the reflux temperature of a reaction mixture, and the reaction time may be an arbitrary time ranging from 5 minutes to 100 hours although it varies depending on the concentration of the reaction substrates or the reaction temperature. [0103] Generally, it is preferable to carry out the reaction by using 1 to 10 equivalents of the compound of formula (6) based on 1 equivalent of the compound of formula (7), optionally in the presence of 1 to 2 equivalents of a base such as potassium carbonate, triethylamine, pyridine, 4-(dimethylamino)pyridine or the like, without solvent or in a solvent such as dichloromethane, chloroform, diethyl ether, tetrahydrofurane, 1,4-dioxane, ethyl acetate, acetonitrile or the like, at a temperature ranging from 0°C to the reflux temperature of these solvents for 10 minutes to 24 hours. Production Method B HO. HO. f (Y)n f? (Y)n H ^ r >"A^ R^ halogenation f^^^Y^J^p^ R^ ^A^ X R^ ^A^ X R^ II II W W (8) (9) base ^-^ ^"A^^'^C^^R^ II W (1) [0104] Hydroxamic chloride of formula (9) wherein A\ A^ A^ W, Y, R\ R^ and n are as defined above, J means halogen atom such as chlorine atom and bromine atom can be obtained by halogenating the compound of formula (8) wherein A \ A^ A^ W, Y, R\ R^ and n are as defined above using a halogenating reagent optionally 67 by using a solvent inactive for ihe reaction, optionally in the presence of a base. [0105] Halogenating agents include for example N-halosuccinimides such as N¬chlorosuccinimide, N-bromosuccinimide or the like, hypohalogenous acid ail^ali metal salts such as sodium hypochlorite or the like, hypohalogenous acid esters such as hypochlorous acid-t-butyl ester or the like, simple substance halogens such as chlorine gas or the like, and it can be used in an amount of 1,to 10 equivalents based on the compound of formula (8). [0106] In case where a solvent is used, the solvent is not specifically-limited if it dose not inhibit the progress of the reaction, but it includes for example aromatic hydrocarbons such as benzene, toluene, xylene or the like, aliphatic hydrocarbons such as hexane, heptane or the like, alicyclic hydrocarbons such as cyclohexane or the lifle, aromatic halogenated hydrocarbons such as chlorobenzene, dichlorobenzene or the like, aliphatic halogenated hydrocarbons such as dichloro methane, chloroform, carbon tetrachloride, 1,2-dichloroethane, 1,1,1-trichloroethane, trichloroethylene, tetrachloroethylene or the like, ethers such as diethyl ether, 1,2-dimethoxyethane, tetrahydrofuran, 1,4-dioxane or the like, esters such as ethyl acetate, ethyl propionate or the like, amides such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrolidone or the like, alcohols such as methanol, ethanol, ethylene glycol or the like, carboxylic acids such as acetic acid, propionic acid or the like, acetonitrile and water, and the like. These solvents may be used alone or in a mixture of two or more. [0107] The reaction temperature may be an arbitrary temperature ranging from -60°C to the reflux temperature of a reaction mixture, and the reaction time may be an arbitrary time ranging from 5 minutes to 24 hours although it varies depending on the concentration of the reaction substrates or the reaction ternperature. [0108] The compounds of formula (1) wherein A'', A^ A^ G, W, X, Y, R\ R^ R^ m and n are as defined above according to the present invention can be obtained by reacting the compound of formula (9) with the compound~of formula (10) wherein G, X, R^ and m are as defined above in the presence of a base optionally by use of a solvent inactive for the reaction. [0109] The reaction substrates can be used in an amount of 1 to 5 equivalents of the compound of formula (10) based on 1 equivalent of the compound of formula (9). [0110] The used base includes for example alkali meta! hydroxides such as sodium hydroxide, potassium hydroxide or the like, alkali metal carbonates such as sodium carbonate, potassium carbonate or the like, alkali metal bicarbonates such as sodium hydrogen carbonate,,potassium hydrogen carbonate or the like, organic bases such as triethyamine, tributylamine, N,N-dimethylaniline, pyridine,' 4-(dimethy!amino)pyndine, imidazole, 1,8-diazabicyclo[5.4.0]-7-undecene, and the like can be used in an amount of 1 to 5 equivalents based on the compound of formula (9). [0111] In case where a solvent is used, the solvent is not specifically limited if it dose not inhibit the progress of the reaction, but it includes for example aromatic hydrocarbons such as benzene, toluene, xylene or the like, aliphatic hydrocarbons ' such as hexane, heptane or the like, alicyclic hydrocarbons such as cyclohexane or the like, aromatic halogenated hydrocarbons such as chlorobenzene, dichlorobenzene or the like, aliphatic halogenated hydrocarbons such as dichloro methane, chloroform, carbon tetrachloride, 1,2-dichloroethane, 1,1,1-trichloroethane, trichloroethylene, tetrachloroethylene or the like, ethers such as diethyl ether, 1,2-dimethoxyethane, tetrahydrofuran, 1,4-dioxane or the like, esters such as ethyl acetate, ethyl propionate or the like, amides such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrolidone or the like, and acetonitrile, and the like. These solvents may be used alone or in a mixture of two or more. [0112] The reaction temperature may be an arbitrary temperature ranging from -60°C to the reflux temperature of a reaction mixture, and the reaction time may be an arbitrary time ranging from 5 minutes to 100 hours although it varies depending on the concentratiorv of the reaction substrates or the reaction'temperature. [0113] Generally, the compound of formula (9) can be obtained for example by carrying out the reaction by using 1 to 2 equivalents of a halogenating agent such as N-chlorosuccinimide, sodium hypochlorite aqueous solution, hypochlorous acid-t¬butyl ester, chlorine gas or the like based on 1 equivalent of the compound of formula (8) in a solvent such as dichloromiethane, chloroform, 1,2-dimethoxyethane, tetrahydrofurane, 1,4-dioxane, N,N-dimethylformamide or the like, at a temperature ranging from 0°C to the reflux temperature of these solvents for 10 minutes to 2 hours. Then, preferably without the isolation of the compound of formula (9), 1 to 2 equivalents of the compound of formula (10) and 1 to 2 equivalents of a base such as sodium carbonate, sodium hydrogen carbonate, triethyl amiine or the like are . added, and the reaction is carried out at a temperature ranging from 0°C to the reflux temperature of these solvents for 10 minutes to 24 hours. Production Method C K^ Rv°~If W. ^'•-'' (X) f T^A^ (18) (19) (10) ^ -v\ X /v/ base V y i^ J (12) [0139] That is, the compounds of formula (12) wherein A\ A^ A^ G, X, Y, R^ m, n and J"* are as defined above oan b.Q obtained by halogenating the compound of formula (18) wherein A\ A^ A^ Y, n and J" are as defined above under a condition similar to that of Production Method B to obtain the compound of formula (19) wherein A\ A^ A^ Y, n, f and J^ are as defied above, and then reacting it with the compound of formula (10) wherein G, X, R^ and m are as defined above. [0140] The compound of formula (18) can be easily synthesized by use of the corresponding known substituted aromatic aldehyde similarly to the process described in Reaction Scheme 2. [0141] The compound of formula (14) can be synthesized for example acccording to Reaction Scheme 5 or Reaction Scheme 6. Reaction Scheme 5 (Y)n ? (Y)n ^yJ^^A' R' C0/HC(0)0H H^^Y%' f II II w w ^ , (20) (14) [0142] The compounds of formula (14) wherein A\ A^ A^ W, Y, R\ R^ and n are as defined above can be obtained by subjecting the compound of formula (20) wherein A\ A^ A^ W, Y, R\ R^ n and J"* are as defined above to CO insertion reaction according to known methods disclosed in documents, for example the reaction by use of a transition metal catalyst such as palladium or the like in the presence of hydride source such as formic acid or the like stated in Bull. Chem. Soc. Jpn., 1994, vol. 67, p. 2329, J. Am. Chem. Soc, 1986, vol. 108, p. 452, or the like. Reaction Scheme 6 R^ ? (Y)n ^RI ? (Y)„ II . 11 o o (21) \ / (14-1) Al ,'X .J' (6) A C II O (22) [0143] The compounds of formula (14-1) wherein A\ A^ A^ Y, R\ R^ and n are as defined above that are the compounds of formula (14) wherein W is oxygen atom can be synthesized by reacting the known compound of formula (21) wherein A\ A^ A^ Y and n are as defined above with the compound of formula (6) wherein R^ and R^ are as defined above by use of the method similar to Production Method A. [0144] The compounds of formula (17) can be synthesized as follows, for 77 example. Reaction Scheme 7 o / o o \ Vly ---,_j24) V (25) / (23 ) ^^^^"^"^^•"^---^^ ^ , O ^ Catalyst ^^---^^ P^)m n (1) ^yx\A{^i) ^^^^...^'--^-^^^^ (X)m_^^j8 ---'''''^ O / t? ff \ ^-^ {21) \ (25) / (26) [0145] That is, the compounds of formula (17) wherein X, R^ and m are as defined above, G is benzene ring can be obtained by reacting the known compound of formula (23) wherein X and m are as defined above, G is benzene ring with the known compound of formula (24) wherein R^ is as defined above, J'' is a leaving group such as halogen atom, trifluoromethanesulfonyioxy, 2-pyridyloxy or the like, or the known compound of formula (25) wherein R^ is as defined above according to a genaral acyiating reaction of aromatic ring disclosed in documents, for example a method stated in Chem. Lett., 1990, p. 783, J. Org. Chem., 1991, vol. 56, p. 1963 or the like. [0146] In addition; the compound of formula (17) wherein G, X, R^ and m are as defined above can be obtained according to general methods disclosed in documents for example by a method stated in J. Am-. Chem. Sbc, 1955, vol. 77, p. 3657, Tetrahedron Lett., 1980, vol. 21, p. 2129 and 1991, vol. 32, p. 2003, US 5,514,816 in which the compound of formula (26) wherein G, X and m are as defined above, J^ is bromine atom or iodine atom is lithiated and the resulting compound is reacted with the known compound of formula (27) wherein R^ is as defined above, J^ is halogen atom, hydroxy, metal salt (for example, -OLi, -CNa), C^-C^alkoxy (for example, methoxy, ethoxy), di(Ci-C4alkyl)amino (for example, diethylamino), C,¬C4alkoxy Ci-C4alkyl amino(for example 0,N-dimethylhydroxyamino) or cyclic amino (for example, piperidin-1-yl, morphol(n-4-yl, 4-methylpiperadin-1-yl), or the known compound of formula (25), or by a method stated in Heterocycles, 1987, vol. 25, p. 221, Synth. Commun., 1985, vol, 15, p. 1291 and 1990, vol. 20, p. 1469, DE 19727042, or the like in which a Grignard reagent is formed and then it is reacted with the compound of formula, (27) or the compound of formula (25). [0147] The compounds of formula (20) can be synthesized according to for example Reaction Scheme 8 or Reaction Scheme 9. Reaction Scheme 8 (Y)n ^R1 (Y)n II 11 ' o o (28) \ y (20-1) ^ f ^P' / H-N II o (29) [0148] The compounds of formula (20-1) wherein A \ A^ A^ Y, R\ R^ n and J" are as defined above that are the compounds of formula (20) wherein W is oxygen atom can be obtained by reacting the known compound of formula (28) wherein f\\ A^ A^ Y, n and J'' are as defined above with the compound of formula (6) wherein R"" and R^ are as defined above by use of the method similar to Production Method A. Reaction Scheme 9 (Y)n (Y)„ II II o s (20-1) (20-2) [0149] The compounds of formula (20-2) wherein A \ A^ A^ Y, R\ R^ n and J^ are as defined above that are the compounds of formula (20) wherein W is sulfur atom can be obtained by reacting the compound of formula (20-1) wherein A\ A^, A^ Y, R\ R^ n and J" are as defined above that are the compounds of formula (20) wherein W is oxygen atom with a sulfurizing agent such as diphosphorus 79 pentasulfide, diphosphorus pentasuifide-HMDO (hexamethyldisiloxane), Lawesson's Reagent (2,4-bis(4-methoxyphenyi)-1,3,2,4-dithiadiphosphetane-2,4-disulfide) under a condition similar to that of Production Metiiod D. [0150] In each reaction, after the completion of the reaction, each production intermediate that is a starting compound in Production Method A to Produciton Method C can be obtained by carrying out normal post-treatments. [0151] in addition, each production intermediate produced by the above-mentioned methods can be used for the following reaction step as^such without isolation or purification. [0152] The active compounds included in the present invention concretely include for example the compounds shown in Tables 2 and 3. The compounds that can be used as novel production intermediates for producing the active compounds included in the present invention concretely include for example the compounds shown in Tables 4 to 6. In the interim, the compounds shown in Tables 2 to 6 are for purposes of illustration and the present invention is not limited thereto. [0153] In the meantime, in Tables, the indication "Et" means ethyl, hereinafter similarly thereto, "n-Pr" and "Pr-n" mean normal propyl, "i-Pr" and "Pr-i" mean isopropyl, "c-Pr" and "Pr-c" mean cyclopropyl, "n-Bu" and "Bu-n" mean normal butyl, "s-Bu" and "Bu-s" mean secondary butyl, "i-Bu" and "Bu-i" mean isobutyl, "t-Bu" and "Bu-t" mean tertiary butyl, "c-Bu" and "Bu-c" mean cyclobutyi, "n-Pen" and "Pen-n" mean normal pentyl, "c-Pen" and "Pen-c" mean cyclopentyl, "n-Hex" and "Hex-n" mean normal hexyl, "c-Hex" and "Hex-c" mean cyclohexyl, "Hept" means heptyl, "Oct" means octyl, "Ph" means phenyl, "1-Naph" means 1-naphthyl, "2-Naph" means 2-naphthyl, and in Tables, aromatic heterocyclic rings of D-la to D-59a are the following structures, respectively z ^-U-.JT} D-lb: ^ ^-U:J[y^ Z D-2a : ,^J^O D-2b : ^J^O D-3a : ^ > z z ¬ O O ij Z »-4^ -• -^ S D-4b : ^4 ^ D.5a : _NQ ^ CH3 Z CH3 z z D-8b : ^,X7 o D-9a : ^^ N D-9b : ^J i Z D-lOa : ,Ji\ D-lOb : ^JC% D-lla :..:,,JO S O O N Z Z D-llb : ^J^S D-12b : ,.JQ N D-13a : ^JC% Z Z D-13b : ^ ; N D-14a : ^N ^ D-14b : ^N ^ 81 N=:riD-14C : ^N^y~^ 2 R^^ N-N D-i5a : ^Jl^ D-15b : /CH3 N-N , ^JlJ> /CH3 Z Z Z , D-16C : D-18a : X ^ k^^ „Y <-W3ZN-r y ^ ^o D-17a : ^J^^ j ^ R^^Z N-/ D-18b : ^ ^ o D-17b : D-18c : ^Jl \ j ^ CH3 N-Tv J V o ^ D-19a : ^ JN D-19b : ^ ^ ^ N ^ D-20a : ^^ O \ D-20b : /;-N J ^o ^^ D-21a : N-^ J } s D-21b : Z N-/ J A s D-21C : ^ X I>-22a : ^ J D-22b :, ^ ^ S ^ N • N ^ CH 3 D-23a : ,^^ 3s/= ND-24a : ^N ^ i D-23b : ^J^^y sRJ^ N-n D-25a : ^ j i ¬^ I>-23c : ^%^ ^ s CH3 .isf—< D-25b : A V ^ ^ CH3 z R, D-25C : J x }^ D-26a.: ^^ N^-^is ^^'^^a : ^„.^ N -"^N : . , ^-/ ^ ^-^ CH3 Z N-/ /7-S ^N D-27b : J^ \ D-28a : ^ . N I>-29a : ^ > z z~¬ V-N N=rx N=r< D-29b : ^ N D-30a : ^4^ ^O I>-30b : ^ ^ ^O S" N N z z N-Tv N-/ N=/ D-31a : ^ ^N D-31b : ^ N D-32a : ^ /s Z N-7y N-/ N-N D-33a : J \ D-33b : ^J \ D-34a : ^J \^ s" s" o N-N N-N N-N D-34b : J ^^ D-35a : J } D-35b : ^->^^ o s s -^ Z r=N \=N ^N D-36a : ^ ^b D-36b : ^ ^b D-37a : ,^^ \ N N N Z \=:N N=rA N=r>^ D-37b : ^ ;s D-38a : ^N^ . N I>-39a : ^ N. ,5 N ^^ N z RJ^ CH3 N=/ N-N N-N D-39b : ^ >^ D-40a : ^ > D-40b : ^ >^ N *-^3 N N ^ 83 D-42a : R^'N-T. ^ L NN ^ I^-'^^b : ••¬ •. CH3 Z is-/ ^ ^ N N ^ N . I>-43a : ^N ^ ,_^N N Z \= ND-43b : ^N , .,N^N" N=A I>-44a : ^N ^ .^N N D-45a : HN-N '^J^ "^ N D-45b :' ^ N-N^ 'NN' D-46a : ^ N-NH ^N N ' D-46b : N-N ' J ^'^ N ' Z D-47a : -^ N D-47b : -^ N D-47c : ^ N D-47d : ^ fl N I D-47e : fj -^ N j Z D-47f: || ^ ^ N j D-47g : -^ N CI D-48a : ^^--^Z I D-48b : ¬y^^' X ^ D-48c : I I D-48d : I I D-48e : „' j | CI D-48f: I D-48g : I D-49a : 1 D-49b : I f D-49c : Jj j D-49d : || j Z 84 D-50a : || D-50b : || D-50c : n Z -^ /N. /N. ^Z D-51d : II I D-52a : I D-52b : I y^^ y^^ y^^'^ z D-52c : I D-53a : D-53b : z D-53c : I D-53d : | D-54a : I D-54b : I D-55a : 1 D-56a : ij | ^ N ^ ^^ ^ N D-57a : || I D-58a : || i D-59a : ij I /^N^N J^^ >l^N For example, the indication "[CH2(D-17a)CH3]" means 1-methyipyrazol-5-yi methyl, the indication "[CH2(D-22b)CH3] means 2-methylthiazoW-yl methyl. In addition, aliphatic heterocyclic rings of E-4a to E-43b are the following structures, respectively E-4a : ^J^ E-4h : ^^^ ^ E-5a : ^J^o O ^ O E-5b : ^J O E-5c : ^^J Q E-6a : ^ 7 \ o E-7d : ^^(^^s E-8a : J ^ E-8b : ,X\ o E-9a : J^^^^22 E-9b : ^X~N-~R2 3 E-lOa : ^J ^ O R22p—X ^-O r-O E-lOb : X J E-lla : ^ ^ E-llb : J ^ V,, o o o ^ E-llc : ^1 \/CH3 E-12a : ^1 \ E-12b : ^^V \ ^ CH3 ^ ^ ^ E-18a : J ) E-lSb^: ^ ) E-23a : I J E-24a : r^o E-25b : I E-26a : E-28a : [ I E-29a : E-30a : f I E-30b : r N E-31a : J E-31b : O ^ E-32b : E-34a : -4-/ E-35b : E-40a : I I r^ f JR" f IO r N f f^% 1 ^^"^ I E-21a : ^ >^ E-25a : ! J r^ E-27a : ! E-29b : f R^3 E-30c : f I o ^ E-32a : | O^ E-35a : i A^ E-41a : I E-42a : I E-42b : f E-43a : I E-43b : For example, the indication "[CH2(E-10b)CH3r means 2-methyi-1,3-dioxplan-2-yi methyl, the indication "[CH2(E-8a)CH3]" means N-methylpyrrolidin-2-yl methyl. Further, in Tables, partially saturated heterocyclic rings of M-2a to M-16a are the following structures, respectively •' r-N I \ O-N i—O r-N /—S M-8a : ^ ^ M-9a : ^ ^^ M-lOa : ^ ^ N ^ O ^ N -^ M-14a : M-15a : Y M-16a : 1 For example, the indication "[CH2(M-5a)CH3]" means 3-methyt-4,5-dihydoisoxazol¬5-yl methyl. Further, in Tables, T-1 to T-38 are the following structures, respectively T-l : T-19 : ^ JN ^ T-20 : <( I N" ^ T-21 : ^ "^ N""^ T-22 : ^ J T-23 : H (\ J T-24 : (\ ) S--\ HN-^ /. T-25 : -H(\ > T-26 : —<\ ) T-27 : -N ^ OCH3 /^ /^ r-0 T-28 : —N J T-29 : —N J T-30 : —-N J O S 7^0 /^s T^s T-31 : —N J T-32 : —N J T-33 : —N J O T-34 : —N ) T-35 : —N O T-36 : —N S T-37 : —N N-CH3 T-38 : —N \ / v_y Table 2 In the table, the number showing the substitution position of substituent (X)^, corresponds to the position number indicated in the following structural formulae. The indication "-" means no-substitution. R^ p-N R^ P~N \L^^4 . ^/^ C II R^ ^-^ 4 . ^^^^C II R^ 5 O 5 §• [1]-1 > [l]-2, R3 O^N R3 O-N [l]-3 , [l]-4 R^ P^N R3 O-N [l]-5 , [l]-6 R^ P^N R3 O-N (X),2 X X / . (X)m2 X Jl 4 ^ I II • 4 . ¬ II 5 Br O 5 Br S [lJ-7 , [l]-8 R3 p-f^ R^ P^N [l]-9 , [1]-1Q R3 O-N R^ P^ N 4'i^' 5 CH3[1]-11 II O , 4 ^ 5 I CH3 [1]-12 II S R3 0~pq R3 O^ N 4^ 5 Et[1]-13 II O , 4 r 5 I Et [1]-14 II S R3 0-N R^ P^ N 4 ^5 I CF3[1]-15 II O , 4 . 5 ¬I CF3 [1]-16 II S 5 CH3O O 5 CH3O S [1]-17 , -[Ij-lS R3 p-N R^ P~N 41 11 4 c I 11 5 cHFjO O 5 CHF2O S [1]-19 , [l]-20 R3 O^N R^ P~^N (X).2 V X .-. , ^^^-"^ XJk/<:^. 4 , II 4 . I II 5 CF3O O 5 CF3O S [1]-21 , [l]-22 R3 0~N R^ P-~N 4 ^ I II • 4 . .' " 5 CH3S O 5 CH3S S [l]-23 , [l]-24 93 4^ 5 CHF2S[l]-25 II O , 4 ^ 5 I CIBF2S [l]-26 II S R3 p-NVTA ^iX ^ R^ X X P-N IIX "^i 5 CF3S[l]-27 O , ^ 5 CF3S [l]-28 S R3 p-N R^ P-N 4^ 5 NO2[l]-29 II O , 4 . 5 1 NO2 [l]-30 II S R3 p-N(X)m 2 A i l / .^>v^ R' 4 ^ I IT • • 4 ^ I II 5 CH3S O 5 CH3S S [l]-49 , [lJ-50 R^ P-N R^ P^N V_^ ^f^^C R^ ^-^ T^ C R^ 4 ^ I II 4 . I 11 5 CH3 O 5 CH3 S [1]-51 , [l]-52 R^ p-^N R^ P-^N (X)„,2 X X ^ (^)-^ X A /^ \/==r/ ^^ >f ^N R^ Nf==A Ti N R^ 3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-C!2 CF3¬ 3,5-Ci2 CF3 3,5-Cl2 CF3 •3,5-012 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-C!2 CF3 3,5-Cl2 CF3 3,5-01^ CF3 3,5fCl2 CF3 3,5-^012 CF3 3,5-Ci2 CF3 3,5-C!2 CF3 3,5-Cl2 CF3 3,5-0!^ CF3 3,5-Ci2 CF3 3,5-Cl2 CF3 3,5-CU CF3 3,5-C!; CF3 3,5-Cl2 CF3 3,5-Cl, CF3 3,5-Ci; CF3 3,5-Cl2 CF3 3,5-Cl 2 CF3 3,5-Cl 2 CF3 3,5-Cl 2 CF3 3,5-Cl 2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl 2 CF3 3,5-Cl2 CF3 3,5-Cl 2 CF3 3,5-Cl 2 CFg 3,5-Cl 2 ^ CF3 3,5-Cl 2 CF3 3,5-Cl 2 CF3 3,5-Cl 2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 H CH2(Ph-2-NHS02CF3) H CH2(Ph-3-NHS02CF3) H CH2(Ph-4-NHS02CF3) H CH2[Ph-2-N(CH3)2] H CH2[Ph-4-N(CH3)2] H CH2(Ph-2-N02) H CH2(Ph-3-N02) H CH,(Ph^-N02) CH3 CH^CPh^-NO^) H CH2(Ph-2-CN) H CH2(Ph-3-CN) H CH2(Ph-4-CN) H CH2[Ph-2-C(0)OCH3] H CHJPh-S-CppCHs] H CH2[Ph-4-C(0)OCH3] H CH2[Ph-2-C(0)NH2] H CH2[Ph-3-C(0)NH2] H CH2[Ph-4-C(0)NHJ H CH2[Ph-2-C{S)NHJ H CH2[Ph-3-C(S)NH2] H CH2[Ph-4-C(S)NH2] . H CH2(Ph-3-CH=NOCH3) H CH2(Ph-4-CH=NOCH3) H CH2lPh-4-C(CH3)=NOCH3] H CH2(Ph-2,4-F2) H CH2(Ph-2,5-F2) H CH2(Ph-2,6-F2) H CH2(Ph-3,4-F2) H CH2(Ph-3,5-F2) H CH2(Ph-2-F^-CI) H CH2(Ph-2-CM-F) H CH2(Ph-2-F^-CI) H CH2,(Ph-3-F-4-CI) H . CH2'(Ph-3-CI-4-F) H CH2(Ph-2,3-Cl2) H . CH2(Ph-2,4-Cl2) H ¬ CH2(Ph-2,5-Cl2) H CH2(Ph-2,6-Cl2) H CH2(Ph-3,4-Cl2) H CH2(Ph-3,5-Cl2) H CH2(Ph-2-F-4-Br) H CH2(Ph-2-F-5-Br) H CH2(Ph-3-Br-4-F) H CH2(Ph-2-F-3-CF3) H CH2(Ph-2-F^-CF3) H CH2(Ph-2-CF3-4-F) 143 3,5-CL CF3 H CH2(Ph-2-F-5-CF3) 3,5-Cl2 CF3^ H CH,(Ph-2-CF3-5-F) 3,5-CU CF3 H CH,(Ph-2-F-6-CF3) 3,5-CU CF3 H CH2(Ph-3-CF3^-F) 3,5-CU CF3 • H CH2(Ph-3-F-5-CF3) 3,5-CL CF3 H CHJPh-3,4:(OH),] 3 5-CU CF3 H CH2(Ph-3-OCH3^-OH) 3!5-CU CF3 H CHJ.Ph-2,3-(OCH3)2] 3,5-CU CF3 H CH2[Ph-2,4-(OCH3)2] 3,5-CU CF3 H CHJPh-2,6-(OCH3)2] 3,5-CU CF3 H CH2[Ph-3,4-(OCH3)2] 3,5-CU CF3 H CH2[Ph-3,5-(OCH3)2] 3,5-Ci2 CF3 H CH2(Ph-3-OCH20-t) 3,5-CU CF3 H CH2(Ph-2,3,4-F3) 3,5-CU CF3 H CH2(Ph-2,3,5-F3) 3,5-eU CF3 H CH2(Ph-2,3,6-F3) 3,5-GU CF3 H CH2(Ph-2,4,5-F3) 3,5-CU CF3 H CH2(Ph-3,4,5-F3) 3,5-CU CF3 H CH2[Ph-2,4,6-(OCH3)3] 3,5-CU CF3 H CH2[Ph-3,4,5-(OCH3)3] 3,5-Ci, CF3 H CH(CH3)Ph 3,5-Ci; CF3 H CH(CH3)Ph(R) 3,5-CU CF3 H CH(CH3)Ph(S) 3,5-CU CF3 H CH(Et)Ph 3,5-CU CF3 H CH(Et)Ph(R) 3,5-CU CF3 H CH(CF3)Ph 3,5-CU CF3 H CH(CF3)Ph(R) 3,5-CU CF3 H CH(CF3)Ph(S) 3,5-CU CF3 H CH(CH20H)Ph(R) 3,5-CU CF3 H CH(CH20H)Ph(S) 3,5-CU CF3 H CH(CH20CH3)Ph 3,5-CU CF3 H CH(CH,0CH3)Ph(R) 3,5-CU CF3 H CH(CH20CH3)Ph(S) 3,5-CU CF3 H CH(0CH3)Ph 3,5-CU CF3 H CH(OEt)Ph 3,5-CU CF3 H . CH(CN)Ph 3,5-CU CF3 H CH(CN)Ph(R) 3,5-CU CF3 H CH(CN)Ph(S) 3,5-CU CF3 H C(CH3)2Ph 3,5-CU CF3 H C(CH3)2CH2Ph 3,5-CU CF3 H CH^CH^CH^Ph 3,5-CU CF3 H CH(CH3)CH2CH2Ph 3,5-CU CF3 H CH2(1-Naph) 3,5-CU CF3 CH3 CHgO-Naph) 3,5-CU CF3 H CH2(D-1a) 3,5-CU CF3 CH3 CH2(D-1a) 144 3,5-Cl, CF33,5-CI, CF,3,5-Ci2 CF33,5-Cl, CF33,5-0!^ CFg3,5-CI, CF33 5-CL CF3 •3,5-012 CF33,5-CI, CF33,5-Cl2 CF33,5-C!2 CF33,5-CI, CF33,5-Cl2 CF33,5-CU CF33,5-Ci; CF33,5iCl2 CF33,5-CL CF33,5-Cl2 CF33,5-CU CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-CI, CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-C!3 CF33,5-CL CF33,5-Cl2 CF33,5-Cl2 CF33,5-CU CF33,5-Ci2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-CI, CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-0!^ CF33,5-Cl2 CF33,5-C!2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF3 H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H 145 CH,(D-1b)Br CH2(D-1c)CI CH2(D-1c)Br CH,(D-1c)CH3 CH2(D-1c)CF3 CH,(D-1c)SCH3 CH2(D-1c)S02CH3 CH,{D-^c)m, CH(CH3){D-1a) CH(CH3)(D-1a)(R) CH(CF3)(D-ra) CH(CN)(D-1a) CH2(D-2a) CH2(D-2b)Br CH2(D-3a) CH2(D-3b)CH3 CH2(D-3c)CI CH2(D-3c)Br CM2(D-3c)SCH3 CH2(D-3c)S02CH3 CH2(D-3c)N02 CH2(D-3d)F CH2(D-3d)CI CH2(D-3d)Br CH2(D-3d)l CH2(D-3d)CH3 CH2.(D-3d)CF3 CH2(D-3d)N02 CH,(D-3d)SCH3 CH2(D-3d)S02CH3 CH2(D-3d)CN CH(CH3)(D-3a) CH(CF3)(D-3a) CH(CN)(D-3a) CH^CD^a) CH3(D^b)CI CH2(D-4b)Br CH2(D4b)N02 CH2(D^b)CN CH2(D-6a)CI CH2(D-6a)Br CH2(D-6b)CI CH2(D-6b)Br CH2(D-8a) CH2(D-8b)CI CH2(D-8b)Br SyiTcir CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3, H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-CU CF3- H 3:ml CF3 H 3,5-Cl2 CF3 H •3,5-CU CF3 H 3,5-Ci; CF3 H 3,5-Cl2 CF3 H 3,5-0!^ CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5:€C' " " CF3 H 3,5-Cl2 CF3 H 3,5-C!2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H . 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H Srs^l-l CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3.5-Ci2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 ' CF3 H 3,5-CU CF3 H Si^et^ ^ CF3 H 3,5-Cl2 CF3 CH2OCH3 3,5-Cl2 CF3 CH^CN 3,5-Cl2 CF3 CH^C^CH 3,5-Cl2 CF3 C(0)CH3 3,5-CI, CF3 C(0)Et 3,5-Cl2 CF3 C(0)0CH3 3,5-Cl2 CF3 H 3,5-Cl2 CF3 CH2OCH3 3,5-C!2 CF3 CH2CN 3,5-Cl2 CF3 CHgC^CH 3,5-Cl2 CF3 C(0)CH3 3,5-Cl2 CF3 C(0)Et 3,5-Cl2 CF3 C(0)0CH3 146 CH2(D-8b)eH-3-^ CH(CH3)(D-8a) CH2(D-10a) CH2(D-10b)CI CH2(D-10b)Br CH,(D-10b)CH3 CH2(D-10b)eF3 CH2(D-10b)DCH3 CH2(D-10b)SCH3 CH2(D-11a) CH2(D-11b)CI CH2(D-11b)Br CH2(D-11b)Cff3 CH2(D-13a) CH2(D-13b)CHi CH2(D-14a) CH2(D-14b)CI CH2(D-14c)Cl CH(CF3)(D-14a) CH(CN)(D-14a) CH2(D-15a)CH3 CH(CH3)(D-15a)CH3 CH(CF3)(D-15a)CH3 CH(CN)(D-15a)GH3 CH2(D-15b)CI CH2(D-15c)CI CH2(D-16a)CH3 CH2(D-16a)CHF2 CH2(D-16a)CF2Br CH2,(D-16b)CI CH2(D-16b)CH3 CH2(D-16c)CI CH2(D-17a)ei4^ CH2(D-17a)CH3 CM2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)Ci 3,5-Cl2 CF3 " H 3,5-Cl2 CF3 H 3,5-Cl2 CF3: H 3,5-Ci2 CF3 H 3,5-Cl2 CF3 H 3,5-Clo CF3 ¬ CH2OCH3 3,5-Cl2 CF3 'CH2CN 3,5-Cl, CF3 CHsC^CH 3,5-Cl2 CF3 C(0)CH3 3,5-Cl2 CF3 C(0)Et 3,5-Cl2 CF3 C(0)0CH3 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 CH2OCH3 3,5-Cl2 CF3 CH2CN 3,5-Cl2 CF3 CH2C=CH 3,5-Cl2 CF3 C(0)CH3 3,5-Cl2 CF3 C(0)Et 3,5-Cl2 CF3 C(0)0CH3 3.5-Ci, CF3 H 3,5-Ci; CF3 H 3,5-Cl2 CF3 H 3,5-C!2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-C!2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 CH2OCH3 3,5-Cl2 CF3 CH2CN 3,5-Cl2 CF3 CH2C-CH 3,5-Cl2 CF3 C(0)CH3 3,5-Cl2 CF3 C(0)Et 3,5-Cl2 CF3 C(0)0CH3 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 147 CH2(D-17b)Br CH2(D-17b)CH3 CH2(D-17b)CF3 CH(CH3)(D-17a)CH3 CH(CH3)(D-17a)CH3(R) CH(CH3)(D-17a)CH3 CH(CH3)(D-17a)CH3 CH(CH3)(D-17a)CH3 CH(CH3)(D-17a)CH3 CH(CH3)(D-17a)CH3 CH(CH3)(D-17a)CH3 CH(CH3)(D-17b)CI CH(CH3)(D-17B)CI(R) CH(CH3)(D-17b)CI CH(CH3)(D-17b)CI CH(CH3)(D-17b)CI CH(CH3)(D-17b)CI CH(CH3)(D-17b)CI CH(CH3)(D-17b)CI CH(CF3)(D-17a)CH3 CH(CF3)(D-17b)CI CH(CN)(D-17a)CH3 CH(CN)(D-17b)CI CH2(D-18a) CH2(D-18b)CH3 CH2(D-18c)CH3 CH(CH3)(D-18a) CH2(D-19a) CH2(D-19b)CI CH2(D-19b)Br CH2(D-19b)CH3 CH(CH3)(D-19a) CH2(D-20a) CH2(D-20b)Cl CH2(D-20b)Br CH2(D-20b)CH3 CH(CH3)(D-20a) CH2(D-21a) CH 2(0-21 a) CH2(D-21a) CH2(D-21a) CH 2(0-21 a) CH2(0-21a) CH2(D-21a) CH2(D-21b)Br CH2(D-21b)CH3 H H H H H H H CH3 Et c-Pr CH2CF3 CH2OCH3 CH^OB 3,5-Ci2 CF3 3,5-Cl2 CF3 3,5-CI, CF3 3,5-Ci; CF3 3,5-Cl2 CF3 3,5-CI, CF3¬ 3.5-C!2 " CF3 3,5-Cl2 CF3 '3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 35-CI2 CF3 3I5-CI2 CF3 3,5fCl2 CF3 3,5-Ci2 CF3 3,5-Ci2 CF3 3,5-Ci2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 • 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Ci2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-C!2 ' CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-C(2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-C!2 CF3 3,5-Cl2 CF3 35-CI2 CF3 3,5-Cl2 CF3 35-CI2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 CH2(D-21c)Ci CH2(D-21c)Br CH2(D-21c)CH3 CH,(D-21c)CF3 CH2(D-21c)N02 CH(CH3)(D-21a) CH2(D-22a). CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a)~' CH2CH2OCH3 CH2(D-22a) CH2OCH2CH2CI CH2(D-22a) CH2OCH2CH2OCH3 CH2(D-22a) CH2SCH3 CH2CN CH2CH=CH2 CH^C^CH C(0)CH3 C(0)Et C(0)Pr-n C(0)Pr-i C(0)Pr-c C(0)Bu-t C(0)0CH3 C(0)OEt CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CCOpCHsCHsCI CH2(D-22a) C{0)OCH,CH,OCH, . CH2(D-22a) C(0)OCH2CH=CH2 CH2(D-22a) C(0)SCH3 C(S)0CH3 C(S)SCH3 OH 0C(0)CH3 0C(0)0CH3 OSO^CHg' SCCI3 SN(Bu-n)2 S(T-35) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) SN(Pr-i)CH2CH2C(0)OEt CH2(D-22a) SN(CH2Ph)CH2CH2C(0)OEt CH2(D-22a) SN(CH3)C(0)0Bu-n CH2(D-22a) H CH2(D-22b)CI H CH2(D-22b)Br 148 3,5-Ci2 CF3 3,5-Cl, CF3 3,5-Cl, CF. 3,5-0!; CF3 3,5-Cl2 CF3 3,5-Clo CF3'¬ 3,5-Ci; CF3 3,5-Ci; CF3 •3,5-012 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Ci2 CF33,5-Cl 2 CF33,5-CI 2 CF33,5'-CI, CF33,5-Cl2 CF33,5-Cl 2 CF33,5-Cl 2 CF33,5-CI 2 CF33,5-Cl2 CF33,5-C!2 CF33,5-Ci 2 CF33,5-CI 2 CF33,5-C!2 CF33,5-C!2 CF33,5-Cl2 CF33,5-C!2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-C!2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-CI 2 CF33,5-CI 2 CF3 3,5-CI 2 CF33,5-Cl2 CF33,5-CI 2 CF33,5-CI 2 CF33,5-CI 2 CF33,5-Cl2 CF33,5-C!2 CF33,5-CI 2 CF33,5-Cl2 CF3 H H H H H H H H H H H H H H H CH2OCH3 CH^CN CH^C^CH C(0)CH3 C(0)Et C(0)0CH3 H H H CH2OCH3 CH2CN CH2C=CH C(0)CH3 C(0)Et C(0)0CH3 H H H H H H H H H H H H H H H H 149 CH2(D-22b)CH3 CH,(D-22b)Et CH2(D-22b)Pr-i CH2(D-22b)CF3 CH2(D-22b)CF2C! CH2(D-22b)CF2Br CH2(D-22b)CH2S02CH3 CH2(D-22b)CH2CN CH2(D-22b)OCH3 CH2(D-22b)SCH3 CH,(D-22b)NH2 CH2(D-22b)MHCH3 CH2(D-22b)NtCH3)2 CH(CH3)(D-22a) CH(CH3)(D-22a)(R) CH(CH3)(D-22a) CH(CH3)(D-22a) CH(CH3)(D-22a) CH(CH3)(D-22a) CH(CH3)(D-22a) CH(CH3)(D-22a) CH(CF3)(D-22a) CH(CF3)(D-22a)(R) CH(CF3)(D-22a)(S) CH(CF3)(D-22a) CH(CF3)(D-22a) CH(CF3)(D-22a) CH(CF3)(D-22a) CH(CF3)(D-22a) CH(CF3)(D-22a) CH(CN)(D-22a) CH2(D-23a) CH2(D-23b)CI CH2(D-23b)Br CH2(D-23b)CH3 CH2(D-23c)CI CH2(D-23c)Br CH2(D-23c)CH3 CH2(D-24a) CH(CF3)(D-24a) CH(CN)(D-24a) CH2(D-25a)CH3 CH2(D-25b)Cl CH2(D-25b)Br CH2(D-25b)CF3 CH2(D-25c)CI 3,5-Cl2 CF33,5-Cl2 CF33,5-C!2 CF,,3,5-01^ CF33,5-C!2 CF33,5-C\, CF33,5-Ci2 CF33,5-Cl2 CF33,5-C!2 CF33,5-Cl2 CF33,5-Cl, CF33,5-Ci; CF33,5-Cl2 CF33,5-Cl2 CF33,5-CL CF33,5-Cl2 CF33,5-€i. CF33,5.01; CF33,5-C!2 CF33,5-Cl2 CF33,5-CL CF33,5-Cl3 CF33,5-CL CF33,5-CL CF33,5-CL CF33,5-Ci3 CF33,5-CL CF33,5-CL CF33,5-Cl2 CF33,5-CL CF33,5-CL CF33,5-Cl2 CF33,5-Cl2 CF33,5-CL CF33,5-CL CF33,5-Ci2 CF33,5-Ci2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF3 H H H H H H H H H CH2OCH3 CH2CN CH^C^CH C(0)CH3 C(0)Et C(0)0CH3 H H H H H H H H H H H H H H CH2OCH3 CH^CN CH^C^CH C(0)CH3 C(0)Ef C(0)0CH3 H H H H H CH2OCH3 CH2CN CH^C^CH C(0)CH3 C{0)Et C(0)OCH3 CH2(D-25c)Br CH2(D-25c)N02 CH2(D-26a)CH3 CH2(D-27a)CH3 CH2(D-27b)CI CH2(D-27b)Br CH2(D-27b)SCH3 CH2(D-27b)N6, CH2(D-28a) CH2(D-28a) CH2(D-28a) CH2(D-28ah CH2(D-28a) ^ CH2(D-28a) CH2(D-28a) CH(CH3)(D-28a) CH2(D-29a) CH2(D-29b)CH3 CH2(D-30a) CH2(D-30b)SCH3 CH2(D-31a) CH,(D-31b)CI CH2(D-31b)Br CH2(D-31b)CH3 CH2(D-31b)SCH3 CH2(D-32a)CI CH2(D-33a) CH2(D-33b)CH3 CH2(D-34a) CH2(D-34a) CH2(D-34a) CH2(D-34a) CH2(D-34a) CH2(D-34a) CH2(D-34a) CH2(D-34b)CI CH2(D-34b)Br CH2(D-34b)CH3 CH(CH3)(D-34a) CH2(D-35a) CH2(D-35a) CH2(D-35a) CH2(D-35a) CH2(D-35a) CH2(D-35a) CH2(D-35a) 3,5-Cl2 CF3 H CH2(D^35b)Ci 3.5-CI2 CF3 H CH,(D-35b)Br 3 5-C!, CF3 H CH,(D-35b)CH3 3'5-Cl CF3 H CH2(D-35b)SCH3 35-013 CF3 H CH(CH3)(D-35a) 3,5-CL CFa^ H CH2(D-36a) 3 5-C!, CF3 H CH,(D-36b)CH3 3,5-Ci; CF3 H CH2(D-37^) •3,5-CI, CF3 H CH2(D-37b)CH3 3,5-Ci; CF3 H CH2(D-38a) 3,5-Cl2 CF3 CH2OCH3 CH2(D-38a) 3,5-Cl2 CF3 CH2CN CH2(D-38a) 35-CI2 CF3 CH^C^CH CH2(D-38a)" 3,5-Cl2 CF3 C(0)CH3 CH2(D-38a) 35-CI2 CF3 C(0)Et CH2(D-38a) 35-CI2 CF3 C(0)0CH3 CH2(D-38a) 3,5~a, CF3 H CH(CF3)(D-38a) 3,5-Cl2 CF3 CH2OCH3 CH(CF3)(D-38a) 3,5-CL CF3 CH^CN CH(CF3)(D-38a) 3,5-Ci; CF3 CH^C^CH CH(CF3)(D-38a) 3,5-Cl2 CF3 C(0)CH3 CH(CF3)(D-38a) 3,5-Cl2 CF3 C(0)Et CH(CF3)(D-38a) 3,5-C!2 CF3 C(0)0CH3 CH(CF3)(D-38a) 3,5-C!2 CF3 H CH(CN)(D-38a) 3,5-Cl2 CF3 H CH2(D-39b)CI 3,5-Cl2 CF3 H CH2(D-39b)Br 3,5-Cl2 CF3 H CH2(D^0a)CH3 3,5-Cl2 CF3 H CH2(D-40b)CI 3,5-Cl2 CF3 H CH2(D-40b)Br 3,5-Cl2 CF3 H CH2(D-42b)Cl 3,5-Cl2 CF3 H CH3(D-i2b)Br 3,5-Cl2 CF3 H CH2(D-47a) 3,5-Cl2 CF3 CH3 CH2(D-47a) 3,5-Cl2 CF3 Et CH2(D-^7a) 3,5-Cl2 CF3 n-Pr . CK^(D^7a) 3,5-Cl2 CF3 i-Pr CH2(D-47a) 3,5-C!2 CF3 c-Pr , CH2(D^7a) 3,5-Cl2 CF3 n-Bu _ CH2(D-47a) 3,5-Cl2 CF3 CH2CF3 CH2(D-47a) 3,5-Cl2 CF3 CH2OCH3 CH2(D-47a) 3,5-Cl2 CF3 CH^OEt CH2(D-47a) 35-CI2 CF3 CH2CH2OCH3 CH2(D-47a) 3,5-CL CF3 CH(CH3)CH20CH3 CH2(D^7a) 3,5-aI CF3 CH2OCH2CH2CI CH2(D-47a) 3,5-Cl2 CF3 CH2OCH2CH2OCH3 CH2(D-47a) 3,5-Cl2 CF3 CH20CH2Ph CH2(D-47a) 151 3 5-C! CFg35.01' CF335.01' CF335.01' CF335.01' CF335.01' CP'335.01' CF335 01 OF33501' OF335-01' CF3 35.01 CF335-01 CF335-012 CF33 5-01 CF3 35.01 OF335-01 CF335.CI, OF3 35.01 OF33 5-01 CF3 , 35.01 OF33 5-01 CF335-01 CF335-01 CF3 35.01 OF335-OI2 CF335-OL CF33'5-OL CF335.01, CF33'5-CI CF33'5-OU CF33;5-Ol2 CF33,5-012 CF33 5-012 CF3 35.01 OF33;5-Ol2 CF33,5-012 CF33,5-012 CF33,5-012 CF33,5-Ol2 CF33,5-0(2 CF33,5-012 CF33,5-Ci2 CF33,5-Ol2 CF33,5-Ol2 CF335-CI2 CF33!5-Ol2 CF3 CH2SCH3 CH2(D-47a) CH2SO2CH3 CH.iMla) CH2SCF3 CH2(D-47a) CHsSPh CH,{D-47a) CH2CHO CH2(D-47a) CH2C(0)OCH3 CH2(D-47a) OH^CCOpEt CH2(D-47a) 0H2C(0)0Pr-n CH2(D^7a) CH2C(0)0Bu-t OH2(D-i7a) CH2ON 0H2(D^7a) OH20H=CH2 CH2(D^7a) OH^C^OH CH2(D^7a-> CH^Ph 0H3(D-47a) ~ OH2Si(OH3)3 CH2(D^7a) C(0)0H3 CH2(D^7a) C(0)Et CH2(D^7a) C(0)Pr-n CH2(D^7a) C(0)Pr-i CH2(D^7a) C(0)Pr-c OH2(D-47a) C(0)Bu-t 0H2(D-47a) 0(0)OH=OH2 CH2(D-47a) C(0)OOH3 0H2(D^7a) C(0)OEt 0H2(D-47a) C(0)OPr-n OH2(D^7a) 0(0)OPr-i OH2(D^7a) C(0)OPr-c 0H2(D-47a) OPpOHsOH^OI 0H2(D-47a) 0(O)O0H20H2O0H.3 CH2(D-47a) 0(0)OOH2CH=OH2' CH2(D-47a) 0(0)S0H3 0H2(D-47a) C(0)SEt 0H,(D-47a) 0(S)O0H3 0H2(D-47a) C(S)OEt 0H2(D-47a) 0(S)S0H3 0H2(D^7a) C(S)SEt 0H2(D-47a) Ph OH2(D^7a) OH 0H2(D-47a) OOH3 . 0H2(D-47a) O0H2Ph 0H2(D-47a) 00(0)CH3 0H2(D-47a) 00(0)OF3 CH2(D-i7a) 00(0)OOH3 0H2(D-47a) 00(0)NHCH3 CH2(D-47a) OSO2CH3 0H2(D-47a) OSO2CF3 CH2(D-47a) SCH3 0H2(D^7a) 3,5-Cl2 CF33,5-a, CF33,5-Cl2 CF,3,5-Cl2 CF33,5-C!2 CF33,5-a, CF33,5-Cl2 CF33 5-Ci2 CFg35-012 CF335-CI2 CF3sis-CIs CF335-CI2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5fCl2 CF33,5^Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Ci2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF335-CI2 CF33,5-Cl2 CF335-CI2 CF33,5-Cl2 CF33,5-Cl2 CF3 3,5-Cl2 CF33,5-Ci2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF3 SCCI3 CH2(D-47a) SPh CH2(D-^7a) SN(Et)2 CH,iD-47a) SN(Pr-i)2 CHaCCMTa) SN(Bu-n)2 CH2([>47a) S(T-35) CHaCD^Ta) SN(CH3)CH2CH2C(0)OEt CH2(D-47a) SN(Et)CH2CH2C(0)OEt CH2(D^7a) SN(Pr-i)CH2CH2C(0)OEt CH2(D-47a) SN(CH2ph)CH2CH2C(0)OEt CH2(D^7a) SN(CH3)C(0)0Et CH2(D^7a) SN(CH3)C(0)0Pr-n -CH2(D47a)' SN(CH3)C(0)0Bu-n ^ CH2(D^7a) SN(CH3)C(0)0Hex-n CH2(D^7a) SN(Et)C(0)OEt CH2(D^7a) SN(Et)C(0)OPr-n CH2(D-47a) SN(Et)C(0)OBu-n CH2(D^7a) SN(Pr-i)C(0)OEt CH2(D^7a) SN(Pr-i)C(0)OPr-n CH2(D-47a) SN(Pr-i)C(0)OBu-n CH2(D-47a) SO2CH3 CH2(D^7a) S02Et CH2(D^7a) NH2 CH2(D^7a) NHCH3 CH2(D-47a) NHEt CH2(D-47a) NHPr-i CH2(D-47a) NHCH2C-CH CH2(D-47a) N(CH3)2 CH2(D-47a) NHCHO CH2(D-47a) NHC(0)CH3 CH2(D-47a) NHC(0)Et CH2(D^7a) NHC(0)CF3 CH2(D^7a) NHC(0)Ph CH2(D-47a) NHC(0)0CH3 CH2(D^7a) NHC(0)OEt CH2(D^7a) NHC(6)0Bu-t CH2(D^7a) NHC(0)NHCH3 CH2(D^7a). NHC(0)NHPh CH2(D-47a) N(CH3)C(0)CH3 CH2(D-47a) N[C(0)CH3l2 CH^(D^7a) NHPh CH2(D^7a) NHSOgCHg CH2(D-47a) NHSO2NH2 CH2(D^7a) NHSO2NHCH3 CH2(D^7a) NHSOgNHPh CH2(D47a) NHSOgPh CH2(D-47a) 153 3 5-CU CF3sis-CI, CF33 5-CL CF3Sis-Cl. CF33,5-Ci: CF33,5-CI. CF3.3,5-Ci: CF33 5-C!, CF3 •35-CU CF33,5-Cl2 CF33,5-Ci2 CF33,5-CU CF33,5-CI, CF33,5-CI, CF33,5-CI, CF33,5-CI, CF33.5.CI2 CF335-CI2 CF33,5-CI, CF33,5-CI, CF33 5-CU CF33,5-Cl2 CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF3 3,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF33,5-CU CF3 N=CHCH3 N=C(CH3)3 N=CHPh H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H CH2OCH3 CH2OCH3 CH2CN CH2CN CHsC^CH" CH2C=CH C(0)CH3 C(0)CH3 C(0)Et C(0)Et C(0)0CH3 C(0)0CH3 154 CH^CD-^Ta) CH2([M7a) CH^CD^Ta) CH,(D^7b)Cl CH2(D-i7b)Br CH2(D^7b)CH3 CH,(D^7b)OCH3 CH2(D^7b)SCH3 CH2(D^7c)CI CH2(D-47c)Br CH2(D-47c)CH3 CH2(D-47c)GF3 CH2(D-47c)OCH3 CH2(D-^7c)CN CH2(D^7cl)F CH,(D^7d)Cl CH2(D-47d)Br CH2(D-47d)CH3 CH2(D^7d)CF3 CH2(D-47d)OCH3 CH2(D^7d)N02 CH2(D-47d)CN CH2(D^7e)F CH2(D-47e)CI CH,{D^7e)Br CH2(D-47e)CH3 CH2(D-47e)CF3 CH2(D^7e)OCH3 CH2(D^7e)CN CH2(D-47f) CH2(D-47g) CH(CH3)(D-47a) CH(CH3)(D^7a)(R) CH(CH3)(D-47a)(S) CH(CH3)(D-47a) CH(CH3)(D-^7a)(R) CH(CH3)(D-47a) CH(CH3)(D^7a)(R) CH(CH3)(D-47a) CH(CH3)(D-47a)(R) CH(CH3)(D-47a) CH(CH3)(D^7a)(R) CH(CH3)(D-47a) CH(CH3)(D-47a)(R) CH(CH3)(D-47a) CH(CH3)(D^7a)(R) 3 5-CU CF3 H 35.01 CF3 H a's-C! CF3 H 3'5-CI CF3 CH2OCH3 s's-Cl! CF. CH^CN 35.01" CF' ^ CH2CSCH 3'5-CL CF3 C(0)CH3 3'5-CI CF3 C(0)Et 3'5-CL CF3 C(0)0CH3 s's-Cl! CF3 H 35-Ci: CF3 H 3'5-CL CF3 H 3;5-CI, CF3 H 35-CI2 CF3 H 3 5-CL CF3 H sis-CL CF3 H 3 5-Ci: CF3 H 3'5-CL CF3 H 3'5-CL CF3 H s's-CI^ CF3 H 35-CI2 CF3 H 3'5-Cl2 CF3 H 3 5-CI 2 CF3 H 35-CI2 CF3 H s's-CIs CF3 H 3'5-CL CF3 H 3,5-Ci2 CF3 H 35-CI2 CF3 H 3,'5-Cl2 CF3 H 3,5-Cl2 CF3 H 35-CI2 ' CF3 CH3 3i5-Cl2 CF3 Et 3,5-C!2 CF3 H 3,5-Cl2 CF3 H 3 5-CL CF3 H 3,5-Ci; CF3 H 3,5-CL CF3 H 3,5-Cl2 CF3 H 3,5-Cl3 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 •CF3 c-Pr 3,5-Cl2 CF3 H 3,5-Cl2 CF3 Et 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 155 CH(CF3)(D-47a) CH(CF3)(D-47a)(R) CH(CF3)(D-47a)(S) CH(CF3)(D-47a) CH(CF3)(D-47a) CH(CF3)(D-*7a) CH(CF3)(D-47a) CH(CF3)(D^7a) CH(CF3)(D-t7a) CH(CN)(D^7a) CH(CN)(D-47a)(R) CH(CN)(D-47a)(S) CH2(D^8a) " CH2(D-t8b)F CH2(D^8b)CI CH2(D^8b)Br CH2(D-^8b)CH3 CH2(D-48b)OCH3 CH2(D-48b)SCH3 CH2(D-48b)CN CH2(D^8c)CI CH2(D^8c)CH3 CH2(D-48c)CF3 CH2(D-48c)CH20CH3 CH2(D-48d)Br CH2(D^8d)CH3 CH2(D-48d)OCH3 CH2(D^8d)CN CH,(D-^8e)F CH2(D-48e)CI CH2(D-48e)Cl CH2(D-48e)CI CH2(D-48e)Br CH2(D-48e)CH3 CH2(D^8e)CF3 CH2(D^8e)OCH3 CH2(D-48e)SCH3 CH2(D-48e)CN CH2(D^8f) CH2(D-48g) CH2(D^9a) CH2(D-49a) CH2(D-i9b)F CH2(D-49b)F CH2(D^9b)CI CH2(D-49b)Br 3 5-CU CF3 3'5-Cl CF3 3 5-0! CF,3 3'5-CL CF3 sis-CI, Cr3 3,5-CU CF3 3,5.01, CF3 3 5-CI CF3 • 3;5.cL CF3 3 5-CI CF3 3!5-CL CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-CI, CF3 3,5-Ci; CF3 3,5-Cl2 CF3 3,5-C!2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 35-CI2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Ci2 CF3 3,5-C!2 CF3 3,5-Cl2 ' CF3 3,5-Cl2 CF3 3,5-C!2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Ci2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 H CH3(D-49b)CH3 H CH,(D-49b)CN H CH2(D-49c)CI H CH2(D^9c)OCH3 H CH,(D^9c)N02 H CH2(D-49c)CN H CH2(D^9d), H CH2(D-50a) CH2OCH3 CH2(D-50a) CH2CN CH2(D-50a) CH^C^CH CH^CD-SOa) C(0)CH3 CH2(D-50a7^ C(0)Et CH2(D-50a) C(0)0CH3 CH2(D-50a) H CH2{D-50b)CI H CH2(D-50b)CH3 H CH2(D-50b)CF3 H CH2(D-50b)OCH3 H CH2(D-50c)F H CH2(D-50c)CI H CH2(D-50c)Br H CH2(D-50c)OCH3 H CH2(D-50c)NO2 H CH2(D-50c)CN H CH2(D-50c)C(O)NH2 H CH(CH3)(D-50a) H CH2(D-51a) H CH2(D-51b)CI H CH2(D-51b)CH3 H CH2(D-51b)OCH3 H CH2(D-51b)SCH3 H CH2(D-51b)CN H CH2(D-51c)CI H CH2(D-51c)CH3 H CH2(D-51c)OCH3 H CH2(D-51c)SCH3 H CH2(D-51c)CN H _ CH2(D-51d)F H CH2(D-51d)OCH3 H CH2(D-51d)CN H eH(CH3)(D-51a) H CH2(D-52a) H CH2(D-52b)Ci H CH2(D-52b)Br H CH2(D-52b)OCH3 H CH2(D-52b)SCH3 156 3 5-Cl, CF335-CI CF3s's-Cl^ CF,,3 5-Cl CF33!5-Cl, CF33 5-CL CF-3¬sis-Ci: CF33,5-Ci; CF33 5-CL CF3sis-CI, CF33,5-Ci; CF33,5-Cl2 CF33,5-C!2 CF33,5-Ci2 CF33,5-0!^ CF33,5-Cl2 CF335:01, CF33,5-bL CF33,5-C(, CF3 . 3,5-Cl2 CF33,5-CU CF33,5-Cl2 CF33,5-Cl, CF33,5-Ci2 CF33,5-C!2 CF33,5-Cl2 CF33,5-CL CF33,5-C!; CF33,5-Cl2 CF33,5-CL CF33,5-Ci; CF33,5-Cl2 CF33,5-CI, CF33,5-C!: OF 33,5-C!; CF33,5-CU CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-C! 2 CF33,5-Cl2 CF33,5-C!2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-CL CF33,5-C[2 CF3 H CH2(D-52c)Ci H CH,(D-52c)OCH3 H CH2(D-53a) H CH,(D-53b)Cl H CH,(D-53b)Br H CH2{D-53b)CH3 H CH2(D-53b)OCH3 H CH3(D-53b)'CN H CH2(D-53b)C(0)NH, H CH2(D-53c)F H CH2(D-53c)CI H CH 2(0-530)0+13 H CH2(D-53c)OCH3 H CH2(D-53c)CN H CH2(D-53d)CI H CH2(D-53d)OCH3 H CH2(D-53d)SCH3 H GH2.(D-53d)CN H CH(CH3)(D-53a) H GH2(D-54a) H CH2(D-54b)CI H CH2(D-54b)OCH3 H CH(CH3)(D-54a) H CH2(D-55a) H CH2(D-56a) H CH2(D-57a) H CH2(D-58a) H CH2(D-59a) H CH2CH,(D^8a) H OCH3 . H 0CH2CH=CHCI H OCH^Ph H N(CH3)2 H N(Et)2 H N(Rr-n)2 H N(CH3)Bu-n H N(Bu-n)2 H . N(Bu-i)2 H T-27 H T-28 H T-29 H T-34 H T-38 H NHCH2CF3 H N(CH3)CH2CF3 H T-35 157 3,5-C!, CF3 H 3 5-Ci CF3 H 3,5-CI, CF,3 H 3,5-Cl2 CF3 H 3,5-Cl2 'CF3 H 3 5-C!. GFs H sis-cC CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-C!2 CF3 H 3,5-CI, CF3 H 3,5-Ci; CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-CI, CF3 H 3,5-Ci2 CF3 H 3 5-CI 2 CF3 H 3',5-Cl2 CF3 H 3,5-C!2 CF3 H 3,5-CI, CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-C!2 CF3 H 3,5-CI, CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 CH3 3,5-Cl2 CF3 CH2OCH3 3,5-Cl2 CF3 CH^CN 3,5-Cl2 CF3 CH2CH=CH2 3,5-Cl2 CF3 CH^C^CH 3,5-Cl2 CF3 C(0)CH3 . 3,5-Cl2 CF3 C(0)Et . 3,5-Cl2 CF3 C(0)0CH3 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Cl2 CF3 H 3,5-Ci2 CF3 H 3,5-Cl2 CF3 H 158 T-37 N(CH3CH=CH,), NHCHO N(CH3)CH0 N(Et)CHO N(Bu-n)CHO N(Ph)CHO, NHC(0)CH3 N(CH3)C(0)CH3 N(Ph)C(0)CH3 N(Ph)C(0)Et N(CH2Ph)C(O)CH20Ph ' NHC(0)Ph ^' NHC(0)0CH3 N{CH3)C(0)OCH3 N(Ph)C(0)0CH3 NHC(0)OPh NHCCOpCH^Ph N(Ph)C(0)SCH3 N(Ph)C(S)0CH3 N(CH3)C(S)SCH3 N(Ph)C(S)SCH3 N(CH3)C(S)NH2 N(CH3)C(S)NHCH3 NHC(S)N(CH3)2 N(CH3)C(S)NHPh N(Ph)C(S)NHPh T-31 T-33 NHPh N(CH3)Ph N(CH3)Ph N(CH3)Ph N(CH3)Ph c N(CH3)Ph N(CH3)Ph N(CH3)Ph N(CH3)Ph N(CH3)Ph N(CH20CH3)Ph N(CH20Et)Ph N(CH2SCH3)Ph N(CH2CN)Ph N(CH2CH=CH2)Ph N(CH2C=CH)Ph N(CH2Ph)Ph 3 5-CL CF3 35-Cl CF3 3'5-CI CF , 3'5-CI CF3^ 3'5-CI CF3 sis-CU CF3¬ 3 5-Ci: CF3 3'5-Ci CF3 3'5-C! CF3 3'5-C! CF3 3'5-CI CF3 3'5-CL CF3 3'5-CU CF3 3'5-C! CF3 3 5-CL CF3 3'5-CL CF3 3 5-CL CF3 Z,5-CU CF3 3 5-CL CF3 3 5-CL CF3 3 5-CL CF3 3,5-Cl2 CF3 3,5-CL CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-CI, CF3 3,5-C!2 CF3 3,5-Cl2 • CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-CU CF3 3,5-Ci2 CF3 3,5-Cl2 CF3 3,5-C!2 CF3 3,5-Cl2 CF3 3,5-C!2 CF3 H N(CH3)(Ph-2-F) H N(CH3)(Ph-3-F) H N(CH3)(Ph^-F) H N(CH3)(Ph-2-CI) H N(CH3)(Ph-3-C!) H NH(Ph^-CI) H N(CH3)(Ph-^-CI) H N(CH3)(Ph-4-Br) H N(CH3)(Ph-2-CH3) H N(CH3)(Ph-3-CH3) H N(CH3)(Ph-4-CH3) H N(CH3)(Ph^^F3) H N(CH3)(Ph^-OCH3) H N(CH3)(Ph^-0CHF,) H N(CH3){Ph^-OCF3) H N(CH3)(Ph^-SCH3) H N(CH3)(Ph-4-S03CH3) H N(CH3)(Ph-t-SCF3) H N(CH3)(Ph-4-S02NH2) H N(CH3)[Ph^-N(CH3)3] H N(CH3)(Ph-2-N02) H NH(Ph-3-N02) H N(CH3)(Ph-3-NO,) H NH(Ph-i-NO,} H N(CH3)(Ph^-N02) H NH(Ph-4-CN) H N(CH3)(Ph-4-CN) H N(CH3)(Ph-2,4-F2) H N(CH3)(Ph-2,5-F2) _ H N(CH3)(P-h-2,6-F2) H N(CH3)(Ph-3,4-F2) H N(CH3)(Ph-3,5-F2) H NH(D-3a) ¬ H N(CH3)(D-3a) H NH(D-4a) H • N(CH3)(D^a) H NH(D-21a) H ' N(CH3)(D-21a) H N(Et)(D-21a) H NH(D-47a) H N(CH3)(D-47a) CH2OCH3 N(CH3)(D-17a) CH3CN N(CH3)(D-47a) CH2C=CH N(CH3)(D-47a) C(0)CH3 N(CH3)(D-47a) C(0)Et N(CH3)(D^7a) 159 3 5-CL CF335-Ci CF3S'.S-C! CF3.35-Ci CF335-Ci: CF33'5-C! CFv3'5-CI CF33'5-CI CF33,'5-CI, CF3 3 5-CI CF33,'5-C!, CF33 5-CL CF33,5-CI, CF33.5-CL CF33,5-CI, CF33,5-C!3 CF33,5SCl2 CF33 5-CL CF33 5-CL CF33,5-CL CF33,5-CL CF33 5-CL CF33,5-CL CF33,5-Cl, CF33,5-CL CF33,5-CL CF33,5-Cl2 CF33,5-CL CF33,5-Cl2 CF33 5-CL CF33!5-CL CF33,5-CI, CF33,5-CL CF33 5-CL CF33,5-CL CF33,5-Cl2 CF33,5-Cl3 CF33,5-Cl2 CF33,5-CI, CF33,5-Cl2 CF33,5-Cl2 CF33,5-01, CF33,5-CU CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF3 C(0)0CH3 N(CH3)(D-47a) H N(Et)(D-47a) H NH(D^7b)CI H NH(D-l7d)F H NH(D^7d)CI H N(CH3)(D^7d)CI H NH(D^7d)CF3 H NH(D^7d)N02 H NH(D-l7e)CI H NH(D-47e)OCH3 H NH(D^7f) H N(CH3)(D-47f) H NH(D-50a) CH3 NH(D-50a) Et NH(D-50a) H N(CH3)(D-50a) CH2OCH3 N(CH3)(D-50a) CH^CN N(CH3)(D-50a) CH^C^CH N(CH3)(D-50a) C(0)CH3 N(CH3)(D-50a) C(0)Et N(CH3)(D-50a) C(0)0CH3 N(CH3)(D-50a) H N(Et)(D-50a) H NH(D-50b)CF3 H NH(D-51a) H N(CH3)(D-51a) H NH(D-53a) H N(CH3)(D-53a) H NH(D-53b)CH3 H NH(D-53b)OCH3 H NH(D-53c)CH3 H NH(D-54a) H N(CH3)(D-54a) H NH(D-54b)C! H NH(D-54b)CH3 H NH(D-54b)OCH3 H C(0)NHCH3 H ^ C(0)N(CH3)2 H C(0)NHEt H C(0)N(CH3)Et H C(0)N(Et)2 H C(0)NHPr-n H C(0)N(CH3)Pr-n H C(0)N(Pr-n)2 H C(0)NHPr-i H C(0)N(CH3)Pr-i 3,5-Cl2 CF3 H C(0)NHPr-c 3,5-Cl2 CF3 H C(0)NHBu-n 3,5-Cl3 CF.3 H C(0)NHBu-i 3,5-CL CF^3 H C(0)NHBu-s 3,5-Cl2 CF3 H C(0)NHBu-c 3,5-CU CF3 H C(0)NHBu-t 3,5-Cl2 CF3 H C(0)NHCH,CH2F 3,5-CL CF3 H C(0)N(CH3)CH2CH2F 3,5-CL CF3 H C(0)NHCH3CH2CI 3,5-CI, CF3 H C(0)N(CH3)CH2CH2CI 3,5-CL CF3 H C(0)NHCH2CH2Br 3.5-CU CF3 H C(0)NHCH2^F3 3,5-Cl2 CF3 H C(0)N(CH3)CH2CF3 3,5-CU CF3 H C(0)NHCH2CH2CH2CI 3,5-Cl2 CF3 H C(0)NHCH3CH20CH3 3,5-Ci2 CF3 H C(0)NHCH2CH2SCH3 3,5-CI, CF3 H C(0)NHCH2CH2S02CH3 3,5-Cl2 CF3 H C(0)NHCH2CN 3,5-Ci2 CF3 H C(0)NHCH2CH=CH2 3,5-Cl2 CF3 H C(0)N(CH3)GH2CH=CH2 3,5-Cl2 CF3 H C(0)N(CH2CH=CH2)2 3,5-CL CF3 H C(0)NHCH2CCNCH2 3,5-Cl2 CF3 H C(0)NHCH2C=CH 3,5-Cl2 CF3 H C(0)N(GH3)CH2C=CH 3,5-Cl2 CF3 H C(0)NHCH2Ph 3,5-Cl2 CF3 H C(0)NHCH2(D-22a) 3,5-Cl2 CF3 H C(0)NHCH2(D-^7a) 3,5-Cl2 CF3 H C(0)NHPh 3,5-CU CF3 H C(0)(T-28) 3,5-CU CF3 H C(O)(T-30) 3,5-Cl2 CF3 H C(0)CT-32) 3,5-CI, CF3 H C(0)(T-34) 3,5-Cl2 CF3 H C(0)(T-35) 3,5-CU CF3 H C(0)(T-36) 3,5-CU CF3 H C(S)NHCH3 3,5-CU CF3 H C(S)NHEt 3,5-CU CF3 H C(S)NHPr-n 3 5-CU CF3 H _ C(S)NHPr-i 3,5-Cl2 CF3 H C(S)NHPr-c 3,5-Cl2 CF3 H C(S)NHBu-n 3,5-Cl2 CF3 . H C(S)NHBu-i 3,5-Cl2 CF3 H C(S)NHBu-s 3,5-CU CF3 H C(S)NHBu-c 3,5-CU CF3 H C(S)NHBu-t 3,5-CL CF3 H C(S)NHCH2CH2F 3,5-CU CF3 H C(S)NHCH2CH2CI 161 3,5-Ci2 CF3 3,5-0!^ CF3 3,5-CL CF3 3,5-Cl2 CF3 3,5-Cl2 GF3 3,5-CU CF3¬ 3,5-Cl2 CF3 3,5-CU CF3 •3,5-Ci; CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-C!2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 ' CF3 3,5-Ci2 CF3 3,5-Cl2 CF3 3,5-C!2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3.5-CI2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 3,5-Cl2 CF3 H C(S)NHCH2CH2Br H C(S)NHCH2CF3 H C(S)NHCH2CH2CH2C1 H C(S)NHCH2CH30CH3 H C(S)NHCH2CH2SCH3 H C(S)NHCH2CH2S02CH3 H C(S)NHCH2CN H C(S)NHCH2CH=CH2 H C(S)NHCH2CC!=CH2 H CCSJNHCH^C^CH H C(S)NHCH2Ph H C(S)NHCH2(D-22a) H C(S)NHCH2([J-47a) H C(S)NHPh H Ph-4-F H Ph-4-CI H Ph-4-CH2SCH3 H Ph^-CH2S(0)CH3 H Ph-4-CH2S02CH3 H Ph^-0CH3 H Ph-4-OCHF2 H Ph-4-OS02CH3 H Ph^-SCHa H Ph-1-S(0)CH3 H Ph-4-S02CH3 H Ph^-S02NH2 H Ph^-NHC(0)CH3 H Ph^-NHSOsCHs H Ph^-NOs H Ph-2-CN H Ph-3-CN H Ph-4-CN H Ph^-C(0)NH2 H Ph-4-C(S)NH2 H D-8a H (D-8b)CH3 H D-9a H • (D-10b)CH3 H " (D-11b)CH3 H (D-12b)CI H (D-13b)CH3 H (D-15a)CH3 H (D-16b)CH3 H (D-17a)CH3 H D-21a H (D-21b)CH3 162 3,5-Ci, CF3 H (D-21c)C! 3,5-Cl2 CF3 H (D-21c)CH3 3,5-Cl2 CF3 H (D-21c)N02 3,5-C!, CF3 H D-22a 3,5-C!, CF3 H D-23a 3,5-C!2 eF3 H (D-26a)CH3 3,5-CL CF3 H ¬ (D-27a)CH3 , 3,5-C!, CF3 H D-29a ' • 3,5-CU CF3 H (D-30b)CH3 3,5-Cl, CF3 H (D-31b)CI 3,5-Cl2 .CF3 H (D-31b)CH3 3,5-Cl2 CF3 H (D-32a)CH3 ¬ 3,5-Cl2 CF3 H D-33a 3,5-C!2 CF3 H (D-33b)CH3 3,5-Cl2 CF3 H D-34a 3,5-Cl2 CF3 H (D-34b)CH3 3,5-Cl2 CF3 H D-35a 3,5-Cl2 CF3 H (D-35b)CH3 3,5-Cl2 CF3 H D-36a 3,5-Cl2 CF3 H (D-36b)CH3 3,5-Cl2 CF3 H D-37a 3,5-Cl2 CF3 H (D-39a)CH3 3,5-Ci2 CF3 H (D-40a)CH3 3,5-C!, CF3 H (D-42a)CH3 3,5-Cl2 CF3 H (D-45b)CH3 3,5-Cl2 CF3 H D-47a 3,5-Ci2 CF3 H D-48a 3,5-Cl2 CF3 H D-49a 3,5-Cl2 CF3 H D-50a 3,5-Cl2 CF3 H D-51a 3,5-Ci2 ' CF3 H D-52a 3,5-CU CF3 H D-53a 3,5-Cl2 CF3 H D-54a 3,5-Cl2 CF3 H D-SSa 3,5-Cl2 CF3 H D-56a 3,5-Cl2 CF3 H D-58a 3,5-Cl2 CF2CI ,, H Et 3,5-Cl2 CF2CI Et " Et 3,5-Cl2 CF2CI H c-Pr 3,5-Cl2 CF2CI H CHaPr-c 3,5-Cl2 CF2CI H c-Bu 3,5-Cl2 CF2CI H CH2CF3 3,5-Cl2 CF2CI CH2OCH3 CH2CF3 3,5-C!2 CF2CI CH2CN CH2CF3 3,5-Cl2 CF2CI CHaC^CH CH2CF3 3,5-Cl2 CF2CI C(0)CH3 CH2CF3 3,5-CU CF,C! C(0)Et CH2CF3 3,5-CL CF2CI C(0)Pr-c CH2CF3 3,5-CL CF2PI C(0)Bu-t CH2CF3 3 5-CL CF2CI C(0)0CH3 CH2CF3 3 5-CL CF^Ci CPpCH^CH^OCHg CH^CFg 35-01. CP2G! C(0)OCH2CH=CH2 CH2CF3 3'5-CL CF^Ci C(0)SCH3 CH2CF3 3'5-Cl, CF2CI C(S)0CH3 CH2CF3 •3,5-Ci; CF2CI C{S)SCH3 CH2CF3 3,5-CL CF^Cl H CH;CF,CF 3 3,5-CU CF2CI H CH2CH2OCH3 35-CI2 CF2CI H CH(CH3)CH£eCH3 3,5-Cl2 CF2CI H CH2CH(OCH3l2 3,5-Cl2 CF2CI H CH2(E-4a) 3,5-Cl3 CF^Ci H CH2(E-5a) 3,5-Cl2 CF2C! H CH2(E-10a) 3,5-;Cl2 CF2CI H CH2CH2SCH3 3,5-Cl2 CF2CI H CH2CH2S(0)CH3 3,5-Cl2 CF^Ci H CH2CH2SO2CH3 3,5-Cl2 CF2CI H CH2CH(CH3)SCH3 3,5-Cl2 CF2CI H CH2CH(CH3)S(0)CH3 3,5-Cl2 CF2C! H CH2CH(CH3)S02CH3 3,5-Cl2 CF2CI H CH(CH3)CH2SCH3 3,5-Cl2 CF^Ci H CH(CH3)CH2S(0)CH3 3,5-CI, CF2CI H CH(CH3)CH2S02CH3 3,5-Ci; CF2CI H CH2C(0)CH3 3,5-Cl2 CF2CI H CH2CH=NOCH3 3,5-Cl2 CF2CI H CH2C(CH3)=NOCH3 3,5-Cl2 CF2CI H CH2CN 3,5-Cl2 CF2CI H CH2C(0)NHCH3 3,5-Cl2 CF2CI H CH2C(0)N(CH3)2 3,5-Cl2 CF2CI H CH2C(0)NHEt 3,5-Cl2 CF2CI H CH2C(0)NHCH2CH2F 3,5-Cl2 CF2CI H CH2C(0)NHCH2CH2CI 3,5-Cl2 CF2CI H CH,2C(0)NHCH2CF3 35-CI2 CF2CI H CH2C(0)NHCH2CH=CH2 3,5-Cl2 CF2CI . H CH2C(0)NHCH2C=CH 35-CI2 CF2CI H CH(CH3)C(0)NHCH2CH2CI 3,5-Cl2 CF2CI H CH2C(S)NHEt 3,5-Ci2 CF2CI H CH2CH=CH2 3,5-Cl2 CF2CI H CH2CCI=CH2 3,5-Cl2 CF2CI H CH2CCI=CHCI 3,5-Cl2 CF2CI H CH2C=CH 3,5-Cl2 CF2CI H CH(CH3)Ph(R) 3,5-Cl2 CF2CI H CH(CF3)Ph 3,5-Cl2 CF2CI H CH2(Ph-4-F) 164 3 5-CI2 CF^CI H CH2(Ph-4-OCH3) 3 5-CU CF^CI H CH2(Ph^-N02) 3 5-Ci: CF2CI H CH2(Ph^-CN) 3,5-01^ CF^C! H CH(CH3)(D-1a)(R) 3,5-Ci2 CF^C! H CH2(D-17a)CH3 3 5-CJ2 Cf-,Gi CH2OCH3 CH2(D-17a)CH3 ib-a^ CF2CI CH^CN CH2(D-17a)CH3 3 5-CI2 CF2C! CHsC^CH CH2(D-17a)CH3 3,5-Cl2 CF2CI C(0)CH3 CH2(D-17a)CH3 3,5-Cl2 CF2CI C(0)Et CH2(D-17a)CH3 3,5-Cl2 CF2CI C(0)0CH3 CH2(D-17a)CH3 3,5-CU CF^Ci H CH2(D-17b)Gl 3,5-Ci2 CF2CI CH2OCH3 CH2(D-17b)CI 35-CI2 CF^Ci CH2CN CH2(D-17b)CI 35-012 CF2C! CHsC^CH CH2(D-17b)CI 3,5-Cl2 CF2CI C(0)CH3 CH2(D-17b)Ci 3,5Cl2 CF2CI C(0)Et CH2(D-17b)CI 3 5^Cl2 CF2CI C(0)0CH3 CH2(D-17b)CI 3!5-Cl2 CF2Ci H CH2(D-19a) 3,5-Cl2 CF2CI H CH2(D-21a) 3,5-Cl2 CF2CI H CH2(D-22a) 3,5-Cl2 CF2CI CH2OCH3 CH2(D-22a) 3,5-Cl2 CF2CI CH2CN CH2(D-22a) 3,5-Cl2 CF2CI CHgC-CH CH2(D-22a) 3,5-Ci, CF2Ci C(0)CH3 CH2(D-22a) 3,5-CU CF2CI C(0)Et CH2(D-22a) 3,5-Cl2 CF2CI C(0)Pr-c CH2(D-22a) 3,5-Cl2 CF2CI C(0)Bu-t CH2(D-22a) 3,5-Cl2 CF2Ci C(0)0CH3 CH2(D-22a) 3,5-Cl2 CF2CI CCOpCHsCHsOCHg CH2(D-22a) 3,5-Cl2 CF2CI C(0)OCH2CH=CH3 CH2(D-22a) 3,5-Cl2 CF2CI C(0)SCH3 CH2(D-22a) 3,5-Ci, CF2Ci C(S)0CH3 CH2(D-22a) 3,5-Cl2 CF2CI C(S)SCH3 CH2(D-22a) 3,5-Cl2 CF2CI H CH(CH3)(D-22a) 3,5-Cl2 CF2CI H CH2(D-28a) 3,5-Cl2 CF2CI H CH2(D-34a), 3,5-Cl2 CF2CI H CH2(D-35a) 3,5-Cl2 CF2CI H CH2(D-38a) 3,5-Cl2 CF2CI H CH(CF3)(D-38a) 3,5-Cl2 CF2CI H CH2(D-47a) 3,5-Ci2 CF2CI CHsOCHg CH2(D-47a) 3,5-Cl2 CF2CI CH2CN CH2(D-47a) 3,5-Cl2 CF2CI CHsC^CH CH,{D^7a) 3,5-Cl2 CF2C! C(0)CH3 CH2(D^7a) 3,5-Ci2 CF2CI C(0)Et CH2(D^7a) 165 3,5-Cl2 CF2CI3,5-Cl., CF2CI3,5-CI.^ CF^CI3,5-Cr, CF;CI3,5-CU CF2CI3,5-Cl2 CF^Cl3,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-CU CF2CI3,5-CL CF2CI3,5-Cl2 CF2CI3,5-Cl 2 CF2CI3,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-Cl 2 CF2CI3,5-Cl 2 CF2CI3,5hCl2 CF2CI3,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-C!2 CF2CI3,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-Cl2 CF2CI 3,5-Cl 2 CF2CI3,5-Cl 2 CF2CI3,5-Cl 2 CF2CI3,5-Cl 2 CF2CI3,5-Cl 2 CF2CI3,5-Cl 2 CF2CI3,5-Cl2 CF2CI3,5-Cl 2 CF2CI3,5-Cl2 CF2CI3,5-Cl 2 CF2CI3,5-Cl 2 CF2CI3,5-Cl 2 CF2CI3,5-Cl 2 CFsBr3,5-Cl 2 CFgBr3,5-Cl2 CF2Br3,5-Cl 2 CF2Br3,5-Cl2 CFgBr3,5-Cl2 CFgBr3,5-Cl2 CF2Br3,5-Ci2 CF2Br3,5-Cl2 CFaBr3,5-Cl2 CF2Br 3,5-Cl2 CFgBr C(0)Pr-c CH2(D-47a) C(0)Bu-t CH2(D-47a) C(0)0CH3 CH2(D-47a) C(0)0CH2CH20CH3 CHgCD^Ta) C(0)OCH2CH=CH2 CH^CD^Ya) C(0)SCH3 CH^CD^Za) C(S)0CH3 CH2(D-47a) C(S)SCH3 CH2(D-47a) H CH(CH3)(D-^7a) C(0)0CH3 CH(CH3)(D-47a) H CHaCD-SOa) H CH2(D-51a)^ H CH2(D-53a) H NHNHCH2CF3 H N(CH3)Ph C(0)CH3 N(CH3)Ph C(0)Et N(CH3)Ph C(0)0CH3 N(CH3)Ph H N(CH2C=CH)Ph H N(CH3)(D^7a) C(0)CH3 N(CH3)(D-47a) C(0)Et N(CH3)(D-47a) C(0)0CH3 N(CH3)(D^7a) H NH(D-50a) CH3 NH(D-50a) H N(CH3)(D-50a) C(0)CH3 N(CH3)(D-50a) C(0)Et N(CH3)(D-50a) C(0)0CH3 N(CH3)(D-50a) H (D-13b)CH3 H (D-15a)CH3 H D-21a H D^7a H D-50a H D-51a H CH2Pr-c H c-Bu H . CH2CF3 C(0)CH3 CH2CF3 C(0)Et CH2CF3 C(0)0CH3 CH2CF3 H CH2CH2OCH3 H CH2(E-10a) H CH(CH3)CH2S02CH3 H CH2CH=NOCH3 H CH2C(0)NHCH2CH2C! 166 3,5-CI, CF^Br3,5-Ci: CF^Br3,5-C!.; CF,Br3 5-CU CFgBr3.5-Ci; CF3r3,5-01,, CR,Br.3,5-C!2 CF^Br3,5-CU CF^Br •3,5-CU CF,Br3,5-Cl2 CF,Br3,5-CU CF.Br3,5-Ci; CF^Br3,5-Cl2 CF2Br3,5-Cl2 CF^Br 3,5-Cl2 CF^Br 3,5-Cl2 CF^Br3,5.012 CF^Br3,5-CI, CF^Br3,5-Cl2 CFgBr3,5-Cl2 CF2Br3,5-Cl2 CFgBr3,5-CI 2 CFsBr3,5-Cl2 CF2Br3,5-Ci2 CFgBr3,5-CI 2 CF2I3,5-Cl2 CFCI23,5-CI 2 CFCIBr3,5-Cl2 CFBr23,5-Cl2 CCI33,5-Cl2 CF2CHF23,5-Cl2 CF2CHF23,5-Cl2 CF2CHF23,5-Cl2 CF2CHF23,5-Cl2 CF2CHF23,5-Cl2 CF2CHF23,5-CI 2 CF2CHF23,5-Cl2 CF2CHF23,5-Cl2 CF2CHF23,5-Cl2 CF2CHF23,5-Cl2 CF2CHF23,5-Cl2 CF2CHF23,5-Ci, CF2CHF23,5-Cl2 CF2CHF2 3,5-Ci2 CF2CHF23,5-Cl2 CF2CHF23,5-Cl2 CF2CHF2 H H H H H H C(0)CH3 C(0)Et C(0)0CH3 H CH2OCH3 CH^CN CH^C^CH C(0)CH3 C(0)Et C(0)0CH3 C(0)0CH3 H C(0)0CH3 C(0)0CH3 H C(0)0CH3 H H C(0)0CH3 H H H H H H C(0)CH3 C(0)Et C(0)0CH3 H H H H H H H H C(0)CH3 C(0)Et C(0)0CH3 H 167 CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-21a) CH2(D-22a) CH,(D-22a) CH2(D-22a) CH2(D-22a) CH^CD^ya) CH2(D-i7a) CYi,{DA7ay CH2(D-47ar CH3(D-i7a) CH^iD-47a) CH2(D^7a) CH(CH3)(D-47a) N(CH3)Ph N(CH3)Ph N(CH3)(D^7a) N(CH3)(D-50a) N(CH3)(D-50a) (D-13b)CH3 (D-15a)CH3 CH2(D^7a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-^7a) c-Bu CH2CF3 CH2CF3 CH2CF3 CH2CF3 CHgCH^OCHa CH2(E-10a) CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-22a) CH2(D-22a) CH2(D--22a) CH2(D-22a) CH2(D-47a) 3 5-CI, CF3CHF, CH^CN 3 5-Ci. CF.CHF^ C(0)CH3 s's-CU CF0CHF2 C(0)Et 3 5-CL CF.,CHF, C(0)0CH3 3'5-CU CF2CHF2 C(0)0CH3 3;5-CI, CF.CHF, ' H 3 5-CI, CF2CHF2 H 35-012 CF2CHF2 C(0)0CH3 3!5-Cl2 CF2CF3 H 3,5-Cl2 CF,CF3 H . 3,5-Cl2 CF2CF3 C(0)CH3 3,5-CU CF,GF3 C{0)Et 3,5-CU CF2CF3 C(0)0CH3 3,5-Cl2 CF.CFg H 3,5-CI, CF,CF3 H 3 5-CI, CF2CF3 H 3'5-CL CF3CF3 H 3,5-CU CF2CF3 H 3,5-Cl2 CF2CF3 H 3,5-Cl2 CF2CF3 H 3,5-Cl2 CF2CF3 H 3,5-Cl2 CF2CF3 C(0)CH3 3,5-Ci3 CF,CF3 C(0)Et 3,5-Cl2 CF2CF3 C(0)0CH3 3,5-CI, CF3CF3 H 3,5-CU CF2CF3 CH2CN 3,5-Ci; CF2CF3 C(0)CH3 3,5-Cl2 CF2CF3 C(0)Et 3,5-Ci2 CF2CF3 C(0)0CH3 3,5-Cl2 CF2CF3 C(0)0CH3 3,5-Cl2 CF2CF3 H 3,5-Cl2 CF2CF3 H 3,5-Cl2 CF2CF3 C(0)0CH3 3,5-Ci2 CF2CF2CI CH2CN 3,5-Ci2 CFCICF3 H 3,5-Cl2 CFCICF2CI H 3,5-Cl2 CF^CF^Br H 3,5-Cl2 CFBrCFg H 3,5-Cl2 CF2CHFCF3 C(0)CH3¬ 3,5-Cl2 CF2CF3CF3 H 3,5-Cl2 CF2CF2CF3 C(0)CH3 3 5-CU CF2CF2CF3 H i5-C\l CF2CF2CF3 H 3,5-Cl2 CF2CF2CF3 H 3,5-Cl2 CF2CF2CF3 H 3,5-C!2 CF2CF2CF3 CH2CN 168 CH,(D-47a) CH2(D-47a) CH,(D-t7a) CH3(D-47a) CH(CH3)(D^7a) N(CH3)Ph N(CH3)(D-50a) N(CH3)(D-50a) c-Bu CH,CF3 CH2CF3 CH3CF3 ^ CH2CF3 ¬ CH2CH2OCH3 CH2(E-10a) CH2C(0)NHCH2CH2CI CH3C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D^7a) CH2(D-t7a) CH2(D^7a) CH,(D-47a) CH2(D^7a) CH(CH3)(D-47a) N(CH3)Ph N(CH3)(D-50a) N(CH3)(D-50a) CH2(D^7a) N(GH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2(D-47a) CH2CF3 CH2CF3 CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D^7a) N(CH3)Ph N(CH3)(D-50a) 3 5-CI2 CF2CF2CF3 C(0)Et CH2(D-47a) 3'5-Ci CF^CF.CFs H CH(CH3)Ph(R) 3'5-CU CF.CF^CFa H N(CH3)Ph 35-CL CF2CFXF3 H N(CH3)(D-50a) 3,5-01, CF(CF3h H N(CH3)(D-50a) 35-CI2 CB^CFCICF^C! H CH2(D-22a) 35-01, CF^CFBrCF^Cl H CH2(D-47a) 3'5-OL OF2CF2CF2OHF2 C(0)Et CH2(D^7a) 3!5-0!, CF.CF.CF^CFs H N(CH3)(D-50a) 35-OI2 CF(CF3)CF,CF3 H 'CH2C(0)NHCH2CF3 35-012 CF.OF.OFaCF^CI H CH2(D-22a) 35-OI2 OF2OF2OF2CF2CF2CF3 H 0H^-17b)C! 3-Cl-5-Br CF3 CH^C^CH CH2(D-17b)CI 3-CI-5-Br CF3 C(0)CH3 CH2(D-17b)Ci 3-CI-5-Br CF3 C(0)Et CH2(D-17b)C! 3-Cl-5-Br CF3 C(0)0CH3 CH2(D-17b)CI 3-CI-5-Br CF3 H CH^CD-IQa) 3-CI-5-Br CF3 H CH^CD-aia) 3-CI-5-Br CF3 H CH2(D-22a) 3-CI-5-Br CF3 CH2OCH3 CH2(D-22a) 3-Cl-5-Br CF3 CH2CN CH2(D-22a) 3-Ci-5-Br CF3 CH2C=CH CH2(D-22a) 3-CI-5-Br CF3 C(0)CH3 CH2(D-22a>¬ 3-Cl-5-Br CF3 C(0)Et CH2(D-22a) ^ 3-CI-5-Br CF3 C(0)Pr-c CH2(D-22a) 3-Cl-5-Br CF3 C(0)Bu-t CH2(D-22a) 3-CI-5-Br CF3 C(0)OCH3 CH2(D-22a) 3-CI-,5-Br CF3 C(0)OCH2CH2 0CH3 CHgCD¬ 22a)' 3-CI-5-Br CF3 C(0)OCH2CH=CH2 CH2(D-22a) , 3-Cl-5-Br CF3 C(0)SCH3 CH2(D-22a) 3-CI-5-Br CF3 C(S)0CH3 CH2(D-22a) 3-CI-5-Br CF3 C(S)SCH3 CH2(D-22a) 3-CI-5-Br CF3 H CH(CH3)(D-22a) 3-CI-5-Br CF3 H CH2(D-28a) 3-Cl-5-Br CF3 H CH2(D-34a) 3-CI-5-Br CF3 H CH2(D-35a) 3-Cl-5-Br CF3 H CH2(D-38a) 3-CI-5-Br CF3 H CH(CF3)(D-38a) 3-CI-5-Br CF3 H CH2(D-47a) 3-CI-5-Br CF3 CH2OCH3 CH2(D-47a) 3-CI-5-Br CF3 CH2CN CH2(D^7a) 3-CI-5-Br CF3 CHaC^CH CH2(D^7a) 3-CI-5-Br CF3 C(0)CH3 CH2(D-47a) 3-CI-5-Br CF3 C(0)Et CH2(D-47a) 3-CI-5-Br CF3 C(0)Pr-c CH2(D-47a) 3-CI-5-Br CF3 C(0)Bu-t CH2(D-47a) 3-CI-5-Br CF3 C(0)CH20CH3 CH2(D-47a) 3-CI-5-Br CF3 C(0)CH2SCH3 CH2(D^7a) 3-CI-5-Br CF3 C(0)0CH3 CH2(D-47a) 3-CI-5-Br CF3 CCOpCHsCHsOCHa CH2(D¬ 47a) 3-CI-5-Br CF3 C(0)OCH2CH=CH2 CH2(D47a) 3-CI-5-Br CF3 C(0)SCH3 CH2(D^7a) 3-CI-5-Br CF3 C(S)0CH3 CH2(D-47a) 3-CI-5-Br CF3 C(S)SCH3 CH2(D-47a) 3-CI-5-Br CF3 H CH(CH3)(D^7a) 176 3-Cl-5-Br CF3 3-CI-5-Br CF3 3-Cl-5-Br CF3 3-Cl-5-Br CF. 3-CI-5-Br CF3 3-CI-5-Br CF3¬ 3-CI-5-Br CF3 3-CI-5-Br CF3 • 3-Cl-5-Br CF3 3-Cl-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-Ci-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-Cl-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-C!-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-Cl-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-Cl-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI C(0)0CH3 H H H H H C(0)CH3 C(0)Et C(0)0CH3 H H C(0)CH3 C(0)Et C(0)0CH3 H CH3 H C(0)CH3 C(0)Et C(0)0CH3 H H H H H H H H H C(0)CH3 C(0)Et C(0)0CH3 H H H H H H H H H H H C(0)CH3 C(0)Et C(0)0CH3 177 CH(CH3)(D^7a) CH^CD-SOa) CH^CD-SIa) CH2(D-53a) NHNHCH^CFg N(CH3)Ph N(CH3)Ph N(CH3)Ph N(CH3)Ph N(CH2C=CH)Ph N(CH3)(D^7a) N(CH3)(D^a) N(CH 3)(D-47ar) N(CH 3)(D-^7a) NH(D-50a) NH(D-50a) N(CH3)(D-50a) N(CH3)(D-50a) N(CH3)(D-50a) N(CH3)(D-50a) (D-13b)CH3 (D-15a)CH3 D-21a D-47a D-50a D-51a CHsPr-c c-Bu CH2CF3 CH2CF3 CH2CF3 CH2CF3 CH2CH2OCH3 CHgCE-lOa) CH(CH3)CH,S02CH3 CH2CH=NOCH3 CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-21a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) 3-CI-5-Br CF2CI 3-C!-5-Br CF^CI 3-CI-5-Br CF.Ci 3-Cl-5-Br CF^CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2G! 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI •3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF2CI 3-CI-5-Br CF^Br 3-Ct-5-Br CFgBr 3-Ci-5-Br CFsBr 3-CI-5-Br CF2Br 3-CI-5-Br CF2CHF2 3-CI-5-Br CF2CHF2 3-CI-5-Br CF2CHF2 3-CI-5-Br CF2CHF2 3-Cl-5~Br CF2CF3 3-CI-5-Br CF2OCH3 3-CI-5-Br CF2SCH3 3,4-Br2 CF3 3,4-Br2 CF3 3,4-Br2 CF3 3,4-Bro CF3 3,4-Br2 ' CF3 3,4-Br2 CFg 3,4-Br2 CF3 3 4-Br2 CF3 3,4-Br2 CF3 3,4-Br2 CF3 3,4-Br2 CF3 3,4-Br2 CF3 3,4-Br2 CF3 3,4-Br2 CF3 3,4-Br2 CF3 3,4-Br2 CF3 3,4-Br, CF3 3,4-Br2 CF3 3,4-Br2 CF3 3,4-Br2 CFg H CH2(D-47a) CH^OCHg CH^lD^Ta) CH^CN CH^CD^/a) CH,C=CH CHsCD^Ta) C(d)CH3 CH^lD^ya) C(0)Et CH2(D^7a) C(0)0CH3 CH2(D-47a), C(P)0CH3 CH(CH3)(D-47a) H N(CH3)Ph C(0)0CH3 N(CH3)Ph C(0)0CH3 N(CH3)(D-17a) H N(CH3)(D-50a) C(0)0CH3 N(CH3)(D-50a) H (D-13b)CH3 H (D-15a)CH3 H CH2CF3 H CH2C(0)NHCH2CF3 H CH2(D-22a) H CH2(D^7a) H CH2CF3 H CH2C(0)NHCH2CF3 H CH2(D-22a) H CH2(D-47a) C(0)0CH3 CH2(D^7a) H N(CH3)(D-50a) H CH2C(0)NHCH2CF3 H c-Bu H CH2CF3 C(0)CH3 CH2CF3 C{0)Et CH2CF3 C(0)0CH3 CH^CFg H CH2CH2OCH3 H CH2(E-10a) H CH2C{0)NHCH2CH2CI H CH2C(0)NHCH2CF3 H CH(CH3)Ph(R) H CH2(D-17a)CH3 H . CH 2(0-17b)CI H CH2(D-22a) C(0)CH3 CH2(D-22a) C(0)Et CH2(D-22a) C(0)0CH3 CH2(D-22a) H CH2(D^7a) CH2CN CH2(D^7a) C(0)CH3 CH2(D^7a) C(0)Et CH2(D-47a) 178 3 5-Br, CF3Sis-Br^ CF33,5-Br, CF:335.Br, CF:,S.'s-Br, CF33 5-Br2 CF.S's-Br, CF ;3_5.Br, CF335.Br, CF33 5-Br, CF3Sis-Br, CF335.Br, CF335-Br, CF33^5.Br, CF33,5-Br2 CF33,5-Br2 CF33,5-Br2 CF3 3,4-Br2 CF3 C(0)0CH3 CH^lD^Ta) 3,4-Br2 CF3 C(0)0CH3 CH(CH3)(D-47a) 3,4-Br2 CF3 H N(CH3)Ph 3,4-Br, CF3 H N(CH3)(D-50a) 3,4-Br; CF3 C(0)0CH3 N(CH3)(D-50a) 3,5-Br2 CHF.2 H CH^CFg 3,5-Br2 CHF2 H CH2C(0)NHCH2CF3 3,5-Br2 CHF2 H CH2(D-22a) •3,5-Br2 CHF2 H CH2(D-*7a) 3,5-Br2 CHFC! H CH2(D-22a) 3,5-Br2 CHCI2 H CH2(D-47a) 3,5-Br2 CHFBr C(0)CH3 CH^CCMYa)^ 3,5-Br2 CF3 H Et 3,5-Br2 CF3 Et Et 3,5-Br2 CF3 H c-Pr 3,5-Br2 CF3 H CH^Pr-c 3,5TBr2 CF3 H c-Bu 3,5-br2 CF3 H CH2CF3 3,5-Br2 CF3 CH2OCH3 CH2CF3 3,5-Br2 CF3 CH2CN CH2CF3 3,5-Br2 CF3 CH2CSCH CH2CF3 3,5-Br2 CF3 C(0)CH3 CH2CF3 3,5-Br2 CF3 C(0)Et CH2CF3 3,5-Br2 CF3 C(0)Pr-c CH2CF3 3,5-Br2 CF3 C(0)Bu-t CH2CF3 3,5-Br2 CF3 C(0)0CH3 CH2CF3 3,5-Br2 CF3 C(0)OCH2CH20CH3 CH3CF3 3,5-Br2 CF3 C(0)OCH2CH=CH2 CH2CF3 3,5-Br2 CF3 C(0)SCH3 CH2CF3 3,5-Br2 CF3 C(S)0CH3 CH2CF3 3,5-Br2 CF3 C(S)SCH3 CH2CF3 3,5-Br2 CF3 H CH2CF2CF3 3,5-Br2 CF3 H CH2CH2OCH3 3,5-Br2 CF3 H CH(CH3)CH20CH3 3,5-Br2 CF3 H CK,CH(OCH3)2 3,5-Br2 CF3 H CH^CE^a) 3,5-Br2 CF3 H CH2(E-5a) 3,5-Br2 CF3 H CH2(E-10a) 3,5-Br2 CF3 H CH2CH2SCH3 3,5-Br2 CF3 H CH2CH2S(0)CH3 3,5-Br2 CF3 H CH2CH2SO2CH3 3,5-Br2 CF3 H CH2CH(CH3)SCH3 3,5-Br2 CF3 H CH2CH(CH3)S(0)CH3 3,5-Br2 CF3 H CH2CH(CH3)S02CH3 3,5-Br2 CF3 H CH(CH3)CH2SCH3 3,5-Br2 CF3 H CH(CH3)CH2S(0)CH3 179 3d-Br, CF3 3,5-Br2 CF33,5-Br2 CF33.5-Br2 CF33,5-Br2 CF33,5.Br, CF33,5-Br2 CF33,5-Br, CF33,5-Br2" CF33,5.Br, CF33,5-Br, CF33,5-Br2 CF33,5-Br2 CF33,5-Br, CF33,5-Br2 CF33,5-Br2 CF33,5-Br2 CF33 5-Br2 CF33'5-Br2 CF33 5-Br2 CF33,'5-Br2 CF33,5-Br2 CF33,5-Br2 CF33,5-Br2 CF33,5-Br2 CF33,5-Br2 CF33,5-Br2 CF33,5-Br2 CF33,5-Br2 CF3 H H H H H H H H H H H H H H H H H H H H H H H H H H H CH2OCH3 CH,CN CH2C=CH C(0)CH3 C(0)Et C(0)0CH3 H CH,0CH3 CH2CN CH,C=CH C(0)CH3 C(0)Et C(0)0CH3 H H H CH2OCH3 CH2CN CHgC^CH 180 CH(CH3)CH2S02CH3 CH2C(0)CH3 CH,CH=^40CH3 CH3C(CH3)=NOCH3 CH^CN CH2C(0)NHCH3 CH2C(0)N{CH3)2 CH,C(0)NHEt CH,C(0)NHCH,CH2F CH2C(0)NHCH,CH,CI CH3C(0)NHCH,CF3 CH,C(0)NHCH,CH=CH2 . CH^CCONHCH^C^CH CH(CH3)C(0)NHCH,CH2CI CH2C(S)NHEt CH,CH=CH, CH2CCNCH2 CH,CC1=CHCI CH3CSCH CH(CH3)Ph(R) CH(CF3)Ph CH3(Ph-4-F) CH,(Ph-4-OCH3) CH^CPh^-NO^) CH2(Ph-4-CN) CH(CH3)(D-1a)(R) CH3(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH,(D-17a)CH3 CH2(D-17a)CH3 CH,(D-17a)CH3 CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)Ci CH2(D-17b)CI CH2(D-17b)CI CH2(D-19a) CH2(D-21a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) 3,5-Br2 CF3 3,5-Br3 CF3 3,5-Br2 CF3, 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3¬ 3 5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 • CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 C(0)CH3 CH2(D-22a) C(0)Et CH2(D-22a) C(0)Pr-c CH,iD-22a) C{0)Bu-t CH,{D-22a) C(0)0CH3 CH2(D-22a) C(0)OCH2CH20CH3 CH2{D-22a) C(0)OCH2CH=CH2 CH2(D-22a) C(0)SCH3 CH2(D-22a) C(S)0CH3 CH2(D-22a) C(S)SCH3 CH2(D-22a) H CH(CH3)(D-22a) H CH2(D-28a)¬H CH2(D-34a) H CH2(D-35a) H CH2(D-38a) H CH(CF3)(D-38a) H CH2(D-47a) CH2OCH3 CH2(D^7a) CH2CN CH2(D^7a) CH2C=CH CH2(D-47a) C(0)CH3 CH2(D-47a) C(0)Et CH2(D^7a) C(0)Pr-c CH2(D-47a) C(0)Bu-t CH2(D-^7a) C(0)CH20CH3 CH2(D47a) C(0)CH2SCH3 CH2(D^7a) C(0)0CH3 CH2(D-*7a) C(0)OCH2CH20CH3 CH2(D^7a) C(0)OCH2CH=CH2 CH2(D47a) C(0)SCH3 CH2(D-47a) C(S)0CH3 CH2(D-i7a) C(S)SCH3 CH2(D-47a) H CH(CH3)(D-47a) C(0)0CH3 CH(CH3)(D-47a) H CH.^(D-50a) H CH2(D-51a) H CH2(D-53a) H NHNHCH2CF3 H N(CH3)Ph C(0)CH3 N(CH3)Ph C(0)Et N(CH3)Ph C(0)0CH3 N(CH3)Ph H N(CH2C=CH)Ph H N(CH3)(D-47a) C(0)CH3 N(CH3)(D^7a) C(0)Et N(CH3)(D-47a) 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br, CP3 3,5-Br; CF3 3,5-Br3 GF; 3,5-Br2 CF3 3,5-Br, CF3 - 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF3 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3.5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3 5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 • CF2C! 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 . CF^CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2Ci 3,5-Br2 CF2Ci 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br2 CF2CI 3,5-Br, CF2Ci 3,5-Br; CF2Ci 3,5-Br2 CF2C! C(0)0CH3 N(CH 3)(D-47a) H NH(D-50a) CH3 NH(D-50a) H N(CH3)(D-50a) C(0)CH3 N(CH3)(D-50a) C(0)Et N(CH3)(D-50a) C(0)0CH3 N(CH3)(D-50a) H (D-13b)CH3 H (D-15a)CH3 H D-21a H D^7a H D-50a ^ H D-51a H CH^Pr-c H c-Bu H CH2CF3 C(0)CH3 CH^CFg C(0)Et CH2CF3 C(0)0CH3 CH^CFg H CH2CH2OCH3 H CH2{E-10a) H CH(CH3)CH2S02CH3 H CH2CH=NOCH3 H CH2C(0)NHCH2CH2CI H CH2C(0)NHCH2CF3 H CH(CH3)Ph(R) H CH2(D-17a)CH3 H CH2(D-17b)CI H CH2{D-21a) H CH2(D-22a) C(0)CH3 CH2(D-22a) C(0)Et CH2(D-22a) C(0)0CH3 CH2(D-22a) H CH2(D^7a) CH2OCH3 CH2(D^7a) CHgCN CH2(D-47a) CH2C=CH CH2(D-47a) C(0)CH3 CH2(D^7a) C(0)Et " CH2(D^7a) C(0)0CH3 CH2(D-47a) C(0)0CH3 CH(CH3)(D^7a) H N(CH3)Ph C(0)0CH3 N(CH3)Ph C(0)0CH3 N(CH3)(D-47a) H N(CH3)(D-50a) C(0)0CH3 N(CH3)(D-50a) 182 3,5-Br, CF.CI 3,5-Br, CF^C! 3,5-Br2 CF,Br 3 5-Br! CF^Br Sis-Br, CF^Br 3,5-Br3 CF^Br 3,5-Br2 CF2CHF2 3 5-Br CF3CHF, 3;5-Br, CF3CHF2 3,5-Br, CF.CHF, 3,5-Br, CF,CF3 3,5-Br2 CF2OCH3 35-Br, CF2SCH3 3-F-5-I CF3 3-CI-5-I CF3 3,5-12 CF3 3-eH3-4-F CF33-Fi4-CH3 CF32-F-5-CH3 CF33-F-5-CH CF33-F-5-CH3 CF33-F-5-CH3 CF33-F-5-CH3 CF33-CH3-4-CI CF33-CI-4-CH3 CF33-CI-5-CH3 CF3 3-CI-5-CH3 CF3 3-CI-5-CH3 CF3 3-CI-5-CH3 CF3 3-CI-5-CH3 CF3 3-CI-5-CH3 CF3 3-CI-5-CH3 CF3 3-CI-5-CH3 CF3 3-CI-5-CH3 CF3 3-CI-5-CH3 CF3 3-CI-5-CH3 CF3 3-CH3^-Br CF3 3-Br-5-CH3 CF3 3-Br-5-CH3 CF3 3-Br-5-CH3 CF3 3-Br-5-CH3 CF3 3-Br-5-CH3 CF3 3-Br-5-CH3 CF3 3-Br-5-CH3 CF3 3-Br-5-CH3 CF3 3-Br-5-CH3 CF3 H H H H H H H H H H H C(0)CH3 H H H H C(0)Et H H H H H H H H H C(0)CH3 H H H H CH^CN C(0)Et H H H C(0)CH3 H C(0)CH3 H H H H CH^CN C(0)Et H 183 (D-13b)CH3 (D-15a)CH3 CH^CFg CH3C(0)NHCH2CF3 CH,(D-22a) CH,(D-47a) CH2CF3 CH,C(0)NHCH3CF3 CH2(D-22a) CH,(D-47a) CH^lD-^Ta) CH^CD^ya) N(CH3)(D-50a) CH3C(0)NHCH2CF3 CH2(D-22a) CH,(D^7a) CH,(D-47a) N(CH3)(D-50a) CH,C(0)NHCH2CF3 CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D-22a) CH2(D-47a) CH2CF3 CH2CF3 CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-t7a) CH2(D-47a) CH2(D^7a). CH(CH3)Ph(R) N(CH3)Ph N(CH3)(D-50a) CH2(D-47a) CH^CFg CH^CFg CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D^7a) CH2(D^7a) CH(CH3)Ph(R) 3-Br-5-CH33-Br-5-CH32,4-(CH3)22,6-(CH3)23,4-(CH3)23,5-(CH3)23,5-(CH3),3,5-(CH3)23,5-(CH3)23-Br-5-Et3-CH3-5-Et3,5-(Et)23-CI-5-Pr-i3.Br-5-Pr-i3-CH3-5-Pr-i3,5-(Pr-i)23-CH3-5-Bu-n3,5-(Bu-s)23-CI-5-Bu-t3-Br-5-Bu-t3-CH3-5-Bu-t .3,5-(Bu-t)2 "•2-CF3^-F2-CF3-5-F2-F-3-CF33-CF3-4-F3-CF3^-F3-CF3^-F3-CF3-4-F3.CF3-4-Fa-CFg^-F3-CF3-4-F3-CF3-4-F3.CF3-4-F3-CF3-4-Fa-CFg-^-F3-CF3-4-F3-CF3^-F3.CF3^-F3-CF3-4-FS-CFs^-F3-CF3-4-F3-CF3-4-F3-CF3^-FS-CFg^-F3-CF3-4-F CF3 H CF3 H CF3 H CF3 H 'CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 C(0)0CH3 CF3 H CF3 H CF3 H CF3 H CF3 CH2CN CF3 H CF3 H CF3 H CF3 H CF3 C(0)Et CF3 • H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 C(0)CH3 CF3 C(0)Et CF3 C(0)0CH3 CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 C(0)CH3 CF3 C(0)Et CF3 C(0)0CH3 CF3 H 184 N(CH3)Ph N(CH3)(D-50a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-i7a) CH2(D-47a) CH2(D-47a) N(CH3)(D-5Q9) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2Pr-c c-Bu CH2CF3 CH2CF3 CH2CF3 CH2CF3 CH2CH2OCH3 CH2(E-10a) CH(CH3)CH2S02CH3 CH2CH=NOCH3 CfH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)Cl CH 2(0-21 a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-47a) 3-CF3-^-F CF3 CH2OCH3 • CH2(D-i7a) 3-CF3-i-F CF3 CH^CN CH2(D^7a) 3-CF3-4-F CF3 CH2C=CH CH2(D-47a) 3-CF3-^-F CF3 C(0)CH3 CH2(D-47a) 3-CF3^-F CF3 C(0)Et CH2(D-47a) 3-CF3^-F CF.3 C(0)0CH3 CH2(D-47a) 3-CF3-;-F CF3 C(0)0CH3 CH(CH3)(D-47a) 3-CF3-I-F CF3 H N(CH3)Ph 3-CF3-4-F CF3 C(0)0CH3 N(CH3)Ph 3-CF3-4-F CF3 C(0)0CH3 N(CH3)(D-47a) 3-CF3-4-F CF3 H N(CH3)(D-50a) 3-CF3-4-F CF3 C(0)0CH3 N(CH3)(D-50a) 3-CF3-4-F CF3 H (D-13b)CH3 ^ 3-CF3-4-F CF3 H (D-15a)CH3 2-F-4-CF3 CF3 C(0)0CH3 CH2(D-47a) 3-F-4-CF3 CF3 H N(CH3)(D-50a) 2-F-5-CF3 CF3 H CH2C(0)NHCH2CF3 3-F-5-CF3 CHF2 H CH2(D-22a) 3-F-5-CF3 CHCI2 H CH2(D-47a) 3-F-5-CF3 CF3 H Et 3-F-5-CF3 CF3 Et Et 3-F-5-CF3 CF3 H CH^Pr-c 3-F-5-CF3 CF3 H c-Bu 3-F-5-CF3 CF3 H CH2CF3 3-F-5-CF3 CF3 C(0)CH3 CH2CF3 3-F-5-CF3 CF3 C(0)Et CH2CF3 3-F-5-CF3 CF3 C(0)0CH3 CH2CF3 3-F-5-CF3 CF3 H CH2CH2OCH3 3-F-5-CF3 CF3 H CH2CH(OCH3)2 3-F-5-CF3 CF3 H CH^iE-Aa) 3-F-5-CF3 CF3 H CH2(E-5a) 3-F-5-CF3 CF3 H CH2(E-10a) 3-F-5-CF3 CF3 H CH2CH2SO2CH3 3-F-5-CF3 CF3 H CH2CH{CH3)S02CH3 3-F-5-CF3 CF3 H C.H(CH3)CH2S02CH3 3-F-5-CF3 CF3 H CH2CH=NOCH3 3-F-5-CF3 CF3 H CH^CCONHCH^CH^F 3-F-5-CF3 CF3 H CH2C(0)NHCH2CH2Ci 3-F-5-CF3 CF3 H CH2C(0)NHCH2CF3 3-F-5-CF3 CF3 H CH2C(0)NHCH2CH=CH2 3-F-5-CF3 CF3 H CH2C(0)NHCH2C=CH 3-F-5-CF3 CF3 H CH(CH3)C(0)NHCH2CF3 3-F-5-CF, CF3 H CH2CH=CH2 3-F-5-CF; CF3 H CH2C.C1=CH2 3-F-5-CF3 CF3 H CH2C-CH 3-F-5-CF3 CF3 H CH(CH3)Ph(R) 185 3-F-5-CF3 CFs ¬ H CH(CF3)Ph 3-F-5-CF3 CF3 H CH2(D-17a)CH3 3-F-5-CF3 CF3 H CH3(D-17b)CI 3-F-5-CF3 CPl H CH2(D-21a) 3-F-5-CF3 CF3 H CH2(D-22a) 3-F-5-CF3 CF3: . C(0)CH3 CH2(D-22a) 3-F-5-CF3 CF3 C(0)Et CH2(D-22a) 3-F-5-CF3 CF3 C(0)0CH3 CH2(D-22a) •3-F-5-CF3 CF3 C(0)OCH2CH=CH2 CH2(D-22a) 3-F-5-CF3 CF3 H CH3(D-28a) 3-F-5-CF3 CF3 H CH2(D-34a) 3-F-5-CF3 CF3 H CH2(D-35aK 3-F-5-CF3 CF3 H CH2(D-38a) ^ 3-F-5-CF3 CF3 H CH^iDAJa) 3-F-5-CF3 CF3 CH2OCH3 CH2(D-47a) 3-F-5-CF3 CF3 CH3CN CH2(D-47a) 3-F-5-CF3 CF3 CH2C=CH CH2(D^7a) 3-F-icF3 CF3 C(0)CH3 CH2(D-47a) 3-F-5-CF3 CF3 C(0)Et CH2(D^7a) 3-F-5-CF3 CF3 C(0)0CH3 CH2(D^7a) 3-F-5-CF3 CF3 C(0)OCH2CH=CH2 CH2(D^7a) 3-F-5-CF3 CF3 H CH(CH3)(D^7a) 3-F-5-CF3 CF3 C(0)0CH3 CH(CH3)(D-47a) 3-F-5-CF3 CF3 H CH2(D-50a) 3-F-5-CF3 CF3 H CH2(D-51a) 3-F-5-CF3 CF3 H CH2(D-53a) 3-F-5-CF3 CF3 H N(CH3)Ph 3-F-5-CF3 CF3 C(0)CH3 N(CH3)Ph 3-F-5-CF3 CF3 C(0)Et N(CH3)Ph 3-F-5-CF3 CF3 C(0)0CH3 N(CH3)Ph 3-F-5-CF3 CF3 H N(CH3)(D-47a) 3-F-5-CF3 CF3 C(0)CH3 N(CH3)(D^7a) 3-F-5-CF3 CF3 C(0)Et N(CH3)(D-17a) 3-F-5-CF3 CF3 C(0)0CH3 N(CH3)(D-47a) 3-F-5-CF3 CF3 H NH(D-50a) 3-F-5-CF3 CF3 H N(CH3)(D-50a) 3-F-5-CF3 CF3 C(0)CH3 N(CH3)(D-50a) 3-F-5-CF3 CF3 C(0)Et N(CH3)(D-50a) 3-F-5-CF3 CF3 C(0)0CH3 " N(CH3)(D-50a) 3-F-5-CF3 CF3 H (D-13b)CH3 3-F-5-CF3 CF3 H (D-15a)CH3 3-F-5-CF3 CF3 H D-21a 3-F-5-CF3 CF3 H D-50a 3-F-5-CF3 CF2CI H CH2CF3 3-F-5-CF3 CF2C! C(0)CH3 CH2CF3 3-F-5-CF3 CF2CI H CH^CCONHCHgCHsCI 186 3-F-5-CF3 CF^Cl 3-F-5-CF3 CF2CI 3-F-5-CF3 CF^Ci 3-F-5-CF3 CF.,CI 3-F-5-CF3 CF^Cl 3-F-5-CF3 .:CF3CI 3-F-5-CF3 CF;C I 3_F-5-CF3 CF2CI , 3-F-5-CF3 CF^Br 3-F-5-CF3 CF^Br 3-F-5-CF3 CF^Br 3_F-5-CF3 CF^Br 3-F-5-CF3 CF2CHF2 3-F-5-CF3 CF2CF3 3-F-5-CF3 CF2OGH3 2-F^-CF3 CF3 3-CF3^-CI CF3 3-iSF3-4-Cl CF3 3.CF3^-CI CF3 3-CF3^-CI CF3 3-CF3^-CI CF3 3-CF3-4-CI CF3 3-CF3-4-CI CF3 3-CF3^-CI CF3 3-CF3-4-CI CF3 3-CF3-4-CI CF3 3-CF.^-CI CF3 3-CF3^-CI CF3 3-CF3-4-CI CF3 3-CF3-4-CI CF3 3-CF3-4-CI . CF3 3-CF3-4-CI CF3 3-CF3-4-CI CF3 3-CF3-4-CI CF3 3-CF3^-CI CF3 3-CF3^-Cl CF3 3-CF3-4-CI CF3 3-CF3-4-CI CF3 3-CF3-4-CI CF3 3-CF3-4-CI CF3 3-CF3-4-CI CF3 3-CF3-4-C! CF3 3-CF3-4-CI CF3 3-CF3-4-CI CF3 3-CF3-4-CI CF3 3-CF3-4-CI CF3 H CH^CCONHCH^CFg H CH2(D-22a) H CH2(D-47a) CH^CN CH2(D-47a) C(0)Et CH2(D-47a) H CH(CH3)Ph(R) H N(CH3)Ph H N(CH3)(D-50a) H CH2CF3 H CH2C(0)NHCH2CF3 H CH2(D-22a) H CH^CD-tTa). CH2CN CH2{D-47a) H N(CH3)(D-50a) H CH3C(0)NHCH2CF3 H CH3(D-22a) H CH3Pr-c H c-Bu H CH3CF3 C(0)CH3 CH3CF3 C(0)Et CH3CF3 C(0)0CH3 CH2CF3 H CH2CH3OCH3 H CH3(E-10a) H CH(CH3)CH3S03CH3 H CH3CH=NOCH3 H CH2C(0)NHCH3CH3CI H CH3C(0)NHCH3CF3 H CH(CH3)Ph(R) H CH3(D-17a)CH3 H CH3(D-17b)CI H CH3(D-21a) H CH3(D-22a) C(0)CH3 CH3(D-22a) C(0)Et CH3(D-22a) C(0)0CH3 CH3(D-22a) H CH3(D^7a) CH2OCH3¬ CH 3(0-473) CH3CN ¬ CH3(D-47a) CH3C=CH CH3(D-^7a) C(0)CH3 CH2(D^7a) C(0)Et CH3(D^7a) C(0)0CH3 CH2(D-47a) C(0)0CH3 CH(CH3)(D-47a) H N(CH3)Ph C(0)0CH3 N(CH3)Ph 3-CF3-4-C1 CF3 3-CF3-^-CI CF3 3-CF3-4-CI CF, 3-CF3^-CI CF3, 3-CF3^-Ci CFs 2-CW-CF3 CEa: 2-CI-5-CF3 CF3 3-CI-5-CF3 CHF2 3-CI-5-CF3 CHFCI 3-CI-5-CF3 CHCI2 3-CI-5-CF3 CHFBr 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-Clr5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-Ci-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 C(0)0CH3 N(CH3)(D^7a) H N(CH3)(D-50a) C(0)0CH3 N(CH3)(D-50a) H (D-13b)CH3 H (D-15a)CH3 C(0)CH3 CH3(D^7a) H N(CH3){D-50a) H CH2C(0)NHCH2CF3 H CH2(D-22a) H CH2(D^7a) C(0)Et CH2(D-47a) H Et ^ Et Et H c-Pr H CH^Pr-c H c-Bu H CH2CF3 CH2OCH3 CH2CF3 CH2CN CH2CF3 C(0)CH3 CH2CF3 C(0)Et CH2CF3 C(0)Pr-c CH2CF3 C(0)Bu-t CH2CF3 C(0)0CH3 CH2CF3 C(0)SCH3 CH2CF3 C(S)0CH3 CH2CF3 C(S)SCH3 CH2CF3 H CH2CH2OCH3 H CH(CH3)CH20CH3 H CH2CH(OCH3)2 H CH2(E-4a) H CH2(E-5a) H CH2(E-10a)¬ H CH2CH2SO2CH3 H CH,CH(CH3)S02CH3 H CH(CH3)CH2S02CH3 H CH2CH=NOCH3 H • CH2C(CH3)=NOCH3 H CH2CN H CH2C(0)NHCH3 H CH2C(0)N(CH3)2 H CH2C(0)NHEt H CH2C{0)NHCH2CH2F H CH2C(0)NHCH2CH2C! H CH2C(0)NHCH2CF3 H CH2C(0)NHCH2CH=CH2 3-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF3 "3-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF3 3-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF33-CI-5-CF3 CFg CF3 CF3 CFg CF3 •eF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CFg CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 H CH2C(0)NHCH2C=CH H CH(CH3)C(0)NHCH2CH2CI H H H H H H H H H H H H H CH2OCH3 CH2CN CH2C-CH C(0)CH3 C(0)Et C(0)0CH3 H CH2OCH3 CH2CN CHaC^CH C(0)CH3 C(0)Et C(0)0CH3 H H H CH2OCH3 CH2CN CH2C=CH C(0)C.H3 C(0)Et C(0)Pr-c . C(0)Bu-t ¬ C(0)0CH3 CH2C(S)NHEt CH2CH=CH2 CH2CCI=CH2 CH2CCI=CHCi CH2C=CH CH(CH3)Ph(R) CH(CF3)Ph CH2(Ph^-F) CH2(Ph-4-OCH3) CH,(Ph-4-fQP2) CH2(Ph-4-CN) CH(CH3)(D-1a)(R) CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)Ci CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI CH2(D-19a) CH 2(0-21a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) ©H2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) H CH2(D-34a) CF3 C(0)OCH2CH20CH3 CH2(D-22a) CFg C(0)0CH2CH=CH, CH2(D-22a) CF3 C(0)SCH3 CH2(D-22a) CF3 C(S)0CH3 CH2(D-22a) CF3 C(S)SCH3 CH2(D-22a) CF3 H CH(CH3)(D-22a) CF3 H CH2(D-28a) 189 3-CI-5-CF3 CFg 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF^3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 • 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-GI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 '¬ CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CF3 3-CI-5-CF3 CFgCi 3-CI-5-CF3 CF2CI 3-CI-5-CF3 CFgCi H CH2(D-35a) H CH2(D-38a) H CH(CF3)(D-38a) H CH^CD^Ta) CH2OCH3 CH2(D^7a) CH^CN CH^(D^7a) CH2C=CH CH.(D47a) C(0)CH3 CH2(D^7a) C(0)Et CH2(D-47a) C(0)Pr-c CH2(D-47a) C(0)Bu-t CH2(D-47a)¬ C(0)0CH3 CH2(D^7a) CCOpCHgCHaOCHa CH2(D-47a) C(0)OCH2CH=CH2 CH2(D-47a) C(0)SCH3 C(S)0CH3 C(S)SCH3 H C(0)0CH3 H H H H C(0)CH3 C(0)Et C(0)0CH3 H H C(0)CH3 C(0)Et C(0)0CH3 H CH3 H C(0)CH3 C(0)Et , C(0)0CH3. H H H H H H H C(0)CH3 CH2(D-47a) CH2(D-47a) CH2(D^7a) CH(CH3)(D-t7a) CH(CH3)(D^7a) CH2(D-50a) CH2(D-51a) CH2(D-53a) N(CH3)Ph N(CH3)Ph N(CH3)Ph N(CH3)Ph N(CH2C=CH)Ph N(CH3)(D-47a) N(CH3)(D-47a) N(CH3)(D-47a) N(CH3)(D^7a) NH(D-50a) NH(D-50a) N(CH3)(D-50a) N(CH3)(D-50a) N(CH3)(D-50a) N(CH3)(D-50a) (D-13b)CH3 (D-15a)CH3 D-21a D-50a D-51a c-Bu CH2CF3 CH2CF3 3-CI-5-CF3 CF^Ci3-CI-5-CF3 CF2CI3-Ci-5-CF3 CF.CI3-CI-5-CF3 CF2CI3-Ci-5-CF3 CF2CI3-CI-5-CF3 CF^C!3-CI-5-CF3 CF2CI3-CI-5-CF3 CF2CI •3-CI-5-CF3 CF2CI3-CI-5-CF3 CF2CI3-CI-5-CF3 CF^Ci3-CI-5-CF3 CF2CI3-CI-5-CF3 CF^Ci3-CI-5-CF3 CF2CI3-Ci-5-CF3 CF2CI3-CI-5-CF3 CF2CI3-CI-5-CF3 CF2CI3-ci-5-CF3 CF2CI3-CI-5-CF3 CF2CI , 3-CI-5-CF3 CF2CI3-CI-5-CF3 CF2CI3-CI-5-CF3 CF2CI3-CI-5-CF3 CFaBr3-CI-5-CF3 CF^Br3-CI-5-CF3 CF^Br3-CI-5-CF3 CF^Br3-CI-5-CF3 CF2CHF23-CI-5-CF3 CF2CF33-CI-5-CF3 CF2OCH33-Br-5-CF3 CHF^3-Br-5-CF3 CHFCI3-Br-5-CF3 CHCI23-Br-5-CF3 CHFBr3-Br-5-CF3 CF33-Br-5-CF3 CF33-Br-5-CF3 CF33-Br-5-CF3 CF33-Br-5-CF3 CF33-Br-5-CF3 CF33-Br-5-CF3 CF33-Br-5-CF3 CF33-Br-5-CF3 CF33-Br-5-CF3 CF33-Br-5-CF3 CF33-Br-5-CF3 CF33-Br-5-CF3 CF3 C(0)Et CH^CFg C(0)0CH3 CH2CF3 H CH2CH2OCH3 H CH2(E-10a) H CH2C(0)NHCH2CH2CI H CH2C(0)NHCH2CF3 H CH(CH3)Ph(R) H CH2(D-17a)CH3 H CH2(D-17b)CI H CH2(D-22a) C(0)CH3 CH2(D-22a) C(0)Et CH2(D-22a)¬ C(0)0CH3 CH2(D-22a) H CH2(D^7a) CH2CN CH2(D-47a) C(0)CH3 CH2(D-47a) C(0)Et CH2(D^7a) C(0)0CH3 CH2(D-47a) C(0)0CH3 CH(CH3)(D-47a) H N(CH3)Ph H N(CH3)(D-50a) C(0)0CH3 N(CH3)(D-50a) H CH2CF3 H CH2C(0)NHCH2CF3 H CH2(D-22a) H CH2(D^7a) H N(CH3)(D-50a) H CH2C(0)NHCH2CF3 H CH2(D-22a) H CH2(D-47a) C(0)0CH3 CH2(D^7a) H N(CH3)(D-50a) H CH2C(0)NHCH2CF3 H Et Et Et • H c-Pr H . CHaPr-c H . c-Bu H CH2CF3 CH2OCH3 CH2CF3 CH2CN CH2CF3 C(0)CH3 CH2CF3 C(0)Et CH2CF3 C(0)Pr-c CH2CF3 C(0)Bu-t CH2CF3 C(0)0CH3 CH2CF3 191 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 'CF3 3-Br-5-CF3 SF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 • 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 ' CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 C(0)SCH3 CCSpCHg C(S)SCH3 H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H CH2OCH3 CH2CN CHsC^CH C(0)CH3 C(0)Et C(0)0CH3 H CH2OCH3 CH2CN 192 CH2CF3 CH^CFg CH^CFg CH2CH2OCH3 CH(CH3)CH20CH3 CH^CHCOCHg)^ CH^CE^a) CH^CE-Sa) CHsCE-lOa) CH^CH^SO^CHg CH2CH(CH3)S02CH3 CH(CH 3)01+280 ^CH 3 ¬ CH2CH=NOCH3 CH2C(CH3)=NOCH3 CH^CN CH^CCONHCHs CH2C(0)N(CH3)3 CH2C(0)NHEt Q.WS:,{0)mQW^QW^V CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH2C(0)NHCH2CH=GH2 CH2C(0)NHCH2C=CH CH(CH3)C(0)NHCH2CH2CI CH2C(S)NHEt CH2CH=CH2 CH2CCNCH2 CH2CCNCHCI CH2C=CH CH(CH3)Ph(R) CH(CF3)Ph CH2(Ph^-F) CH^CPh^-OCHg) CH2(Ph-4-N02) CH2(Ph-4-CN) CH(CH3)(D-1a)(R) CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI 3-Br-5-CF3 CF3 CH^C^CH CH2(D-17b)CI 3-Br-5-CF3 CF3 C(0)CH3 CH2(D-17b)CI 3-Br-5-CF3 CR,3 C(0)Et CH2(D-17b)CI 3-Br-5-CF3 CF3 C(0)0CH3 CH2(D-17b)CI 3-Br-5-CF3 tf, H CH2(D-19a) 3-Br-5-CF3 6F3 H CH2(D-21a) 3-Br-5-CF3 CF3 H CH2(D-22a). 3-Br-5-CF3 CF3 CH2OCH3 CH2(D-22a) 3-Br-5-CF3 CF3 CH2CN CH2(D-22a) 3-Br-5-CF3 CF3 CH2C=CH CH2(D-22a) 3-Br-5-CF3 CF3 C(0)CH3 CH2(D-22a) 3-Br-5-CF3 CF3 C(0)Et CH2(D-22a)¬ 3-Br-5-CF3 CF3 C(0)Pr-c CH2(D-22a) 3-Br-5-CF3 CF3 C(0)Bu-t CH2(D-22a) 3-Br-5-CF3 CF3 C(0)0CH3 CH2(D-22a) 3-Br-5-CF3 CF3 C(0)OCH2CH20CH3 CH2(D-22a) 3-Bf-5-CF3 CF3 C(0)OCH2CH=CH2 CH2(D-22a) 3-Br-5-CF3 CF3 C(0)SCH3 CH2(D-22a) 3-Br-5-CF3 CF3 C(S)0CH3 CH2(D-22a) 3-Br-5-CF3 CF3 C(S)SCH3 CH2(D-22a) 3-Br-5-CF3 CF3 H CH(CH3)(D-22a) 3-Br-5-CF3 CF3 H CH2(D-28a) 3-Br-5-CF3 CF3 H CH2(D-34a) 3-Br-5-CF3 CF3 H CH2(D-35a) 3-Br-5-CF3 CF3 H CH2(D-38a) 3-Br-5-CF3 CF3 H CH(CF3)(D-38a) 3-Br-5-CF3 CF3 H CH2(D-47a) 3-Br-5-CF3 CF3 CH2OCH3 CH2(D-47a) 3-Br-5-CF3 CF3 CH2CN CH2(D-47a) 3-Br-5-CF3 CF3 CH2C=CH CH2(D-47a) 3-Br-5-CF3 CF3 C(0)CH3 CH2(D-47a) 3-Br-5-CF3 CF3 C(0)Et CH2(D-47a) 3-Br-5-CF3 CF3 C(0)Pr-c CH2(D-47a) 3-Br-5-CF3 CF3 C(0)Bu-t CH2(D^7a) S-Br-S-CFg CF3 C(0)0CH3 CH2(D-47a) 3-Br-5-CF3 CF3 C(0)OCH2CH20CH3 CH2(D-47a) 3-Br-5-CF3 CF3 C(0)OCH2CH=CH2 CH2(D-47a) 3-Br-5-CF3 CF3 C(0)SCH3 CH2(D^7a) 3-Br-5-CF3 CF3 C(S)0CH3 CH2(D-47a) 3-Br-5-CF3 CF3 C(S)SCH3 CH2(D^7a) 3-Br-5-CF3 CF3 H CH(CH3)(D-47a) 3-Br-5-CF3 CF3 C(0)0CH3 CH(CH3)(D^7a) 3-Br-5-CF3 CF3 H CH2(D-50a) 3-Br-5-CF3 CF3 H CH2(D-51a) 3-Br-5-CF3 CF3 H CH2(D-53a) 3-Br-5-CF3 CF3 H N(CH3)Ph 193 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 GF3 3-Br-5-CF3 'GF3 3-Br-5-CF3 eF-3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 3-Br-5-CF3 CF3 S-Br-S-CFg CF3 3-Br-5-CF3 CFgCI 3-Br-5-CF3 CF^CI 3-Br-5-CF3 CF^Ct 3-Br-5-CF3 CF^CI 3-Br-5-CF3 CF^CI 3-Br-5-CF3 Cffi3-Br-5-CF3 CF^CI 3-Br-5-CF3 CF2CI 3-Br-5-CF3 CFgCI 3-Br-5-CF3 CF^CI 3-Br-5-CF3 CF^CI 3-Br-5-CF3 CF^CI 3-Br-5-CF3 CF^CI 3-Br-5-CF3 " CF2CI 3-Br-5-CF3 CF2CI 3-Br-5-CF3 CF2CI 3-Br-5-CF3 CFgCI 3-Br-5-CF3 CF2CI 3-Br-5-CF3 CF2CI 3-Br-5-CF3 CF2CI 3-Br-5-CF3 CF2CI 3-Br-5-CF3 CF2CI 3-Br-5-CF3 CF2CI 3-Br-5-CF3 CFgCI 3-Br-5-CF3 CFsCi 3-Br-5-CF3 CFaBr 3-Br-5-CF3 CFgBr C(0)CH3 C(0)Et C(0)0CH3 H H C(0)CH3 C(0)Et C(0)0CH3 H CH3 H C(0)CH3 C(0)Et C(0)0CH3 H H H H H H H C(0)CH3 C(0)Et C(0)0CH3 H H H H H H H H C(0)CH3 C(0)Et C(0)0CH3 H CH2CN C(0)CH3 . C(0)Et C(0)0CH3 C(0)0CH3 H H C(0)0CH3 H H 194 N(CH3)Ph N(CH3)Ph N(CH3)Ph N(CH2C=CH)Ph N(CH3)(D-47a) N(CH3)(D-47a) N(CH3)(D-47a) N(CH3)(D^7a) NH(D-50a) NH(D-50a) N(CHa)(D-50a) N(CH3)(D-^0a) N(CH3)(D-50a) N{CH3)(D-50a) (D-13b)CH3 (D-15a)CH3 D-21a D-50a D-51a c-Bu CH2CF3 CH2CF3 CH2CF3 CH2CF3 CH^CH^OCHg CH^CE-lOa) CHsCCONHCHaCH^CI CH^C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-47a) CH2(D-47a) CH2(D^7a) CH2(D-47a) CH2(D^7a) CH(CH3)(D^7a) N(CH3)Ph N(CH3)(D-50a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 3-Br-5-CF3 CF2Br H 3-Br-5-CF3 CF2Br H 3-Br-5-CF3 CfsCHFs H 3-Br-5-CF3 Cft^CFg H 3-Br-5-CF3 CF2OCH3 CH2CN 3-CH3-5-CF3 -'•CF3 H 3-CH3-5-CF3 CF3 H 3-CH3-5-CF3 CF3 C(0)CH3 3-CH3-5-CF3 CF3 C(0)Et 3-CH3-5-CF3 CF3 C(0)0CH3 3-CH3-5-CF3 CF3 H 3-CH3-5-CF3 CF3 H 3-CH3-5-CF3 CF3 H 3-CH3-5-CF3 CF3 H 3-CH3-5-CF3 CF3 H 3-CH3-5-CF3 CF3 H 3-GH3-5-CF3 CF3 H 3-CH3-5-CF3 CF3 H 3-CH3-5-CF3 CF3 C(0)CH3 3-CH3-5-CF3 CF3 C(0)Et 3-CH3-5-CF3 CF3 C(0)0CH3 3-CH3-5-CF3 CF3 H 3-CH3-5-CF3 CF3 CH2CN 3-CH3-5-CF3 CF3 C(0)CH3 3-CH3-5-CF3 CF3 C(0)Et 3-CH3-5-CF3 CF3 C(0)0CH3 3-CH3-5-CF3 CF3 C(0)0CH3 3-CH3-5-CF3 CF3 H 3-CH3-5-CF3 CF3 H 3-CH3-5-CF3 CF3 C(0)0CH3 3-Et-5-CF3 ' CF3 H 3-Pr-i-5-CF3 CF3 H 3-Bu-t-5-CF3 CF3 H 3,5-(CF3)2 CHF2 H 3,5-(CF3)2 CHF2 H 3,5-(CF3)2 CHF2 H 3,5-(CF3)2 CHF2 H 3,5-(CF3)2 CHFCI C(0)Et 3,5-(CF3)2 CHCi2 H 3,5-(CF3)2 CHFBr H 3,5-(CF3)2 CF3 H 3,5-(CF3)2 CF3 Et 3,5-(CF3)2 CF3 H 3,5-(CF3)2 CF3 H 3,5-(CF3)2 CF3 H 3,5-(CF3)2 CF3 H 195 CH2(D-22a) CH^CD^Ta) CH2(D-22a) CH2(D-47a), CH2(D^7a) c-Bu CH2CF3 CH2CF3 CH2CF3 CH2CF3 CH2CH2OCH3 CH2(E-10a) CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 . CH2(D-17b)CI CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-^7a) CH2(D^7a) CH2(D-47a) CH2(D^7a) CH2(D-^7a) CH(CH3)(D-t7a) N(CH3)Ph N(CH3)(D-50a) N(CH3)(D-50a) N(CH3)(D-50a) CH2(D-22a) CH2(D-47a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-17a) CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 Et Et c-Pr CH2Pr-c c-Bu CH2CF3 3,5-(CF3)2 CF3 CH2OCH3 CH2CF3 3,5-(CF3)2 CF3 CH^CN CH2CF3 3,5-(CF3)3 CF3; CH^C^CH CH^CFg 3,5-(CF3)2 CF3 C(0)CH3 CH,CF3 3,5-(CF3)2 CF3 C(0)Et CH2CF3 3,5-(CF3)2 CFs-, C(0)Pr-c CH2CF3 3,5-(CF3)2 CF3 C(0)Bu-t CH2CF3 3,5-(CF3)2 CF3 C(0)0CH3 CH2CF3 •3,5-(CF3)2 CF3 CCOpCH^CH^OCHg CH.CFg 3,5-(CF3)2 CF3 C(0)OCH2CH=CH2 CH2CF3 3,5-(CF3)2 CF3 C(0)SCH3 CH2CF3 3,5-(CF3)2 CF3 C(S)0CH3 CH2CF3 -¬ 3.5-(CF3)2 CF3 C(S)SCH3 CH2CF3 ' 3.5-(CF3)2 CF3 H CH.CF^CFs 3,5-(CF3)2 CF3 H CH2CH3OCH3 3.5-(CF3), CF3 H CH(CH3)CH20CH3 3,5;(CF3)2 CF3 H CH2CH(OCH3)2 3,5-(;CF3)2 CF3 H CH^CE^a) 3,5-(CF3)2 CF3 H CH2(E-5a) 3,5-(CF3)2 CF3 H CH2(E-10a) 3,5-(CF3)2 CF3 H CH2CH2SCH3 3.5-(CF3)2 CF3 H CH2CH2S(0)CH3 3,5-(CF3)2 CF3 H CH2CH2SO2CH3 3,5-(CF3)2 CF3 H CH2CH(CH3)SCH3 3,5-(CF3), CF3 H CH,CH(CH3)S(0)CH3 3,5-(CF3)2 CF3 H CH2CH(CH3)S02CH3 3,5-(CF3)2 CF3 H CH(CH3)CH2SCH3 3,5-(CF3)2 CF3 H CH(CH3)CH2S(0)CH3 3.5-(CF3)2 CF3 H CH(CH3)CH3S02CH3 3,5-(CF3)2 CF3 H CH2C(0)CH3 3,5-(CF3)2 CF3 H CH2CH=NOCH3 3,5-(CF3)2 CF3 H CH2C(CH3)=NOCH3 3,5-(CF3)2 CF3 H CH^CN 3,5-(CF3), CF3 H CH2C(0)NHCH3 3,5-(CF3)2 CF3 H CH,C(0)N(CH3)2 3,5-(CF3)2 CF3 H CH2C(0)NHEt 3,5-(CF3)2 CF3 H CH2C(0)NHCH2CH2F 3,5-(CF3)2 CF3 H CH2C(0)NHCH2CH3C! 3,5-(CF3)2 CF3 H CH3C(0)NHCH2CF3 3,5-(CF3)2 CF3 H CH2C(0)NHCH2CH=CH2 3,5-(CF3)2 CF3 H CH2C(0)NHCH2C^CH 3,5-(CF3)2 CF3 H CH(CH3)C(0)NHCH2CH2CI 3,5-(CF3)2 CF3 H CH2C(S)NHEt 3,5-(CF3)2 CF3 H CH2CH=CH2 3,5-(CF3)2 CF3 H CH2CCNCH2 3,5-(CF3)2 CF3 H CH2CCNCHCI 195 3,5-(CF3)2 CF3 H CH^C^CH 3,5-(CF3)2 CF3 H CH(CH3)Ph(R) 3,5-(CF3)2 CFL3 H CH(CF3)Ph 3,5-(CF3)2 CF^ H CH^CPh^-F) , 3,5-(CF3)2 CF3 H CH2(Ph-4-OCH3) 3,5-(CF3)2 GF3.^ H CH2(Ph-4-N02) 3,5-(CF3)2 CF3 H CH2(Ph-t-CN) 3,5-(CF3)2 CF3 H CH(CH3)(D-ia)(R) 3,5-(CF3)2 CF3 H CH2(D-17a)CH3 3,5-(CF3)2 CF3 CH2OCH3 CH2(D-17a)CH3 3,5-(CF3)2 CF3 CH3CN CH2(D-17a)CH3 3,5-(CF3)2 CF3 CH^C^CH CH2(D-17a)CH3 3,5-(CF3)2 CF3 C(0)CH3 CH2(D-17a)CH3 3,5-(CF3)2 CF3 C(0)Et CH2(D-17a)CH3 3,5-(CF3)a CF3 C(0)0CH3 CH2(D-17a)CH3 3,5-(CF3), CF3 H CH2(D-17b)CI 3,5KCF3)2 CF3 CH2OCH3 CH2(D-17b)CI 3,5-(CF3)3 CF3 CH2CN CH2(D-17b)CI 3,5-(CF3)2 CF3 CH2C=CH CH2(D-17b)CI 3,5-(CF3)2 CF3 C(0)CH3 CH2(D-17b)CI 3,5-(CF3)2 CF3 C(0)Et CH2(D-17b)CI 3,5-(CF3)2 CF3 C(0)0CH3 CH2(D-17b)Cl 3,5-(CF3)2 CF3 H CH2(D-19a) 3,5-(CF3)2 CF3 H CH2(D-21a) 3.5-(CF3)2 CF3 H CH2(D-22a) 3,5-(CF3)2 CF3 CH2OCH3 CH2(D-22a) 3.5-(CF3)2 CF3 CH2CN CH2(D-22a) 3,5-(CF3)2 CF3 CH^C^CH CH2(D-22a) 3,5-(CF3)2 CF3 C(0)CH3 CH2(D-22a) 3,5-(CF3)2 CF3 C(0)Et CH2(D-22a) 3,5-(CF3)2 * CF3 C(0)Pr-c CH2(D-22a) 3.5-(CF3)2 CF3 C(0)Bu-t CH2(D-22a) 3,5-(CF3)2 CF3 C(0)0CH3 CH2(D-22a) 3,5-(CF3)2 CF3 CCOpCH^CH^OCHs CH2(D-22a) 3,5-(CF3)2 CF3 C(0)OCH2CH=CH2 , CH2(D-22a) 3,5-(CF3)2 CF3 C(0)SCH3 CH2(D-22a) 3,5-(CF3)2 CF3 C(S)0CH3 CH2(D-22a) 3,5-(CF3)2 CF3 C(S)SCH3' CH2(D-22a) 3,5-(CF3)2 CF3 H CH(CH3)(D-22a) 3,5-(CF3)2 CF3 H CH2(D-28a) 3,5-(CF3)2 CF3 H CH2(D-34a) 3,5-(CF3)2 CF3 H CH2(D-35a) 3,5-(CF3)2 CF3 H CH2(D-38a) 3,5-(CF3)2 CF3 H CH(CF3)(D-38a) 3,5-(CF3)2 CF3 H CH2(D-47a) 3,5-(CF3)2 CF3 CH2OCH3 CH2(D-47a) 197 3.5-(CF3)2 CF3 CH,CN CH2{D-^7a) 3,5-(CF3)2 CF3 CHsC^CH CHsCD^Ta) 3,5-(CF3)2 CFs' C(0)CH3 CH^iDAJa) 3,5-(CF3)2 CF3 C(0)Et CH2(D-47a) 3,5-(CF3)2 CF3 C(0)Pr-c CH^lD^Ta) 3,5-(CF3)2 CP3¬ C(0)Bu-t CH2(D^7a) 3,5-(CF3)2 CF3 C(0)0CH3 CH2(D-47a) 3,5-(CF3)2 CF3 CCOpCH^CH^OCHg CH2(D^7a) '3,5-(CF3)2 CF3 C(0)OCH2CH=CH2 CH,(D-47a) 3,5-(CF3)2 CF3 C(0)SCH3 CH2(D-47a) 3,5-(CF3)2 CF3 C(S)0CH3 CH2(D-47a) 3,5-(CF3)2 CF3 C(S)SCH3 CH2(D-47ah 3,5-(CF3)2 CF3 H CH(CH3)(D-47a) 3,5-(CF3)2 CF3 C(0)0CH3 CH(CH3)(D-47a) 3,5-(CF3)2 CF3 H CH2(D-50a) 3,5-(CF3)2 CF3 H CH2(D-51a) 3,5-.(CF3)2 CF3 H CH2(D-53a) 3,5-(CF3)3 CF3 H NHNHCH2CF3 3,5-(CF3)2 CF3 H N(CH3)Ph 3,5-(CF3)2 CF3 C(0)CH3 N(CH3)Ph 3,5-(CF3)2 CF3 C(0)Et N(CH3)Ph 3.5-(CF3)2 CF3 C(0)0CH3 N(CH3)Ph 3,5-(CF3)2 CF3 H N(CH2C=CH)Ph 3,5-(CF3)2 CF3 H N(CH3)(D-47a) 3,5-(CF3)2 CF3 C(0)CH3 N(CH3)(D^7a) 3,5-(CF3)2 CF3 C(0)Et N(CH3)(D^7a) 3,5-(CF3)2 CF3 C(0)0CH3 N(CH3)(D^7a) 3,5-(CF3)3 CF3 H NH(D-50a) 3,5-(CF3)2 CF3 CH3 NH(D-50a) 3,5-(CF3)2 CF3 H N(CH3)(D-50a) 3,5-(CF3)2 CF3 C(0)CH3 . N(CH3)(D-50a) 3,5-(CF3)2 CF3 C(0)Et N(CH3)(D-50a) 3,5-(CF3)2 CF3 C(0)0CH3 N(CH3)(D-50a) 3,5-(CF3)2 CF3 H (D-13b)CH3 3,5-(CF3)3 CF3 H (D-t5a)CH3 3,5-(CF3)2 CF3 H D-21a 3,5-(CF3)2 CF3 H . D-17a 3,5-(CF3)2 CF3 H _ D-50a 3,5-(CF3)2 CF3 H D-51a 3,5-(CF3)2 CF2CI H CH^Pr-c 3.5-(CF3)2 CF2CI H c-Bu 3,5-(CF3)2 CF2CI H CH2CF3 3,5-(CF3)2 CF2CI C(0)CH3 CH2CF3 3,5-(CF3)2 CF2CI C(0)Et CH2CF3 3,5-(CF3)2 CF2CI C(0)0CH3 CH2CF3 3,5-(CF3)2 CF2C! H CH2CH2OCH3 198 3,5-(CF3)2 CF2CI3,5-(CF3)2 CF2CI3,5-(CF3)2 CF:,CI3.5-(CF3)2 CF2CI3,5-(CF3)2 CF2CI3,5-(CF3), eF,C!3.5-(CF3)2 CF2CI3,5-(CF3)2 CF^CI3,5-(CF3)2 CF.CI3,5-(CF3)2 CF2CI3,5-(CF3)2 CF2CI3,5-(CF3)2 CF^CI3,5-(CF3)3 CF2CI3,5-(CF3)2 CF2CI3,5-(CF3)2 CF2CI3,5-{CF3)2 CF2CI3,5-(CF3)3 CF2CI3,5-(CF3)2 CF2CI3,5-(CF3)2 CF^CI3,5-(CF3)2 CF2CI3,5-(CF3)2 CF2CI3,5-(CF3)2 CF.CI3,5-(CF3)2 CF2CI3,5-(CF3)2 CF2CI3,5-(CF3)2 CF2CI3,5-(CF3)2 CF2CI3,5-(CF3)2 CF2CI3,5-(CF3)2 CF2CI3,5-(CF3)2 CFaBr3,5-(CF3)2 CF^Br3,5-(CF3)2 CF^Br3,5-(CF3)2 CF^Br3,5-(CF3)2 CF2CHF23,5-(CF3)2 CF2CHF23,5-(CF3)2 CF2CHF23,5-(CF3)2 CF2CHF23,5-(CF3)2 CF2CF33,5-(CF3)2 CF2OCH33,5-(CF3)2 CF2SCH33-Ci-5-CF2CF3 CF33-CI-5-CF2CF3 CF33-CI-5-CF2CF3 CF33-CI-5-CF2CF3 CF33-CI-5-CF2CF3 CF33-CI-5-CF2CF3 CF33-CI-5-CF2CF3 CF3 H H H H H H H H H H C(0)CH3 C{0)Et C(0)0CH3 H CH2OCH3 CH2CN CH2C=CH C(0)CH3 C(0)Et C(0)0CH3 C(0)0CH3 H C(0)0CH3 C(0)0CH3 H C(0)0CH3 H H H H H H H H H H • H H C(0)0CH3 H H H H H CHgCN H 199 CH,(E-10a) CH(CH3)CH2S02CH3 CH2CH=NOCH3 CH^CCONHCH.CH^CI CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)CI CH3(D-21a) CH2(D-22a) CH2(D-22a) CH2(D-22a)^ CH2(D-22ar CH3([M7a) CH2(D^7a) CH2(D^7a) CH2(D-47a) CH2(D-47a) CH2(D-t7a) CH2(D^7a) CH(CH3)(D^7a) N(CH3)Ph N(CH3)Ph N(CH3)(D-47a) N(CH3)(D-50a) N(CH3)(D-50a) (D-13b)CH3 (D-15a)CH3 CH^CFg CHsCCONHCH^CFg CH2(D-22a) CH2(D-47a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D-22a) CH2(D-t7a) CH2(D-47a) CH2CF3 CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D^7a) N(CH3)(D-50a) S-Br-S-CFgCFa CF3 H CH2CF3 3-Br-5-CF2CF3 CF3 H CH2C(0)NHCH2CH2CI 3-Br-5-CF2CF3 CF;3 H CH2C(0)NHCH2CF3 S-Br-S-CFaCFg CFg H CH2(D-22a) a-Br-S-CFgCFa CF3 H CHgCD^/a) S-Br-S-CFsCFg GFg C(0)CH3 CH^iDAJa) 3-Br-5-CF2CF3 CF3 H N(CH3)(D-50a) 3-CH3-5-CF2CF3 CF3 H CH2CF3 3-CH3-5-CF2CF3 CF3 H CH2C(0)NHCH2CF3 3-CH3-5-CF2CF3 CF3 H CH2(D-22a) 3-CH3-5-CF2CF3 CF3 H CH2(D^7a) 3-Ci-5-CF2CF2CF3 CF3 H CH2CF3 ^ 3-CI-5-CF2CF2CF3 CF3 H CH2C(0)NHCH2CH2CI 3-CI-5-CF2CF2CF3 CF3 H CH2C(0)NHCH2CF3 3-CI-5-CF2CF2CF3 CF3 H CH2(D-22a) 3-CI-5-CF2CF2CF3 CF3 H CH2(D-47a) S-GI-S-CFgCFgCFs CF3 C(0)Et CH2(D-47a) 3-Ci-5-CF2CF2CF3 CF3 H ' N(CH3)(D-50a) 3-Br-5-CF2CF2CF3 CF3 H CH2CF3 S-Br-S-CFsCFgCFs CF3 H CH2C(0)NHCH2CH2CI 3-Br-5-CF2CF2CF3 CF3 H CH2C(0)NHCH2CF3 3-Br-5-CF2CF2CF3 CF3 H CH2(D-22a) 3-Br-5-CF2CF2CF3 CF3 H CH2{D-47a) 3-Br-5-CF2CF2CF3 CF3 C{0)OCH^ CH2(D-*7a) 3-Br-5-CF2CF2CF3 CF3 H N(CH3)(D-50a) 3-CH3-5-CF2CF2CF3 CF3 H CH2CF3 3-CH3-5-CF2CF2CF3 CF3 H CH2C(0)NHCH2CF3 3-CH3-5-CF2CF2CF3 CF3 H CH2(D-22a) 3-CH3-5-CF2CF2CF3 CF3 H CH2(D^7a) 3-CI-5-CF(CF3)2 CF3 H CH2CF3. 3-CI-5-CF(CF3)2 '¬ CF3 H CH2C(0)NHCH2CH2C1 3-CI-5-CF(CF3)2 CF3 H CH2C(0)NHCH2CF3 3-CI-5-CF(CF3)2 • CF3 H CH2(D-22a) 3-CI-5-CF(CF3)2 CF3 H CH2(D^7a) 3-CI-5-CF(CF3)2 CF3 CH2CN CH2(D-47a) 3-Ci-5-CF(CF3)2 CF3 H N(CH3)(D-50a) 3-Br-5-CF(CF3)2 CF3 H CH2CF3 3-Br-5-CF(CF3)2 CF3 H " CH2C(0)NHCH2CH2CI 3-Br-5-CF(CF3)2 CF3 H CH2C(0)NHCH2CF3 3-Br-5-CF(CF3)2 CF3 H CH2(D-22a) 3-Br-5-CF(CF3)2 CF3 H CH2(D-47a) 3-Br-5-CF(CF,)2 CF3 C(0)CH3 CH2(D-^7a) 3-Br-5-CF(CF3)2 CF3 H N(CH3)(D-50a) 3-CH3-5-CF(CF3)2 CF3 H CH2CF3 3-CH3-5-CF(CF3)2 CF3 H CH2C(0)NHCH2CF3 3-CH3-5-CF(CF3)2 CF3 H CH2(D-22a) 200 3-CH3-5-CF(CF3),3-CH3-5-CH2OCH33-CH3-5-CH2OCH2CF33-CF3-5-CH2SCH33-CF3-5-CH2S(0)CH33-CF3-5-CH2SO2CH33-Cl-5-C(CF3)20H3-CI-5-C(CF3)20H3-CI-5-C(CF3)20H3-CI-5-C(CF3)20H3-Br-5-C(CF3)20H3-Br-5-C(CF3)20H3-Br-5-C(CF3)20H3-Br-5-C(CF3)20H3-CH3-5-C(CF3)20H3-CH3-5-C(CF3)20H3-GH3-5-C(CF3)20H3-CH3-5-C(CF3)20H3-CI-5-C(CF3)20CH33-CI-5-C(CF3)20CH33-CI-5-C(CF3)20CH33-CI-5-C(CF3)20CH33-Br-5-C(CF3)20CH33-Br-5-C(CF3)20CH3S-Br-S-CCCFgjgOCHg3-Br-5-C(CF3)20CH33-CH3-5-C(CF3)20CH33-CH3-5-C(CF3)20CH33-CH3-5-C(CF3)20CH3 3-CH3-5-C(CF3)20CH33,5-(CH20CH3)2 '3,5-[C(CF3)20H]23,5-[C(CF3)20CH3]23-OCH3^-F2-F-4-OCH32-F-5-OCH33-CI-4-OCH33-CI-5-OCH33-Br-5-OCH33-Br-5-OCH33-Br-5-OCH33-Br-5-OCH33-Br-5-OCH33-Br-5-OCH33-Br-5-OCH33-CH3-5-OCH3 CF3 H CF3 H , CF3 H 'CF3 H " CF3 H ¬ -CF3 C(0)Et CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 C(0)0CH3 CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 CHgCN CF3 H CF3 H 201 CHa(D^7a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH^iDAla) CH2(D^7a) CH2CF3 , CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2CF3 CH2C(0)NHCH2CF3 ¬ CH2(D-22af CH2(D-47a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2CF3 GH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) eCH2(D^7a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2CF3 CHaCCOjNHCHgCHaCI CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2(D-47a) N(CH3)(D-50a) CH2(D-47a) 3-CF3-5-OCH33-CF3-5-OCH33-CF3-5-OCH33-CF3-5-OCH33-CF3-5-OCH33-CF,-5-OCH33-CF3-5-OCH33-CH2OCH3-5-OCH3 • 3-CH,SCH3-5-OCH33-OCH3-^-OH2,3-(OCH3)22,4-(OCH3)22,6-{OCH3)23,4-(OCH3)33,5-(OCH3)23-OEt-4-CI3,5-(OEt)23,5-(OPr-n)23-OCHoO^S-OCH^CH^O^3-F^-OCHF23-CI-4-OCHF23-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF3 '3-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF33-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF23-CI-5-OCHF.3-CI-5-OCHF23-CI-5-OCHF2 CF3 CF3 CF3 eF3 CF3 ^C-F3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 . CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 H H H H H C(0)CH3 H C(0)Et H H H H C(0)0CH3 H H H H CH^CN H H H H H H H C(0)CH3 C(0)Et C(0)0CH3 H H H H H H H H H H H C(0)CH3 C(0)Et C(0)0CH3 H CH2OCH3 CH2CN CH^C^CH 202 CH2CF3 CH^CCONHCH.CH^Cl CH3G(0)NHCH3CF3 CH2(D-22a) CH2(D-47a) CH2(D-47a) N(CH3)(p-50a) CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-^7a)_ CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CHgPr-c c-Bu CH2CF3 CH2CF3 CH2CF3 CH3CF3 CH2CH2OCH3 . CH2(E-10a) CH(CH3)CH2S02CH3 CH2CH=NOCH3 CH2C(0)NHCH2CH2C1 CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-21a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D^7a) CH2(D-47a) CH2(D^7a) CH2(D-47a) 3-CI-5-OCHF2 CF3 3-CI-5-OCHF2 CF3 3-CI-5-OCHF2 C!f3 3-CI-5-OCHF2 CF3 3-CI-5-OCHF2 GF3 3-CI-5-OCHF2 eF3 3-CI-5-OCHF2 CF3 3-CI-5-OCHF2 CF3 3-CI-5-OCHF2 CF3 3-CI-5-OCHF2 CF3 3-CI-5-OCHF2 CF3 3-Br-4-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CFg 3-Bi:-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CFg 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF, CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-Br-5-OCHF2 CF3 3-CH3-5-OCHF2 CF3 3-CF3-5-OCHF2 CF3 3-CF3-5-OCHF2 CF3 3-CF3-5-OCHF2 CF3 3-CF3-5-OCHF2 CF3 3-CF3-5-OCHF2 CF3 3-CF3-5-OCHF2 CF3 3-CF3-5-OCHF2 CF3 3-CF3-5-OCHF2 CF3 C(0)CH3 C(0)Et C(0)0CH3 C(0)0CH3 H C(0)0CH3 C(0)OCH3 H C(0)0CH3 H H C(0)CH3 H H C(0)CH3 C(0)Et C(0)0CH3 H H H H H H H H C(0)CH3 C(0)Et C(0)0CH3 H CH2CN C(0)CH3 C(0)Et C(0)0CH3 CppCHg H H C{0)0CH3 H H H C(0)CH3 C(0)Et C(0)0CH3 H H H CHaCD^Ta) CH2(D-47a) CH2(D-47a) CH{CH3)(D-^7a) N{CH3)Ph N(CH3)Ph N(CH3)(D-t7a) N(CH3)(D-50a) N(CH3)(D-50a) (D-l'3b)CH3 (D-15a)CH3 CH2(D-47a) c-Bu CH2CF3 CH2CF3 CH2CF3 CH2CF3 CH2CH2OCH3 CH2(E-10a) CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-47a) CH2{D-47a) CH2(D-47a) CH2(D-47a) CH2(D-47a) CH(CH3)(D-47a) N(CH3)Ph N(CH3)(D-50a) N(CH3)(D-50a) N(CH3)(D-50a) c-Bu CH2CF3 CH2CF3 CH2CF3 CH2CF3 CH2CH2OCH3 CH2(E-10a) CHzCiOJNHCH^CH^Cl 3-CF3-5-OCHF, CFa H 3-CF3-5-OCHF2 CF3 H 3-CF3-5-OCHF2 PF3 H 3-CF3-5-OCHF2 :GF3 H 3-CF3-5-OCHF2 CF3 H 3-CF3-5-OCHF2 GF3 C(0)CH3 3-CF3-5-OCHF2 CF3 C(0)Et 3-CF3-5-OCHF2 CF3 C(0)0CH3 3-CF3-5-OCHF2 CF3 H 3-CF3-5-OCHF2 CF3 CH^CN 3-CF3-5-OCHF2 CF3 C(0)CH3 3-CF3-5-OCHF2 CF3 C(0)Et 3-CF3-5-OCHF2 CF3 C(0)0CH3 3-CF3-5-OCHF2 CF3 C(0)0CH3 3-CF3-5-OCHF2 CF3 H 3-CF3-5-OCHF2 CF3 H 3-eF3-5-OCHF2 CF3 C(0)0CH3 3,5-(OCHF2)2 CF3 H 3-F-4-OCF3 CF3 H 3-CI-4-OCF3 CF3 H 3-CI-5-OCF3 CF3 H 3-CI-5-OCF3 CF3 H 3-CI-5-OCF3 CF3 H 3-CI-5-OCF3 CF3 C(0)CH3 3-CI-5-OCF3 CF3 C(0)Et 3-CI-5-OCF3 CF3 C(0)0CH3 3-CI-5-OCF3 CF3 . H 3-CI-5-OCF3 CF3 H 3-CI-5-OCF3 CF3 H 3-CI-5-OCF3 CF3 H 3-CI-5-OCF3 CF3 H 3-CI-5-OCF3 CF3 H 3-CI-5-OCF3 ^ CF3 H 3-CI-5-OCF3 CF3 H 3-CI-5-OCF3 CF3 H , 3-CI-5-OCF3 CF3 H 3-CI-5-OCF3 CF3 H 3-CI-5-OCF3 CF3 C(0)CH3 . 3-CI-5-OCF3 CF3 C(0)Et 3-CI-5-OCF3 CF3 C(0)0CH3 3-CI-5-OCF3 CF3 H 3-CI-5-OCF3 CF3 CH2OCH3 3-CI-5-OCF3 CF3 CH2CN 3-CI-5-OCF3 CF3 CH^C^CH 3-CI-5-OCF3 CF3 C(0)CH3 3-C[-5-OCF3 CF3 C(0)Et 204 CH^CCONHCH^CFs CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)Ci CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-47a) 'CH2(D-47a) CH2(D^7a) CH2(D^7a) CH2(D^7a) CH(CH3)(D^7a) N(CH3)Ph N(CH3)(D-50a) N(CH 3)(D-50a) CH^CCONHCHsCFg CH2(D-22a) CH2{D^7a) CH^Pr-c c-Bu CH2CF3 CH2CF3 CH2CF3 CH2CF3 CH2CH2OCH3 Cht2(E-10a) CH(CH3)CH2S02CH3 CH2CH=NOCH3 CH3C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 GH2(D-17b)CI CH2(D-21a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D^7a) CH2(D-47a) CH2(D^7a) CH2(D-47a) CH2(D-47a) CH2(D-47a) 3-CI-5-OCF3 CFg 3-CI-5-OCF3 CF3 3-CI-5-OCF3 CF, 3-Ci-5-OCF3 CF3' 3-CI-5-OCF3 CF3 3-Ci-5-OCF3 GF3¬ 3-CI-5-OCF3 CF3 3-CI-5-OCF3 CF3 3-CI-5-OCF3 CF3 3-Br-4-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Brf5-OCF3 CF3 3-Br-5-OCF3 ^ CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-Br-5-OCF3 CF3 3-CH3-5-OCF3 CF3 3-CF3-5-OCF3 CF3 3-CF3-5-OCF3 CF3 3-CF3-5-OCF3 CF3 3-CF3-5-OCF3 CF3 3-CF3-5-OCF3 CF3 3-CF3-5-OCF3 CF3 3-CF3-5-OCF3 CF3 3-CF3-5-OCF3 CF3 3-CF3-5-OCF3 CF3 3-CF3-5-OCF3 CF3 C(0)0CH3 CH2(D-^7a) C(0)0CH3 CH(CH3)(D^7a) H N(CH3)Ph C(0)0CH3 N(CH3)Ph C(0)0CH3 N(CH3)(D^7a) H N(CH3)(D-50a) C(0)0CH3 N(CH3)(D-50a) H (D-13b)CH3 H (D-15a)CH3 C(0)Et CH'(D-47a) H c-Bu H CH2CF3 ^ C(0)CH3 CH^CFg ^ C(0)Et CH^CFg C(0)0CH3 CH2CF3 H CH2CH2OCH3 H CHsCE-lOa) H CH2C(0)NHCH2CH2CI H CH2C(0)NHCH2CF3 H CH(CH3)Ph(R) H CH2(D-17a)CH3 H CH2(D-17b)CI H CH^iD-lZa) C(0)CH3 CH2(D-22a) C(0)Et CH2(D-22a) C(0)0CH3 CH2(D-22a) H CH2(D-47a) CHgCN CH2(D-47a) C(0)CH3 CH2(D-47a) C(0)Et CH2(D-47a) C(0)0CH3 CH2(D^7a) C(0)0CH3 CH(CH3)(D-47a) H N(CH3)Ph H N(CH3)(D-50a) C(0)0CH3 N(CH3)(D-50a) H • N(CH3)(D-50a) H c-Bu H CH2CF3 C(0)CH3 " CH2CF3 C(0)Et CH2CF3 C(0)0CH3 CH2CF3 H CH2CH2OCH3 H CH2(E-10a) H CH,C(0)NHCH2CH2CI H CH2C(0)NHCH2CF3 H CH(CH3)Ph(R) 3-CF3-5-OCF3 3-CF3-5-OCF3 3-CF3-5-OCF3 3-CF3-5-OCF3 3-CF3-5-OCF3 3-CF3-5-OCF3 3-CF3-5-OCF3 3-CF3-5-OCF3 3-CF3-5-OCF3 3-CF3-5-OCF3 3-CF3-5-OCF3 3-CF3-5-OCF3 3-CF3-5-OCF3 3-CF3-5-OCF3 3-CF3-5-OCF3 3-F-5-OCF2Br 3-(tl-5-OCF2Br 3-CH3-5-OCF2Br 3-F-5-OCF2CHF2 3-CI-5-OCF2CHF2 3-CH3-5-OCF2CHF2 3-F-5-OCF2CHFCI 3-CI-5-OCF2CHFCI3-Br-5-OCF2CHFCI3-F-5-OCF2CHFCF33-CI-5-OCF2CHFCF33-CH3-5-OCF2CHFCF33-F-5-OCF2CHFOCF33-CI-5-OCF2CHFOCF33-CH3-5-OCF2CHFOCF33-CF2OCF2O-43-OCF20^3-OCF2CF20^3-OPh-4-F3-CI-5-SCH33-CI-5-S(0)CH33-CI-5-SO2CH33-Br-5-SCH33-Br-5-S(0)CH33-Br-5-S02CH3 3-CI-5-SCF33-CI-5-SCF33-CI-5-SCF33-CI-5-SCF33-CI-5-SCF33-CI-5-SCF3 CFa H CF3 H GF3 H CF3 C(0)CH3 CF3 C(0)Et CFg C(0)0CH3 CF3 H CF3 CH2CN CF3 C(0)CH3 CF3 C(0)Et CF3 C(0)0CH3 CF3 C(0)0CH3 CF3 H CF3 H CF3 C(0)0CH3 CF3 H CF3 H CF3 H CF3 C(0)0CH3 CF3 H CFg H CF3 H CF3 H CF3 CH2CN CF3 H CF3 H CF3 H CF3 H CF3 C(0)CH3 CFg H CF3 H CF3 H CF3 H CF3 C(0)Et CF3 H . CF3 H CF3 H CF3 H CF3 CCOpCHg CF3 H CF3 H CF3 H CF3 H CF3 C(0)CH3 CF3 C(0)Et CF3 C(0)0CH3 206 CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-47a) CH2(D-47a) CH2(D^7a) CH2(D^7a) CH2(D^7a) CH(CH3XP^7a) N(CH3)Ph N(CH3)(D-50a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D^7a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2(D^7a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2(D^7a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D^7a) N(CH 3)(D-50a) CHgPr-c c-Bu CH2CF3 CH2CF3 CH2CF3 CH2CF3 3-CI-5-SCF3 CF3 3-Ci-5-SCF3 CF3 3-Ci-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 GF3 3-CI-5-SCF3 eF-3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-GI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-SCF3 CF3 3-CI-5-S{0)CF3 CF3 3-CI-5-S(0)CF3 " CF3 3-CI-5-S(0)CF3 CF3 3-CI-5-S(0)CF3 CF3 3-CI-5-S(0)CF3 CF3 3-CI-5-S(0)CF3 CF3 3-Cl-5-S(0)CF3 CF3 3-CI-5-SO2CF3 CF3 3-CI-5-SO2CF3 CF3 3-CI-5-SO2CF3 CF3 3-CI-5-SO2CF3 CF3 3-CI-5-SO2CF3 CF3 3-CI-5-SO2CF3 CF3 3-CI-5-SO2CF3 CF3 3-Br-5-SCF3 CF3 3-Br-5-SCF3 CF3 3-Br-5-SCF3 CF3 H H H H H H H H H H H C(0)CH3 C(0)Et C(0)0CH3 H CH2OCH3 CH^CN CH^C^CH C(0)CH3 C(0)Et C(0)0CH3 C(0)0CH3 H C(0)0CH3 C(0)0CH3 H C(0)0CH3 H H H H H H H CH2CN H H H " H H H C(0)CH3 H H H C(0)CH3 207 CH^CH^OCHs CH2(E-10a) CH(CH3)CH2S02CH3 CH2CH=NOCH3 CH2C(0)NHCH2CH3CI CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-21a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-47a) CH^lD^Ta) CH2(D^7a) CH2(D-47a) CH2(D-47a) CH2(D^7a) CH2(D-47a) CH(CH3)(D^7a) N(CH3)Ph N(CH3)Ph N(CH3)(D^7a) N(CH3)(D-50a) N(CH3)(D-50a) (D-13b)CH3 (D-l5a)CH3 CH2CF3 CH^CCONHCH^CH^Cl CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-^7a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2(D-47a) N(CH3)(D-50a) c-Bu CH2CF3 CH^CFg 3-Br-5-SCF3 3-Br-5-SCF3 3-Br-5-SCF3 a-Br-S-SCFg 3-Br-5-SCF3 3-Br-5-SCF3 3-Br-5-SCF3 3-Br-5-SCF3 •3-Br-5-SCF33-Br-5-SCF33-Br-5-SCF33-Br-5-SCF33-Br-5-SCF33-Br-5-SCF33-Br-5-SCF3 '3-Br-5-SCF33-Br-5-SCF33-Br-5-SCF33-Br-5-SCF33-Br-5-SCF33-Br-5-SCF33-Br-5-SCF33-Br-5-S(0)CF33-Br-5-S(0)CF33-Br-5-S(0)CF33-Br-5-S(0)CF33-Br-5-S(0)CF33-Br-5-S(0)CF33-Br-5-S(0)CF33-Br-5-S02CF3S-Br-S-SOsCFg '3-Br-5-S02CF3S-Br-S-SOgCFgS-Br-S-SOgCFg3-Br-5-S02CF33-Br-5-S02CF33-CI-5-SCF2CHFCI3-CI-5-SCF2CHFCI3-CI-5-SCF2CHFCI3-CI-5-SCF2CHFCI3-CI-5-SCF2CHFCI3-CI-5-SCF2CHFCI3-CI-5-SCF2CHFCI3-Cl-5-S(0)CF2CHFCI 3-CI-5-SO2CF2CHFCI3-Br-5-SCF2CHFCI CF3 C(0)Et CF3 qopCH g CF3 H CF3 H GF3 H GF3 H CF3 H CF3 H CF3 H CF3 H CF3 C(0)CH3 CF3 C(0)Et CF3 C(0)0CH3 CF3 H CF3 CH2CN CF3 C(0)CH3 CF3 C(0)Et CF3 C(0)0CH3 CF3 C(0)0CH3 CF3 H CF3 H CF3 C(0)0CH3 CF3 H CF3 H CF3 H CF3 H CF3 H CF3 C(0)Et CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 C(0)0CH3 CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 CH2CN CF3 H CF3 H CF3 H CF3 H 208 CH2CF3 CH^CFg CH^CH^OCHs CH^CE-lOa) CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-22a) CH2(D-22a) CH2(D-22a)~ CH2(D-22a) CH2(D^7a) CH2(D-47a) CH2(D-47a) CH2(D^7a) CH2(D-47a) CH(CH3)(D^7a) N(CH3)Ph N(CH3)(D-50a) N(CH3)(D-50a) CH2CF3 CH2C{0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) ,CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CH2C1 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2CF3 S-Br-S-SCF^CHFCIa-Br-S-SCF^CHFClS-Br-S-SCF^CHFCIS-Br-S-SCF^CHFCIS-Br-S-SCF^CHFCIa-Br-S-SCF^CHFCI3-Br-5-S(0)CF2CHFClS-Br-S-SO^CFaCHFCI3-CI-5-SPh3-CI-5-S(0)PhS-CI-S-SO^Ph3-CI-5-SO2OCH33-CH3-5-SO2OCH33-CI-5-SO2NH23-CH3-5-SO2NH23-CI-5-SO2NHCH33-Cl-5-S02N(CH3)23-Cl-5-NHC(0)CF33-CI-5-N(CH3)C(0)CF33-CI-5-N(Et)C(0)CF33-CI-5-N(CH3)C(0)CF2CI3-CI-5-N(Et)C(0)CF2CI3-CI-5-N(CH3)C(0)CF2Br3-CI-5-N(Et)C(0)CF2Br3-Cl-5-N(CH3)S02CF33-CI-5-N(Et)S02CF33-CF3-5-NHC(0)CH33-CF3-5-NHC(0)CF33-CF3-5-N(CH3)C(0)CH3 3-CF3-5-N(Et)C(0)CH3 3-CF3-5-N(CH3)C(0)CF3 3-CF3-5-N(Et)C(0)CF3 3-CF3-5-N(CH3)C(0)CF2Cl 3-CF3-5-N(Et)C(0)CF2CI 3-CF3-5-N(CH3)C(Q)CF2Br 3-CF3-5-N(Et)C(0)CF2Br 3-CF3-5-N(CH3)S02CF3 3-CF3-5-N(Et)S02CF3 3-NO2-4-F 2-F-5-NO2 3-F-5-NO2 3-NO2-4-CI 3-CI-5-NO2 3-CI-5-NO2 3-CI-5-NO2 3-CI-5-NO2 CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CF3 H CF3 H CF3 H CF3 H CF3 C(0)CH3 -CF3 H CF3 H CF3 C(0)Et CF3 H CF3 H CF3 H CF3 H CF3 C(0)OCH3 CF3 H CF3 H CF3 H CF3 H CF3 CHgCN CF3 H CF3 H CF3 H CF3 H CF3 C{0)CH^ CF3 H CF3 H CF3 H CF3 H CF3 C(0)Et CF3 H CF3 H CF3 H CF3 H CF3 C(0)0CH3 CF3 H CF3 H CF3 H CF3 H CF3 CH2CN CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 C(0)CH3 CF3 C(0)Et 209 CHsCD^Ta) N(CH3)(D-50a) CH2(D-47a) CH^iDAla) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH^{D-A7B) CH2(D^7a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D-47a) N(CH 3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2(D-47a) N(CH 3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2(D-47a) N(CH3)(D-50a) ., CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D^7a) N(CH3)(D-50a) ..CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-^7a) c-Bu CH2CF3 CH2CF3 CH2CF3 3-C[-5-N023-CI-5-NO23-CI-5-NO23-CI-5-NO23-CI-5-NO23-C1-5-NO,3-CI-5-NO23-CI-5-NO23-CI-5-NO23-CI-5-NO23-CI-5-NO23-CI-5-NO23-CI-5-NO23-CI-5-NO23-CI-5-NO23-CI-5-NO23-CI-5-NO23-CI-5-NO23-CI-5-NO23-CI-5-NO23-CI-5-NO23-CH3-5-NO23-CF3-4-NO23-CF3-5-NO23,5-(N02)23-N02-5-NHC{0)CH33.CN-4-F3-F-4-CN3-CI-4-CN3-CH3-4-CN 3-F-5-CN3-CI-5-CN3-CI-5-CN3-CI-5-CN3-C1-5-CN3-CI-5-CN3-CI-5-CN3-CI-5-CN3-Ci-5-CN3-CI-5-CN3-CI-5-CN3-CI-5-CN3-CI-5-CN3-C1-5-CN3-CI-5-CN3-CI-5-CN CF3 CF3 CF3 CFl CF3 eF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 C(0)0CH3 CH2CF3 H CH2CH2OCH3 H CH2(E-10a) H CH2C(0)NHCH2CH2C1 H CH2C(0)NHCH2CF3 H CH(CH3)Ph(R) H CH2(D-17a)CH3 H CH2(D~17b)Cl H CH2(D-22a) C(0)CH3 CH2(D-22a) C(0)Et CH2(D-22a) C(0)0CH3 CH2(D-22a) H CH2(D^7a) ~ CH2CN CH2(D^7a) C(0)CH3 CH2(D-47a) C(0)Et CH2(D^7a) C(0)0CH3 CH2(D-47a) C(0)0CH3 CH(CH3)(D-47a) H N(CH3)Ph H N(CH3)(D-50a) C(0)0CH3 N(CH3)(D-50a) C(0)CH3 CH2(D-47a) H N(CH3)(D-50a) H CH2C(0)NHCH2CF3 H CH2(D-22a) H CH2(D-47a) C(0)Et CH2(D^7a) H N(CH3){D-50a) H CH2C(0)NHCH2CF^ H CH2(D-22a) H CH2(D^7a) H c-Bu H CH2CF3 C(0)CH3 CH2CF3 C(0)Et CH2CF3 C(0)0CH3 CH2CF3 H , CH2CH2OCH3 H . CH2(E-10a) H CH2C(0)NHCH2CH2CI H CH2C(0)NHCH2CF3 H CH(CH3)Ph(R) H CH2(D-17a)CH3 H CH2(D-17b)CI H CH2(D-22a) C(0)CH3 CH2(D-22a) C(0)Et CH2(D-22a) 3-CI-5-CN CFs C(0)0CH3 3-CI-5-CN CF3 H 3-CI-5-CN CF3 CH2CN 3-CI-5-CN CF3 C(0)CH3 3-Ci-5-CN Cf, C(0)Et 3-CI-5-CN -eF3 C(0)0CH3 3-CI-5-CN CF3 C{0)0CH3 3-CI-5-CN CF3 H 3-CI-5-CN CF3 H 3-CI-5-CN CF3 C(0)0CH3 3-Br-5-CN CF3 H 3-Br-5-CN CF3 H 3-Br-5-CN CF3 C(0)CH3 3-Br-5-CN CF3 C(0)Et 3-Br-5-CN CF3 C(0)0CH3 3-Br-5-CN CF3 H S-^Br-S-CN CF3 H 3-Br-5-CN CF3 H 3-Br-5-CN CF3 H 3-Br-5-CN CF3 H 3-Br-5-CN CF3 H 3-Br-5-CN CF3 H 3-Br-5-CN CF3 H 3-Br-5-CN CF3 C(0)CH3 3-Br-5-CN CF3 C(0)Et 3-Br-5-CN CF3 C(0)0CH3 3-Br-5-CN CF3 H 3-Br-5-CN CF3 CH2CN 3-Br-5-CN CF3 C(0)CH3 3-Br-5-CN CF3 C(0)Et 3-Br-5-CN CF3 CpOCH g 3-Br-5-CN CF3 C(0)0CH3 3-Br-5-CN CF3 H 3-Br-5-CN CF3 H 3-Br-5-CN CF3 C(0)0CH3 3-CH3-5-CN CF3 C(0J0CH3 3-CF3-5-CN CF3 H 3-CF3-5-CN CF3 H 3-CF3-5-CN CF3 C(0)CH3 3-CF3-5-CN CF3 C(0)Et 3-CF3-5-CN CF3 C(0)OCH3 3-CF3-5-CN CF3 H 3-CF3-5-CN CF3 H 3-CF3-5-CN CF3 H 3-CF3-5-CN CF3 H 3-CF3-5-CN CF3 H 211 CH2(D-22a) CH2(D^7a) CH2(D-47a) CH2(D^7a) CH2(D^7a) CH2(D-47a) CH(CH3)(D-47a) N(CH3)Ph N(CH3)(D-50a) N(CH3)(D-50a) c-Bu CH2CF3 ^ CH2CF3 CH2CF3 CH2CF3 CH2CH2OCH3 CH2(E-10a) CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D^7a) CH2(D-47a) CH2(D^7a) CH2(D^7a) CH2(D-47a) CH(CH3)(D^7a) N(CH3)Ph N(CH3)(D-50a) Nl(CH 3)(D-50a) CH2(D^7a) c-Bu CH2CF3 CH2CF3 CH2CF3 CH2CF3 CH2CH2OCH3 CH2(E-10a) CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH(CH3)Ph(R) 3-CF3-5-CN3-CF3-5-CN3-CF3-5-CN3-CF3-5-CN3-CF3-5-CN3-CF3-5-CN3-CF3-5-CN3-CF3-5-CN3-CF3-5-CN3-CF3-5-CN3-CF3-5-CN3-CF3-5-CN3-CF3-5-CN3-CF3-5-CN3-CF3-5-CN3-NO2-5-CN3,5;-(CN)23,5-(CN)23,5-(CN)23,5-(CN)23-F-5-C(0)OCH33-F-5-C(0)NH23-F-5-C(0)NHCH33-F-5-C(0)N(CH3)23-CI-5-C(0)OCH33-CI-5-C(0)NH23-CI-5-C(0)NHCH33-CI-5-C(0)N(CH3)23-Br-5-C(0)OCH33-Br-5-C(0)NH2 3-Br-5-C(0)NHCH3"3-Br-5-C(0)N(CH3)23-CH3-5-C(0)OCH3¬3-CH3-5-C(0)NH23-CH3-5-C(0)NHCH.33-CH3-5-C(0)N(CH3)23-CF3-5-C(0)OCH33-CF3-5-C(0)NH23-CF3-5-C(0)NHCH33-CF3-5-C(0)N(CH3)23-OCH3-5-C(0)OCH33-OCH3-5-C(0)NH23-OCH3-5-C(0)NHCH33-OCH3-5-C(0)N(CH3)23-N02-5-C(0)OCH33-N02-5-C(0)NH2 CFg H CF3 H CFg H C'Fs C(0)CH3 CFa C(0)Et -CF3 C(0)0CH3 CF3 H CF3 CH2CN CF3 C(0)CH3 CF3 C(0)Et CF3 C(0)0CH3 CF3 C(0)0CH3 CF3 H CF3 H CF3 C(0)0CH3 CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 H CF3 CH2CN CF3 H CF3 H CF3 H CF3 H CF3 C(0)CH3 CF3 H CF3 H CF3 H CF3 H CF3 C(0)Et CF3 H CF3 H CF3 H CF3 H CF3 C(0)0CH3 CF3 H CF3 H CF3 H CF3 H CF3 CH2CN CF3 H CF3 H 212 CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D^7a) CH2(D^7a) CH2(D^7a) CH2(D-47a) CH2(D^7a) CH(CH3KD^7a) N(CH3)Ph N(CH3)(D-50a) N(CH3)(D-50a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2C{0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D^7a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CHi(D-47a) CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2(D-47a) .N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 3-N02-5-C(0)NHCH33-N02-5-C(0)N(CH3)23,5-[C(0)OCH3]23,5-[C(0)NH2]2 3,5-[C(0)NHCH3]2 3,5-[C(0)N(CH3)2]23-CH3-5-Ph2-CH=CHCH=CH-33-CH=CHCH=CH^2,3,4-F32,3,5-F32,3,6-F32,4,5-F32,4,6-F33,4,5-F33,4,5-F33,4,5-F33,4,'5-F33,4,5-F33,4,5-F33,4,5-F33,4,5-F33,4,5-F33,4,5-F33,4,5-F33,4,5-F33.4,5-F33,4,5-F33,4,5-F33,4,5-F33,4,5-F33,4,5-F33,4,5-F33,4,5-F33,4,5-F33,4,5-F33,4,5-F33,4,5-F33,4,5-F32,6-F2-3-CI3,5-C!2^-F3,5-Cl2^-F3,5-Cl2-4-F3,5-Cl2^-F3,5-Cl2-4-F3,5-Cl2-4-F CF3 H CH2(D-22a) CF3 H CH2(D-47a) CF3 C(0)CH3 CH^CD^/a) CFi H N(CH3)(D-50a) CF3 H CH2C(0)NHCH2CF3 GF3¬ H CH2(D-22a) CF3 H CH2(D^7a) CF3 C(0)Et CH2(D-47a) CF3 H N(CH3)(D-50a) CF3 H CH2C(0)NHCH2CF3 CF3 H CH2(D-22a) CF3 H CH2(D-47a)¬ CF3 C(0)0CH3 CH2(D-47a)¬ CF3 H N(CH3)(D-50a) CF3 H c-Bu CF3 H CH2CF3 CF3 C(0)CH3 CH2CF3 CF3 C(0)Et CH3CF3 CF3 C(0)0CH3 CH2CF3 CF3 H CH2CH2OCH3 CF3 H CH2(E-10a) CF3 H CH2C(0)NHCH2CH2CI CF3 H CH2C(0)NHCH2CF3 CF3 H CH(CH3)Ph(R) CF3 H CH2(D-17a)CH3 CF3 H CH2(D-17b)CI CF3 H CH2(D-22a) CF3 C(0)CH3 CH2(D-22a) CF3 C(0)Et CH2(D-22a) CF3 C(0)0CH3 CH2(D-22a) CF3 H CH2(D^7a) CF3 CH2CN CH2(D-47a) CF3 C(0)CH3 CH2(D-t7a) CF3 C(0)Et CH2(D-47a) CF3 C(0)0CH3 CIH2(D-47a) CF3 C(0)0CH3 CH(CH3)(D-47a) CF3 H N(CH3)Ph CF3 H " N(CH3)(D-50a) CF3 C(0)0CH3 ' N(CH3)(D-50a) CF3 H CH2C(0)NHCH2CF3 CF3 • H CHgPr-c CF3 H c-Bu CF3 H CH2CF3 CF3 C(0)CH3 CH2CF3 CF3 C(0)Et CH2CF3 CF3 C(0)0CH3 CH2CF3 3,5-Cl2-4-F CF3 3,5-Cl2-4-F CF3 3 5-CL-4-F CF, 3 5-CL-4-F CF3 SVCI^^-F CF3 3 5-Cl2-t-F CF3 3,5-Cl3-4-F CF3 3,5-CI,-4-F CF3 • 3,5-Cl2-4-F CF3 3,5-Cl2-4-F CF3 3,5-Cl2-4-F CF3 3_5.Cl,-4-F CF3 3,5-Cl2-4-F CF3 3,5-Cl2-i-F CF3 3,5-Cl2^-F CF3 3,5-Cl2-4-F CF3 3,5-Cl2-4-F CF3 3,5-Cl2-4-F CF3 3,5-Cl2-4-F CF3 3,5-Cl2-4-F CF3 3,5-Cl2-4-F CF3 3,5-Cl2-*-F CF3 3,5-Cl2-4-F CF3 3,5-Cl2-4-F CF3 3,5-Cl3-4-F CF3 3,5-Cl3^-F CF3 3,5-Cl3-4-F CF3 3,5-Cl3-*-F CF3 3,5-Cl3-4-F CF3 3,5-Cl2^-F CF2CI 3,5-Cl2-4-F CF2CI 3,5-Cl3-l-F CF2CI 3,5-Cl2-4-F CF2CI 3,5-Cl2^-F CF2CI 3,5-Ci2^-F CF2CI 3,5-Cl2-4-F CF2CI 3,4,5-Cl3 CHF3 3,4,5-Ci3 CHF3 3,4,5-Cl3 CHF3 3,4,5-Cl3 CHF2 3,4,5-Cl3 CHFCI 3,4,5-Cl3 CHCI2 3,4,5-Cl3 CHFBr 3,4,5-Cl3 CF3 3,4,5-Cl3 CF3 3,4,5-Cl3 CF3 H CH2CH2OCH3 H CH2(E-10a) H CH(CH3)CH2S02CH3 H CH2CH=NOCH3 H CH,C(0)NHCH,CH2CI H CH3C(0)NHCH2CF3 H CH(CH3)Ph(R) H CH2(D-17a)CH3 H CH2(D-17b)Cl H CH2(D-21a) H CH2(D-22a) C(0)CH3 CH,(D-22aK C(0)Et CH2(D-22a) ' C(0)0CH3 CH2(D-22a) H CH3(D-*7a) CH2OCH3 CH2(D-^7a) CH2CN CH2(D^7a) CH^C^CH CH3(D-47a) C(0)CH3 CH3(D^7a) C(0)Et CH2(D-47a) C(0)0CH3 CH2(D-*7a) C(0)0CH3 CH(CH3)(D-47a) H N(CH3)Ph C(0)0CH3 N(CH3)Ph C(0)0CH3 N(CH3)(D-47a) H N(CH3)(D-50a) C(0)0CH3 N(CH3)(D-50a) H (D-13b)CH3 H (D-15a)CH3 H CH2CF3. H CH2C(0)NHCH2CH3CI H CH2C(0)NHCH2CF3 H CH2(D-22a) H CH2(D-47a) C(0)0CH3 QH2(D-47a) H N(CH3)(D-50a) H CH2CF3 H " CH2C(0)NHCH2CF3 H CH2(D-22a) H CH2(D^7a) H CH2(D-22a) H CH2{D-47a) CHgCN CH2(D-47a) H Et Et Et H c-Pr 214 3,4,5-C!3 CF3 H CH^Pr-c 3,4,5-Cl3 CF3 H c-Bu 3,4,5-Cl3 CF3, H CH2CF3 3,4,5-Cl3 CF3 CH2OCH3 CH2CF3 3,4,5-Cl3 CF3 CH3CN CH2CF3 3,4,5-Cl3 CF'3 ¬ CH^C^CH CH^CFg 3,4,5-Cl3 CF3 C(0)CH3 CH2CF3 3,4,5-Cl3 CF3 C(0)Et CH2CF3 3,4,5-Cl3 CF3 C(0)Pr-c CH^CFg 3,4,5-Cl3 CF3 C(0)Bu-t CH2CF3 3A5-CI3 CF3 C(0)0CH3 CH2CF3 3,4,5-Cl3 CF3 C{0)OCH^CH^OCH, ¬CH^CF, ¬ 3.4,5-Cl3 CF3 C(0)OCH2CH=CH2 ^ CH2CF3 3A5-CI3 CF3 C(0)SCH3 CH2CF3 3,4,5-Cl3 CF3 C(S)0CH3 CH2CF3 3A5-CI3 CF3 C(S)SCH3 CH2CF3 3,4,5-Cl3 CF3 H CH2CF2CF3 3A5-CI3 CF3 H CH2CH2OCH3 3,4,5-Cl3 CF3 H CH(CH3)CH20CH3 3,4,5-Cl3 CF3 H CH2CH(OCH3)2 3,4,5-Cl3 CF3 H CH^CE^a) 3,4,5-Cl3 CF3 H CH2(E-5a) 3,4,5-Cl3 CF3 H CH2(E-10a) 3,4,5-Cl3 CF3 H CH2CH2SCH3 3,4,5-C!3 CF3 H CH2CH2S(0)CH3 3,4,5-Cl3 CF3 H CH2CH2SO2CH3 3,4,5-Cl3 CF3 H CH2CH(CH3)SCH3 3,4,5-Cl3 CF3 H CH2CH(CH3)S(0)CH3 3,4,5-Cl3 CF3 H CH2CH(CH3)S02CH3 3,4,5-Cl3 CF3 H CH(CH3)GH2SCH3 3A5-CI3 " CF3 H CH(CH3)CH2S(0)CH3 3,4,5-Cl3 CF3 H CH(CH3)CH2S02CH3 3,4,5-Cl3 CF3 H CH2C(0)CH3 3,4,5-Cl3 CF3 H CH2CH=NOCH3 3,4,5-Cl3 CF3 H CH,C(CH3)=NOCH3 3,4,5-Cl3 CF3 H CH2CN 3,4,5-Cl3 CF3 H . CH2C(0)NHCH3 3,4,5-Cl3 CF3 H . CH2C(0)N{CH3)2 3,4,5-Cl3 CF3 H CH2C(0)NHEt 3,4,5-Cl3 CF3 H CH2C(0)NHCH2CH2F 3 4,5-Cl3 CF3 H CH2C(0)NHCH2CH2CI 3,4,5-Cl3 CF3 H CH2C(0)NHCH2CF3 3,4,5-Cl3 CF3 H CH2C(0)NHCH2CH=CH2 3,4,5-Cl3 CF3 H CH2C(0)NHCH2C=CH 3,4,5-Cl3 CF3 H CH(CH3)C(0)NHCH2CH2C i 215 3,4,5-Cl3 CFa 3,4,5-Cl3 CF3 34,5-Cl3 CF, 3,4,5-Cl3 CF3 3.4.5-CI3 CF3 3 4,5-Cl3 CF3¬ 3!4,5-Cl3 CF3 3,4,5-Cl3 CF3 • 3,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF334.5-CI3 CF33,4,5-Cl3 CF33A5-CI3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4.5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CFa3,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33A5-CI3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Ci3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF33,4,5-Cl3 CF3 H H H H H H H H H H H H H CH2OCH3 CH^CN CH^C^CH C(0)CH3 C(0)Et C(0)0CH3 H CH2OCH3 CH^CN CH^C^CH C(0)CH3 C(0)Et C(0)0CH3 H H H CH2OCH3 CH2CN CH^C^CH C(0)CH3 C(0)Et C(0)Pr:C C(0)Bu-t C(0)0CH3 CH,C(S)NHEt CH3CH=CH, CH2CCNCH2 CH^CCI^CHCI CH.C^CH CH(CH3)Ph(R) CH(CF3)Ph , CH^CPh-t-F) CH^CPh^-OCHa) CH,{Ph^-m,) CH^CPh-t-CN) CH(CH3)(D--ra)(R) CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI CH2(D-19a) CH2(D-21a) CH2'(D-22a) CH2(D-22a) CH3(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CHc2(D-22a) CH2(D-22a) CH3(D-22a) C(0)OCH3CH20CH3 CH2(D-22a) C(0)OCH3CH=CH3 CH3(D-22a) C(0)SCH3 C(S)0CH3 C(S)SCH3 H H H H 216 CH3(D-22a) CH3(D-22a) CH3(D-22a) CH(CH3)(D-22a) CH2(D-28a) CH3(D-34a) CH2(D-35a) 3,4,5-Cl3 CF3 H CH2(D-38a) 3,4,5-Cl3 CF3 H CH(CF3)(D-38a) 3,4,5-Cl3 CF3, H CH2(D^7a) 3,4,5-Cl3 CF3 CH2OCH3 CH2(D-47a) 3,4,5-Cl3 CF3 CH2CN CH2(D^7a) 3,4,5-Cl3 CP3 CH2C-CH CH2(D-47a) 3,4,5-Cl3 CF3 C(0)CH3 CH2(D-47a) 3,4,5-Cl3 CF3 C(0)Et CH2(D-47a) •3,4,5-013 CF3 C(0)Pr-c CH2(D-47a) 3,4,5-Cl3 CF3 C(0)Bu-t CH2(b-47a) 3,4,5-Cl3 CF3 C(0)0CH3 CH2(D-47a) 3,4,5-Cl3 CF3 C(0)OCH2CH20CH3 •eH2(D-47a) ' 3,4,5-Cl3 CF3 C(0)OCH2CH=CH2 CH2(D-47a) 3,4,5-Cl3 CF3 C(0)SCH3 CH2(D^7a) 3,4,5-Cl3 CF3 C(S)0CH3 CH2(D^7a) 3,4,5-Cl3 CF3 C(S)SCH3 CH2(D-47a) 3,4,5-Cl3 CF3 H CH(CH3)(D^7a) 3,4,5-Cl3 CF3 C(0)0CH3 CH(CH3)(D^7a) 3,4,5-Cl3 CF3 H CH2(D-50a) . 3,4,5-Cl3 CF3 H CH2(D-51a) 3,4,5-Cl3 CF3 H CH2(D-53a) 3,4,5-Cl3 CF3 H NHNHCH2CF3 3,4,5-Cl3 CF3 H N(CH3)Ph 3,4,5-Cl3 CF3 C(0)CH3 N(CH3)Ph 3,4,5-Cl3 CF3 C(0)Et N(CH3)Ph 3,4,5-Cl3 CF3 C(0)0CH3 N(CH3)Ph 3,4,5-Cl3 CF3 H N(CH2C=CH)Ph 3,4,5-Cl3 CF3 H N(CH3)(D-47a) 3,4,5-Cl3 CF3 C(0)CH3 N(CH3)(D^7a) 3,4,5-Cl3 CF3 C(0)Et N(CH3)(D-47a) 3.4,5-Cl3 CF3 C(0)0CH3 N(CH3)(D-47a) 3,4,5-Cl3 CF3 H NH(D-50a) 3,4,5-Cl3 CF3 CH3 NH(D-50a) 3,4,5-Cl3 CF3 H N(CH3)(D-50a) 3,4,5-Cl3 CF3 C(0)CH3 N(GH3)(D-50a) 3,4,5-Cl3 CF3 C(0)Et N(CH3)(D-50a) 3,4,5-Cl3 CF3 C(0)0CH3 N(CH3)(D-50a) 3,4,5-Cl3 CF3 H _(D-13b)CH3 3,4,5-Cl3 CF3 H (D-15a)CH3 3,4,5-Cl3 CF3 H D-21a 3,4,5-Cl3 CF3 H D^7a 3,4,5-Cl3 CF3 H D-50a 3,4,5-Cl3 CF3 , H D-51a 3,4,5-Cl3 CFgC! H CHgPr-c 3,4,5-Cl3 CF,Ci H c-Bu 3,4,5-Cl3 CFgCi H CH2CF3 217 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-C!3 CF^CI 3,4,5-Ci3 CF;C 1 3,4,5-Cl3 CF2CI • 3,4,5-Cl3 CF^Gi 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF^Ci '3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,i5-Cl3 CF2CI 3,4,5-013 CF2CI 3,4,5-Cl3 CF2CI 3.4,5-Cl3 CF2CI 3.4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 '^ CF2CI 3,4,5-Cl3 CF2CI 3,4,5-Cl3 CF2Br 3,4,5-Cl3 CF2Br 3,4,5-Cl3 CF2Br 3,4,5-Cl3 CF2Br 3,4,5-Cl3 CF2CHF2 3,4,5-Cl3 CF2CHF2 3,4,5-Cl3 CF2CHF2 3,4,5-Cl3 CF2CHF2 3,4,5-Cl3 CF2CF3 3,4,5-Cl3 CF2OCH3 3,4,5-Cl3 CF2SCH3 3,5-Br2^-F CF3 S.S'-Bra^-F CF3 3,5-Br2-4-F CF3 C(0)CH3 .C(0)Et C(0)0CH3 H H H H H H H H H H H C(0)CH3 C(0)Et C(0)0CH3 H CH2OCH3 CH2CN CH2C=CH C(0)CH3 C(0)Et C(0)0CH3 C(0)0CH3 H C(0)0CH3 C(0)0CH3 H C(0)0CH3 H H H H H H H H H H H H H H H C(0)CH3 218 CH2CF3 CH2CF3 CH2CF3 CH2CH2OCH3 CH2(E-10a) CHCCHaPH^SO^CHg CH2CH=NOGH3 CH2C(0)NHCH2CH2C1 CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)Gt CH2(D-21a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-47a) CH2(D^7a) CH2(D-47a) CH2(D-47a) CH2(D-47a) CH2(D-47a) CH2(D^7a) CH(CH3)(D-47a) N(CH3)Ph N(CH3)Ph N(CH3)(D-47a) N(CH3)(D-50a) N{CH3)(D-50a) (D-13b)CH3 (D-15a)CH3 CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CHaPr-c CH2CF3 CH2CF3 3,5-Br2-4-F CF3 3,5-Br2-^-F CF3 3,5-Br2-4-F CF3 3,5-Br2-4-F CF3 3,5-Br2^-F CF3 3,5-Br2-4-F GF, 3,5-Br2-i-F CF3 3,5-Br2-4-F CF3 3,5-Br2^-F CF3 3,5-Br2-4-F CF3 3,5-Br2^-F CF3 3,5-Br2-4-F CF3 3,5-Br2-4-F CF3 3,5-Br2^-F CF3 3,5-Br2^-F CF3 3,5-Br2-=i-F CF3 3,^-Br2^-F CF3 3,5-Br2-4-F CF3 3,5-Br2-4-F CF3 3,5-Br2-4-F CF3 3,5-Br2^-F CF3 3,5-Br2-4-F CF3 3,5-Br2-4-F CF3 3,5-Br2^-F CF3 3,5-Br2^-F CF2CI 3,5-Br2-4-F CF^CI 3,5-Br2-4-F CF^CI 3,5-Br2-4-F CF2CI 3,5-Br2-4-F CF2CI 3,4,5-Br3 CF3 3,4,5-Br3 ' CF3 3,4,5-Br3 CF3 3,4,5-Br3 CF3 3,4,5-Br3 CF3 2,6-F2-3-CH3 CF3 2,3-F2^-CH3 CF3 3,5-F2-4-CH3 CF3 3,5-F2-4-CH3 CF3 3,5-F2-*-CH3 CF3 3,5-F2-4-CH3 CF3 3,5-F2-4-CH3 CF3 2,3-F2^-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 C(0)Et C(0)0CH3 H H H H H H H C(0)CH3 C(0)Et C(0)0CH3 H CH2OCH3 CH2CN CH^C^CH C(0)CH3 C(0)Et C(0)0CH3 H C(0)0CH3 C(0)0CH3 H C(0)0CH3 H H H H H H H H H H H C(0)CH3 H H H H H H H H H C(0)CH3 219 CH^CFg CH^CFa CH2CH2OCH3 CH^CE-lOa) CH2CH=NOCH3 CH^CCONHCH.CFg CH(CH3)Ph(R) CH2(D-17b)CI CH2(D-22a) CFl2(D-22a) CH2(D-22a) CH2(D-22a)_ CH^CD^ya) CH2(D-*7a) CH2(D-47a) CH2(D-47a) CH,iD-47a) CH2(D-47a) CH2(D^7a) N(CH3)Ph N(CH3)Ph N(CH3)(D-47a) N(CH3)(D-50a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3. CHsCCONHCHsCFa CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2(D-i7a) CH2(D-47a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) N(CH3)(D-50a) CHjPr-c c-Bu CH2CF3 CH2CF3 3,4-F2-5-CF3 CF3 3,4-F,-5-CF3 CF3 3,4-F2-5-CF3 CF, 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 GF3 3,4-F2-5-CF3 CFg 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 •3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4^F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 3,4-F2-5-CF3 CF3 2-F-3-CI-5-CF3 CF3 3-CI-4-F-5-CF3 CF3 3-CI-4-F-5-CF3 CF3 3-CI-4-F-5-CF3 CF3 3-CI-4-F-5-CF3 CF3 3-CM-F-5-CF3 CF3 2,4-Cl2-6-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2^-CH3 CF3 3,5-Cl2^-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Ci2-4-CH3 CF3 C(0)Et C(0)0CH3 H H H H H H H H H H H C(0)CH3 C(0)Et C(0)0CH3 H CH2OCH3 CH2CN CH2C-CH C(0)CH3 C(0)Et C(0)0CH3 C(0)0CH3 H C(0)0CH3 C(0)0CH3 H C(0)0CH3 H H H H H H H H H • H H H C(0)CH3 C(0)Et C(0)0CH3 H H 220 CH2CF3 CH2CF3 CH2CH2OCH3 CH2(E-10a) . CH(CH3)CH2S02CH3 CH2CH=NOCH3 CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH;(D-17a)CH3 CH2(D-17b)CI CH2(D-21a)¬ CH2(D-22a) ^ CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-47a) CHsCD^Ta) CH2(D-47a) CH2(D^7a) CH2(D-47a) CH2(D-47a) CH2(D-i7a) CH(CH3)(D-47a) N(CH3)Ph N(CH3)Ph N(CH3)(D^7a) N(CH3)(D-50a) N(CH3)(D-50a) (D-13b)CH3 (D-15a)CH3 CH2C(0)NHCH2CF3 CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2(D-22a) CHgPr-c c-Bu CH2CF3 CH2CF3 CH2CF3 CH2CF3 CH2CH2OCH3 CH2(E-10a} 3,5-C!2-4-CH3 CF3 3,5-Ci2^-CH3 CF3 3,5-Cl2-4-CH3 CFg 3,5-Cl2^-CH3 CF3 3,5-Cl2^-CH3 GF3 3,5-C!2-4-CH3 CF3¬ 3,5-Ci2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3.5-CI,-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CFg 3,5-Cl2^-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5'4C)2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2^-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2^-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2^-CH3 CF2CI 3,5-Cl2^-CH3 CF2CI 3,5-C!2-4-CH3 CF2CI 3,5-Cl2-4-CH3 ' CF2CI 3,5-Cl2-4-CH3 CF2CI 3,5-Cl2^-CH3 CF2Ci 3,5-Cl2-4-CH3 CF2CI 3,5-Br2-4-CH3 CF3 3,5-Br2-4-CH3 CF3 3,5-Br2-4-CH3 CF3 3,5-Br2-4-CH3 CF3 3,5-Br2^-CH3 CF3 3,5-Br2^-CH3 CF3 3,5-Br2-4-CH3 CF3 3,5-Br2^-CH3 CF3 3,5-Br2-4-CH3 CF3 3,5-Br2-4-CH3 CF3 3,5-Br2^-CH3 CF3 3,5-Br2-4-CH3 CF3 H H H H H H H H H C(0)CH3 C(0)Et C(0)0CH3 H CH2OCH3 CH2CN CH2C=CH C{0)CH3 C(0)Et C(0)0CH3 C(0)0CH3 H C(0)0CH3 C(0)0CH3 H C(0)0CH3 H H H H H H H C(0)0CH3 H H . H C(0)CH3 . C(0)Et ¬ C(0)0CH3 H H H H H H H 221 CH(CH3)CH2S02CH3 CH2CH=NOCH3 CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-21a) CH,(D-22a) Chl2(D-22a) CH2(D-22a) CH2(D-22a)_ CH2(D-47a) CH2(D^7a) CH2(D-47a) CH2(D-47a) CH2(D-47a) CH2(D^7a) CH2(D^7a) CH{CH3)(D-47a) N(CH3)Ph N(CH3)Ph N(CH3)(D-47a) N(CH3)(D-50a) N(CH3)(D-50a) (D-13b)CH3 (D-15a)CH3 CH2CF3 CH2C(0)NHCH2CH-2CI CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2(D^7a) N(CH3)(D-50a) CHgPr-c CH2CF3 CH2CF3 CH2CF3 CH2CF3 CH2CH2OCH3 CH2(E-10a) CH2CH=NOCH3 CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17b)CI CH2(D-22a) 3,5-Br2-4-CH3 CF3 C(0)CH3 3,5-Br2-4-CH3 CF3 C(0)Et 3,5-Br2^-CH3 CF3 C(0)0CH3 3,5-Br2-4-CH3 CFgi H 3,5-Br2-4-CH3 CF3 CH2OCH3 3,5-Br2-4-CH3 CF3 CH2CN 3,5-Br2-4-CH3 CF V CHaC^CH 3,5-Br2^-CH3 CF3 C(0)CH3 3,5-Br2-4-CH3 CF3 C(0)Et 3,5-Br2-4-CH3 CF3 CppCH g 3,5-Br2-4-CH3 CF3 H 3,5-Br2-4-CH3 CF3 CppCH g 3,5-Br2^-CH3 CF3 C(0)0CH3 3,5-Br2-4-CH3 CF3 H 3,5-Br2^-CH3 CF3 CCOpCHg 3,5-Br2-4-CH3 CFgCI H 3,5-Br2-4-CH3 CF2CI H 3,5-Br2^-CH3 CF2CI H 3,5-Br2-4-CH3 CF2CI H 3,5-Br2^-CH3 CF2CI H 3,5-F2-4-OCH3 CF3 H 3,5-Fo-4-OCH3 CF3 H 3,5-F2^-OCH3 CF3 H 3,5-F2-4-OCH3 CF3 H 3,5-F2-4-OCH3 CF3 H 3,5-F2-4-OCF3 CF3 H 3,5-F2-4-OCF3 CF3 H 3,5-F2-4-OCF3 CF3 H 3,5-F2-4-OCF3 CF3 H 3,5-F2-4-OCF3 CF3 H 3,5-Cl2-4-OH ., CF3 H 3,5-Cl2^-OH CF3 H 3,5-Cl2-4-OH CF3 H 3,5-Cl2-4-OH CF3 H 3,5-Cl2-4-OH CF3 H 3,5-Cl2-4-OCH3 CF3 H 3,5-Cl2^-OCH3 CF3 H 3,5-Cl2^-OCH3 CF3 C(0)CH3 3,5-Cl2-4-OCH3 CF3 C(0)Et 3,5-Cl2-4-OCH3 CF3 C(0)0CH3 3,5-Cl2^-OCH3 CF3 H 3,5-Cl2-4-OCH3 CF3 H 3,5-Cl2-4-OCH3 CF3 H 3,5-Cl2^-OCH3 CF3 H 3,5-Cl2^-OCH3 CF3 H 3,5-Cl2-4-OCH3 Cr3 H 222 CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-47a) CH2(D^7a) CH2(D-47a) CH^iD^la) CH^iD^Ja) CH^{DA7a) CH2(D-47a) N(CH3)Ph N(CH3)Ph _ N(CH3)(D^7a) N(CH3)(D-50a) N(CH 3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) NlCHgXD-SOa) CHgCFg CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2Pr-c CH2CF3 CH2CF3 CH2CF3 CH2CF3 CH2CH2OCH3 CH2(E-10a) CH2CH=NOCH3 CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17b)Ci 3,5-C!2-4-OCH33,5-Cl2^-OCH33,5-Cl2-4-OCH33,5-Cl2-4-OCH33,5-Cl2-4-OCH33,5-Cl2-4-OCH33,5-Cl2^-OCH33,5-Cl2-4-OCH33,5-Cl2^-OCH33,5-Cl2-4-OCH33,5-Cl2^-OCH33,5-Cl2-4-OCH33,5-Cl2-4-OCH33,5-Cl2^-OCH33,5-Cl2^-OCH33,5-Cl2-4-OCH33,5rCl2^-OCH33,5'-C!2-4-OCH33,5-Ci2-4-OCH33,5-Cl2-4-OCH33,5-Cl2-4-OCH33,5-Cl2^-OEt3,5-Cl2^-OEt3,5-Cl2^-OEt3,5-Cl2-4-OEt3,5-Cl2^-OEt 3,5-Cl2^-OPr-n3,5-Cl2^-OCH2CH=CH23,5-Cl2^-OCH2C=CH3,5-Cl2-4-OTMS3,5-Cl2-4-OSi(CH3)2Bu-t3.F-5-Br-4-OCH33-F-5-Br-4-OCH33-F-5-Br-4-0CH33-F-5-Br-4-OCH33-F-5-Br-4-OCH33-CI-5-Br-4-OCH33-C!-5-Br-4-OCH33-Ci-5-Br-4-OCH33-CI-5-Br-4-OCH33-CI-5-Br-4-OCH33,5-Br2-4-OH3,5-Br2^-OH3,5-Br2-4-OH3,5-Br2-4-OH3,5-Br2-4-OH CF3 CF3 C.F3 CF3 CF3 -CF3 CF3 CF3 CF3 CFg CF3 CF3 CF3 CF3 CF3 CF3 CF2CI CF2CI CF2CI CF2CI CF2CI CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 Cf^ H C(0)CH3 C(0)Et C(0)0CH3 H CH2OCH3 CH2CN CH2C=CH C(0)CH3 C(0)Et C(0)0CH3 H C(0)0CH3 C(0)0CH3 H C(0)0CH3 H H H H H H H H H H H CH2CN H H H H H H H H H H H H H H H H H H 223 CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-47a) CH^CD^Ta) CH2(D-47a) CH2(D-47a) CH2(D-47a) CH2(D^7a) CH2(D^7a) N(CH3)Ph^ N(CH3)Ph"^ N(CH3)(D-47a) N(CH3)(D-50a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N{CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2(D^7a) CH2(D-47a) N(CH3)(D-50a) CH2C(Q)NHCH2CF3 CH2(D-22a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-it7a) N(CH3)(D-50a) CH2CF3 CH,C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) 3,5-Br2^-OCH3 CF3 3,5-Br2^-OCH3 CF3 3,5-Br2-4-OCH3 CF3 3,5-Br2-4-OCH3 CF3 3,5-Br2^-OCH3 "CF3 3,5-Br2-4-OCH3 GF.3 3,5-Br2^-OCH3 CF3 3,5-Br2-4-OCH3 CF3 •3,5-Br2-4-OCH3 CF3 3,5-Br2-4-OCH3 CF3 3,5-Br2-4-OCH3 CF3 3,5-Br2^-OCH3 CF3 3,5-Br2-4-OCH3 CF3 3,5-Br2-4-OCH3 CF3 3,5-Br2^-OCH3 CF3 3,5-Br2-4-OCH3 CF3 3,5|Br2^-OCH3 CF3 3,5-Br2-4-OCH3 CF3 3,5-Br2^-OCH3 CF3 3,5-Br2^-OCH3 CF3 3,5-Br2-4-OCH3 CF3 3,5-Br2-4-OCH3 CF3 3,5-Br2^-OCH3 CF3 3,5-Br2-4-OCH3 CF3 3,5-Br2^-OCH3 CF3 3,5-Br2-4-OCH3 CF3 3,5-Br2-4-OCH3 CF3 3,5-Br2^-OCH3 CF2CI 3,5-Br2-4-OCH3 CF2CI 3,5-Br2-4-OCH3 CF2CI 3,5-Br2-4-OCH3 . CF2CI 3,5-Br2-4-OCH3 CF2CI 3,5-Br2^-OEt CF3 3,5-Br2^-OEt CF3 3,5-Br2^-OEt CF3 3,5-Br2^-OEt CF3 3,5-Br2^-OEt CF3 3,5-12-4-OH CF3 3,5-l2-4-OH CF3 3,5-12^-OH CF3 3,5-12-4-OH CF3 3,5-12-4-OH CF3 2,4,6-(OCH3)3 CF3 3,4,5-(OCH3)3 CF3 3,5-Cl2-4-NH2 CF3 3,5-Cl2^-NH2 CF3 H H C(0)CH3 C(0)Et C(0)0CH3 H H H H H H H C(0)CH3 C(0)Et CJOpCHg H CH2OCH3 CH2CN CH2C=CH C(0)CH3 C(0)Et CpjOCHg H C(0)0CH3 C(0)0CH3 H C(0)0CH3 H H H H H H H H H H H H " H H H H C(0)0CH3 H H 224 CHzPr-c CH2CF3 CH2CF3 CH2CF3 , CH2CF3 CH2CH2OCH3 CH2(E-10a) CH2CH=N6CH3 CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17b)CI CH^iD-lla)¬ CH2{D-22ar CH2(D-22a) CH2(D-22a) CH2(D-47a) CH2(D-47a) CH2(D-47a) CH2(D-47a) CH2(D-47a) CH2(D-47a) CH2(D-47a) N(CH3)Ph N(CH3)Ph N(CH3)(D-47a) N(CH3)(D-50a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2(D^7a) CH2(D-47a) CH2CF3 CH2C(0)NHCH2CF3 3,5-Cl2^-NH2 CF3 H CH2(D-22a) 3,5-Cl2^-NH2 CF3 H CH2(D-47a) 3,5-Cl2^-NH2 CFg H N(CH3)(D-50a) 3,5-Br2^-NH2 CF3 H CH2CF3 3,5-Br2-4-NH2 CF3 H CH2C(0)NHCH2CF3 3,5-Br2^-NH2 GF3-H CH2(D-22a) 3,5-Br2^-NH2 CF3 H CH2(D^7a), 3,5-Br2^-NH2 CF3 H N(CH3)(D-50a) '3,5-l2^-NH2 CF3 H CH2CF3 3,5-l2-4-NH2 CF3 H CH2'C(0)NHCH2CF3 3,5-l2^-NH2 CF3 H CH2(D-22a) 3,5-l2-4-NH2 CF3 H CH2(D-47a) ^ 3,5-l2-4-NH2 CF3 H N(CH3)(D-50a) 3,5-Cl2-4-N02 CF3 H CH2CF3 3,5-Cl2^-N02 CF3 H CH2C(0)NHCH2CF3 3,5-Cl2-4-N02 CF3 H CH2(D-22a) 3,5-pi2-4-N02 CF3 H CHgCD^ya) 3,5-Cl2-4-N02 CF3 H N(CH3)(D-50a) 3,5-F2-4-CN CF3 H CH2CF3 , 3,5-F2-=i-CN CF3 H CH2C(0)NHCH2CF3 3,5-F2-4-CN CF3 H CH2(D-22a) 3,5-F2^-CN CF3 H CH2(D-47a) 3,5-F2-4-CN CF3 H N(CH3)(D-50a) 3,5-Cl2^-CN CF3 H CH2CF3 3,5-Cl2-4-CN CF3 H CH2C(0)NHCH2CF3 3,5-Cl2-4-CN CF3 H CH2(D-22a) 3,5-Cl2-4-CN CF3 H CH2(D-47a) 3,5-Cl2-4-CN CF3 H N(CH3){D-50a) 3,5-Br2^-CN CF3 H CH2CF3 3,5-Br2^-CN CF3 H CH2C(0)NHCH2CF3 3,5-Br2^-CN CF3 H CH2(D-22a) 3,5-Br2-4-CN CF3 H CH2(D-47a) 3,5-Br2^-CN CF3 H N(CH3)(D-50a) 2,3,5,6-F4 CF3 H N(CH3)(D-50a) 2,3,4,5,6-F5 CF3 H CH2G(0)NHCH2CF3 Table 3 In the table, the number showing the substitution position of substituents (X)^ and (Y)n corresponds to the position number indicated in the following structural formulae. The indication "-" means no-substitution. CF3. P-N (Y)„ CF3 0-N (Y)„ (G) / 1; vy ^ 2 II • 2 II ^ O._ V, S [2]-l , [2]-2 CICF2. P~N (Y)„ CICF2^0~N (Y)„ V / I ' V y 0 1 ' 9 II 9 II ^ o ^ s , [2]-3 or [2]-4 In addition, substituent G in the formulae [2]-1 to [2]-4 is the structure shown by the following G-1 to G-22, respectively. '^^ ^^N 3 ^ . ^^3 «^. 45^6^ 2 2 G-1 G-2 G-3 G-4 G-5 Q^m-.[==( (^)m-~~fr\ i^)m-^r=\ i^)m^Jir{ (Xk-./=( 4V« ^'5V2 4^S 3X3>2 3 \ > 5 5 G-11 G-12 G-13 G-14 G-16 (^n.^^{r{ (^)m-/^ QQr^^^M Wm"^"/ (X)„, .,(=( 5 S^'^ 3 S'^'~-CH3 4 ^ S 2 C^^ 5 N^S CH3 ^ G-17a G-19a G - 20 0-21 G-22 G (XL (Y)„ R^ R^ G-1 3-CF3 2-Pr-i H CH2CF3 G-1 3-CF3 2-OEt H G-1 3-CF3 2-OPr-i H G-1 3-CF3 2-OSO2CH3 H G-1 3-CF3 2-SEt ' H G-1 3-CF3 2-SPr-i . H G-1 3-CF3 2-NHGH^ H G-1 3-CF3 2-NHEt H G-1 3-CF3 2-NHPr-i H G-1 3-CF2CF3 2-Pr-i H G-1 3-CF2CF3 2-OEt H G-1 3-CF2CF3 2-OPr-i H G-1 3-CF2CF3 2-OSO2CH3 H G-1 3-CF2CF3 2-SEt H G-1 3-CF2CF3 2-SPr-i H G-1 3-CF2CF3 2-NHCH3 H G-1 3-CF2CF3 2-NHEt H G-1 i 3-CF2CF3 2-NHPr-i H G-1 ' 3-SF5 2-P M H G-1 3-SF5 2-OEt H . G-1 3-SF5 2-OPr-i H G-1 3-SF5 2-OSO2CH3 H G-1 3-SF5 2-SEt H G-1 3-SF5 2-SPr-i H G-1 3-SF5 2-NHCH3 H G-1 3-SF5 2-NHEt H G-1 3-SF5 2-NHPr-i H G-1 3-F-5-CI 2-Pr-i H G-1 3-F-5-CI 2-OEt H G-1 3-F-5-CI 2-OPr-i H G-1 3-F-5-CI 2-OSO2CH3 H G-1 3-F-5-CI ^ 2-SEt H G-1 3-F-5-CI 2-SPr-i H G-1 3-F-5-CI 2-NHCH3 H G-1 3-F-5-CI 2-NHEt H G-1 3-F-5-C! 2-NHPr-i H G-1 3,5-Cl2 3-F H G-1 3,5-Cl2 3-CI H G-1 3,5-Cl2 3-Br H G-1 3,5-Cl2 3-CH3 H G-1 3,5-Cl2 3-Et H G-1 3,5-Cl2 2-Pr-n H G-1 3,5-Cl2 2-Pr-i H G-1 3,5-Cl2 2-Pr-i C(0)CH3 G-1 3,5-Cl2 2-Pr-i H G-1 3,5-Cl2 2-Pr-i H G-1 3,5-Cl2 2-Pr-i H 227 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-5pa) CH2CF3 CH,C(0)NHCH,CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D<22a) CH2(D-*7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH3(D^7a) N(GH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) GH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH,CF3 CH2C(0)NHCH2CF3 CH2CF3 CH2CF3 CHjCPJNHCHgCHsCI CH2C(0)NHCH2CF3 CH2(D-22a) G-1 3,5-Cl2 2-Pr-i H G-1 3,5-Cl2 2-Pr-i CH^CN G-1 3,5-Cl2 2-Pr-i ; C(0)Et G-1 3,5-Cl2 2-Pr-i ' H G-1 3,5-Cl2 2-Pr-J' H G-1 3,5-Cl2 2-Pr-i:.¬. H G-1 3,5-Cl2 2-Bu-n H G-1 3,5-Cl2 2-Bu-s H G-l 3,5-Cl2 2-Bu-t H G-1 3,5-Cl2 2-CF2CF3 H G-1 3,5-Cl2 2-CH2OH H G-1 3,5-Cl2 2-CH2OCH3 H G-1 3,5-Cl2 2-CH2OCH3 H G-1 3,5-Cl2 2-CH2OCH3 H G-1 3,5-Cl2 2-CH2OCH3 H G-1 3,5-Cl2 2-CH2OCH3 H G-1 3,5-Cl2 2-CH20Et H G-l' 3,5-Cl2 2-CH20Pr-n H G-1 3,5-Cl2 2-CH20Pr-i H G-1 3,5-Cl2 2-CH20Pr-c H G-1 3,5-Cl2 2-CH2OCH2CF3 H G-1 3,5-Cl2 2-CH2CH2OCH3 H G-1 3,5-Cl2 2-CH2SCH3 H G-1 3,5-Cl2 2-CH2SCH3 H G-1 3,5-Ci2 2-CH2SCH3 H G-1 3,5-Cl2 2-CH2SCH3 H G-1 3,5-Cl2 2-CH2SCH3 H G-1 3,5-Cl2 2-CH2S(0)CH3 H G-1 3,5-Cl2 2-CH2SO2CH3 H G-1 3,5-Cl2 2-CH2SCF3 H G-1 3,5-Cl2 • 2-CH2SCF3 H G-1 3,5-Cl2 2-CH2SCF3 H G-1 3,5-Cl2 ' 2-CH2SCF3 H G-1 3,5-Cl2 2-CH2SCF3 H G-1 3,5-Cl2 2-CH2S(0)CF3 H G-1 3,5-Cl2 2-CH2SO2CF3 H G-1 3,5-Cl2 2-CH2Ph H G-1 3,5-Cl2 2-CH2(D-14a) H G-1 3,5-Cl2 2-CH2(D-24a) H G-1 3,5-Cl2 2-CH2(D-38a) H G-1 3,5-Cl2 3-OCH3 H G-1 3,5-Ci2 2-OEt H G-1 3,5-Cl2 2-OEt C(0)CH3 G-1 3,5-Cl2 2-OEt H G-1 3,5-CI, 2-OEt H G-1 3,5-Cl2 2-OEt H 228 CH2(D-47a) CH2(D-47a) CH^CD^Za) CH(CH3)Pii(R) N(CH3)Ph N(CH3)(D-50a) CH2(D-22a) CH^CD^Ta) N(CH 3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2CF3¬ CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-t7a) N(CH3)(D-50a) CH2(D-22a) CH2(D-^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2CF3 CH2CF3 CH2C(0)NHCH2CH,C1 CH2C(0)NHCH2CF3 CH2(D-22a) G-1 3,5-C!2 2-OEt H G-1 3,5-Cl2 2-OEt CH2CN G-1 3,5-Cl2 2-OEt C(0)Et G-1 3,5-Cl2 2-OEt ' H G-1 3,5-Cl2 2-OEt H G-1 3,5-Cl2 2-OEt :. H G-1 3,5-Cl2 2-OPr-n H G-1 3,5-Cl2 2-OPr-i H G-1 3,5-Cl2 2-OPr-i C(0)CH3 G-1 3,5-Cl2 2-OPr-i H G-1 3,5-Cl2 2-OPr-i H G-1 3.5-CI2 2-OPr-i H G-1 3,5-Cl2 2-OPr-i H G-1 3,5-Cl2 2-OPr-i CH2CN G-1 3,5-Cl2 2-OPr-i C(0)Et G-1 3,5-Cl2 2-OPr-i H G-1 , 3,5-Cl2 2-OPr-i H G-1 ' 3,5-Cl2 2-OPr-i H G-1 3,5-Cl2 2-OBu-n H G-1 3,5-Cl2 2-OPen-n H G-1 3,5-Cl2 2-OHex-n H G-1 3,5-Cl2 2-OCF2Br H G-1 3,5-Cl2 2-OCF2CHF2 H G-1 3,5-Cl2 2-OCF2CHFCI H G-1 3,5-Cl2 2-OCF2CHFCF3 H G-1 3,5-Cl2 2-OCF2CHFOCF3 H G-1 3,5-Cl2 2-OSO2CH3 H G-1 3,5-Cl2 2-OSO2CH3 C(0)CH3 G-1 3,5-Ci2 2-OSO2CH3 H G-1 3,5-Cl2 2-OSO2CH3 H G-1 3,5-Cl2 ^. 2-OSO2CH3 H G-1 3,5-Cl2 2-OSO2CH3 H G-1 3,5-Cl2 2-OSO2CH3 CH2CN G-1 3,5-Cl2 2-OSO2CH3 C(0)Et G-1 3,5-Cl2 2-OSO2CH3 H G-1 3,5-Ci2 2-OSO2CH3 H G-1 3,5-Cl2 2-OSO2CH3 H G-1 3,5-Cl2 2-OS02Et H G-1 3,5-Cl2 2-OS02Pr-i H G-1 3,5-Cl2 2-OSO2CF3 H G-1 3,5-Cl2 2-OPh H G-1 3,5-Cl2 2-S(0)CH3 H G-1 3,5-Cl2 2-SO2CH3 H G-1 3,5-Cl2 2-SEt H G-1 3,5-Ci2 2-SEt C(0)CH3 G-1 3,5-Cl2 2-SEt H CH2(D-47a) CH2(D-47a) CH2(D-47a) CH(CH3)Ph(R) N(CH3)Ph N(CH3)(D-50a) CH2(D-22a) CH2CF3 CH2CF3 CH2C(0)NHCH2CH2C1 CH2C(0)NHCH2CF3 CH2(D-22a)^ CH2(D-47a) ^ CH2{D-47a) CH2(D-47a) CH(CH3)Ph(R) N(CH3)Ph N(CH3)(D-50a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2CF3 CH2CF3 CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH^{b-22a) CH2(D^7a) CH2(D-47a) CH2(D^7a) CH(CH3)Ph(R) N(CH3)Ph N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2CF3 CH2CF3 CH2C(0)NHCH2CH2CI G-1 3,5-Cl2 2-SEt G-1 3,5-Cl2 2-SEt G-1 3,5-Cl2 2-SEt G-1 3,5-Cl2 2-SEt ' G-1 3,5-01^ 2-SEt G-1 3,5-Cl2 2-SEt.¬. G-1 3,5-Cl2 2-SEt G-1 3,5-Cl2 2-SEt •G-1 3,5-Cl2 2-S(0)Et G-1 3,5-Cl2 2-S02Et G-1 3,5-Cl2 2-SPr-n G-1 3,5-Cl2 2-S(0)Pr-n G-1 3,5-Cl2 2-S02Pr-n G-1 3,5-Cl2 2-SPr-i G-1 3,5-Cl2 2-SP H G-1 3,5-Ci2 2-SPr-i G-1, 3,5-Cl2 2-SPr-i G-1 3,5-Cl2 2-SPr-i G-1 3,5-Cl2 2-SPr-i G-1 3,5-Cl2 2-SPr-i G-1 3,5-Cl2 2-SPr-i G-1 3,5-Cl2 2-SPr-i G-1 3,5-Cl2 2-SPr-i G-1 3,5-Cl2 2-SPr-i G-1 3,5-Cl2 2-S(0)Pr-i G-1 3,5-Cl2 2-S02Pr-i G-1 3,5-Cl2 2-S(0)CHF2 G-1 3,5-Cl2 2-SO2CHF0 G-1 3,5-Cl2 2-S(0)CF3 G-1 3,5-Cl2 2-SO2CF3. G-1 3,5-Cl2 2-SCF2Br G-1 3,5-Cl2 2-S(0)CF2Br G-1 3,5-Cl2 2-S02CF2Br G-1 3,5-Cl2 2-SCF2CHFCI G-1 3,5-Cl2 2-S(0)CF2CHFCI G-1 3,5-Cl2 2-SO2CF2CHFCI G-1 3,5-Cl2 2-SPh G-1 3,5-Cl2 2-S(0)Ph G-1 3,5-Cl2 2-S02Ph G-1 3,5-Cl2 2-NHCH3 G-1 3,5-Cl2 2-NHCH3 G-1 3,5-Cl2 2-NHCH3 G-1 3,5-Cl2 2-NHCH3 G-1 3,5-Cl2 2-NHCH3 G-1 3,5-Cl2 2-NHCH3 G-1 3,5-Cl2 2-NHCH3 H H H CH2CN C(0)Et H H H H H H H H H C(0)CH3 H H H H CH2CN C(0)Et H H H H H H H H H H H H H H H H H • H H H C(0)CH3 C(0)Et C(0)0CH3 H H 230 CH2C(0)NHCH2CF3 CH2(D-22a) CH^CD^ya) CH^lD^Ta) CH2(D-47a). CH(CH3)Ph(R) N(CH3)Ph N(CH 3)(D-50a) CH2(D-22a) eH2(D-47a) N(CH3)(D-50a) CH2CF3 ¬ CH2C(0)NHCH2CF3 CH2CF3 CH2CF3 CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CHgCD^Ta) CH2(D-47a) CH(CH3)Pli(R) N(CH3)Ph N(CH3)(D-50a) CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 , CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 c-Bu CH2CF3 CH2CF3 CH2CF3 CH2CF3 CH2CH2OCH3 CH2(E-10a) G-1 3,5-C!2 2-NHCH3 H G-1 3,5-Cl2 2-NHCH3 H G-1 3,5-Cl2 2-NHCH3 H G-1 3,5-Cl2 2-NHCH's H G-1 3,5-Cl2 2-NHCH3 H G-1 3,5-Ci2 2-NHCH3 H G-1 3,5-Cl2 2-NHCH3 C(0)CH3 G-1 3,5-Cl2 2-NHCH3 C(0)Et G-l 3,5-Cl2 2-NHCH3 CppCH s G-1 3,5-Cl2 2-NHCH3 H , G-1 3,5-Cl2 2-NHCH3 CH2CN G-1 3,5-Cl2 2-NHCH3 C(0)CH3 G-1 3,5-Cl2 2-NHCH3 C(0)Et G-1 3,5-Cl2 2-NHCH3 C(0)OCH3 G-1 3,5-Cl2 2-NHCH3 C(0)0CH3 G-1 3,5-Cl2 2-NHCH3 H G-1 3,5-Cl2 2-NHCH3 H G-l' 3,5-Cl2 2-NHCH3 C(0)0CH3 G-1 3,5-Cl2 2-NHEt H G-1 3,5-Cl2 2-NHEt C(0)CH3 G-1 3,5-Cl2 2-NHEt H G-1 3,5-Cl2 2-NHEt H G-1 3,5-Cl2 2-NHEt H G-1 3,5-Cl2 2-NHEt H G-1 3,5-Cl2 2-NHEt CH2CN G-1 3,5-Cl2 2-NHEt C(0)Et G-1 3,5-Cl2 2-NHEt H G-1 3,5-Cl2 2-NHEt H G-1 3,5-Cl2 2-NHEt H G-1 3,5-Cl2 2-NHPr-n H G-1 3,5-Cl2 . 2-NHPr-n H G-1 3,5-Cl2 2-NHPr-n H G-1 3,5-Cl2 2-NHPr-n H G-1 3,5-Cl2 2-NHPr-n H G-1 3,5-Cl2 2-NHPr-i H G-1 3,5-Cl2 2-NHPr-i C(0)CH3 G-1 3,5-Cl2 2-NHPr-i H G-1 3,5-Cl2 2-NHPr-i H G-1 3,5-Cl2 2-NHPr-i H G-1 3,5-C!2 2-NHPr-i H G-1 3,5-Cl2 2-NHPr-i CH2CN G-1 3,5-Cl2 2-NHPr-i C(0)Et G-1 3,5-Cl2 2-NHPr-i H G-1 3,5-Cl2 2-NHPr-i H G-1 3,5-Cl2 2-NHPr-i H G-1 3,5-Gl2 2-N(CH3)2 H 231 CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH(CH3)Ph(R) CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-47a) CH2(D^7a) CH2(l>47a) CH2(D-47a) CH2(D-47a) CH(CH3)(D-47a) N(CH3)Ph N(CH3)(D-50a) N(CH3)(D-50a) CH2CF3 CH2CF3 CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2{D^7a) CH2(D^7a) CH(GH3)Ph(R) N(CH3)Ph N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2CF3 CH2C(0)NHCH2CH2CI CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) CH2(D^7a) CH2(D^7a) CH(CH3)Ph(R) N(CH3)Ph N(GH3)(D-50a) CH2CF3 G-1 3,5-Cl2 2-HiCH,), G-1 3.5-CI2 2-N(CH3)2 G-1 3,5-Cl2 2-N(CH3).2 G-1 3,5-Cl2 2-N(CH3y^ G-1 3,5-Cl2 2-N(CH3)Et G-1 3.5-CI2 2-N(Et)'2^ ¬ G-1 3,5-Cl2 2-NHCHO G-1 3,5-Cl2 2-NHCHO G-1 3,5-Cl2 2-NHCHO G-1 3,5-Cl2 2-NHCHO G-1 3,5-Cl2 2-NHCHO G-1 3,5-Cl2 2-NHC(0)CH3 G-1 3,5-Cl2 2-NHC(0)CH3 G-1 3,5-Cl2 2-NHC(0)CH3 G-1 3,5-Cl2 2-NHC(0)CH3 G-1 3,5-Cl2 2-NHC(0)CH3 G-1.< 3,5-Cl2 2-NHC(0)Et G-1 ' 3,5-Cl2 2-NHC(0)Pr-n G-1 3,5-Cl2 2-NHC(0)Pr-i G-1 3,5-Cl2 2-NHC(0)Pr-c G-1 3,5-Cl2 2-NHC(0)Bu-t G-1 3,5-Cl2 2-NHC(0)CF3 G-1 3,5-Cl2 2-NHC(0)CF3 G-1 3,5-Cl2 2-NHC(0)CF3 G-1 3,5-Cl2 2-NHC(0)CF3 G-1 3,5-Cl2 2-NHC(0)CF3 G-1 3,5-C!2 2-NHC(0)OCH3 G-1 3,5-Cl2 2-NHC(0)OCH3 G-1 3,5-Cl2 2-NHC(0)0CH3 G-1 3,5-Cl2 2-NHC(0)OCH3 G-1 3,5-Cl2 •• 2-NHC(0)OCH3 G-1 3,5-Cl2 2-NHC(0)0Et G-1 3,5-Cl2 2-NHC(0)SCH3 G-1 3,5-Cl2 2-NHC(0)SCH3 G-1 3,5-Cl2 2-NHC(0)SCH3 G-1 3,5-Cl2 ' 2-NHC(0)SCH3 G-1 3,5-Cl2 2-NHC(0)SCH3 G-1 3,5-Cl2 2-NHC(0)SEt G-1 3,5-Cl2 2-NHC(S)OCH3 G-1 3,5-Cl2 2-NHC(S)OCH3 G-1 3,5-Cl2 2-NHC(S)OCH3 G-1 3,5-Cl2 2-NHC(S)OCH3 G-1 3,5-Cl2 2-NHC(S)OCH3 G-1 3,5-Cl2 2-NHC(S)0Et G-1 3,5-Cl2 2-NHC(S)SCH3 G-1 3,5-Cl2 2-NHC(S)SCH3 H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H CH2C(0)NHCH2CF3 CH2(D-22a) CH,{D^7a) N(CH3)(D-5Pa) CH2(D-22a) CH2(D-47a) CH^CFg CH2C(0)NHCH2CF3 CH2(D-22a) CH^CD^Ta) N(CH3)(D-50a) CH^CFg-¬ CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH gXD-SOa) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CHaCD^Ya) N(CH3)(D-50a) CH2CF3 GH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 ,CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2CF3 CH2C(0)NHCH2CF3 G-1 3,5-Cl2G-1 3,5-C!2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Ci2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 .3,5-Cl2.G-1 3,5-Cl2. G-l} 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2 . G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Ci2G-1 3,5-Cl2G-1 3,5-Cl2G-1 3,5-Cl2 2-NHC(S)SCH3 H 2-NHC(S)SCH3 H 2-NHC{S)SCH3 H 2-NHC(^)SEt H 2-NHSO2CH3 H 2-NHSO;-CH3 H 2-NHSO2CH3 H 2-NHSO2CH3 H 2-NHSO2CH3 H 2-NHSO2CF3 H 2-NHSO2CF3 H 2-NHSO2CF3 H 2-NHSO2CF3 H 2-NHSO2CF3 H 2-N(CH3)CHO H 2-N(CH3)CHO H 2-N(CH3)CHO H 2-N(CH3)CHO H 2-N(CH3)CHO H 2-N(CH3)C(G)CH3 H 2-N(CH3)C(0)Et H 2-N(CH3)C(0)Pr-n H 2-N(CH3)C(0)Pr-i H 2-N(CH3)C(0)Pr-c H 2-N(CH3)C(0)Bu-t H 2-N(CH3)C(0)CF3 H 2-N(CH3)C(0)OCH3 H 2-N(CH3)C(0)OEt H 2-N(CH3)C(0)SCH3 H 2-N(CH3)C(0)SEt H 2-N(CH3)C(S)OCH3 H 2-N(CH3)C(S)OEt H 2-N(CH3)C(S)SCH3 H 2-N(CH3)C(S)SEt H 2-N(CH3)S02CH3 H 2-N(CH3)S02CF3 H 2-N(Et)CH0 H 2-N(Et)C{0)CH3 H 2-N(Et)C(0)Et H 2-N(Et)C(0)Pr-n H 2-N(Et)C(0)Pr-i H 2-N(Et)C(0)Pr-c H 2-N(Et)C(0)Bu-t H 2-N(Et)C(0)CF3 H 2-N(Et)C(0)OCH3 H 2-N(Et)C(0)0Et H 233 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2(D-22a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-:22a) CH2(b^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D--22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CHsCD^/a) N(CH3)(D-50a) CH^(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH,(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) G-1 3,5-Cl2 2-N(Et)C(0)SCH3 H G-1 3,5-Cl2 2-N(Et)C(0)SEt H G-1 3,5-Cl2 2-N(Et)C(S)OCH3 H G-1 3.5-CI2 2-N(EtC(S)0Et H G-1 3,5-Cl2 2-N(Et)G(S)SCH3 H G-1 3,5-Cl2 2-N(Et)i3(S)SEt H G-1 3,5-Ci2 2-N(CH3)S02CH3 H G-1 3,5-Cl2 2-N(CH3)S02CF3 H G-1 3,5-Cl2 2-N=CHOCH3 H G-1 3,5-Cl2 2-N=C(CH3)OCH3 H G-1 3,5-Cl2 2-N=C(CH3)OCH3 H G-1 3,5-Cl2 2-N=C(CH3)OCH3 H G-1 3,5-Cl2 2-N=C(CH3)OCH3 H G-1 3,5-Cl2 2-N=C(CH3)OCH3 H G-1 3,5-Cl2 2-(D-5a) H G-1 3,5-Cl2 2-NHCH2¬ G-1,: 3,5-Cl2 2-N(CH3)CH2¬ G-1 • 3,5-Cl2 2-N(Et)CH2¬ G-1 3,5-Cl2 2-C(0)OCH3 H G-1 3,5-Cl2 2-C(0)NH2 H G-1 3,5-Cl2 2-(T-21) H G-1 3,5-0(2 2-C(S)NH2 H G-1 3,5-Cl2 2-C(S)NH2 H G-1 3,5-Cl2 2-C(S)NH2 H G-1 3,5-Cl2 2-C(S)NH2 H G-1 3,5-Cl2 2-C(S)NH2 H G-1 3,5-Cl2 2-(T-22) H G-1 3,5-Cl2 2-Ph H G-1 3,5-Cl2 2-(D-14a) H G-1 3,5-Cl2 2-(D-24a) H G-1 3,5-Ci2 " 2-(D-38a) H G-1 3,5-Cl2 2-(D^3a) H G-1 3,5-Cl2 2-(D^3b)CH3 H G-1 3,5-Cl2 2-(D-^a) H G-1 3,5-Cl2 2-(D-45a) H G-1 3,5-Cl2 2-(D-^5b)CH3 H G-1 3,5-Cl2 2-(D-46a) H G-1 3,5-Cl2 2-(D46b)CH3 H G-1 3,5-Cl2 2.3-F2 H G-1 3,5-Cl2 2-F-3-CI H G-1 3,5-Cl2 2-F-3-Br H G-1 3,5-Cl2 2-F-3-CN H G-1 3,5-Cl2 2-F-3-OCH3 H G-1 3,5-Cl2 2,5-F2 H G-1 3,5-Cl2 2-F-5-CI H G-1 3,5-C!2 2-F-5-Br H CH^CFg CH2C(0)NHCH2CF3 CH2(D-22a) CH^CD^Ta)^ N(CH3)(D-50a) CH2CF3 CH2C(Q)NHCH2CF3 CH2(D-22a) CH^iDAJa) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CHaCD^Ta) N(CH3)(D-50a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH-2(D-22a) CH^CD^ya) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 • 234 G-1 3,5-Ci3 2-F-5-CH3 G-1 3,5-Cl2 2-F-5-CF3 G-1 3,5-Cl2 2-F-5-OCH3 G-1 3,5-Cl2 2,6-F^ G-1 3.5-CI2 2-F-6-CI G-1 3,5-Cl2 2-F-6-Br- G-1 3,5-CU 2-F-6-CF3 G-1 3,5-Cl2 2-F-6-NO2 •G-1 3,5-Cl2 2-C1-3-F G-1 3,5-Cl2 2,3-Cl2 G-1 3,5-Cl2 2-CI-3-CH3 G-1 3,5-Ci; 2-CI-3-OCH3 G-1 3,5-Cl2 2-C1-3-CN G-1 3,5-Cl2 2-CI-5-F G-1 3,5-Cl2 2,5-Cl2 G-1 3.5-CI2 2-CI-5-Br G-1 3,5-Cl2 2-CI-5-CH3 G-1 3,5-Cl2 2-CI-5-CF3 G-1 3,5-Cl2 2-Ci-5-OCH3 G-1 3,5-Cl2 2,6-Cl2 G-1 3,5-Cl2 2-CI-6-Br G-1 3,5-Cl2 2-CI-6-CH3 G-1 3,5-CI 2 2-CI-6-CF3 G-1 3,5-Cl2 2-CI-6-OCH3 G-1 3,5-Cl2 2-Br-3-F G-1 3,5-Cl2 2-Br-3-OCH3 G-1 3,5-Cl2 2-Br-5-F G-1 3,5-CI 2 2-Br-5-CI G-1 3,5-Cl2 2,5-Br2 G-1 3,5-CI 2 2-Br-5-CH3 G-1 3,5-Cl2 2-Br-5-CF3 G-1 3,5-Cl2 2-Br-5-OCH3 G-1 3,5-Ci2 2,6-Br2 G-1 3,5-Ci2 2-CH3-3-F G-1 3,5-Cl2 2-CH3-3-F G-1 3,5-CI 2 2-CH3-3-F G-1 3,5-CI 2 2-CH3-3-F G-1 3,5-CI 2 2-CH3-3-F G-1 3,5-CI 2 2-CH3-3-CI G-1 3,5-Cl2 2-CH3-3-Br G-1 3,5-Cl2 2,3-(CH3)2 G-1 3,5-Cl2 2-CH3-3-CF3 G-1 3,5-CI 2 2-CH3-3-OCH3 G-1 3,5-CI 2 2-CH3-3-CN G-1 3,5-Cl2 2-CH,-5-F G-1 3,5-Ci 2 2-CH3-5-CI H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H 235 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH3C(0)NHCH3CF3 CH3(D-22a) CH2(D-47a) N(CH3)(D-50a) CH^CFg CH2C(0)NHCH2CF3 CH2(D-22a) CH^CD^ZaJ N(CH3)(D-50a) CH^CFg CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 G-1 3,5-Cl2 2-CH3-5-Br G-1 3,5-Cl2 2,5-(CH3)2 G-1 3,5-Cl2 2-CH3-5-eF3 G-1 3,5-Cl2 2-CH3-5-dCH3 G-1 3,5-Cl2 2-CH3-6-F G-1 3,5-Cl2 2-CH3-6-F¬ G-1 3,5-C!2 2-CH3-6-F G-1 3,5-Cl2 2-CH3-6-F G-1 3,5-Cl2 2-CH3-6-F G-1 3,5-Cl2 2-CH3-6-CI G-1 3,5-Cl2 2,6-(CH3)2 G-1 3,5-Cl2 2-CH3-6-CF3 G-1 3,5-Cl2 2-CH3-6-OCH3 G-1 3,5-Cl2 2-CF3-5-F G-1 3,5-Cl2 2-CF3-5-CI G-1 3,5-Cl2 2-CF3-5-Br G-1 i 3,5-Cl2 2-CF3-5-CH3 G-1 3,5-Cl2 2-CF3-6-OCH3 G-1 3,5-Cl2 2-OCH3-3-F . G-1 3,5-Ci2 2-OCH3--13-Br- G-1 3,5-Cl2 2-OCH3-5-F G-1 3,5-Cl2 2-OCH3-5-CI G-1 3,5-Cl2 2-OCH3-5-Br G-1 3,5-Cl2 2-OCH3-5-CH3 G-1 3,5-Cl2 2-CN-3-F G-1 3-F-5-Br 2-Pr-i G-1 3-F-5-Br 2-OEt G-1 3-F-5-Br 2-OPr-i G-1 3-F-5-Br 2-OSO2CH3 G-1 3-F-5-Br 2-SEt G-1 3-F-5-Br " 2-SPr-i G-1 3-F-5-Br 2-NHCH3 G-1 3-F-5-Br 2-NHEt G-1 3-F-5-Br 2-NHPr-i G-1 3-CI-5-Br , 2-Pr-i G-1 3-CI-5-Br 2-OEt G-1 3-CI-5-Br 2-OPr-i G-1 3-CI-5-Br 2-OSO2CH3 G-1 3-C{-5-Br 2-SEt G-1 3-Cl-5-Br 2-SP H G-1 3-CI-5-Br 2-NHCH3 G-1 3-CI-5-Br 2-NHEt G-1 3-C[-5-Br 2-NHPr-i G-1 3,5-Br2 2-P H G-1 3,5-Br2 2-OEt G-1 3,5-Br2 2-OPr-i H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H H 236 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH'2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7^ N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N{CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) G-1 3,5-Br2 2-OSO2CH3 H G-1 3,5-Br2 2-SEt H G-1 3,5-Br2 2-SPr-i H G-1 3,5-Br2 2-NHCH'3 H G-1 3,5-Br2 2-NHEt H G-1 3,5-Br2 2-NHR]:-i. H G-1 3-F-5-CF3 2-Pr-i H G-1 3-F-5-CF3 2-OEt H G-l 3-F-5-CF3 2-OPr-i H G-1 3-F-5-CF3 2-OSO2CH3 H G-1 3-F-5-CF3 2-SEt H G-1 3-F-5-CF3 2-SPr-i H G-1 3-F-5-CF3 2-NHCH3 H G-1 3-F-5-CF3 2-NHEt H G-1 3-F-5-CF3 2-NHPr-i H G-1 3-CI-5-CF3 2-Pr-i H G-1| 3-CI-5-CF3 2-OEt H G-t' 3-CI-5-CF3 2-OPr-i H G-1 3-CI-5-CF3 2-OSO2CH3 H G-r¬ ¬ 3-GI-5-CF3 2-SEt H G-1 3-CI-5-CF3 2-SPr-i H G-1 3-CI-5-CF3 2-NHCH3 H G-1 3-CI-5-CF3 2-NHEt H G-1 3-CI-5-CF3 2-NHPr-i H G-1 3-Br-5-CF3 2-Pr-i H G-1 3-Br-5-CF3 2-OEt H G-1 3-Br-5-CF3 2-OPr-i H G-1 3-Br-5-CF3 2-OSO2CH3 H G-1 3-Br-5-CF3 2-SEt H G-1 3-Br-5-CF3 2-SPr-i H G-1 3-Br-5-CF3 . 2-NHCH3 H G-1 3-Br-5-CF3 2-NHEt H G-1 3-Br-5-CF3 2-NHPr-i H G-1 3,5-(CF3)2 2-Pr-i H G-1 3,5-(CF3)2 2-OEt H G-1 3,5-(CF3)2 2-OPr-i H G-1 3,5-(GF3)2 2-OSO2CH3 H G-1 3,5-(CF3)2 2-SEt H G-1 3,5-(CF3)2 2-SPr-i H G-1 3,5-(CF3)2 2-NHCH3 H G-1 3,5-(CF3)2 2-NHEt H G-1 3,5-(CF3)2 2-NHPr-i H G-1 3,4,5-Ci3 2-Pr-i H G-1 3,4,5-Cl3 2-OEt H G-1 3,4,5-Cl3 2-OPr-i H G-1 3,4,5-Cl3 2-OSO2CH3 H 237 CH2(D-47a) N(CH 3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3¬ CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a). CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D,22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3¬ CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) G-1 3,4,5-Cl3 2-SEt H G-1 3,4,5-Cl3 2-SPr-i H G-1 3,4,5-Cl3 2-NHCH3 H G-1 3,4,5-Cl3 2-NHEt ' H G-1 3,4,5-Cl3 2-NHPr-i , H G-2 4-CI 2-CH3-. . H G-2 4-Br 2-CH3 H G-2 4-CF3 2-CI H G-2 4-CF3 2-Br H G-2 4-CF3 2-1 H G-2 4-CF3 2-CH3 H G-2 4-CF3 2-Et H G-2 4-CF3 2-CF3 H G-2 4-CF3-6-CH3 2-CI H G-2 4-CF3-6-CH3 2-Br H G-2 4~CF3-6-CH3 2-1 H G-2., 4-CF3-6-CH3 2-CH3 H G-2 4-CF3-6-CH3 2-Et H G-2 4-CF3-6-CH3 2-CF3 H G-3 5-CI 2-CH3 H - G-3 5-CF3 2-GI H G-3 5-CF3 2-Br H G-3 5-CF3 2-1 H G-3 5-CF3 2-CH3 H G-3 5-CF3 2-Et H G-3 5-CF3 2-GF3 H G-3 5-CF3-6-CI 2-CH3 H G-3 5-NO2-6-CI 2-CH3 H G ^ 2-CI 2-CH3 H G-4 2-Br 2-CH3 H G ^ 2,6-Cl2 ^' ¬ H G ^ 2,6-Cl2 2-F H G-4 2,6-Cl2 2-CI H G ^ 2,6-Cl2 2-CI H G-4 2,6-Cl2 2-CI H G ^ 2,6-Cl2 2-CI H G ^ 2,6-Cl2 2-CI H G-4 2,6-Cl2 2-Br H G-4 2,6-Cl2 2-Br H G-4 2,6-Cl2 2-Br H G-4 2,6-Cl2 2-Br H G 4 2,6-Cl2 2-Br H G-4 2,6-Cl2 2-1 H G4¬ 2,6-Cl2 2-1 H G-4 2,6-Cl2 2-1 H G ^ 2,6-Cl2 2-1 H 238 N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3_ CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) GH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D:47a) N(GH3)(D-50a) CH2CF3 CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D47a) N(CH3)(D-50a) CH2CF3 CH2CrO)NHCH2CF3 CH2(D-22a) CH2(D47a) G-* 2,6-Cl2 2-1 H G 4 2,6-C!2 2-CH3 H G ^ 2,6-Cl2 2-CH3 H G-4 2,6-Cl2 2-CH3 '• H G-^ 2,6-Cl2 2-CH3 C(0)CH3 0-A 2,6-CI, 2-CH3. . C(0)Et GA 2,6-Cl2 2-CH3 C(0)0CH3 G-4 2,6-Cl2 2-CH3 H •GA 2,6-Cl2 2-CH3 H G-^ 2,6-Cl2 2-CH3 H G-^ 2,6-Cl2 2-CH3 H G-* 2.6-CU 2-CH3 H G-4 2,6-Cl2 2-CH3 H G-^ 2,6-Cl2 2-CH3 H GA 2,6-Cl2 2-CH3 H G ^ 2,6-Cl3 2-CH3 C(0)CH3 G ^ 2,6-Cl2 2-CH3 C(0)Et G-4 2,6-Cl3 2-CH3 C(0)0CH3 G-4 2,6-01^ 2-CH3 H GA 2,6-Cl2 2-CH3 CH3CN G-4 2,6-CU 2-CH3 C(0)CH3 G-4 2,6-Cl2 2-CH3 C(0)Et G-4 2,6-Cl2 2-CH3 C(0)0CH3 GA 2,6-Cl3 2-CH3 C(0)0CH3 GA 2,6-Cl2 2-CH3 H G-A 2,6-Cl2 2-CH3 H G-4 2.6-CI3 2-CH3 C(0)0CH3 G-* 2,6-Cl2 2-Et H G ^ 2,6-Cl2 2-CF3 H G-* 2,6-Cl2 2-CF3 H GA 2,6-Cl3 ' 2-CF3 H G-4 2,6-Cl3 2-CF3 H G-4 2,6-CU 2-CF3 H G-4 2,6-Cl2 2--OCH3 H G-4 2,6-Cl2 2-OCHF2 H GA 2,6-Cl2 2-OCF3 H G-4 2,6-Cl2 2-SCH3 H GA 2,6-Cl3 2-SCF3 H G ^ 2,6-Cl2 2-NO2 H G-4 2,6-Cl2 2-NHCH3 H G-4 2,6-Cl2 2-NHEt H G-5 2-CF3 2-CI H G-5 2-CF3 2-Br H G-5 2-CF3 2-1 H G-5 2-CF3 2-CH3 H G-5 2-CF3 2-Et H 239 N(CH3)(D-50a) CH^Pr-c c-Bu CH2CF3 CH2CF3 CH3CF3 CH2CF3 CH2CH2OCH3 CH2(E-10a) CH3C(0)NHCH2CH,CI CH2C(0)NHCH2CF3 CH(CH3)Eh(R) CH2(D-17a)CH3 CH2(D-17b)CI CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D-22a) CH2(D^7a) CH2(D^7a) CH2(D-47a) CH2(D^7a) CH^(S>A7a) CH(CH3)(D-47a) N(CH3)Ph N(CH3)(D-50a) N(CH3)(D-50a) CH3C(0)NHCH2CF3 CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2(D-22a) CH2(D-47a) N(CH3)(D-50a) CH2CF3 CH3C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH3CF3 CH,(D-22a) CH2(D-47a) N(CH3)(D-50a) G-5 2-CF3 2-CF3 H CHoCFa^ G-5 6-CF3 2-CI H CH2C(0)NHCH2CF3 G-5 6-CF3 2-Br H CH2(D-22a) G-5 6-CF3 2-! ' H CH2(D^7a) G-5 6-CF3 2-CH3 H N(CH3)(D-50a) G-5 6-CF3 2-Et.. _ H CH2CF3 G-5 6-CF3 2-CF3 H CH^CCOjNHCHsCFs G-5 2,6-Cl2 2-CI H CH2(D-22a) •G-5 2,6-Cl2 2-Br H CH^CD^Ta) G-5 2,6-Cl2 2-i H N(GH3)(D-50a) G-5 2,6-Cl2 2-CH3 H CH2CF3 G-5 2,6-Cl2 2-Et H CH2C(0)NHCH2CF3 G-5 2,6-Cl2 2-CF3 H CH2(D-22a)= G-5 2-CH3-6-CI 2-CH3 H GH2(D^7a) G-5 2-CI-6-CF3 2-CI H . N(CH3)(D-50a) G-5 2-CI-6-CF3 2-Br H CH2CF3 G-5, 2-CI-6-CF3 2-1 H CH2C(0)NHCH2CF3 G-5" 2-CI-6-CF3 2-CH3 H CH2(D-22a) G-5 2-CI-6-CF3 2-Et H CH2(D^7a) G-5 2-CI-6-CF3 2-CF3 H N(CH3)(D-50a) G-5 2-Br-6-CF3 2-CI H CH2CF3 G-5 2-Br-6-CF3 2-Br H CH2C(0)NHCH2CF3 G-5 2-Br-6-CF3 2-1 H CH2(D-22a) G-5 2-Br-6-CF3 2-CH3 H CHgCD^ya) G-5 2-Br-6-CF3 2-Et H N(CH3)(D-50a) G-5 2-Br-6-CF3 2-CF3 H CH2CF3 G-5 2-CH3-6-CF3 2-CI H CH2C(0)NHCH2CF3 G-5 2-CH3-6-CF3 2-Br H CH2(D-22a) G-5 2-CH3-6-CF3 2-1 H CH2(D^7a) G-5 2-CH3-6-CF3 2-CH3 H N(CH3)(D-50a) G-5 2-CH3-6-CF^ 2-Et H CH2CF3 G-5 2-CH3-6-CF3 2-CF3 H CH2C(0)NHCH2CF3 G-5 2,6-(CF3)2 2-CI H CH2(D-22a) G-5 2,6-(CF3)2 2-Br H CH2(D-47a) G-5 2,6-(CF3)2 2-1 H N(CH 3)(D-50a) G-5 2,6-(CF3)2 2-CH3 H 'CH2CF3 G-5 2,6-(CF3)2 2-Et H CH2C(0)NHCH2CF3 G-5 2,6-(CF3)2 2-CF3 H CH2(D-22a) G-5 2-SCH3-6-CI 2-CH3 H CH2(D-47a) G-5 2-SCH3-6-CF3 2-CH3 H N(CH3)(D-50a) G-11 5-CF3 2-CI H CH2CF3 G-11 5-CF3 2-Br H CH2C(0)NHCH2CF3 G-11 5-CF3 2-1 H CH2(D-22a) G-11 5-CF3 2-CH3 H CH2(D^7a) G-11 5-CF3 2-Et H N(CH3)(D-50a) G-11 5-CF3 2-CF3 H CH2CF3 240 G-12 4-CF3 2-CI H G-12 4-CF3 2-Br H G-12 4-CF3 2-1 H G-12 4-CF3 2-CH3 H G-12 4-CF3 2-Et H G-12 4-CF3 2-CF3.¬, H G-13 5-CF3 2-F H G-13 5-CF3 2-CI H G-13 5-CF3 2-Br H G-13 5-CF3 2-1 H G-13 5-CF3 2-CH3 H G-13 5-CF3 2-CH3 H G-13 5-CF3 2-CH3 H G-13 5-CF3 2-CH3 H G-13 5-CF3 2-CH3 H G-13 5-CF3 2-Et H G-13 5-CF3 2-CF3 H G-1^ 5-CF3 2-SCH3 H G-13 5-CF3 2-NHCH3 H G-14 4-CF3 2-F H G-14 4-CF3 2-CI H G-14 4-CF3 2-Br H G-14 4-CF3 2-1 H G-14 4-CF3 2-CH3 H G-14 4-CF3 2-CH3 H G-14 4-CF3 2-CH3 H G-14 4-CF3 2-CH3 H G-14 4-CF3 2-CH3 H G-14 4-CF3 2-Et H G-14 4-CF3 2-CF3 H G-14 4-CF3 '- 2-SCH3 H G-14 4-CF3 2-NHCH3 H G-16 3-CF3 2-CI H G-16 3-CF3 2-Br H G-16 3-CF3 2-1 H G-16 3-CF3 2-CH3 H G-16 3-CF3 2-Et H G-16 3-CF3 2-CF3 H G-17a 5-CF3 2-F H G-17a 5-CF3 2-CI H G-17a 5-CF3 2-Br H G-17a 5-CF3 2-1 H G-17a 5-CF3 2-CH3 H G-17a 5-CF3 2-CH3 H G-17a 5-CF3 2-CH3 H G-17a 5-CF3 2-CH3 H 241 CH^C(0)mCH,CF, CH2(D-22a) CH2(D-47a) N(CH3)(D:50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) N(CH 3)(D-50a) CH2CF3 CH2CF3 CH2C(0)NHCH2CF3 . CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-*7a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D^7a) N(CH3)(D-50a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2CF3 CH2C(0)NHCH2CF3 CH2(D-22a) CH2(D-47a) G-17a 5-CF3 2-CH3 H N(CH3)(D-50a) G-17a 5-CF3 2-Et H CH^CD^Ta) G-17a 5-CF3 2-CF3; H N(CH3)(D-50a) G-17a 5-CF3 2-SCHl H CH2CF3, G-17a 5-CF3 2-^4HCH3 H CH.CCOjNHCH^CFj G-19a 3-CF3 2-Ci;.. _ H CH2(D-22a) G-19a 3-CF3 2-Br H CH2(D^7a) G-19a 3-CF3 2-1 H N(CH3)(D'-50a) •G-19a 3-CF3 2-CH3 H CH2CF3 G-19a 3-CF3 2-Et H CH2C(0)NHCH2CF3 G-19a 3-CF3 2-CF3 H CH2(D-22a) G-20 4-CF3 2-Cl H CH2(D^7-a) G-20 4-CF3 2-Br H N(CH gXD-^Oa) G-20 4-CF3 2-1 H CH2CF3 G-20 4-CF3 2-CH3 H CH2C(0)NHCH2CF3 G-20 4-CF3 2-Et H CH2(D-22a) G-2p 4-CF3 2-CF3 H CH2(D-47a) G-2b 5-CF3 2-CI H N(CH3)(D-50a) G-2b 5-CF3 2-Br H CH2CF3 G-20 5-CF3 2-1 H CH2C(0)NHCH2CF3 G-20 5-CF3 2-CH3 H CH2(D-22a) G-20 5-CF3 2-Et H CH2(D^7a) G-20 5-CF3 2-CF3 H N(CH3)(D-50a) G-21 2-CF3 2-Cl H CH2CF3 G-21 2-CF3 2-Br H CH2C(0)NHCH2CF3 G-21 2-CF3 2-1 H CH2(D-22a) G-21 2-CF3 2-CH3 H CH2(D^7a) G-21 2-CF3 2-Et H N(CH3)(D-50a) G-21 2-CF3 2-CF3 H CH2CF3 G-22 2-Cl 2-Cl H CH2C(D)NHCH2CF3 G-22 2-Cl • 2-Br H CH2(D-22a) G-22 2-Cl 2-1 H CH2(D-47a) G-22 2-Cl 2-CH3 H N(CH3)(D-50a) G-22 2-Cl 2-Et H CH2CF3 G-22 2-Cl 2-CF3 H ^,eH2C(0)NHCH2CF3 Table 4 In the table, the number showing the substitution position of substituents (X)n,and (Y)n corresponds to the position number indicated in the following structural formulae. The indication "-" means no-substitution. R^ 0~N R^ /^^N ^ 5 (Y)„[3]-l "^ " , "^ 5 (Y)„ [3]-2 R^ P-N R^ P-N 1 5 (Y)„[3]-3 , "^ 5 (Y)„ [3]-4 R^ P-N R^ P^N ^ 5 (Y)„[3]-5 , "^ 5 (Y)„ [3]-6 R^ P-N R^ P^N ^^-^^5 Y ^ (Y)„[3]-7 OSO2F , ^^^-^ 5 T ^ (Y)„ [3]-8 OSO2CF3 j^3 O^N R^ P^N 'v5' V^cN '^ ' V"c-^« 4 . I 4 . I II 5 (Y)„ 5 (Y)^ O [3]-9 , 243 P^l^ ^—^ T Tt-4 I II 4 5 (Y)„ O" 5 00.0 [3]-11 . [31-12 . " 5 J)„ O " 5 (Y)„ O [3]-13 . Pl-14 [3]-15 . PJ-IO ^ 5 (Y)„ O ^ ^^)n ^ [3]-17 , [3]-18 p3 O^N R^ P~^N [3]-19 , ^^ [3]-20 R3 O-N R^ P^ N ^ 5 (y)„ •• 4 5 (Y)„ [3] - 21 , [3] - 22 R3 P-N R^ P^N (x)„2 V J[ (x),2 X n 4 . 4 . I II , 5 (Y)„ 5 (Y)„ O ^ [3]-23 , [3]-24 R3 P-N R^ P-N 4 c T II 4 ^ J. II 5 (Y)„ O 5 (Y)„ o [3]-25 , [3]-26 R3 O-N R^ P~N (Xk2 X A ^"yrK ^1 1 ^ (^>-^ X X . / ^ -^Ycx II ~"^ ^ \ } ^ V-A.^.OPr-n 'V__/.6 ^^ ^ OBu-t 4 c I 11 4 . I II 5 (Y)„ O 5 (Y)„ O [3] - 27 or [3] - 28 (XL R^ (Y)n (XL R' (Y)n 3-F CF3 CH3 3-CI-5-Br CF3 SCH3 3-CI CF3 CH3 3-CI-5-Br CF3 SCHFg 3-Br CF3 CH3 3-Cl-5-Br CF3 SCF3 3-1 CF3 CH3 3-CI-5-Br CF3 NO 2 3-CF3 CHF2 CH3 3-CI-5-Br CF3 N(CH3)2 3-CF3 CF3 F 3-CI-5-Br CF3 CN 3-CF3 CFa CI 3-CI-5-Br CF^CI F 3-CF3 CF3 Br 3-C!-5-Br CF2CI CI 3-CF3 CF3 I, 3-CI-5-Br CF2C! Br 3-CF3 CF3 CH3 3-CI-5-Br CFfi\ I 3-CF3 CF3 Et, 3-CI-5-Br CFgCi CH3 3-CF3 CF3 X-F3 3-CI-5-Br CF2CI Et 3-CF3 CF3 SCH3 3-CI-5-Br CF2CI; CF3 3-CF3 CF3 NO2 3-CI-5-Br CF2CI SCH3 '3-CF3 CF2CI CI 3-CI-5-Br CF2CI NO2 3-CF3 CF2CI Br 3-Cl-5-Br CFaBr CH3 3-CF3 CF2CI I 3-CI-5-Br CF2CHF2 CH3 3-CF3 CF2CI CH3 3-CI-5-Br CF2CF7 CH3 3-CF3 CF2CI Et 3,4-Br2 CF3 CH3 3-CF3 CF2CI CF3 3,5-Br2 CHF2 CH3 3-CF3 CF2Br CH3 3,5-Br2 CHFCI CH3 3-CF3 CF2CHF2 CH3 3,5-Br2 CHCI2 CH3 3-CF2CF3 CF3 F 3,5-Br2 CHFBr CH3 3-CF2CF3 CF3 CI 3,5-Br2 CF3 ¬ 3-CF2CF3 CF3 Br 3,5-Br2 CF3 F 3-CF2CF3 CF3 I 3,5-Br2 CF3 CI 3-CF2CF3 CF3 CH3 3,5-Br2 CF3 Br 3-CF2CF3 CF3 Et 3,5-Br2 CF3 I 3-CF2CF3 CF3 CF3 3,5-Br2 CF3 CH3 3-CF2CF3 CF3 SCH3 3,5-Br2 CF3 Et 3-CF2CF3 CF3 NO2 3,5-Br2 CF3 CF3 3-CF2CF3 CF2CI CI 3,5-Br2 CF3 OCH3 3-CF2CF3 CF2CI Br 3,5-Br2 CF3 OCHF2 3-CF2CF3 CF2CI I 3,5-Br2 CF3 OCF3 3-CF2CF3 CF2CI CH3 3,5-Br2 CFg OSO2CH3 3-CF2CF3 CF2CI Et 3,5-Br2 CF3 SCH3 3-CF2CF3 'CF2CI CF3 3,5-Br2 CF3 SCHF2 3-CF2CF2CF3 CF3 CH3 3,5-Br2 CF3 SCF3 3-CF(CF3)2 CF3 CH3 3,5-Br2 CF3 NO 2 3-CF2CF2CF2CF3 CF3 CH3 3,5-Br2 CF3 N(CH3)2 3-C(CF3)20H CF3 CH3 3,5TBr2 ^ CF3 CN 3-C(CF3)20CH3 CF3 CH3 3,5-Br2 CF2CI F 3-OCHF2 CF3 CH3 3,5-Br2. CF2CI CI 3-OCF3 CF3 CH3 3,5-Br2 ¬ CF2Ci Br 3-OCF2Br CF3 CH3 3,5-Br2 CF2CI I 3-OCF2CHF2 CF3 CH3 3,5-Br2 CF2Ci CH3 3-OCF2CHFCI CF3 CH3 3,5-Br2 CF2CI Et 3-OCF2CHFCF3 CF3 CH3 3,5-Br2 CF2CI CF3 3-OCF2CHFOCF3 CF3 CH3 3,5-Br2 CF2CI SCH3 3-SCHF2 CF3 CH3 3,5-Br2 CF2CI NO2 3-SO2CHF2 CF3 CH3 3,5-Br2 CFgBr CH3 3-SCF3 CF3 CH3 3,5-Br2 CF2CHF2 CH3 246 3-S(0)CF3 CF3 CH3 3,5-Br2 CF^CFa CH3 3-SO2CF3 CF3 CH3 3-CI-5-CH3 CF3 CH3 3-SCF2CI CF3 CH3 3-Br-5-CH3 CF3 CH3 3-S(0)CF2CI CF3 CH3 3-CF3^-F CF3 CH3 3-SO2CF2CI CF3 CH3 3-F-5-CF3 CHF2 CH3 3-SCF2Br CF3 GH-3 3-F-5-CF3 CF3 F 3-S02CF2Br CF3 CH3 3-F-5-CF3 CF3 , CI 3-SF5 CHF2 CH3 3-F-5-CF3 CF3 Br '3-SF5 CF3 F 3-F-5-CF3 CF3 I 3-SF5 CF3 CI 3-F-5-CF3 CF3 CH3 3-SF5 CF3 Br 3-F-5-CF3 CF3 Et 3-SF5 CF3 I 3-F-5-CF3 CF3 ¬ CF3 3-SF5 CF3 CH3 3-F-5-CF3 CF3 SCH3 3-SF5 CF3 Et 3-F-5-CF3 CF3 NO 2 3-SF5 CF3 CF3 3-F-5-CF3 CF2CI CI 3-SF5 CF3 SCH3 3-F-5-CF3 CF2CI Br 3-SF5 CF3 NO2 3-F-5-CF3 CF2CI I 3-SF5 CF2CI CI 3-F-5-CF3 CF2CI CH3 3-SF5 CF2CI Br 3-F-5-CF3 CF2CI Et 3-SF5 CF2CI I 3-F-5-CF3 CF2CI CF3 3-SF5 CF2CI CH3 3-F-5-CF3 CFgBr CH3 3-SF5 CF2CI Et 3-F-5-CF3 CF2CHF2 CH3 3-SF5 CF2CI CF3 S-CFg^CI CF3 CH3 3-SF5 CF2Br CH3 3-CI-5-CF3 CHF2 CH3 3-SF5 CF2CHF2 CH3 3-CI-5-CF3 CHCI2 CH3 3,5-F2 CF3 CH3 3-CI-5-CF3 CF3 ¬ 3-CM-F CF3 CH3 3-CI-5-CF3 CF3 F 3-F-5-CI CHF2 CH3 3-CI-5-CF3 OF 3 CI 3-F-5-CI CF3 F 3-CI-5-CF3 CF3 Br 3-F-5-CI CF3 CI 3-CI-5-CF3 CF3 I 3-F-5-CI CF'3 Br 3-CI-5-CF3 CF3 CH3 3-F-5-CI CF3 I 3-CI-5-CF3 CF3 Et 3-F-5-CI CF3 CH3 3-CI-5-CF3 CF3 CF3 3-F-5-CI CF3 Et 3-CI-5-CF3 CF3 OCH3 3-F-5-CI CF3 CF3 3-CI-5-CF3 -CF3 OCHF2 3-F-5-CI CF3 SCH3 3-CI-5-CF3 CF3 OCF3 3-F-5-CI CF3 NO 2 3-CI-5-CF3. CF3 OSO2CH3 3-F-5-CI CF2CI CI 3-CI-5-CF3 . CF3 SCH3 3-F-5-CI CF2CI Br S-Ci-S-CFg CF3 SCHF2 3-F-5-CI CFzCI I 3-CI-5-CF3 CF3 SCFg 3-F-5-CI CF2CI CH3 3-CI-5-CF3 CF3 NO2 3-F-5-Ci CF2CI Et 3-CI-5-CF3 CF3 N(CH3)2 3-F-5-CI CF2CI CF3 3-CI-5-CF3 CF3 CN 3-F-5-CI CFgBr CH3 3-CI-5-CF3 CFgCI CI 3-F-5-CI CF2CHF2 CH3 3-CI-5-CF3 CF2CI Br 3,4-Cl2 CF3 CH3 3-CI-5-CF3 CF2CI I 247 3,5-Cl2 CHF23,5-Cl2 CHF23,5-Cl2 CHF23,5-Cl2 CHF23,5-Ci2 CHF23,5-Cl2 CHF23,5-Cl2 CHFCI3,5-Cl2 CHFCi3,5-Cl2 CHFCI3,5-Cl2 CHFCI3,5-Cl2 CHFCI3,5-Cl2 CHFCI3,5-Cl2 CHFBr3,5-Cl2 CHFBr3,5-Cl2 CHFBr3,5-Cl2 CHFBr3,5-Cl2 CHFBr3,5-Cl2 CHFBr3,5-Cl2 CHCI23,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF3 3,5-Cl2 CF33,5-Cl2 CFg3,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-C!2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF3 CI 3-CI-5-CF3 Br 3-Ci-5-CF3 I ; 3-CI-5-CF3 CH3 3-CI-5-CF3 Et 3-CI-5-CF3 eF3^ 3-CI-5-CF3 CI 3-Br-5-CF3 Br 3-Br-5-CF3 i 3-Br-5-CF3 CH3 3-Br-5-CF3 Et 3-Br-5-CF3 CF3 3-Br-5-CF3 CI 3-Br-5-CF3 Br 3-Br-5-CF3 I 3-Br-5-CF3 CH3 3-Br-5-CF3 Et 3-Br-5-CF3 CF3 3-Br-5-CF3 CH3 3-Br-5-CF3 - 3-Br-5-CF3 F 3-Br-5-CF3 C! 3-Br-5-CF3 Br 3-Br-5-CF3 I 3-Br-5-CF3 CH3 3-Br-5-CF3 Et 3-Br-5-CF3 i-Pr 3~Br-5-CF3 CF3 3-Br-5-CF3 CF2CF3 3-Br-5-CF3 CH2OCH3 3-Br-5-CF3 CH2OCH2CF3 3-Br-5-CF3 CH2SCH3 3-Br-5-CF3 CHgSCOpHg 3-Br-5-CF3 CH2SO2CH3 3-Br-5-CF3 CH2SCF3 3-Br-5-CF3 CH2S(0)CF3 3-CH3-5-CF3 CH2SO2CF3 3,5-(CF3)2 OCH3 3,5-(CF3)2 OEt 3,5-(CF3)2 OPr-l 3,5-(CF3)2 OCHF2 3,5-(CF3)2 OCF3 3,5-(CF3)2 0CF2Br 3,5-(CF3)2 OCF2CHF2 3,5-(CF3)2 OCF2CHFCF3 SMCFJO OSO2CH3 3,5-(CF3)2 248 CF2CI CH3 CF2CI Et CF2CI CF3 CF,Br CH3 CF2CHF2 CH3 CF2CF3 CH3 CHF2 CH3 CHCI2 CH3 CF3 ¬ CF3 F CF3 CI CF3 --Br CF3 ^1 CF3 CH3 CF3 Et CF3 CF3 CF3 OCH3 CF3 OCHF2 CF3 OCF3 CF3 OSO2CH3 CF3 SCH3 CF3 SCHF2 CF3 SCF3 CF3 NOg CF3 N(CH3)2 CF3 CN CF2CI CI CF2CI Br CF2CI I CF2CI CH3 CFgCI Et CF2CI CF3 CFgBr CH3 CF2CHF2 CH3 CF2CF3 CH3 CF3 CH3 CHF2 CH3 CHFCI CH3 CHCI2 CH3 CHFBr CH3 CF3 ¬ CF3 F CF3 CI CF3 Br CF3 I CF3 CH3 3,5-Cl2 CF33,5-Cl2 CF33,5-C!2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF3 •3,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5lCl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF33,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-Cf2 CFgCI3,5-Cl2 CF2CI3,5-Cl2 CFgCI3,5-Cl2 CF2CI3,5-CI.2 CFgCI3,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-Cl2 CF2CI3,5-Cl2 CFgBr3,5-Cl2 CF2Br3,5-Cl2 CF2Br3,5-Cl2 CFgBr3,5-Ci2 CFgBr3,5-Cl2 CF2Br3,5-Ci2 CF2I3,5-Ci2 CFCI2 OSOaEt OSO2CF3 SCH3 ,S(b)CH3 SO2CH3 «Et SPr-i SCHF2 SCF3 S(0)CF3 SO2CF3 SCF2Br NO2 N(CH3)2 CN C(0)0CH3 C(0)NH2 T-21 C(S)NH2 T-22 ¬F CI Br I CH3 Et CF3 OCH3 OCHF2 OCF3 OSO2CH3 SCH3 SCHF2 SCF3 NO2 N(CH3)2 CN CI Br I CH3 Et CF3 CH3 CH33,5-Cl2 CFCIBr 3,5-(CF3)2 CF3 Et 3,5-(CF3)2 CF3 CF3 3,5-(CF3)2 CF3 OCH3 3,5-(CF3)2 CF3 OCHFg 3,5-(CF3)2 CF3 OCF3 3,5-(CF3)2 CF3 OSO2CH3 3,5-(CF3)2 CF3 SCH3 3,5-(CF3)2 CF3 SCHF2 3,5-(CF3)2 CF3 SCF3 3,5-(CF3)2 CF3 NO2 3,5-(CF3)2 CF3 N(CH3)2 3,5-(CF3)2 CF3 ¬ CN 3,5-(CF3)2 CF2CI ' F 3,5-(CF3)2 CF2CI CI 3,5-(CF3)2 CF2CI Br 3,5-(CF3)2 CF2CI I 3,5-(CF3)2 CF2CI CH3 3,5-(CF3)2 CF2CI Et 3,5-(CF3)2 CF2CI CF3 3,5-(CF3)2 CFgCl SCH3 3,5-(CF3)2 CF2CI NO2 3,5-(CF3)2 CFgBr CH3 3,5-(CF3)2 CF2CHF2 CH3 3,5-(CF3)2 CF2CF3 CH3 3-CI-5-CF2CF3 CF3 CH3 3-Br-5-CF2CF3 CF3 CH3 3-CH3-5-CF2CF3 CF3 CH3 3-CI-5-OCH3 CF3 CH3 3-Br-5-OCH3 CF3 CH3 3-CF3-5-OCH3 CF3 OH 3 3-CI-5-OCHF2 CF3 CH3 a-Br-S-OCHFg CF3 CH3 3-CF3-5-OCHF2 CF3 CH3 3-CI-5-OCF3 CF3 CH3 3-Br-5-OCF3 ¬ CF3 CH3 3-CF3-5-OCF3 CF3 CH3 3-CI-5-OCF2Br CF3 CH3 3-CI-5-OCF2CHF2 CF3 CH3 3-CF20CF20^ CF3 CH3 3-OCF20^ CF3 CH3 3-OCF2CF20^ CF3 CH3 3-CI-5-SCH3 CF3 CH3 3-CI-5-S(0)CH3 CF3 CH3 3-CI-5-SO2CH3 CF3 CH3 3-Br-5-SCH3 CF3 CH3 3-Br-5-S(0)CH3 CF3 CH3 249 3,5-Cl2 CFBfs 3,5-Cl2 CCI3 3,5-Cl2 CF2CHF23,5-CU CF2CHF23,5-Cl2 CF2CHF23,5-Cl2 CF2CHF2 3,5-Cl2 CF2CHF23,5-Cl2 CF2CHF23,5-CU CF2CF33,5-Cl2 CF2CF2CI3,5-Cl2 CFaCFgBr 3,5-Cl2 CF2CHFCF3 CH33,5-Cl2 CF2CF2CF3 CH3 CH3 CH3 CH3 Ci ^ Br i '¬ CH3 Et CF3 CH3 CH3 CH3 3,5-Cl2 T-33,5-Cl2 T-43,5-tef2 T-53-Br-4-F CF33-F-5-Br CHF23-F-5-Br CF33-F-5-Br CF33-F-5-Br CF33-F-5-Br CF33-F-5-Br CF33-F-5-Br CF33-F-5-Br CF33-F-5-Br CF33-F-5-Br CF33-F-5-Br CF2CI3-F-5-Br CF2CI3-F-5-Br CF^CI3-F-5-Br CF2CI3-F-5-Br CF2CI3-F-5-Br CF2CI 3-F-5-Br CFaBr3-F-5-Br CF2CHF23-CI-5-Br CHF23-CI-5-Br CHFCI3-CI-5-Br CHCI23-CI-5-Br CHFBr3-CI-5-Br CF33-Cl-5-Br CF33-CI-5-Br CF33-CI-5-Br CF33-CI-5-Br CF33-CI-5-Br CF3 CH3 CH3 CH3 CH3 CH3 F CI Br I CH3 Et CF3 SCH3 NO2 CI Br I CH3 Et CF3 CH3 CH3 CH3 CH3 CH3 CH3 ¬F CI Br I CH3 S-Br-S-SOsCHa CF3 CH3 3-CI-5-SCF3 CF3 CH3 3-C!-5-S(0)CF3 CF3 CH3 3-Ci-5-S02CF3 CF3 CH3 3-Br-5-SCF3 CF3 CH3 3-Br-5-S(0)CF3 CF3 CH3 3-Br-5-S02CF3 CF3 CH3 3-CI-5-NO2 CF3 CH3 3-CF3-5-NO2 CF3 CH3 3-CI-5-CN CF3 CH3 3-Br-5-CN CF3 CH3 3-CF3-5-CN CF3 - CH3 3,4,5-F3 CF3 ~ CH3 3,4,5-Cl3 CHF2 CH3 3,4,5-Cl3 CHFCI CH3 3,4,5-Cl3 CHCI2 CH3 3,4,5-Cl3 CHFBr CH3 3,4,5-Cl3 CF3 ¬ 3,4,5-Cl3 CF3 F 3,4,5-Cl3 CF3 CI 3,4,5-Cl3 CF3 Br 3,4,5-Cl3 CF3 I 3,4,5-Cl3 CF3 CH3 3,4,5-Cl3 CF3 Et 3,4,5-Cl3 CF3 CF3 3,4,5-Cl3 CF3 OCH3 3,4,5-Cl3 CF3 OCHF2 3,4,5-Cl3 CF3 OCF3 3,4,5-Cl3 CF3 OSO2CH3 3,4,5-Cl3 CF3 SCH3 3,4,5-Cl3 CF3 SCHF2 3,4,5-Cl3 CF3 SCF3 3,4,5-Cl3 CF3 NO2 3,4,5-Cl3 CF3 N(CH3)2 3,4,5-Cl3 CF3 CN 3,4,5-Cl3 CF2CI F 3,4,5-Cl3 CF2CI CI 3,4,5-Cl3 CF2CI Br 3,4,5-Cl3 CFgCI I 3,4,5-Cl3 CFaCi CM 3 3,4,5-C!3 CF2CI Et 3,4,5-Cl3 CFgC! CF3 3,4,5-Cl3 CF2CI SCH3 3,4,5-Cl3 CF2CI NOg 3,4,5-Cl3 CFgBr CM 3 3,4,5-Cl3 CFgCHFg CH3 250 Et CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-CI-5-Br CF3 3-Cl-5-Br CF3 3-CI-5-Br CF3 3,5-Cl24-F CF3 3,5-Cl2-^F CF3 3,5-Cl2-4-F ' CF3 3,5-Cl2-4-F CF3 3,5-Cl2^-F CF3 3,5-Cl2-4-F CF3 3,5-Cl2-4-F CF2CI S.S-Br^^-F CF3 3,5-Br2^-F CF3 3,5-Br2-t-F CF3 3,5iBr2-4-F CF3 3,5-Br2^-F CF3 3,5-Br2-4-F CF3 3,5-Br2^-F CF2CI 3,4,5-Br3 CF3 3,5-F2-4-CH3 CF3 3-CM-F-5-CF3 CF3 3-CW-F-5-CF3 CF2CI 3,5-Cl2^-CH3 CF3 3,5-Cl2^-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF3 3,5-Cl2-4-CH3 CF'aCI 3,5-Br2-4-CH3 CF3 3,5-Br2^-CH3 CF3 3,5-Br2^-CH3 CF3 Tables 0^3 ,0CHF2 OCF3 DSO^CHg CI Br I CH3 Et CF3 CH3 CI Br I CH3 Et CF3 CH3 CH3 CH3 CH3 CH3 CI Br I CH3 Et CF3 CH3 CI Br I 3,4,5-Cl3 CF2CF3 CH3 3,4-F2-5-CF3 CF3 CH3 3,5-Cl2^-OH CF3 CH3 3,5-Br2-4-OH CF3 CH3 3,5-Cl2^-NH2 CF3 CH3 3,5-Br2-4-NH2 CF3 CH3 3,5-Br2^-CH3 CF3 CH3 3,5-Br2^CH3 CF3 Et 3,5-Br2^-CH3 CF3 CF3 3,5-Br2^-CH3 CF^CI CH3 3,5-F2^-OCH3 CF3 ^ CH3 3,5-F2-4-OCF3 CF3 . CH3 3,5-Cl2^-OCH3 CF3 CI 3,5-Cl2^-OCH3 CF3 Br 3,5-Cl2-4-OCH3 CF3 I 3,5-Cl2-4-OCH3 CF3 CH3 3,5-Cl2-4-OCH3 CF3 Et 3,5-Cl2-4-OCH3 CF3 CF3 3,5-Cl2^-OCH3 CF2CI CH3 3,5-Cl2^-OEt CF3 CH3 3-F-5-Br-4-OCH3 CF3 CH3 3-CI-5-Br-4-OCH3 CF3 CH3 3,5-Br2-4-OCH3 CF3 CI 3,5-Br24-OCH3 CF3 Br 3,5-Br2^-OCH3 CF3 I 3,5-Br2-4-OCH3 CF3 CH3 3,5-Br2^-OCH3 CF3 Et 3,5-Br2-4-OCH3 CF3 CF3 3,5-Br2^0CH3 CF2CI CH3 3,5-Br2-4-OEt CF3 CH3 3,5-Cl2-4-N02 CF3 CH3 3,5-F24-CN CF3 CH3 3,5-Cl2-4-CN CF3 CH3 3,5-Br2^CN CF3 CH3 lit[4]-l & , I ^ i o [4]-2 «\ ^ R^ H^Y ^ R^ j CI O[4]-3 , Br O [4]-4 HO.J, HO V^C-'^^R'III O[4]-5 , S^C-"^R' I II CH3 O [4]-6 Et O[4]-7 , CF3 .0 [4]-8¬ H if ^ R' • H^Sj ^ R^ CH3O[4]-9 O , CHF2O O [4]-10 HO .NH^Y^ R^ HO, N H-V^ R^ ^ , , il CF3O O[4]-11 , I II CH3S O [4]-12 ^'iT ^ R' H^^^jj-^^N R^ IINO2 O[4]-13 , I II CI O [4]-14 Cl^''\r^^N R^ Cl'^'Nr'^N R^ IIBr O[4]-15 , I 11 CH3 O [4]-16 O [4] - 17 ci-\^ a O[4]-19 Cl-y^ I O[4]-21 ciy^^ Et O[4]-23 F O , [4] - 18 R^ ""^ iTl ^' Br O , [4]-20 R^ ^^^N^ ^' CH3 O ,. [4]-22 R^ *^' iT^ ^' CF3 O , [4]-24 254 HO.^ HO CH3O O CHF2O O [4]-25 , [4]-26 j CF3O O[4]-27 , CH3S O [4]-28 HO.N^^^iT ^ R^ HO. N CI^^^Tj^^N R^ NO2 O[4]-29 , CI O [4]-30 Cl'^'^Tr^^N R^ CI^^^TT^^N R^ ^f^ XI IIBr O[4]-31 R^ or ^ r C I II CH3 O [4]-32 R^ R2 R^ , R' R^ HEtHHH Et Et c-Pr i-Bu CHaPr-c CHaC^CH C(0)CH3 C(0)Et C(0)0CH3 H . CH2(D-17b)CI CH2(D-17b)CI CH2(D-17b)CI CH 2(0-17b)CI CH 2(0-18a) H c-Bu H c-Pen H CH2CH2CI : H CH2CF3 ¬ CH,0CH3 CH2CF3 CH2CN CH2CF3' ^ CH2C-CH CH2CF3 .C(0)CH3 CH2CF3 C(0)Et CH2CF3 C(0)Pr-c CH2CF3 C(0)Bu-t CH2CF3 C(0)0CH3 CH2CF3 CppCHaCHsOCHg CH2CF3C(0)OCH2CH=CH2 CH2CF3C(0)SCH3 CH2CF3C(S)0CH3 CH2CF3C(^)SCH3 CH2CF3H CH2CF2CF3H CH2CF2CF2CF3H CH2CH2OCH3H CH2CH20EtH CH2CH2OCH2CH2CIH CH(CH3)CH20CH3H CH(CH3)CH20C(0)NHEtH CH2CH(OCH3)2H CH2(E-4a)H CH2(E-5a)H CH2(E-10a)H CH2(E-10b)CH3H qH2(E-32a)H CH2CH2SO2CH3H CHgCHaSOgEtH C'H2CH(CH3)S02CH3H CH(CH3)CH2S02CH3H CH2C(0)CH3H CH2C(CH3)=N0CH3H CH2CNCH2CN CH2CNH CH2C(0)OCH3H CH2C(0)0EtH CH2C(0)OCH2CF3H CH(CH3)C(0)OCH3(R)H CH(CH3)C(0)OCH2CF3H CH2C(0)NH2H CH2C(0)NHCH3H CH2C(0)N(CH3)2 256 H CH2(D-19a) H CH2(D-20a) H CH2(D-21a) H CH2(D:21b)CF3 H CH2(D-22a) CH2OCH3 CH2(D-22a) CH2CN CH2(D-22a) CH2C=CH CH2(D-22a) C(0)CH3 . CH2(D-22a) C(0)Et CH2(D-22a) C(0)Pr-c CH2(D^2a) C(0)Bu-t CH2(D-22a) C(0)0CH3 CH2(D-22a) C(0)OCH2CH20CH3 CH2(D-22a) C(0)OCH2CH=CH2 CH2(D-22a) C(0)SCH3 CH2(D-22a) C(S)0CH3 CH2(D-22a) C(S)SCH3 CH2(D-22a) H CH(CH3)(D-22a) H CH2(D-28a) H CH2(D-29a) H CH2(D-29b)CH3 H CH2{D-30a) H CH2(D-34a) H CH2(D-34b)CH3 H CH2(D-35a) H CH2(D-36b)CH3 H CH2(D-37a) H CH2(D-38a) " H CH(CF3)(D-38a) C(0)0CH3 CH(CF3)(D-38a) H CH(CN)(D-38a) H CH2(D-47a) CH3 CH2(D^7a) Et ' CH2(D^7a) n-Pr CH2(D^7a) i-Pr CH2(D-47a) c-Pr CH2(D^7a) CH2CF3 CH2(D^7a) CH2OCH3 CH2(D-47a) CH20Et CH2(D-47a) CH2CN CH2(D-47a) CH2CH=CH2 CH2(D-47a) CH2C=CH CH2(D^7a) C(0)CH3 CH2(D^7a) C(0)Et CH2(D^7a) H CH,C(0)NHEt C(0)Pr-n CU^iDAla) H CH2C(0)NHPr-n C(0)Pr-i CH2(D-47a) H CH2C(0)NHPr.-i C(0)Pr-c CH^iD^Ja) H CH2C(0)NhlChl2CH2F C(0)Bu-t CHsCD^Ta) H CH2C(0)NHCH2CH2C1 C(0)CH20CH3 CH2(D^7a) H CH2C(0)NHCH-2CF3 C(0)CH=CH2 CH2(D^7a) H CH2C(0)NHCH2CH20CH3 C(0)0CH3 CH^iDAla) H CH2C(0)NHCH2CH=CH2 C{0)OEt CH^iDAJa) H CH2C(0)N(CH3)CH2CH=CH2 C(0)OPr-i , CH2(D^7a) H CH2C(0)N(CH2CH=CH2)2 C(0)OCH2CH20CH3 CH2(D^7a) H CH2C(0)NHCH2C=CH C(0)OCH2CH=CH2 CH2(D^7a) H CH2C(0)NHCH2Ph C(0)SCH3 CHJp^la) H CH2C(0)NH0Et C(S)0CH3 CH2(D-47a) H CH2C(0)NHPh C(S)SCH3 CH2(D^7a) H CH(CH3)C(0)NHCH2CH2C1 H CH2(D-47c)CI H CH(CH3)C(0)NHCH2CF3 H CH(CH3)(D^7a) H ; CH2CH=CH2 C(0)0CH3 CH(CH3)(D-47a) H CH2C(CI)=CH2 H CH(CN)(D^7a) H CH2C(CI)=CHCI H CH2(D^8e)CI H CH2C=CH Et CH2(D^8e)CI H CH2Ph H CH2(D-49a) H CH(CH3)Ph c-Pr CH2{D^9a) H CH(CH3)Ph(R) H CH2(D-50a) H CH(CF3)Ph C(0)CH3 CHgCD-SOa) H CH(CN)Ph C(0)Et CH2(D-50a) H CH2(Ph-4-F) C(0)0CH3 CH2(D-50a) H CH2(Ph-4-OCH3) H CH2(D-51a) H CH2(Ph^N02) C(0)CH3 CH2(D-51a) H CH2(Ph^CN) C(0)Et CH2(D-51a) H CH2(Ph-2,5-F2) C(0)0CH3 CH2(D-51a) H 0^2(0-1 a) H CH2(D-53a) H CH(CH3)(D-1a)(R) H CH2(D-53b)CH3 H CH(CN)(D-1a) H N(Ph)C(0)CH3 H CH2(D-3a) H .NHC(0)Pr-n H CH2(D-8b)CH3 H ^ NHC(0)Ph H CH2(D-11a) H N(CH3)C(0)Ph H CH(CF3)(D-14a) H NH(S(0)0CH3 H CH(CN)(D-14a) H N(C;H3)C(0)OCH3 H CH2(D-15a)CH3 H N(Ph)C(0)OCH 3 H CH2(D-16b)CI H NHC{0)OEt H CH2(D-16c)CI H N(CH3)C(0)0Et H CH2(D-17a)CH3 H D-8a CH2OCH3 CH2(D-17a)CH3 H (D-13b)CH3 CH2CN CH2(D-17a)CH3 H (D-15a)CH3 CHgC^CH CH2(D-17a)CH3 H D-21a C(0)CH3 CH2(D-17a)CH3 H D-35a 257 ^ C(0)Et CH2(D-17a)CH3 H D-47a C(0)0CH3 CH,(D-17a)CH3 H D^8a H CH 2(0-17b)Cl. H D-49a CH2OCH3 CH2(D-17b)Ci H D-50a, CH2CN CH 2(0-17b)CI H D-51a •Tables In the table, the number showing the substitution position of substituents {X^)^^ corresponds to the position number indicated in the following structural formulae. The indication "-" means no-substitution. X' X X II ^ 1 { 5 (X')„,i [5] - 1 X^ (X^L, . R^ X^ (X^L, R3 F - CF2CI Br 4-OCH3-5-Br CF2CI F 5-F CF2CI Br 4-OEt-5-Br CF3 F 4,5-F2 CF3 Br 4-NH2-5-Br CF3 F 4-CH3-5-F CF3 Br 4-CN-5-Br CF3 F 4-OCH3-5-F CF3 I - CFg F 4-OCF3-5-F CF3 I - CF2CI F 4-CN-5-F CF3 CF3 - CHF2 CI - CF2CI CF3 - CF2CI CI 4-F CF3 CF3 - CFgBr CI 5-F CHF2 CF3 - CF2CHF2 CI 5-F CF3 CF3 4-F CF3 CI 5-F CF2CI CF3 S-^F CHF2 CI 5-F CFgBr CF3 5-F CF3 CI 5-F CF2CHF2 CF3 5-F CF2CI CI 5-F CF2CF3 CF3 5-F CF2Br CI 4-CI CF3 CF3 5-F CF2CHF2 CI 5-CI CHF2 CF3 5-F CF2CF3 CI 5-Cl CHFCI CF3 4-CI CF3 CI 5-CI CHFBr CF3 5-CI CHF2 CI 5-Cl CHCI2 CF3 5-CI CHCI2 CI 5-Cl CF3 CF3 5-CI CF3 CI 5-CI CF2CI CF3 5-CI CF2CI CI 5-CI CFgBr CF3 5-CI CFsBr CI 5-CI CF2I CF3 5-Cl CF2CHF2 CI 5-Ci CFCI2 CF3 5-CI CF2CF3 CI 5-Cl CFCIBr CF3 5-Br CHF2 CI 5-Cl CFBr2 CF3 5-Br CHCI2 CI 5-Cl CGig, CF3 5-Br CF3 CI 5-Cl CF2CHF2 CF3 5-Br CF2CI CI 5-Cl CF2CF3 CF3 5-Br CFaBr .CI 5-Cl CF2CF2CI CF3 5-Br CF2CHF2 CI 5-Cl CF2CF2Br CF3 5-Br CF2CF3 CI 5-Cl CF2CHFCF3 CF3 5-CH3 CF3 CI 5-Cl CF2CF2CF3 CF3 5-CF3 _ CHF2 CI 5-Cl T-3 CF3 5-CF3 U CHFCI CI 5-Cl T-4 CF3 5-CF3 CHCI2 CI 5-Cl T-5 CF3 5-CF3 CHFBr CI 5-CH3 CF3 CF3 5-CF3 CF2CI CI 5-OCH3 CF3 CF3 5-CF3 CF2Br Cl'l 5-SCH3 CF3 CF3 5-CF3 CF2CHF2 CI 5-S(0)CH3 CF3 CF3 5-CF3 CF2CF3 a 5-SO2CH3 CF3 CF3 5-OCH3 CF3 CI 5-NO2 CF3 CF3 5-NO2 CF3 CI 5-CN CF3 CF3 5-CN CF3 CI 4-F-5-CI CF3 CF3 4,5-F2 CF3 CI 4-F-5-CI CF2CI CF2CF3 - CF3 CI 4,5-Cl2 CHF2 CF2CF3 - CF2CI CI 4,5-Cl2 CHFCI CF2CF3 5-Cl CF3 CI 4,5-Cl2 CHCI2 CF2CF3 5-Br CF3 CI 4,5-Cl2 CHFBr CF2CF3 5-CH3 CFg CI 4,5-Cl2 CF3. CF2CF2CF3 - CF3 CI 4,5-Cl2 CF2CI CF2CF2CF3 5-Cl CF-3 CI 4,5-Cl2^ CF2Br CFgCFgCFg 5-Br CF3 CI 4,5-Cl2' CF2CHF2 CF2CF2CF3 5-CH3 CF3 CI 4,5-Cl2 CF2CF3 CF{CF3)2 - CF3 CI 4-F-5-CF3 CF3 CF(CF3)2 5-Cl CF3 CI 4-F-5-CF3 CF2CI CF(CF3)2 5-Br CF3 CI 4-CH3-5-CI CF3 CF(CF3)2 5-CH3 CF3 a 4-GH3-5-CI CF2CI C(CF3)20H - CF3 CI 4-OH-5-CI CF3 C(CF3)20H 5-Cl CF3 CI 4-OCH3-5-CI CF3 C(CF3)20H 5-Br CF3 CI 4-OCH3-5-CI CF2CI C(CF3)20H 5-CH3 CF3 CI 4-OEt-5-CI CF3 C(CF3)20CH3 - CF3 CI 4-NO2-5-CI CF3 C(CF3)20CH3 5-Cl CF3 CI 4-NH2-5-CI CF3 C(CF3)20CH3 5-Br CF3 CI 4-CN-5-CI CF3 C(CF3)20CH3 5-CH3 CF3 Br - CF3 -CFgOCFaO^ CF3 Br - CF2CI OCHF2 - CF3 Br 4-F CF3 OCHF2 5-Cl CF3 Br 5-F CHF2 OCHF2 5-Br CF3 Br 5-F CF3 OCHF2 5-CF3 CF3 Br 5-F CF2QI OCF3 - CF3 Br 5-F CFaBr OCF3 5-CI CF3 Br 5-F CF2CHF2 OCF3 5-Br CF3 Br 5-F CF2CF3 OCF3 5-CF3 CF3 Br 5-CI CHF2 OCFaBr - CF3 Br • 5-CI CHFCI 0CF2Br 5-CI CF3 Br 5-CI CHCI2 OCF2CHF2 - OF 3 Br 5-CI CHFBr OCF2CHF2 5-CI CF3 Br 5-CI CF3 OCF2CHFCI ~ OF 3 Br 5-CI CF2CI OCF2CHFCI 5-CI " : CF3 Br 5-Cl CFaBr OCFgCHFCI 5-Br CF3 Br 5-CI CF2CHF2 OCF2CHFCF3 - CF3 Br 5-CI CF2CF3 OCF2CHFCF3 5-Ci CF3 Br 4-Br CF3 OCF2CHFOCF3 - CF3 Br j 5-Br CHF^ OCF2CHFOCF3 5-CI CFg Br 5-Br CHFCI -OCF2O-4 CF3 Br 5-Br CHCI2 -OCFaCFgO^ CF3 Br 5-Br CHFBr SCHF2 - CF3 Br 5-Br CF3 SO2CHF2 - CFg Br 5-Br CFgCI SCF3 - CF3 Br 5-Br CF2Br SCF3 5-CI CF3 Br 5-Br CF2CHF2 SCF3 5-Br CF3 Br 5-Br CF2CF3 S(0)CF3 - CF3 Br 5-CH3 CF3 S(0)CF3 5-CI CF3 Br 5-OCH3 CF3 S(0)CF3 5-Br CF3 Br 5-SCH3 CF3 SO2CF3 - CF3 Br 5-S(0)CH3 CF3 SO2CF3 5-C! CF3 Br 5-SO2CH3 CF3 SO2CF3 5-Br CF3 Br 5-CN " CF3 SCF2CI - CF3 Br 4-F-5-Br CF3 S(0)CF2CI - CF3 Br 4-F-5-Br CFgCI SO2CF2CI - CF3 Br 4,5-Br2 CF3 SCF2Br - CF3 Br 4-CH3-5-Br CF3 SOgCFaBr - CF3 Br 4-CH3-5-Br CFgCI SF5 - CHF2 Br 4-OH-5-Br CF3 SF5 - CF3 Br 4-OCH3-5-F CF3 SF5 . - CF2CI Br 4-OCH3-5-CI CF3 SF5 ~ CF2Br Br 4-OCH3-5-Br CFg SF5 ~ CFgCHFg [0154] The compounds of the present invention can effectively control in a low concentration so-called agricultural insects injuring agricultural and horticultural crops and trees, so-called domestic animal pests parasitizing domestic animals and domestic fowls, so-called hygienic pests having an adverse affect on human being's environment such as houses, insects as so-called stored grain insects injuring grains and the like stored in storehouses, and any pests of acarids, crustaceans, mollusks and nematodes generating inJhe similar scenes. [0155] The insects, acarids, crustaceans, mollusks and nematodes that the . compounds of the present invention can control concretely include for example the follov\/ings: Lepidoptera insects, such as Adoxophyes honmai, Adoxophyes orana faciata, Archips breviplicanus, Archips fuscocupreanus, Grapholita molesta, Homona magnanima, Leguminivora glycinivorella, Matsumuraeses phaseoli, Pandemis heparana, Bucculatrix pyrivorella, Lyonetia clerkella, Lyonetia prunifoliella malinella, Caloptilia theivora, Phyllonorycter ringoniella, Phyllocnistis citrella, Acrolepiopsis sapporensis, Acrolepiopsis suzukiella, Plutella xylostella, Stathmopoda masinissa, Helcystogramma triannulella, Pectinophora gossypiella, Carposina sasakii, Cydla pomonella, Chilo suppressalis, Cnaphaiocrocis medinalis, Conogethes punctiferalis, Diaphania indica, Etiella zinckenella, Glyphodes pyloalis, Hellula undalis, Ostrinia furnacalis, Ostrinia scapulalis, Ostrinia nubilalis, Parapediasia teterrella, Parnara guttata, Pieris brassicae, Pieris rapae crucivora, Ascotis selenaria, Pseudoplusia includens, Euproctis pseudoconspersa, Lymantria dispar, Orgyia thyellina, Hyphantria cunea, Lemyra imparilis, Adris tyrannus, Aedia leucomelas, Agrotis ipsilon, Agrotis segetum, Autographa nigrisigna, Ctenoplusia agnata, Helicoverpa armigera, Helicoverpa assulta, Helicoverpa zea, Heliothis virescens, Mamestra brassicae, Mythimnh separata, Naranga aenescens, Spodoptera eridania, Spodoptera exigua,. Spodoptera frugiperda, Spodoptera littoralis, Spo.doptera litura, Spodoptera depravata, Trichoplusia ni, Endopiza viteana, Manduca quinquemaculata, Manduca sexta, or the like; Thysanoptera insects, such as Frankliniella intonsa, Frankliniella occidentalis, Heliothrips haemorrhoidalis, Scirtothrips dorsalis, Thrips palmi, Thrips tabaci, Ponticulothrips diospyrosi, or the like; Hemiptera insects, such as Dolycoris baccarum, Eurydema rugosum, Eysarcoris aeneus, Eysarcoris lewisi, Eysarcoris ventralis, Glaucias subpunctatus, Halyomorpha halys, Nezara antennata, Nezara viridula, Piezodorus hybneri, Plautia crossota, Scotinophora lurida, Cletus punctiger, Leptocorisa chinensis, Riptortus clavatus, Rhopalus msculatus, Cavelerius saccharivorus, Togo hemipterus, Dysdercus cingulatus, Stephanitis pyrioides, Halticus insularis, Lygus lineolaris, Stenodema sibiricum, Stenotus rubrovittatus, Trigonotylus caelestialium, Arboridia apicalis, Balclutha saltuella, Epiacanthus stramineus, Empoasca fabae, Empoasca nipponica, Empoasca onukii, Empoasca sakaii, Macrosteles striifrons, Nephotettix cinctinceps, Psuedatomosceiis seriatus, Laodefphax striatella, Nilaparvata lugens, Sogatella furcifera, Diaphorina citri, Psylla pyrisuga, Aleurocanthus spiniferus, Bemisia argentifolii, Bemisia tabaci, Dialeurodes citri, Trialeurodes vaporariorum, Viteus vitifolii, Aphis gossypii, Aphis spiraecola, Myzus persicae, Toxoptera aurantii, Drosicha corpulenta, Icerya purchasi, Phenacoccus solan'i, Planococcus citri, Pianococcus kuraunhiae, Pseudococcus comstocki, Ceroplastes ceriferus, Ceroplastes rubens, Aonidiella aurantii, Comstockaspis perniciosa, Fiorinia theae, Pseudaonidia paeoniae, Pseudaulacaspis pentagona, Pseudaulacaspis prunicola, Unaspis euonymi, Unaspis yanonensis, Cimex lectularius, or the like; Coleoptera insects, such as Anomala cuprea, Anomala rufocuprea, Gametis jucunda, Heptophylla picea, Popillia japonica, Lepinotarsa decemlineata, Melanotus fortnumi, Melanotus tamsuyensis, Lasioderma serricorne, Epuraea domina, Epilachna varivestis, Epilachna vigintioctopunctata, Tenebrio molitor, Tribolium castaneum, Anoplophora malasiaca, Monochamus alternatus, Psacothea hilaris, Xylotrechus pyrrhoderus, Callosobruchus chinensis, Aulacophora femoralis, Chaetocnema concinna, Diabrotica undecimpunctata, Diabrotica virgifera, Diabrotica barberi, Oulema oryzae, Phyllotreta striolata, Psylliodes angusticollis, Rhynchites heros, Cylas formicarius, Anthonomus grandis, Echinocnemus squameus, Euscepes postfasciatus, Hypera postica, Lissohoptrus oryzophilus, Otiorhynchus sulcatus, Sitophilus granarius',* Sitophilus zeamais, Sphenophorus venatus vestitus, Paederus fuscipes, or the like; Diptera insects, such as Asphondylia yushimai, Sitodiplosis mosellana, Bactrocera cucurbitae, Bactrocera dorsalis, Ceratitis capitata, Hydrellia gfiseoJa, Drosophila suzukii, Agromyza oryzae, Chromatomyia horticola, Liriomyza bryoniae, Liriomyza chinensis, Liriomyza sativae, Liriomyza trifolii, Delia platura, Pegomya cunicularia, Rhagoletis pomonetia, Mayetiola destructor, Musca domestica, Stomoxys calcitrans, Melophagus ovinus, Hypoderma bovis, Hypoderma lineatum, Oestrus ovis, Glossina paipalis, Giossina morsitans, Prosimuiium yezoensis, Tabanus trigonus, Telmatoscopus albipunctatus, Leptoconops nipponensis, Cuiex pipiens pallens, Aedes aegypti, Aedes albopicutus, Anopheles hyracanus sinesis, or the like; Hymenoptera insects, such as Apethymus kuri, Athalia rosae, Arge pagana, Neodiprion sertifer, Dryocosmus kuriphilus, Eciton burchelli, Eciton schmitti, Camponotus japonicus, Vespa mandarina, Myrmecia spp., Solenopsis spp., Monomorium pharaonis, or the iike; Orthoptera insects, such as Teleogryllus emma, Gryllotalpa orientalis, Locusta migratoria, Oxya yezoensis, Schistocerca gregaria, or the like; Collembola insects, such as Onychiurus folsomi, Onychiurus sibiricus, Bourletiella .hortensis, or the like; Dictyoptera insect, such as Periplaneta fuliginosa, Periplaneta japonica, Blattella germanica, or the like; Isoptera insects, such as Coptotermes formosanus, Reticulitermes speratus, Odontotermes formosanus, or the like; Siphonaptera insects, such as Ctenocephalidae felis, Ctenocephalides canis, Echidnophaga gallinacea, Pulex irritans, Xenopsylla cheopis, or the like; Mallophaga insects, such as Menacanthus stramineus, Bovicola bovis, or the like; Anoplura insects, such as Haematopinus eurysternus, Haematopinus suis, Linognathus vituli, Solenopotes capillatus, or the like; Tarsonemid mites, such as Phytonemus pallidus, Polyphagotarsonemus latus, Tarsonemus bilobatus, or the like; Eupodid mites, such as Penthaleus erythrocephalus, Penthaleus major, or the like; Spider mites, such as Oligonychus shinkajii, Panonychus citri, Panonychus mori, Panonychus ulmi, Tetranychus kanzawai, Tetranychus urticae, or the like; Eriophyid mites, such as Acaphylla theavagrans, Aceria tulipae, Aculops lycopersici, Aculops pelekassi, Aculus schlechtendali, Eriophyes chibaensis, Phyllocoptruta oleivora, or the like'; Acarid mites, such as Rhizoglyphus robini, Tyrophagus putrescentiae, Tyrophagus similis, or the like; Bee brood mites, such as Varroa jacobsoni, or thelike; Ixodides, such as Boophilus microplus, Rhipicephalus sanguineus, Haemaphysalis longicornis, Haemophysalisflava, Haemophysalis campanulata, Ixodes ovatus, Ixodes persulcatus, Amblyomma spp., Dermacentor spp., or the like; Cheyletidae, such as Cheyletiella yasguri, Cheyletiella blakei, or the like; Demodicidae, such as Demodex canis, Demodex cati, or the like; Psoroptidae, such as Psoroptes ovis, or the like; Scarcoptidae, such as Sarcoptes scabiei, Notoedres cati, Knemidocoptes spp., or the like; Crustacea, such as Armadillidium vulgare, or the like; Gastropoda, such as Pomacea canaiicuiata, Achatina fulica, Meghimatium bilineatum, Umax Valentiana, Acusta despecta sieboldiana, Euhadra peliomphaia, or the like; , ' Nematodes, such as Prathylenchus coffeae, Prathylenchus penetrans, Prathylenchus vulnus, Globodera rostochiensis, Heterodera glycines, Meloidogyne .hapla, Meloidogyne incognita, Aphelenchoides besseyi, Bursaphetenchus xylophilus, or the like. But the present invention is not limited.thereto. [0156] The endo-parasites of domestic animals, domestic fowls, pets and the like that the compounds of the present invention can control concretely inclDde for example the followings: Nematodes, such as Haemonchus, Trichostrongylus, Ostertagia, Nematodirus, Cooperia, Ascaris, Bunostomum, Oesophagostomum, Chabertia, Trichuris, Storongyius, Trichonema, Dictyocaulus, Capillaria, Heterakis, Toxocara, Ascaridia, Oxyuris, Ancytostoma, Uncinaria, Toxascaris, Parascaris, or the (ike; Filariidae in nematodes, such as Wuchereria, Brugia, Onchoceca, Dirofilaria, Loa, or the like; Dracunculidae in nematodes, such as Deacunculus, or the like; Cestoda, such as Dipylidium caninum. Taenia taeniaeformis. Taenia solium. Taenia saginata, Hymenolepis diminuta, Moniezia benedeni, Diphyllobothrium latum, Diphyllobothrium erinacei, Echinococcus granulosus, Echinococcus multilocularis, or the like; Trematoda, such as Fasciola hepatica,F.gigantica, Paragonimus westermanii,' Fasciolopsic bruski,*Eurytrema pancreaticum,E.coelomaticum, Clonorchis sinensis, Schistosoma japonicum, Schistosoma haematobium. Schistosoma mansoni, or the like; Eimeria spp., such as Eimeria tenella, Eimeria acervulina, Eimeria brunetti, Eimeria maxima, Eimeria necatrix, Eimeria bovis, Eimeria ovinoidalis, or the like; Trypanosomsa cruzi, Leishmania spp., Plasmodium spp., Babesis spp., Trichomonadidae spp., Histomanas spp., Giardia spp., toxoplasma spp.. Entamoeba histolytica, Theileria spp., or the like. But the present invention is not limited thereto. [0157] Further, the compounds of the present invention are effective for pests acquiring high resistance against existing insecticides such as organic phosphorus compounds, carbamate compounds or pyrethroid compounds, etc. [0158] That is, the compounds of the present invention can effectively control pests that belong to insects such as Collembola, Dictyoptera, Orthoptera, Isoptera, Thysanoptera, Hemiptera, Lepidgptera, Coleoptera, Hymenoptera, Diptera, Isoptera and Anoplura, Acarina, Gastropoda and Nematoda, in a low concentration. On the other hand, the compounds of the present invention have an extremely useful charactristic that they have little adverse affect on mammals, fishes, crustaceans and useful insects (beneficial insect such as honeybee, bumblebee or the like, or, natural enemies such as Aphytis lingnanensis, Aphidius colemani, Orius strigicollis, Amblyseius californicus, or the like). [0159] When the compounds of the present invention are used, they^can be generally mixed with a suitable solid carrier or liquid carrier, optionally along with surfactant, penetrating agent, spreading agent, thickner, anti-freezing agent, binder, antircaking agent, disintegrating agent, anti-foaming agent, preservative, stabilizer, and the like, and can be formulated into any desired forms for practical use, such as soluble concentrates, emulsifiable concentrates, wettable powders, water soluble powders, water dispersible granules, water soluble granules, suspension concentrates, concentrated emulsions, suspoemulsions, microemulsions, dustable powders, granules, tablets and emulsifiable gels. From the viewpoint of an elimination or reduction of labor and an improvement of safety, the formulations in any desired forms described above may be included into a water-soluble bag made of water-soluble capsule or water-soluble film. [0160] The solid carrier includes, for example, natural minerals such as quartz, calcite, sepiolite, dolomaite, chalk, kaolinite, pyrofilite, celicite, halocite, methahalocite, kibu§hi clay, gairome clay, pottery stone, zeaklite, allophane, white sand, mica, talc, beritonite, activeted earth, acid china clay, pumice, attapulgite, zeolite and diatomaceous earth, etc., calcined products of natural minerals such as calcined clay, pedite, white sand balloon (loam balloon), vermiculite, attapulgus clay and calcined diatomaceous earth, etc., inorganic salts such as magnesium carbonate, calcium carbonate, sodiuni carbonate, sodium hydrogen carbonate, ammonium sulfate, sodium sulfate, magnesium sulfate, diammonium hydrogen phosphate, ammonium dihydrogen phosphate and potassium chloride, etc., saccharides such as glucose, fructose, sucrose and lactose, etc., polysaccharides such as starch, powder cellulose and dextrin, etc., organic materials such as urea, urea derivatives, benzoic acid and a salt of benzoic acid, etc., plants such as wood powder, cork powder, corn head stem, walnut shell and tobacco stem, etc., fly ash, white carbon (e.g., hydrated synthetic silica, anhydrous synthetic silica and hydrated synthetic silicate, etc.) and feritilizers, etc. [0161] As the liquid carrier, there may be mentioned, for example, aromatic hydrocarbons such as xylene, alkyKCg or C^o, etc.)benzene, phenyixylylethane and alkyl(Ci or C3, etc.)naphthalene, etc., aliphatic hydrocarbons such as machine oil, normal paraffin, isoparaffin and naphthene, etc., a mixture of aromatic hydrocarbons and aliphatic hydrocarbons such as kerosene, etc., alcohols such as ethanol, isopropanol, cyciohexanol, phenoxyethanol and benzylalcohol, etc., polyvalent alcohols such as ethylene glycol, propyleneglycol, diethylene glycol, hexylene glycol, polyethylene glycol and polypropyieneglycol, etc., ethers such as propyl cellosoive, ¬butyl cellosoive, phenyl cellosoive, propyleneglycol monomethyl ether, propyleneglycol monoethyl ether, propyleneglycol monopropyl ether, propyleneglycol monobutyl ether and propyleneglycol monophenyl ether, etc., ketones such as acetophenone, cyciohexanone and y-butyrolactone, etc., esters such as aliphatic acid methyl ester, dialkyi succinate, dialkyi glutamate, dialkyi adipate and dialkyi phthalate, etc., acid amides such as N-alkyl(Ci, Cg or C12, etc.)pyrrolidone, etc., oil and fats such as soybean oil, linseed oil, rapeseed oil, coconut oil, cottonseed oil and caster oil, etc., dimethylsulfoxide and water. [0162] These solid and liquid carriers may be used alone or in combination of two or more kinds in combination. [0163] As the surfactant, there may be mentioned, for example, nonionic surfactants such as polyoxyethylene alkyl ether, polyoxyethylene alkyl (mono- or di-)phenyl ether, polyoxyethylene (mono-, di- or tri-)styrylphenyl ether, polyoxyethylene polyoxypropylene block copolymer, polyoxyethylene fatty acid (mono- or di-)ester,.sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, caster oil-ethylene oxide adducts, acetylene glycol, acetylene alcohol, ethylene oxide adducts of acetylene glycol, ethylene oxide adducts of.acetylene alcohol and alkyl glycoside, etc., anionic surfactants such as alkyl sulfate, alkylbenzenesulfonate, lignine sulfonate, alkylsulfosuccinate, naphthalene sulfonate, alkyinaphthalene sulfonate, formalin condensate salt of naphthalene sulfonic acid, formalin condensate salt of alkyinaphthalene sulfonic acid, polyoxyethylene alkyl ether sulfate or phosphate, polyoxyethylene (mono- or di-)alkylphenyl ether sulfate or phosphate, polyoxyethylene (mono-, di- or tri-)styrylphenyl ether sulfate or phosphate, polycarboxylate (e.g., polyacryaltes, polymaleates and copolymer materials of maleic acid and olefin, etc.) and polystyrenesulfonate, etc., cationic surfactants such as alkylamine salt and alkyl quaternary ammonium salt, etc., amphoteric surfactants such as amino acid type and betaine type, etc., silicone type surfactants and fluorine type surfactants. [0164] A content of these qurfactants is not specifically limited, and it is desirably in the range of 0.05 to 20 partsi)y weight in general based on 100 parts by weight of the preparation according to the present invention. Also, these surfactants may be used alone or in combination of two or more kinds in combination. [0165] A dose of the compound of the present invention to be applied may vary depending on the place to be applied, time to be applied, method to be applied, crops to cultivate, etc., and in general, it is suitable in an amount of about 0.005 to 50 ¬kg or so per a hectare (ha) as an amount of the effective ingredient. [0166] On the other hand, when the compound of the present invention is used for controlling ecto- or endo-parasites of mammals and birds as domestic animals and fDets, the effective amount of the compound of the present invention together with additives for formulations can be administered through oral administration, parenteral administration such as injection (intramuscular, subcutaneous, intravenous, intraperitoneal) or the like; transdermal administration such as dipping, spray, bathing, washing, pouring-on and spotting-on, and dusting, or the like ; transnasal administration. The compound of the present invention can be also administered through a formed product by use of a strip, a plate, a band, a collar, an ear mark, a limb band, a labe apparatus, or the like. In administration, the compound of the present invention can be formed in an arbitrary dosage form that is suited for the administration route. [0167] The arbitrary dosage form includes solid preparations such as a dustable powder, a granule, vyettable powder, a pellete, a tablet, a bolus, a capsule, a formed product containing an active compound; liquid formulations such as an injectable liquid formulation, an oral liquid formulation, a liquid formulation used on skin or in body cavity; solution preparations such as a pour-on agent, a spot-on agent, a flowable agent, an emulsifiable concentrate; semi-solid preparations such as an ointment, gel or the like. The solid preparations can be mainly used through oral administration or transdermal administratin by diluting with water or the like, or by environmental treatment. The solid preparations can be prepared by mixing the active compound with suitable excipients and optionally auxiliary substances and converting to a desired form. The suitable excipients include for example inorganic substances such as carbonates, hydrogen carbonates, phosphates, aluminum oxide, silica, clay or the like, organic substances such as sugar, cellulose, milled cereal, starch or the like. [0168] The injectable liquid formulation can be adntinistered intravenously, intramuscularly and subcutaneously. The injectable liquid formulation can be prepared by dissolving an acitve compound in a suitable solvent and optionally by .adding an additive such as a solubilizing agent, an acid, a base, a buffering salt, an antioxidant, and a protective agent or the like. Suitable solvent is for example water, ethanol, butanol, benzyl alcohol, glycerin, propylene glycol, poethylene glycol, N-methylpyrrolidone, and a mixture thereof, a physiologically permissible vegetable ¬oil, a synthetic oil suitable for injection, or the like. The solubilizing agent includes polyvinyl pyrroiidone, polyoxyethylated castor oil and polyoxyethylated sorbitan ester, or the like. The protective agent includes benzyl alcohol, trichlorobutanol, p¬hydroxybenzoic acid ester and n-butanol or the like. [0169] The oral liquid formulation can be administered directly or after dilution. It can be prepared similarly to the injectable liquid formulation. [0170] The flowable agent and the emulsifiable concentrate can be administered directly or after dilution through transdermal administration or environmental treatment. [0171] The liquid formulation used on skin can be administered by pouring on, spreading, rubbing, atomizing, spraying, or dipping (dipping, bathing or washing). These liquid can be prepared similarly to the injectable liquid formulation. [0172] The pour-on agent and the spot-on agent are poured or atomized on the limited spot on thefekin, thereby the active compound can be penetrated into the skin and act in the whole body. The pour-on agent and the spot-on agent can be prepared by dissolving, suspending or emulsifying an active ingredient in a suitable skin-fitted solvent o,r solvent mixture. If required, an auxiliary substance such as a surfactant, a colorant, an absorption promoting agent, an antioxidant, a light stabilizer and an adhesive, etc. may be added. [0173] Suitable solvent includes water, alkanol, glycol, polyethylene glycol, polypropylene glycol, glycerin, benzyl alcohol, phenylethanol, phenoxyethanol, ethyl acetate, butyl acetate, benzyl benzoate, dipropylene glycol monomethyl ether, diethylene glycol monobutyl ether, acetone, methyl ethyl ketone, aromatic and/or aliphatic hydrocarbon, vegetable or synthetic oil, DMF, liquid paraffin, light-duty liquid ^ paraffin, silicone, dimethylacetamide, N-methylpyrrolidone or2,2-dimethyl-4-oxy¬methylene-1,3-d!oxolane. The absorption promoting agent includes DMSO, isopropyl myristate, dipropyiene glycol pelargonate, silicone oil, aliphatic ester, triglyceride and fatty alcohol. The antioxidant includes sulfite, metabisulfite, ascorbic acid, butylhydroxytoluene, butylhydroxyanisole and tocopherol. [0174] The emusifiable concentrate can be administrated orally, subcutaneously or injectably. The emusifiable concentrate can be prepared by dissolving an active ingredient in a hydrophobic phase or a hydrophilic phase, and then homogenating the resulting solution with a suitable emulsifying agent optionally with further an auxiliary substance such as a colorant, an absortion promoting agent, a protective agent, an antioxidant, a light screen and a thickening agent. [0175] The hydrophobic phase (oil) includes paraffin oil, silicone oil, sesame-seed oil, oil of almonds, castor oil, synthetic triglyceride, ethyl stearate, di-n-butyryl adipate, hexyl laurate, dipropyiene glycol pelargonate, ester of branched short chain length aliphatic acid with saturated aliphatic acid of chain length C16 to C18, isopropyl myristate, isopropyl palmitate, capryl/caprylic acid ester of saturated fatty alcohol of chain length CI2 to CI 8, isopropyl stearate, oleyl oleate, decyl oleate, ethyl oleate, ethyl lactate, wax-like fatty acid ester, dibutyl phthalate, diisopropyl adipate, isotridecyl alcohol, 2-octyldodecanol, cetylstearyl alcohol, oleyl alcohol. [0176] The hydrophilic phase includes water, propylene glycol, glycerin, sorbitol. [0177] The emulsifying agent includes non-ionic surfactants such as polyoxyethylated castor oil, polyoxyethylated sorbitan mono-olefinate, sorbitan monostearate, glycerin monostearate, polyoxyethyl stearate, alkylphenol polyglycol ether; amphoteric surfactants such as di-sodium N-lauryl p-iminodipropionate,' lecithin or the like; ahionic surfactants such as sodium lauryl sulfate, fatty alcohol sulfric acid ether, monoethanol amine salt of mono/dialkylpolyglycol orthophosphate or the like; cationic surfactants such as cetyi chloride trimethylammonium or the like. [0178] The other auxiliary substance includes carbocymeth'yicellulose, methylcellulose, polyacrylate, arginate, gelatin, gum arable, polyvinyl pyrrolidone, polyvinyl aocohol, methylvinyl ether, copolymer of maleic anhydride, polyethylene glycol, wax, colloidal silica. [0179] The semi-solid preparation can be administered by coating or spreading on the skin, or by introducing in body cavity. The gel can be prepared by adding a thickener in an amount enough to provide a clear substance having a viscosity of ointment in a solution prepared for the injectable liquid formulation as mentioned above. [0180] Next, formulation examples of the preparation in case where the compound of the present invention is used are shown below. Provided that formulation examples of the present invention are not limited only thereto. In the interim, in the following Formulation Examples, "part(s)" mean part(s) by weight. (Wettable powder) Compound of the present invention 0.1 to 80 parts ,Solid carrier 5 to 98.9 parts Surfactant 1 to 10 parts Others 0 to 5 parts As other components, there may be mentioned, for example, a non-ca1(ample 3 in 50 mi of 1,2-dichioroethane, 0.68 g of N-bromosuccinic acid imide and a catalytic amount of azobisisobutyronitrile were added, and stirred under nitrogen atmosphere and under reflux with heat for 1 hour. After the completion of the reaction, the reaction mixture was left and cooled to room temperature, poured in 50 ml of water, extracted with chloroform (50 ml x 1). The organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure to obtain crude aimed product as pale yellow oily substance. The ¬resulting product was used as such without purification for the next step. 'H NMR (CDCI3, Me4Si, 4G0MHz) 5 7.45-7.6 (m, 6H), 4.51 (s, 2H), 4.05 (d, J=17.2Hz, 1H), 3.67 (d, J=17.2Hz, 1H). Step 2: Production of 3-(4-acetoxymethyl-3-fluorophenyl)-5-(3,5-dichlorophenyl)¬5-trifluoromethyl-4,5-dihydroisoxazole [0192] In a solution of crude 3-(4-bromomethyl-3-fluorophenyl)-5-(3,5¬dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazole in 30 ml of acetic acid, 1.50 g of potassium acetate was added, and stirred under reflux with heat for 1.5 hour. After the completion of the reaction, the reaction mixture was left and cooled to room temperature, and neutralized by pouring in 100 ml of saturated sodium hydrogen carbonate aqueous solution. The organic phase was collected, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure to obtain-1.50 g of crude aimed product as pale yellow oily substance. The resulting product was used as such without purification for the next step. ^H NMR (CDCI3, Me^Si, 400MHz) 6 7.2-7.55 (m, 6H), 5.20 (s, 2H), 4.05 (d, J=17.2Hz, 1H), 3.67 (d, J=17.2Hz, 1H), 2.14 (s, 3H). Step 3: Production of 5-(3,5-dichlorophenyi)-3-(3-fiuoro-4-hydroxymethylphenyl)¬5-trifluoromethyl-4,5-dihydroisoxazole [0193] In a solution of 1.50 g of crude 3-(4-acetoxymethyl-3-fluorophenyl)-5-(3,5¬dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazole in 10 ml of ethanol, 2.00 g of sodium hydroxide dissolved in 20 ml of water was added, and stirred under reflux with heat for 4.5 hours. After the completion of the reaction, the reaction mixture was cooled with ice, and adjusted to pH 2-3 by carefully adding concentrated hydrochloric acid, and extracted with ethyl acetate (50 ml x 1). The organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced . pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexarle (1:2) to obtain 0.95 g of the aimed product as pale yellow resinous substance. ^H NMR (CDCI3, Me^Si, 400MHz) 5 7.5-7.6 (m, 3H), 7.4-7.45 (m, 3H), 4.81 (s, 2H), 4.06 (d, J=17.2Hz, 1H), 3.68 (d, J=17.2Hz, 1H), 1.87 (bs, 1H). Step 4: Production of 4-[5-(3,5-dichlo^ophenyl)-5-t^ifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-fluoro benzoic acid [0194] In a solution of 0.95 g of 5-(3,5-dichlorophenyl)-3-(3-fluoro-4¬hydroxymethylphenyl)-5-trifluoromethyl-4,5-dihydroisoxazole in 25 ml of acetone, Johnes' Reagent prepared from 1.50 g of chromic acid, 1.2 mi of concentrated sulfuric acid and 7 ml of water was added dropwise under cooling with ice and with stirring, after the completion of the addition dropwise, continued to stir at room temperature for further 1.5 hour. After the completion of the reaction, the reaction mixture was poured in 50 ml of water and extracted with diethyl ether (50 mi x 1). The organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residual solid was washed with hexane to obtain 0.67 g of the aimed product as beige crystal. Melting point 172.0 to 174.0°C 'H NMR (CDCI3, Me^Si, 300MHz) 6 8.05-8.15 (m, 1H), 7.45-7.55 (m, 5H), 4.08 (d, J=17.3Hz, 1H), 3.71 (d, J=17.3Hz, 1H). Step 5: Production of N-benzyl-4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬ 4,5-dihydroisoxazol-3-yl]-2-fluoro benzoic acid amide [0195] In a solution of 0.15 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyI-4,5¬dihydroisoxazol-3-yl]-2-fluo^o benzoic acid in 10 ml of dichloromethane, 0.3 ml of oxalyl chloride and 2 drops of N,N-dimethylformaniide were added at room temperature, and stirred at the same temperature for 1.0 minutes. After the completion of the reaction, the solvent was distilled off Under reduced pressure, the remaining white solid was dissolved in 10 ml of chloroform, and 0.3 ml of benzylamine and then 0.3 ml of triethylamine were added under cooling with ice, after the completion of the addition, continued to stir at room temperature for further 20 minutes. After the completion of the reaction, 40 ml of wate.-- was poured in the reaction mixture, and extracted with ethyl acetate (50 mi x 1). The organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexant^ (1:2) to obtain 0.14 g of the aimed product as white crystal. Melting point 172.0 to 176.0°C'" ^ ^H NMR (CDCI3, Me^Si, 400MH2) 8 8.20 (t, J=8.0Hz, 1H), 7.25-7.55 (m, 10H), 7.05 (t, J=5.6Hz, 1H), 4.68 (d, J=5.6Hz, 2H), 4.07 (d, J=17.6Hz, 1H), 3.70 (d, J=17.6Hz, 1H). Synthetic Example 5 _ 4-[5-(3,5-Dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-2-nitro-N¬(2-pyridylmethyl) benzoic acid amide (Compound of the present invention No. 5-339) Step 1: Production of 4-bromo-3-nitrobenzaldoxime [0196] In a solution of 5.0 g of 4-bromo-3-nitrobenzaldehyde in 50 ml of methanol, 3.6 ml of 50% hydroxyamine aqueous solution was added with stirring at room temperature, and continued to stir at the same temperature for 18 hours. After the completion of the reaction, 60 ml of water was added in the reaction mixture, and precipitated solid was filtered off, washed with water and then dried to obtain 5.0 g of the aimed product as yellow crystal. ^H NMR (CDCIa-DMSO-dg, Me4Si, 400MHz) 5 11.18 (s, 1H), 8.09 (s, 1H), 8.07 (d, J=2.0Hz, 1H), 7.73 (d, J=8.4Hz, 1H), 7.62 (dd, J.=8.4, 2.0Hz, 1H). Step 2: Production of 3-(4-bromo-3-nitrophenyl)-5-(3,5-dichlorophenyl)-5¬trif I uo romethy 1-4,5-d ihyd roisoxazble [0197] In a solution of 1.27 g of 4-bromo-3-nitrobenzaldoxime in 16 ml of N,N¬dimethylformamide, 0.74 g of N-chlorosuccinic acid imide was added, and stirred at 35°C for 90 minutes.' Then, the reaction mixture was cooled with ice, 1.20 g of 3,5¬dichloro-l-(l-trifluoromethylethenyl) benzene synthesized in Step 1 of Synthetic Example 3 and 0.60 g of triethylamine were added, continued'to stir at room temperature for 18 hours. After the completion of the reaction, the reaction mixture was poured in 50 ml of ice water, extracted with ethyl acetate (50 ml x 2), the organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residual solid was subjected to purification with medium-pressure preparative liquid chromatography (Yamazen Corporation, medium pressure preparative system; YFLC-Wprep) that was eluted with ethyl acetate-hexane (1:2 to 1:4 gradient), and 1.10 g of the aimed product was obtained as yellow crystal. 284 Melting point 179.0 to 181.0°C ^H NMR (CDCI3, Me.Si, 400MHz) 8 8.06 (d, J=2.0Hz, 1H), 7.84 (d, J=8.4Hz, 1H), 7.78 (dd, J=8.4, 2.0Hz, 1H), 7.45-7.55 (m, 2H), 7.45 (t, J=1.8Hz, 1H), 4.09 (d, J=17.2Hz, 1H), 3.72 (d, J=17,4Hz, 1H). Step 3: Production of 4-[5-(3,''5-dichlorophenyi)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-nitrobenzoic acid ethyl ester ' [0198] In a solution of 2.0 g of 3-(4-bromo-3-nitrophenyl)-5-(3,5-dichlorophenyl)¬5-trifluoromethyl-4,5-dihydroisoxazole in 30 ml of ethanol in an autoclave, 0.40 g of sodium acetate, 88.0 mg of 1,1'-bis(diphenyIphosphino) ferrocene and^18.0 mg of palladium (II) acetate were added, and stirred under 0.9 MPa carbon nronoxide atmosphere at 100°C for 3 hours. After the completion of the reaction, the reaction mixture was left and cooled to room temperature, and the solvent was distilled off unjder reduced pressure, and the residue was dissolved in 100 ml of ethyl acetate, washed with water, dried over anhydrous sodium sulfate and the solvent was distilled off under reduced pressure. The residual solid was subjected to purification with medium-pressure preparative liquid chromatography (Yamazen Corporation, medium pressure preparative system; YFLC-Wprep) that was eluted with ethyl acetate-hexane (1:2 to 1:4 gradient), and 0.66 g of the aimed product was obtained as pale yellow crystal. Melting point 160.0 to 162.0°C ^H NMR (CDCI3, Me4Si, 400MHz) 6 8.13 (d, J=1.6Hz, 1H), 7.99 (dd, J=8.1, 1.6Hz, 1H), 7.83 (d, J=8.1Hz, 1H), 7.45-7.55 (m, 2H), 7.45 (t, J=1.8Hz, 1H), 4.41 (q, J=7.1Hz, 2H),4.1t(d, J=17.2Hz, 1H), 3.74 (d, J=17.8Hz, 1H), 1.37 (t, J=7.1Hz, 3H). Step 4: Production of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬ 4,5-dihydroisoxazdI-3-yl]-2-nitro-N-(2-pyridylmethyl) benzoic acid amide [0199] In a solution of 0.36 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5¬dihydroisoxazol-3-yl]-2-nitrobenzoic acid ethyl ester in 8 ml of ethanol, a solution of 0.40 g of potassium hydroxide in 2 ml of water was added, and stirred at room temperature for 3 hours. After the completion of the reaction, the reaction mixture was poured in 15 ml of water, adjusted to pH 4 with concentrated hydrochloric acid, then extracted with ethyl acetate (20 ml x 2), the organic phase was washed with water, and then dehydrated with saturated sodium chloride aqueous solution and dried over over anhydrous sodium sulfate and the solvent was distilled off under reduced pressure to obtain 0.40 g of crude 4-[5-(3,5-dichlorophenyl)-5¬trifluoromethyl-4,5-dihydroisoxazol-3-yJ]-2-nitro benzoic acid as pale yellow oily 285 substance. The substance was dissolved in 10 ml of chloroform, and 0.24 g of 2¬picolyiamine, 0.01 g of 4-(N,N-dimethylamino)pyridine and 0.35 g of 1-[3¬(diethylamino)propyl]-3-ethylcart)odiimide hydrochloride were added, and stirred at room temperature for 18 houi's., After the completion of the reaction, the solvent was distilled off under reduced pressure. The residue was subjected to purification with medium-pressure preparative liquid chromatography (Yamazen Corporation, •medium pressure preparative system; YFLC-Wprep) that was eluted with ethyl acetate-hexane (1:1 to 1:0 gradient), and 0.14 g of the aimed product was obtained as colorless resinous substance. _ 'H NMR (CDCIa-DMSO-de, Me4Si, SOOMHz) 5 8.50 (d, J=4.8Hz, 1H), 8.25 (d, J=1.7Hz, 1H), 8.03 (dd, J=8.1, 1.6Hz, 1H), 7.72 (td, J=7.7, 1.6Hz, 1H), 7.68 (d, J=8.1Hz, 1H), 7.51 (d, J=1.5Hz, 2H), 7.45 (t, J=1.8Hz, 1H), 7.43 (bs, 1H), 7.36 (d, J=7.;9Hz, 1H), 7.23 (dd, J=6.8, 5.3Hz, 1H), 4.76 (d, J=4.8Hz, 2H), 4.13 (d, J=17.4Hz, 1H),;3.76(d, J=17.4Hz, 1H). Synthetic Example 6 4-[5-(3,5-Dichiorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-2-methoxy-N-(2,2,2-trifluoroethyl) benzoic acid amide (Compound of the present invention No. 5-317) Step 1: Production of 4-hydroxyiminomethyl-2-methoxyphenyl trifluoromethane sulfonate [0200] In a solution of 3.0 g of 4-hydroxy-3-methoxybenzald,ehyde and 2.4 g of triethylamine in 50 ml of dichloromethane, 5.8 g of trifluoromethane sulfonic acid anhydride was added dropwise under cooling with ice and with stirring, after the completion of the addition dropwise, continued to stir at the same temperature for 30 minutes. After the completion of the reaction, the reaction mixture was washed with 50 ml of water and then with 30 ml of saturated sodium hydrogen carbonate aqueous solution, and dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was was dissolved in a mixture of 30 ml of ethanol and 15 ml of water, 1.4 g of hydroxyamine hydrochloride and 1.7 g of sodium acetate were added with stirring at room temperature, and continued to stir at the same temperature for further 1 hour. After the completion of the reaction, the solvent was ditilled off under reduced pressure, extracted with ethyl acetate (40 ml x 2), the organic phase was washed with water (30 ml x 1), and then dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous magnesiurii sulfate, and then the solvent v^as distilled off under reduced pressure to obtain 5.25 g of the aimed product as brown oily substance. Refractive index nD^°'°^ = 1.5082 ^H NMR (CDCIa-DMSO-dg, Me^bi, 300MHz) 8 8.47 (bs, 1H), 8.11 (s, 1H), 7.32 (s, 1H), 7.24 (d, J=8.1Hz, 1H), 7:4Q (d, J=8.1Hz, 1H), 3.94 (s, 3H). Step 2: Production of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethy!¬ , 4,5-dihydroisoxazol-3-yl]-2-methoxyphenyl trifluoromethane sulfonate [0201] In a solution of 2.0 g of 4-hydroxyiminomethyl-2-methoxyphenyl trifluoromethane sulfonate in 30 ml of N,N-dimethylformamide, 0.9 g oJ[N¬chlorosuccinic acid imide was added, and stirred at 40 to 50°C for 30 nrrinutes. Then, the reaction mixture was left and cooled to room temperature, 1.5 g of 3,5¬dichloro-l-(l-trifluoromethylethenyl) benzene synthesized in Step 1 of Synthetic Example 3 and 0.7 g of triethylamine were added, and stirred at room temperature for 90 minutes. After the completion of the reaction, the reaction mixture was poured in 100 ml of ice water, extracted with ethyl acetate (50 ml x 2), the organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (1:7), and 1.4 g of the aimed product was obtained as colorless resinous substance. ^H NMR (CDCI3, Me4Si, 300MHz) 5 7.50 (s, 2H), 7.44 (s, 1H), 7.25-7.3 (m, 2H), 7.11 (d, J=8.4Hz, 1H), 4.08 (d, J=17.1Hz, 1H), 3.97 (s, 3H), 3.69 (d, J=17.1Hz, 1H), Step 3: Production of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2~methoxy benzoic acid ethyl ester [0202] In a solution of 1.50 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5¬dihydroisoxazol-3-yl]-2-methoxyphenyl trifluoromethane sulfonate in 25 ml of ethanol in an autoclave, 0.27 g of sodium acetate, 31.0 mg of 1,r-bis(diphenylphosphino) ferrocene and 7.0 mg of palladium (II) acetate were added, and stirred under 0.96 Mpa carbon monoxide atmosphere at 100°C for 2 hours.. After the completion of the reaction, the reaction mixture was left and cooled to room temperature, and the reaction mixture was poured in 100 ml of ice water, extracted with ethyl acetate (40 ml x 2). The organic phases together were dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (1:5), and 1.20 g of the aimed product was obtained as white crystal. Melting point 142.0-144.0°C ^H NMR (CDCI3, Me^Si, 300MHz) 5 7.82 (d, J=7.8Hz, 1H), 7.51 (s, 2H), 7.4-7.45 (m, 2H), 7.10 (d, J=7.8Hz, 1H), 4.37 (q, J=7.2Hz, 2H), 4.10 (d, J=17.4Hz, 1H), 3.95 (s, 3H), 3.71 (d, J=17.4Hz, 1H);1.39 (t, J=7.2Hz, 3H). Step 4: Production of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬ • 4,5-dihydroisoxazot-3-yl]-2-methoxy benzoic acid [0203] In a solution of 1.07 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5¬dihydroisoxazol-3-yl]-2-methoxy benzoic acid ethyl ester in 30 ml of etbanol, a solution of 1.0 g of sodium hydroxide in 30 ml of water was added, stirred at 85°C for 1 hour. After the completion of the reaction, the solvent was distilled off under reduced pressure. The residue was adjusted to pH 2 to 3 with concentrated hydrochloric acid, and extracted with ethyl acetate (30 ml x 2). The organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure to obtain 1.0 g of the aimed product as pale yellow resinous substance. 'H NMR (CDCI3, Me^Si, 300MHz) 610.67 (bs, 1H), 8.24 (d, J=7.8Hz, 1H), 7.57 (s, 1H), 7.51 (s, 2H), 7.45 (s, 1H), 7.22 (d, J=7.8Hz, 1H), 4.05-4.15 (m, 4H), 3.74 (d, J=17.4Hz, 1H). Step 5: Production of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-methoxy-N-(2,2,2-trifluoroethyl) benzoic acid amide [0204] In a suspension of 0.25 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-methoxy benzoic acid in 15 ml of dichloromethane, 0.09 g of oxalyl chloride and 1 drop of N,N-dimethylformamide were added, and stirred at room temperature for 1 hour. After the completion of the reaction, the solvent was distilled off under reduced pressure, the residue was dissolved in 15 ml of dichloromethane, and 0.09 g of triethylamine was added under cooling with ice, then 0.07 g of 2,2,2-trifluoroethylamine was added dropwise. After the completion of addition dropwise, the mixture was continued to stir at the same temperature for further 2 hours. Thereafter, the reaction mixture was diluted with 60 ml of chloroform, washed with 50 ml of water, then dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (1:2) to obtain 0.25 g of the aimed product as colorless resinous substance. 'H NMR (CDCI3, Me^Si, 300MHz) 58.2-8.3 (m, 2H), 7.51 (s, 3H), 7.43 (s, 1H), 7.17 (d, J=7.8Hz, 1H), 4.05-4.2 (m, 3H), 4.05 (s, 3H), 3.74 (d, J=17.4Hz, 1H). Synthetic Example 7 1 4-[5-(4-Fluoro-3-methyipheny!)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-N¬(2,2,2-trifluoroethyl) benzoic scrd amide (Compound of the present invention No. 3-141) Step 1: Production of 4-formyl-N-(2,2,2-trifluoroethyl) benzoic acid amide [0205] In a suspension of 1.00 g of 4-formyl benzoic acid in 15 ml of benzene, 0.87 g of thionyl chloride and 2 drops of N,N-dimethylformamide were^added, and stirred under reflux with heat for 2 hours. After the completion of the reaction, the reaction mixture was left and cooled to room temperature, and the solvent was distilled off under reduced pressure to obtain 1.14 g of crude 4-formyl benzoic acid chlpride as white crystal. In a solution of 0.66 g of 2,2,2-trifluoroethylamine and 0.81 g of triethylamine in 6 ml of chlororform, the solution of 1.14 g of the crude 4¬formyl benzoic acid chloride in 6 ml of chloroform was added dropwise under cooling with ice and with stirring, after the completion of the addition dropwise, continued to stir at room temperature for further 18 hours. After the completion of the reaction, the reaction mixture was added in 30 ml of water, extracted with chloroform (20 ml x 3). The organic phase was washed with water, dried over anhydrous sodium sulfate, the solvent was distilled off under reduced pressure, the residual solid was washed with hexane to obtain 1.32 g of the aimed product as white crystal. Melting point 83.0 to 84.0°C ^H NMR (CDCI3, Me4Si, 400MHz) 510.09 (s, 1H), 7.96 (bs, 4H), 6.80 (bs, 1H), 4.05¬ 4.25 (m, 2H). Step 2: Production of 4-hydroxyiminomethyl-N-(2,2,2-trifluoroethyl) benzoic acid amide [0206] In a solution of 4.11 g of 4-formyl-N-(2,2;2-trifluoroethyl) benzoic acid amide in 30 ml of ethanol and 10 ml of water, 1.99 g of hydroxyamine hydochloride and 2.51 g of anhydrous sodium acetate were added, stirred stirred at room temperature for 3.5 hours. After the completion of the reaction, the reaction mixture was poured in 100 ml of water, and then extracted with ethyl acetate (30 ml x 3), the organic phase was washed with 50 ml of saturated sodium hydrogen carbonate aqueous solution, then dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residual solid was washed with hexane to obtain 3.92 g of the aimed product as white crystal. Melting point 153.0 to 154.0°C ^H NMR (CDCI3, Me4Si, 400MHz) 510.89 (s, 1H), 8.08 (s, 1H), 8.03 (bs, 1H), 7.84 (d, J=8.2Hz, 2H), 7.60 (d, J=8.2Hz, 2H), 3.95-4.1 (m, 2H). Step 3: Production of 4-chlor6hydroxyiminomethy!-(2,2,2-trifluoroethyl) benzoic acid amide [0207] In a solution of 3.80 g of 4-hydroxyiminomethyl-N-(2,2,2-trifluoroethyl) benzoic acid amide in 50 ml of tetrahydrofyran, 20 ml of 3N hydrochloric acid was added, 14 mi of 8% sodium hypochlorite aqueous solution was added^dropwise withi stirring under ice cooling over 10 minutes, after the completion of addition dropwise, continued to stir at the same temperature for further 15 minutes. After the completion of the reaction, the reaction mixture was poured in 200 ml of water, exliacted with ethyl acetate (30 ml x 3), the organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure. The resudual solid was washed with hexane to obtain 4.15 g of the product as white crystal. Melting point 158.0 to 160.0°C 'H NMR (CDCI3, Me4Si, 400MHz) S12.03 (s, 1H), 8.05 (t, J=6.0Hz, 1H), 7.93 (bs, 4H), 3.95-4.15 (m,2H). Step 4: Production of 4-[5-(4-fluoro-3-methylphenyl)-5-trifluoromethyl-4,5¬dihydrooxazol-3-yl]-N-(2,2,2-trifluoroethyl) benzoic acid amide [0208] In a solution of 0.21 g of 4-fluoro-3-methylphenyl boric acid and 0.23 g of 2-bromo-3,3,3-trifluoropropene in 6 ml of 1,2-dimethoxyethane and 2 ml of water, 0.24 g of sodium carbonate and 0.05 g of dichlorobis(triphenylphosphine) palladium (II) were added, stir-red at 75°C for 3 hours. Then, the reaction mixture was left and cooled to room temperature, then a solution of 0.25 g of 4¬chlorohydroxyiminomethyl-N-(2,2,2-trifluoroethyl) benzoic acid amide in 4 ml of 1,2¬dimethoxyethane was added, continued to stir at the same temperature for further 18 hours. After the completion of the reaction, the reaction mixture was poured in 50 ml of water, extracted with ethyl acetate (10 ml x 3), the organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure. The resudual solid was purified with silica gel column chromatography that was eluated with chloroform to obtain 0.24 g of the product as white crystal. Melting point 151.0 to 152.OX ^H NMR (CDCts, Me.Si, 400MHz) 57.86 (d, J=8.4Hz, 2H), 7.76 (d, J=8.4Hz, 2H), 7.35-7.5 (m, 2H), 7.0-7.15 (m, 1H), 6.39 (t, J=6.3Hz, 1H), 4.05-4.25 (m, 2H), 4.09 (d, J=17.3Hz, 1H), 3.74 (d, J=17.3Hz, 1H), 2.32 (d, J=1.7Hz, 3H). Synthetic Example 8 4-[5-(3,5-Dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-2-methyl-N-(2,2,2-trifluoroethyi) benzoic acid amide (Compound of the present invention No. 5-075) Step 1: Production of 4-bromo-2-methyl-N-(2,2,2-trifluoroethyl) benzoic acid amide [0209] In a solution of 5.00 g of 4-bromo-2-methyl benzoic acid and 3.45 g of 2,2,2-trifluoroethylamine in 30 ml of N,N-dimethylformamide, 5.79 g ofT-[3¬(diethylamino)propyl]-3-ethylcarbodiimide hydrochloride was added with stirring at room temperature, and stirred at the same temperature for 1.5 hour. After the corjnpletion of the reaction, 80 ml of water was added, and precipitated crystal was filtered off, washed with water and dried to obtain 4.00 g of the aimed product as white crystal. Melting point 124.0 to 125.5°C ^H NMR (CDCI3, Me^Si, 400MHz) 57.40 (s, 1H), 7.36 (d, J=8.4Hz, 1H), 7.22 (d, J=8.4Hz, 1H), 6.15 (bs, 1H), 4.0-4.15 (m, 2H), 2.39 (s, 3H). Step 2; Production of 4-formyl-2-methyl-N-(2,2,2-trifluoroethyl) benzoic acid amide [0210] In a solution of 1.00 g of 4-bromo-2-methyl-N-(2,2,2-trifIuoroethyl) benzoic acid amide in 15 ml of tetrahydrofuran under nitrogen atmosphere, 4.7 ml of n-butyl lithium (1.58M hexane solution) was added dropwise at -70°C with stirring, and then 0.4 ml of N,N-dimethylformamide were added dropwise. After stirring at the same temperature for 30 minutes, 10 ml of IN hydrochloric acid and then 30 ml of water were added, and e>ftracted with ethyl acetate (30 ml x 2). The organic phase was dehydrated with saturated sodiun chloride aqueous solution and dried over anhydrous magnesium sulfate, the solvent was distilled off under reduced pressure to obtain 0.80 g of the aimed product as pale yellow crystal. Melting point 99.0 to 104.OX ^H NMR (CDCI3, Me4Si, 400MHz) 610.00 (s, 1H), 7.7-7.75 (m, 2H), 7.50 (d, J=7.5Hz, 1H), 6.27 (bs, 1H), 4.05-4.2 (m, 2H), 2.49 (s, 3H). Step 3: Production of 4-hydroxyiminomethyl-2-methyl-N-(2,2,2-trifluoroethyl) benzoic acid amide [0211] In a solution of 0.8 g of 4-formyl-2-methyl-N-(2,2,2-trifIuoroethyl) benzoic acid amide in 10 mi of ethanol and 5 ml of water, 0.3 g of hydroxyamine 2.91 hydrochloride and 0.4 g of anhydrous sodium acetate were added with stirring at room temperature, and stirred at the same temperature for 30 minutes. After the completion of the reaction, the solvent was distilled off under reduced pressure, and precipitated crystal was filtered off, washed with water and dried to obtain 0.5 g of the aimed product as white crystal. Melting point 190.5 to 194.0°C ^H NMR (CDCIa-DMSO-dg, Me4Si, 400MHz) 510.98 (s, 1H), 8.43 (bs, 1H), 8.07 (s, 1H), 7.35-7.55 (m, 3H), 3.95-4.1 (m, 2H), 2.43 (s, 3H). Step 4: Production of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-_ 4,5-dihydroisoxasol-3-yl]-2-methyl-N-(2,2,2-trifluoroethyl) benzoic acid amide [0212] In a solution of 0.40 g of 4-hydroxyiminomethyl-2-methyl-N-(2,2,2¬trifluoroethyl) benzoic acid amide in 15 ml of N,N-dimethylformamide, 0.21 g of N¬chlo^rosuccinc acid imide was added, and stirred at 50°C for 30 minutes. Then, the reaction mixture was left and cooled to room temperature, 0.34 g of 3,5-dichloro-1¬(1-trifluoromethylethenyl) benzene synthesized in Step 1 of Synthetic Example 3 and 0.16 g of triethylamine were added, and stirred at room temperature for 18 hours. After the completion of the reaction, the reaction mixture was poured in 50 ml of ice water, extracted with ethyl acetate (50 ml x 1), the organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (1:2), and 0.45 g of the aimed product was obtained as white c-rystal. Melting point 155.5 to 157.0°C ^H NMR (CDCI3, Me4Si, 400MHz) 57.4-7.55 (m, 6H), 6.13 (bs, 1H), 4.05-4.2 (m, 3H), 3.71 (d, J=17.4Hz, 1H), 2.45 (s, 3H). Synthetic Example 9 4-[5-(3,5-Dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-2-methyl-N¬(2-pyridylmethyl) benzoic acid amide (Compound of the present invention No. 5-234) Step 1: Production of 4-bromo-2-methyl-N-(2-pyridylmethyl) benzoic acid amide [0213] In a solution of 3.0 g of 4-bromo-2-methyl benzoic acid in 30 ml of dichloromethane, 2.7 g of oxalyl chloride and 3 drops of N,N-dimethylformamide were added under cooling with ice with stirring, and stirred at room temperature for 1 hour. After the completion of the reaction, the solvent was distilled off under reduced pressure, the residue was dissolved in 30 ml of dichloromethane, 2.1 g of triethylamine and 2.0 g of 2-picolylamine were added under cooling with ice with stirring, and continued to stir at room temperature for 3 hours. After the completion of the reaction, 50 ml of water was added in the reaction mixture, extracted with chloroform (50 ml x 2), the orga^nic phase was washed with water, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solventwas distilled off under reduced pressure. The residual solid was washed with diisopropyletherto obtain 3.7 g of the aimed product as yellow crystal. Melting point 86.0 to 87.5X ^H NMR (CDCI3, Me^Si, 300MHz) 58.52 (d, J=4.8Hz, 1H), 7.69 (td, J=7^8, 1.8Hz, 1H), 7.15-7.4 (m, 6H), 4.73 (d, J=4.8Hz, 2H), 2.45 (s, 3H). Step 2: Production of 4-formyl-2-methyl-N-(2-pyridylmethyl) benzoic acid amide [0214] In a solution of 2.0 g of 4-bromo-2-methyl-N-(2-pyridylmethyl) benzoic acijd amide in 20 ml of N,N-dimethylformamide in an autoclave, 0.67 g of sodium formate and 0.10 g of dichlorobis(triphenylphosphine) palladium (II) were added, and stirred under 1.05 MPa carbon monoxide atmosphere at 110°C for 3 hours. After the completion of the reaction, the reaction mixture was left and cooled to room temperature, and poured in 100 ml of water, and extracted with ethyl acetate (50 ml x 2). The organic phases together were dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (9:1), and 0.50 g of the aimed product was obtained as pale yellow crystal. Melting point 79.5 to 83.0°C ^H NMR (CDCI3, Me4Si, 300MHz) 510.02 (s, 1H), 8.54 (d, J=5.1Hz, 1H), 7.6-7.8 (m, 4H), 7.15-7.4 (m, 3H), 4.77 (d, J=4.8Hz, 2H), 2.55 (s, 3H). Step 3: Production of 4-hydroxyiminomethyl-2-methyl-N-(2-pyridylmethyl) benzoic acid amide [0215] In a solution of 0.50 g of 47formyl-2-methyl-N-(2-pyridylmethyl) benzoic acid amide in 10 ml of ethanol and 5 ml of water, 0.18g. of hydroxyamine hydrochloride was added with stirring at room temperature, and stirred at the same temperature for 12 hours. After the completion of the reaction, solid was filtered off, ethanol was distilled off under reduced pressure, and 30 mi of saturated sodium hydrogen carbonate aqueous solution was added in the remaining aqueous solution. The precipitated crystal was filtered off, washed with water and dried to obtain 0.45 g of the aimed product as pale yellow crystal. Melting point 159.5 to 161.OX 'H NMR (CDCIj-DMSO-dg, Me^Si, 300MHz) 511.89 (bs, 1H), 8.56 (d, J=4.2Hz, 1H), 8.03 (s, 1H), 7.90 (bs, 1H), 7.77:;(t, J=7.8Hz, 1H), 7.47 (d, J=7.5Hz, 1H), 7.0-7.35 (m, 4H), 4.76 (d, J=6.0Hz, 2H), 2.36 (s, 3H). Step 4: Production of 4-[5-(3,5-d!chlorophenyl)-5-t^ifluoromethyl¬4,5-dihyd^oisoxazol-3-yl]-2-methyl-N-(2-pyridylmethyl) benzoic acid amide [0216] In a solution of 0.45 g of 4-hydroxyiminomet[iyl-2-methyl-N-(2¬pyridylmethyl) benzoic acid amide in 10 ml of N,N-dimethylformamide, 0.25 g of N¬chlorosuccinc acid imide was added, and stirred at 70°C for 1 hour. Then, the reaction mixture was left and cooled to room temperature, 0.41 g of 3,5-dichIoro-1¬(1-trifluoromethylethenyl) benzene synthesized in Step 1 of Synthetic Example 3 and 0.25 g of potassium hydrogen carbonate were added, and stirred at room temperature for 3 hours. After the completion of the reaction, the reaction mixture was poured in 50 ml of ice water, extracted with ethyl acetate (60 ml x 1), the organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (3:1), and 0.30 g of the aimed product was obtained as white crystal. Melting point 131.0 to 135.5°C 'H NMR (CDCI3, Me4Si, 300MHz) 58.53 (d, J=5.0Hz, 1H), 7.65-7.75 (m, 1H), 7.2¬ 7.55 (m, 9H), 4.75 (d, J=4.9Hz, 2H), 4.09 (d, J=17.3Hz, 1H), 3.71 (d, J=17.3Hz, 1H), 2.50 (s,3H). Synthetic Example 10 4-[5-(3,5-Dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-N-¬(2-pyridylmethyl)-2-trifluoromethyl benzoic acid amide (Compound of the present invention No. 5-315)" Step 1: Production of 4-[5-(3,5-dichlorpphenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-iodo benzoic acid methyl ester [0217] In a solution of 0.60 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5¬dihydroisoxazol-3-yl]-2-iodo benzoic acid synthesized similarly to Steps 1 to 4 of Synthetic Example 4 in 10 ml of methanol, 2 drops of concentrated sulfuric acid was added, and stirred under reflux with heat for 20 hours. After the completion of the reaction, the solvent was distilled off under reduced pressure, the residue was neutralized with 10 mi of saturated sodium hydrogen carbonate aqueous solution, then extracted with ethyl acetate (10 ml x 2). The organic phase was washed with water, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and'-'then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane'(1:4), and 0.56 g of the aimed product was obtained as colorless oily substance. ^H NMR (CDCI3, Me^Si, 400MHz) §8.22 (d, J=1.5Hz, 1H), 7.85 (d, J=8.2Hz, 1H), 7.75-7.8 (m, 1H), 7.5-7.55 (m, 2H), 7.4-7.45 (m, 1H), 4.07 (d, J=17.7Hz, 1H), 3.95 (s, 3H), 3.69(d, J=17.2Hz, 1H). Step 2: Production of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-trifluoromethyl benzoic acid methyl ester [0218] In a solution of 0.51 g of of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5¬dihydroisoxazol-3-yl]-2-iodo benzoic acid methyl ester in 5 ml of N,N¬dimethylformamide, 0.18 g of copper (I) iodide, 0.06 g of potassium fluoride and 0.27 g of chlorodifluoro acetic acid methyl ester were added, and stirred at 120°C for 5 hours. After the completion of the reaction, the reaction mixture was left and cooled to room temperature, 50 ml of water was added and extracted with ethyl acetate (50 ml X 2). The organic phase was washed with water, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (1:4), and 0.45 g of the aimed product was obtained as pale yellow oily substance. 'H NMR (CDCI3, Me4Si, 400MHz) 58.00 (d, J=1.1Hz, 1H), 7.85-7.95 (m, 2H), 7.5¬ 7.55 (m, 2H), 7.4-7.45 (m, 1H), 4.12 (d, J=7.1Hz, 1H), 3.96 (s, 3H), 3.94 (d, J=7.8Hz, 1H). Step 3: Production of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-trifluoromethyl benzoic acid [0219] In a solution of 0.40 g of of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-trifluoromethyl benzoic acid-methyl ester in 5 ml of methanol, a solution of 0.10 g of sodium hydroxide in 2 ml of water was added, and stirred at room temperature for 18 hours. After the completion of the reaction, 10 ml of water was added in the reaction mixture, washed with 5 ml of toluene, aqueous phase was collected, adjusted to pH 1 to 2 with concentrated hydrochloric acid and then extracted with ethyl acetate (20 ml x 2). The organic phase was washed with water, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure to obtain 0.34 g of the aimed product as pale yellow resinous substance. The resulting product was usee! as such without purification for the next step. Step 4: Production of 4-[5-(3,5.-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-N-(2-pyridylmethyl)-2-trifluoromethyl benzoic acid amide [0220] in a solution of 0.15 g of 4-[5-(3,5-dichlorophenyl)-5-trif!uGromethyl-4,5¬ ' dihydroisoxazol-3-yl]-2-trifluoromethyl benzoic acid in 3 ml of dichloromethane, 0.06 g of oxalyl chloride and 1 drop of N,N-dimethylformamide were added under cooling with ice with stirring, and stirred at room temperature for 2 hours. After the completion of the reaction, the solvent was distilled off under reduced pressure, the residue was dissolved in 3 ml of dichloromethane, and a solution of 0.05 g of 2¬picolylamine and 0.06 g of triethylamine in 1 ml of dichloromethane was added dropwise, after the completion of the addition dropwise, continued to stir at room temperature for 3 hours. After the completion of the reaction, 5 ml of water was added in the reaction mixture, extracted with chloroform (5 ml x 2). The organic phase was washed with water, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (1:3), and 0.05 g of the aimed product was obtained as white crystal. Melting point 69.0 to 70.0°C ^H NMR (CDCI3, Me4Si, 400MHz) S8.5-8.55 (m, 1H), 7.95 (bs, 1H), 7.91 (d, J=1.9Hz, 1H), 7.65-7.8 (m, 2H), 7.5-7.55 (m, 2H), 7.35-7.45 (m, 3H), 7.26 (t,-J=4.9Hz, 1H), 4.77 (d, J=4.9Hz, 2H), 4.11 (d, J=17.4Hz, 1H), 3.73 (d, J=17.2Hz, 1H). Synthetic Example 11 4-[5-(3,5-Dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazo|-3-yl]-2-phenyl-N¬(2-pyridylmethyl) benzoic acid amide (Compound of the present invention No. 5-344) Step 1: Production of 4-[5-(3,5-dichlo.rophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-phenyl benzoic acid methyl ester [0221] In a solution of 0.70 g of 2-bromo-4-[5-(3,5-dichlorophenyl)-5¬trifluoromethyl-4,,5-dihydroisoxazol-3-yl] benzoic acid methyl ester synthesized similarly to Step 1 of Synthetic Example 10 in 20 ml of teirahydrofuran and 10 ml of water, 0.18 g of phenyl boric acid, 0.39 g of potassium carbonate and 0.05 g of dichlorobis(triphenylphosphine) palladium (II) were added, and stirred under reflux with heat for 1.5 hour. After the completion of the reaction, the solvent was distilled off under reduced pressure, the residue was poured in 30 ml of water, tlien extracted with ethyl acetate (50 ml x 1). The organic phase was washed v^^ith water, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and, then the solvent was distilled off under reduced pressure. The residue was prurified with silica gel column chromatography that was eluated with ethyl acetate, and 0.78 g of the aimed product was obtained as brown resinous substance. ^H NMR (CDCI3, Me^Si, 400MHz) 57.89 (d, J=8.4Hz, 1H), 7.74 (dd, J=8.0, 1.8Hz, 1H), 7.62 (d, J=1.4Hz, 1H), 7.51 (d, J=1.8Hz, 2H), 7.35-7.45 (m, 4H), 7^25-7.35 (m, 2H), 4.11 (d, J=16.8Hz, 1H), 3.73 (d, J=16.8Hz, 1H), 3.65 (s, 3H). Step 2: Production of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-phenyl benzoic acid [0222] In a solution of 0.78 g of of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-phenyl benzoic acid methyl ester in 15 ml of ethanol, a solution of 0.30 g of sodium hydroxide in 15 ml of water was added, and stirred at 60°C for 3 hours. After the completion of the reaction, ethanol was distilled off under reduced pressure, adjusted to pH 1 to 2 with 12N hydrochloric acid, and then extracted with ethyl acetate (50 ml x 1). The organic phase was washed with water, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure to obtain 0.70 g of the aimed product as brown glass substance. The resulting product was used as such without purification for the next step. Step 3: Production of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬ is 4,5-dihydroisoxazol-3-yl]-2-phenyl-N-(2-pyridylmethyl) benzoic acid amide [0223] In a solution of 0.3 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5¬dihydroisoxazol-3-yl]-2-phenyl benzoic acid in 10 ml of chloroform, 0.3 ml of oxalyl chloride and a catalytic amount (2 to 3 drops) of N,N-dimethylformamide were added with stirring at room temperature, and stirred at the same temperature for 10 minutes. After the completion of the reaction, the solvent was distilled off under reduced pressure, the residue was dissolved in 10 ml of chloroform, and under cooling with ice with stirring 0.3 ml of 2-picolylamine and then 0.3 ml of triethylamine were added, and continued to stir at room temperature for 20 minutes. After the completion of the reaction, the reaction mixture was poured in 40 ml of water, extracted with ethyl acetate (50 ml x 1). The organic phase was washed with water, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (2:1), and 0.2 g of the aimed product was obtained as white crystal. Melting point 194.0 to 198.0°G V ^H NMR (CDCI3, Me^Si, 400MHz) 58.3-8.35 (m, 1H), 7.25-7.8 (m, 12H), 7.1-7.15 (m, • 1H), 7.40 (d, J=7.8Hz, 1H), 6.65-6.7 (m, 1H), 4.47 (d, J=5.0Hz, 2H), 4.12 (d, J=17.0Hz, 1H), 3.74 (d, J=17.0Hz, 1H). Synthetic Example 12 2-Amino-4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazot-3-yl]¬N-(2,2,2-trifluoroethyl) benzoic acid amide (Compound of the present invention No. 5-329) Step 1; Production of 2-amino-4-[5-(3,5-dichlorophenyi)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl] benzoic acid ethyl ester [0224] In a solution of 0.60 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-nitro benzoic acid ethyl ester synthesized in Steps 1 to 3 of Shynthetic Example 5 in 6 ml of ethyl acetate, 2.0 ml of water, 0.6 ml of acetic acid and 0.46 g of reduced iron were added, and stirred at 75°C for 2 hours. After the completion of the reaction, the organic phase was collected, and the aqueous phase was extracted with ethyl acetate (10 ml x 2). The organic phases together were washed with water, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure to obtain 0.60 g of crude aimed product as brown oily substance. The resulting product was used as such without purification for the next step. Step 2: Production of 2-amino-4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl] benzoic acid [0225] In a solution of 0.6 g of crude 2-amino-4-[5-(3,5-dichlorophenyl)¬5-trifluoromethyl-4,5-dihydroisoxazol-3-yl] benzoic acid ethyl ester in 7 ml of ethanol, a solution of 0.5 g of potassium hydroxide in 2.0 ml of water was added, and stirred at room temperature for 18 hours. After the completion of the reaction, 20 ml of ice water was added in the reaction mixture, adjusted to pH 2 to 3 with concentrated hydrochloric acid, and then extracted with ethyl acetate (20 ml x 2). The organic phase was washed with water, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure to obtain 0.6 g of crude aimed product as yellow oily substance. The resulting product was used as such without purification for the next step. Step 3: Production of 2-amino-4v[5-(3,5-dich!o^ophenyl)-5-trifluoromethyi¬4,5-dihyd^oisoxazol-3-yi]-N-(2,2,2-trifluo^oethyi) benzoic acid amide [0226] In a solution of O.BG-g -of crude 2-amino-4-[5-(3,5-dichlorophenyl)-5¬trifluoromethyl-4,5-dihydroisoxazol-3-yl] benzoic acid in 6 ml of chloroform, 0.20 g of 2,2,2-trifluoroethylamine, 0.02 g of 4-(N,N-dimethylamino) pyridine and 0.33 g of 1¬[3-(diethylamino)propyl]-3-ethylcarbodiimide hydrochloride were added, and stirred at room temperature for 20 hours. After the completion of the reaction, the reaction mixture was subjected to purification with medium-pressure preparative-liquid chromatography (Yamazen Corporation, medium pressure preparative system; YFLC-Wprep) that was eluted with ethyl acetate-hexane (1:4), and 0.14 g of the aimed product was obtained as pale yellow crystal. Melting point 78.0 to 79.0°C 'H NMR {CDCI3, Me4Si, 400MHz) 57.50 (d, J=1.8Hz, 2H), 7.43 (t, J=1.8Hz, 1H), 7.39 (d, J=8.6Hz, 1H), 6.95-7.0 (m, 2H), 6.29 (t, J=7.0Hz, 1H), 5.68 (bs, 2H), 4.05-4.15 (m, 2H), 4.04 (d, J=17.2Hz, 1H), 3.67 (d, J=17.2Hz, 1H). Synthetic Example 13 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-2-methylthio-N¬(2-pyridylmethyl) benzoic acid amide (Compound of the present invention No. 5-323) [0227] In a solution of 0.92 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5¬dihydroisoxazol-3-yl]-2-fluoro-N-(2-pyridylmethyl) benzoic acid amide (Compound of the present invention No. 5-041) synthesized similarly to Synthetic Example 4 in 12 ml of dimethylsulfoxide, 0.12 g of sodium methane thiolate was added with stirring at room temperature, and stirred at 100°C for 90 minutes. After the completion of the reaction, the reaction mixture was poured in 30 ml of water, and extracted with ethyl acetate (20 ml x 3). The organic phase was washed with 30'ml of water, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with chloroform, and 0.89 g of the aimed product was obtained as colorless oily substance. ^H NMR (CDCI3, Me^Si, 300MHz) S8.51 (d, J=4.8Hz, 1H), 7.6-7.75 (m, 4H), 7.52 (bs, 2H), 7.42 (bs, 1H), 7.37 (bs, 1H), 7.34 (bs, 1H), 7.20 (dd, J=6.9, 1.8Hz, 1H), 4.74 (d, J=4.8Hz, 2H), 4.10 (d, J=17.1Hz, 1H), 3.75 (d, J=17.1Hz, 1H), 2.47 (s, 3H). Synthetic Example 14 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5-dihyciroisoxazol-3-yl]-2-nnethylsulfinyl-N-(2,2,2-trifluoroethyl) benzoic',acid amide (Compound of the present invention No. 5-324) [0228] in a solution of 0.38 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5¬dihydroisoxazoi-3-yl]-2-methylthio-N-(2,2,2-trifluoroethyl) benzoic acid amide • (Compound of the present invention No. 5-322) synthesized similarly to Synthetic Example 13 in 6 ml of 1,2-dichloroethane, 0.10 g of N-chlorosuccinic acid imide was - added with stirring at room temperature, and stirred at the same temperature for 11 hours. After the completion of the reaction, the reaction mixture was poured in 30 ml of water, and extracted with ethyl acetate (20 ml x 3). The organic phase was washed with 30 ml of saturated sodium hydrogen carbonate, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (1:2), and 0.17 g of the aimed product was obtained as colorless oily substance. 'H NMR (CDCI3, Me4Si, 300MHz) 58.16 (t, J=8.1Hz, 1H), 7.6-7.8 (m, 3H), 7.55 (d, J=8.1Hz, 1H), 7.51 (d, J=8.1Hz, 1H), 7.15 and 7.11 (t, J=6.3Hz, 1H), 4.18 (qd, J=18.5, 6.3Hz, 2H), 4.15 (d, J=17.7Hz, 1H), 3.80 (d, J=17.7Hz, 1H), 2.79 and 2.78 (s, 3H). Synthetic Example 15 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-2¬methylsulfonyl-N-(2',*2,2-trifluoroethyl) benzoic acid amide (Compound of the present invention No. 5-326) [0229] In a solution of 0.25 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5¬dihydroisoxazoI-3-yl]-2-methylthio-N-(2,2,2-trifluoroethyl) benzoic acid amide (Compound of the present invention No. 5-322) synthesized similarly to Synthetic Example 13 in 6 ml of dichloromethane, 0.17 g of 3-chloroperbenzoic acid was added with stirring at room temperature, and stirred at the same temperature for 3 days. After the completion of the reaction, the reaction mixture was poured in 30 mi of sodium thiosulfate aqueous solution, and extracted with chloroform (10 ml x 3). The organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with chloroform, and 0.20 g of the aimed product was obtained as colorless oily substance. 'H NMR (CDCla, Me4Si, 300MHz) 58.16 (t, J=8.4Hz, 1H), 8.05 (bs, 1H), 8.00 (s, 1H), 7.92 (s, 1H), 7.55 (d, J=8.4Hz, 1H), 7.52 (d, J=8.4H2, 1H), 7.06 and 7.02 (t, J=6.4Hz, 1H), 4.17 (d, J=17.4Hz, 1H), 4.16 (qd, J=18.5, 6.3Hz, 2H), 3.79 (d, J=17.4Hz, 1H), 2.12 (s,3H). Synthetic Example 16 2-Cyano-4-[5-(3,5-dichlorophenyl)-5-trifluoromethyi-4,5-dihydroisoxazol-3-yl]-N-(2¬pyridyimethyl) benzoic acid amide (Compound of the present invention No. 5-341) [0230] In a solution of 0.19 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoroTnethyl-4,5¬dihydroisoxazol-3-yt]-2-iodo-N-(2-pyridylmethyl) benzoic acid amide (Compound of the present invention No. 5-065) synthesized similarly to Synthetic Example 4 in 10 ml of dimethylacetamide, 36.0 mg of zinc cyanide, 4.8 mg of zinc, 11.0 mg of tris(dibenzylideneacetone) dipalladium and 13.5 mg of 1,1'¬bis(diphenylphosphino)ferrocene were added, and stirred under nitrogen atmosphere at 80 to 120°C for 5 hours. After the completion of the reaction, 30 ml of ammonia water and 20 ml of water were added in the reaction mixture, and extracted with ethyl acetate (50 ml x 1). The organic phase was washed with 30 ml of water, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethylacetate-hexane (2:1), and 0.05 g of the aimed product was obtained as brown resinous substance. ^H NMR (CDCI3, Me4Si, 400MHz) 58.5-8.6 (m, 1H), 8.12 (bs, 1H), 7.9-8.0 (m, 2H), 7.15-7.7 (m, 7H), 5.13 (bs, 2H), 4.14 (d, J=17.4Hz, 1H), 3.78 (d, J=17.4Hz, 1H). Synthetic Example 17 2-Acetylamino-4-[5-(3,5-dichlorophenyl)-5-trifiuoromethyl-4,5-dihydroisoxazol-3-yl]¬N-(2,2,2-trifiuoroethyl) benzoic acid amide (Compound of the present invention No. 5-333) [0231] In a solution of 0.05 g of 2-amino-4-[5-(3,5-dichlorophenyl)-5¬trifluoromethyl-4,5-dihydroisoxazol-3-yl]-N-(2,2,2-trifluoroethyl) benzoic acid amide (Compound of the present invention No. 5-329) synthesized in Synthetic Example 12 and 0.15 ml of triethylamine in 2 ml of chloroform, 0.10 ml of acetic anhydride was added under cooling with ice with stirring, and stirred at room temperature for 20 hours. After the completion of the reaction, the reaction mixture was subjected to purification witii medium-pressure preparative liquid chromatography (Yamazen Corporation, medium pressure preparative system; YFLC-Wprep) that was eluted with ethyl acetate-hexane (1:8 to 1:1 gradient), and 0.45 g of the aimed product was obtained as pale yellow resinous substance. ^H NMR (CDCia, Me4Si, 400MHz) 510.90 (bs, 1H), 8.77 (d, J=1.3Hz, 1H), 7.57 (dd, J=8.4, 1.5Hz, 1H), 7.53 (d, J=8.4Hz, 1H), 7.50 (d, J=1.7Hz, 2H), 7.45 (t, J=1.8Hz, • 1H), 6.82 (bs, 1H), 4.1-4.2 (m, 2H), 4.11 (d, J=17.0Hz, 1H), 3.73 (d, J=17.0Hz, 1H), 2.22 (s, 3H). Synthetic Example 18 _ 4-[5-(3,5-Dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-2-methylamino-N-(2,2,2-trifluoroethy!) benzoic acid amide (Compound of the present invention No. 5-331) and 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazoI-3-yl]-2¬dinriethylamino-N-(2,2,2-trifIuoroethyl) benzoic acid amide (Compound of the present invention No. 5-334) [0232] In a solution of 0.25 g of 2-amino-4-[5-(3,5-dichlorophenyl)-5¬trifluoromethyl-4,5-dihydroisoxazol-3-yl]-N-(2,2,2-trifluoroethyl) benzoic acid amide (Compound of the present invention No. 5-329) synthesized in Synthetic Example 12 and 0.06 g of 36% formaldehyde aqueous solution in 7 ml of 1,2-dichloroethane, 1.00 g of sodium triacetoxy borohydride was added with stirring at room temperature in three portions at 1 hour-interval, and continued to stir at the same temperature for further 2 hours. After the completion of the reaction, the reaction mixture was poured to 5 ml of ice water, the organic phase was collected, and the solvent v\/as distilled under reduced pressure. The resudue was subjected to purification with medium-pressure preparative liquid chromatography (Yamazen Corporation, medium pressure preparative system; YFLC-Wprep) that was eluted with ethyl acetate-hexane (0:1 to 1:3 gradient), and 0.13 g of 4-[5-(3,5-dichlorophenyl)-5¬trifiuoromethyl-4,5-dihydroisoxazol-3-yl]-2-methylamino-N-(2,'2,2-trifluoroethyl) benzoic acid amide was obtained as pale yellow crystal, and 0.13 g of 4-[5-(3,5¬dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-2-dimethylamino-N¬(2,2,2-trifluoroethyl) benzoic acid amide was obtained as pale yellow resinous substance. 4-[5-(3,5-dichloropheny!)-5-trifluoromethyI-4,5-dihydroisoxazol-3-yl]-2-methy!amino-N-(2,2,2-trifluoroethyl) benzoic acid amide; Melting point 156.0 to 158.0°C ^H NMR (CDCI3, Me.Si, 400MHz) 67.57 (bs, 1H), 7.52 (d, J=1.6Hz, 2H), 7.43 (t, J=1.8Hz, 1H), 7.38 (d, J=8.2Hz, 1H), 6.92 (d, J=1.6Hz, 1H), 6.84 (dd, J=8.2, 1.6Hz, 1H), 6.31 (t, J=6.4Hz, 1H), 4.0-4.15 (m, 2H), 4.08 (d, J=17.2Hz, 1H), 3.70 (d, J=17.2Hz, 1H), 2.91 (s, 3H). ' 4-[5-(3,5-dichlorophenyl)-5-trifiuoromethyi-4,5-dihydroisoxazol-3-y!]-2¬ dimethylamino-N-(2,2,2-trifludroethyl) benzoic acid amide; ^H NMR (CDCI3, Me^Si, 400MHz) 510.29 (t, J=6.2Hz, 1H), 8.22 (d, J=8.1Hz, 1H), 7.73 (d, J=1.7Hz, 1H), 7.52 (d, J=1.7Hz, 2H), 7.44 (t, J=1.8Hz, 1H), 7.33 (dd, J=8.1, 1.6Hz, 1H), 4.13 (qd, J=9.2, 6.2Hz, 2H), 4.10 (d, J=17.2Hz, 1H), 3.72 (d, J=17.2Hz, 1H),2.78(s, 6H). Synthetic Example 19 4-[5-(3,5-Dichloroplienyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-N-(2¬methoxyiminoethyl)-2-methyI benzoic acid amide (Compound of the present invention No. 5-113) [0233] In a solution of 152 mg of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5¬dihydroisoxazol-3-yl]-N-(2,2-dimethoxyethyl)-2-methyl benzoic acid amide (Compound of the present invention No. 5-083) synthesized similarly to Synthetic Example 5 in 14 ml of methaol-water (6:1) mixed solvent, 38 mg of methoxyamine hydrochloride was added, and stirred under reflux with heat for 8 hours. After the completion of the reaction, the reaction mixture was left and cooled to room temperature, diluted by adding 80 ml of ethyl acetate, washed with water (30 ml x 2), and dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethylacetate-hexane (1:1), and 102 mg of the aimed product was obtained as colorless resinous substance. 'H NMR (CDCI3, Me^Si, 300MHz) 67.45-7.55 (m, 6H), 7.45-7.55 and 6.83 (t, J=4.5Hz, 1H), 7.4-7:45 (m, 1H), 6.28 atid 6.16 (t, J=4.7Hz, 1H), 4.27 and 4.22 (t, J=4.7Hz, 2H), 4.08 (d, J=17.1Hz, 1H), 3.92 and 3.85 (s,.3H), 3.70 (d, J=17.4Hz, 1H), 2.50 and 2.48 (s, 3H). Synthetic Example 20 N-[4-[5-(3,5-Dich!orophenyl)-5-trifluoromethyi-4,5-dihydroisoxazol-3-yl]-2¬methylbenzoyl] glycine (Compound of the present invention No. 5-127) [0234] In a solution of 2.6 g of methyl N-[4-[5-(3,5-dichlorophenyl)-5¬trifluoromethyl-4,5-dihydroisoxazol-3-yl]-2-methylbenzoyl] glycine (Compound of the present invention No. 5-128) synthesized similarly to Synthetic Example 5 in 10 ml of methanol, a solution of 1.0 g of potassiunn hydroxide in 10 ml of water was added with stirring at room temperature, and stirred at the same temperature for further 1 hour. After the completion of the reaction, 10 ml of 12N hydrochloric acid was added and extracted with ethyl acetate (50 ml x 1), the organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced • pressure to obtain 2.4 g of the aimed product as pale yellow resinous resinous substance. 'H NMR (CDCI3, Me^Si, 300MHz) 57.4-7.55 (m, 6H), 6.35-6.85 (m, 2H), 4.23 (d, J=5.7Hz, 2H), 4.08 (d, J=17.1Hz, 1H), 3.71 (d, J=17.1Hz, 1H), 2.44 (s,~3H). Synthetic Example 21 4-[5-(3,5-Dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-2-methyl-N-[N¬(2,2,2-trifluoroethyl) carbamoylmethyl] benzoic acid amide (Compound of the present invention No. 5-151) [0235] In a solution of 1.00 g of N-[4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-methylbenzoyl] glycine (Compound of the present invention No. 5-127) synthesized in Synthetic Example 20 in 30 ml of dichloromethane, 0.65 g of 1-[3-(diethylamino)propyl]-3-ethylcarbodiimide hydrochloride was added, and stirred at room temperature for 15 minutes, then 0.40 g of 2,2,2-trifluoroethylamine and 0.40 g of 4-(N,N-dimethylamino)pyridine were added and stirred at the same temperature for further 2 hours. After the completion of the reaction, the solvent was distilled off under reduced pressure, the residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (1:3), and then crystallized from hexane to obtain 0.48 g of the aimed product as white crystal. Melting point 173.5 to 175.5°C 'H NMR (CDCI3, Me^Si, 300MHz) 57.35-7.55 (m, 7H), 7.03 (t, J=5.1Hz, 1H), 4.21 (d, J=5.1Hz, 2H), 4.09 (d, J=17.4Hz, 1H),.3.85-4.0 (m, 2H), 3.71 (d, J=17.4Hz, 1H), 2.43 (s, 3H). Synthetic Example 22 4-[5-(3,5-Dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-2-methyl-N- (N¬phenylcarbamoylmethyl) benzoic acid amide (Compound of the present invention No. 5-169) [0236] In a solution of 0.40 g of N-[4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-methylbenzoyl] glycine (Compound of the present invention No. 5-127) synthesized in Synthetic Example 20 and 0.08 g of pyridine in 10 ml of dichloromethane, 0.12 g of pivaloyi chloride was added, and stirred at room temperature for 2 hours, then 0.50 g of aniline and 3 ml of triethylamine were added and stirred at the same temperature for further 1 hour. After the completion of the reaction, 20 ml of water was added in the reaction mixture and extracted with ethyl acetate (50 ml x 1), the organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (2:1) to obtain 0.12 g of the aimed product as white crystal. Melting point 181.0 to 183.0°C 'H NMR (CDCIs, Me^Si, 300MHz) 58.54 (bs, 1H), 7.5-7.55 (m, 7H), 7.44 (t, J=2.0Hz, 1H), 7.31 (t, J=8.0Hz, 2H), 7.1-7.2 (m, 1H), 6.95 (bs, 1H), 4.34 (d, J=5.0Hz, 2H), 4.19 (d, J=17.2Hz, 1H), 3.70 (d, J=17.2Hz, 1H), 2.49 (s, 3H). Synthetic Example 23 4-[5-(3,5-Dichlorophenyl)-5-trifluoromethyI-4,5-dihydroisoxazol-3-yl]-2-methyl-N¬methyl-N-(2-pyridylmethyl) benzoic acid amide (Compound of the present invention No. 6-020) [0237] In a solution of 0.35 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyI-4,5¬dihydroisoxazol-3-yl]-2-methyl-N-(2-pyridylmethyl) benzoic acid amide (Compound of the present invention No. 5-234) synthesized similarly to Synthetic Example 5 in 20 ml of N,N-dimethylformamide, 0.04 g of 55% oily sodium hydride was added under cooling with ice with stirring, and stirred at the same temperature for 30 minutes. Then, 0.12 g of methyl iodide was added and thereafter the temperature was raised to room temperature, and continued to stir at the same temperature for further 2 hours. After the completion of the reaction, the reaction mixture was diluted with 80 ml of ethyl acetate, washed with water (50 ml x 2), dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The resudue was purified with high performance liquid chromatography that was eluated with acetonitrile-water (85:15) to obtain 0.25 g of the aimed product as colorless resinous substance. ^H NMR (CDCI3, Me^Si, 300MHz) 68.5-8.6 (m, 1H), 7.6-7.75 (m, 1H), 7.05-7.55 (m, 8H), 4.43 and 4.89 (bs, 2H), 4.06 and 4.09 (d, J=17.4 and 17.1Hz, 1H), 3.68 and 3.71 (d, J=17.4 and 17.1Hz, 1H), 2.85 and 3.13 (s, 3H), 2.35 and 2.38 (s, 3H). Synthetic Example 24 7-[5-(3,5-Dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-1-methyl-3-(2¬ pyridyimethyI)-1,2,3,4-tetrahydi:oquinazolin-4-one (Compound of the present invention No. 6-071) [0238] In a solution of 0.06 g of 4-j;5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5¬ dihydroisoxazol-3-yl]-2-methylamino-N-(2-pyridylmethyl) benzoic acid amide (Compound of the present invention No. 5-332) synthesized similarly to Synthetic Example 18 in 5 ml of dichloromethane, 0.03 g of chloromethylether was added, and stirred at the same temperature for 15 hours After the completion ofjhe reaction, the solvent was distilled off under reduced pressure, and the residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (3:1) to obtain 0.04 g of the aimed product as colorless oily substance. ^KNMR (CDCI3, Me4Si, 300MHz) 58.5-8.6 (m, 1H), 8.04 (d, J=7.8Hz, 1H), 7.6-7.75 (m^ 1H), 7.4-7.55 (m, 4H), 7.15-7.3 (m, 1H), 7.10 (bs, 1H), 6.95-7.05 (m, 1H), 4.86 (s, 2H), 4.06 (s, 2H), 4.09 (d, J=17.4Hz, 1H), 3.70 (d, J=17.4Hz, 1H), 2.90 (s, 3H). Synthetic Example 25 4-[5-(3,5-Dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-2-methyl-N¬(2,2,2-trifluoroethyl) benzoic acid thioamide (Compound of the present invention No. 7-007) [0239] A solution of 0.50 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl-4,5¬dihydroisoxazol-3-yl]-2-methyI-N-(2,2,2-trifluoroethyl) benzoic acid amide (Compound of the present invention No. 5-075) synthesized in Synthetic Example 8 and 0.41 g of Lawesson's Reagent (2,4-bis(4-methoxyphenyl)-1,3,2,4¬dithiadiphosphetan-2,4-disulfide) in 15 ml of toluene was stirred under reflux with heat for 20 hours. After the completion of the reaction, the reaction mixture was left and cooled to room temperature, and the reaction mixture was diluted with 60 ml of ethyl acetate, washed with water (50 ml x 1), then dehydrated with saturated sodium chloride aqueous solution and dried oyer anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (3:1) to obtain 0.40 g of the aimed product as yellow resinous substance. ^H NMR (CDCI3, Me4Si, 300MHz) 57.2-7.5 (m, 7H), 4.55-4.7 (m, 2H), 4.06 (d, J=17.1Hz, 1H), 3.68 (d, J=17.1Hz, 1H), 2.38 (s, 3H). Synthetic Example 26 4-[5-(3-Bromodifluoromethoxyphenyi)-5-trifIuoromethyl-4,5-dihydroisoxazol-3-yl]-2¬ methyl-N-(2,2,2-trifluoroethyl) benzoic acid amide (Compound of the present invention No. 5-014) Step 1: Production of 3-bromodifluoromethoxy-l-iodobenzene [0240] In a suspension of 0.87 g of 55% oily sodium hydride in 20 ml of N,N¬dimethylformamide, a solution" of 4.00 g of 3-iodophenol in 10 ml of N,N¬dimethylformamide was added dropwise with stirring under ice cooling , after the completion of the addition dropwise, stirred at room temperature for 30 minutes. The reaction mixture was added dropwise in a solution of 11.40 g of dibromodiflucromethane in 20 ml of N,N-dimethylformamide under cooling with ice with stirring, after the completion of the addition dropwise, continued to'stir at room temperature for 2 hours. After the completion of the reaction, 50 ml of water was added in the reaction mixture, extracted with ethyl acetate (100 ml x 1), the organic phase was washed with water, then dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with hexane to obtain 2.10 g of the aimed product as colorless oily substance. 'H NMR (CDCI3, Me^Si, 300MHz) 57.65-7.7 (m, 1H), 7.55-7.65 (m, 1H), 7.2-7.3 (m, 1H), 7.15(t, J=9.0Hz, 1H). Step 2: Production of 3-bromodifluoromethoxy-1-(1-trifluoromethylethenyl) benzene [0241] In 10 ml of a solution of 1-trifluoromethylethenyl zinc bromide prepared according to the method described in documents in 1M tetrahydrofuran, 1.0 g of 3-bromodifluoromethoxy-1-iodobenzene and 0.05 g of dichlorobis(triphenylphosphine) palladium (II) were added, and stirred under reflux with heat for 2 hours. After the completion of the reaction, the reaction mixture was poured in 20 ml of diluted hydrochloric acid, extracted with ethyl acetate (50 ml x 1). The organic phase Was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was dissolved in hexane, and high polar impurities were excluded by treating with silica gel to obtain 0.77 g of crude aimed product as colorless oily substance. The resulting product was used as such without purification for the next step. Step 3: Production of 4-[5-(3-bromodifluoromethoxyphenyl)5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-methyl-N-(2,2,2-trifluoroethyl) benzoic acid amide [0242] In a solution of 0.3 g of 4-chlorohydroxyiminomethyl-2-methyl-N-(2,2,2¬ trifluoroethyl) benzoic acid amide synthesized similarly to Steps 1 to 3 of Synthetic Example 7 and 0.2 g of crude 3-bromodifluoromethoxy-1-(1-trifluoromethylethenyl) benzene in 10 ml of 1,2-dimethqxyethane, 0.4 g of potassium hydrogen carbonate was added, and stirred at rodni, temperature for 18 hours. After the completion of the reaction, the reaction mixture was poured in 20 ml of water, extracted with ethyl acetate (50 ml x 1). The organic phase was dehydrated with saturated sodium •chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (1:1) to, obtain 0.29 g of the aimed product as colorless glass substance. ^H NMR (CDCI3, Me4Si, 400MHz) 67.5-7.6 (m, 5H), 7.41 (d, J=7.8Hz, 1H), 7.3-7.5 (m, 1H), 6.16 (t, J=6.6Hz, 1H), 4.05-4.15 (m, 3H), 3.74 (d, J=17.2Hz, 1H), 2.45 (s, 3H). Synthetic Example 27 4-[5-Chlorodifluoromethyl-5-(3,5-dichlorophenyl)-4,5-dihydroisoxazol-3-yl]-2¬methyl-N-(2,2,2-trifluoroethyl) benzoic acid amide (Compound of the present invention No. 5-355) Step 1: Production of 2,3',5'-trichloro-2,2-difluoroacetophenone [0243] In a solution of 5.0 g of 3,5-dichloro-1-iodobenzene in 50 ml of t¬butylmethylether, 12.2 ml of n-butyl lithium (1.58M hexane solution) was added dropwise at -78°C with stirring, after the completion of the addtipn dropwise, stirred at the same temperature for 30 rhinutes. 6.6 g of chlorodifluoroacetic acid methyl ester was added dropwise at -78°C with stirring in the reaction mixture, after the completion of the addition drropwise, continued to stir at 0°C for further 30 minutes. After the completionof the reaction, the reaction mixture was poured in 100 ml of saturated ammonium chloride aqueous solution, extracted with, ethyl acetate (100 ml X 1). The organic phase was dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure to obtain 4.6 g of crude aimed product as pale yellow oily substance. The resulting product was used as such without purification for the next step. 'H NMR (CDCI3, Me^Si, 300MHz) 67.97 (s, 2H), 7.68 (s, IH). Step 2: Production of 3,5-dichloro-1-[1-(chlorodifluorofluoromethyl)ethenyl] benzene [0244] in a solution of 2.89 g of methyltriphenylphosphonium bromide in 15 ml of tetrahydrofuran, 0.91 g of potassium t-butoxide was added, and stirred at room temperature for 1 hour. Then, a solution of 2.00 g of 2,3',5'-trichioro-2,2¬difluoroacetophenone in 5 mi of tetrahydrofuran was added dropwise in the reaction mixture under cooling with ice v/ith stirring, after the completion of the addition dropwise, continued to stir at room temperature for 1 hour. After the completion of the reaction, the reaction mixture was poured in 50 ml of ice water, extracted with ethyl acetate (50 ml x 1), the organic phase was dehydrated with saturated sodium • chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with hexane to obtain 1.50 g of the aimed product as yellow oily substance. 'H NMR (CDCIj, Me^Si, 300MHz) 87.40 (s, 1H), 7.35 (s, 2H), 5.99 (s, 1H), 5.65 (s, 1H). Step 3: Production of 4-[5-chlorodifluoromethyl-5-(3,5-dichlorophenyl)¬4,5-dihydroisoxazol-3-yl]-2-methyI-N-(2,2,2-trifluoroethyl) benzoic acid amide [0245] In a solution of 0.25 g of 4-chlorohydroxyiminomethyl-2-methyl-N-(2,2,2¬trifluoroethyl) benzoic acid amide synthesized similarly to Steps 1 to 3 of Synthetic Example 7 and 0.26 g of 3,5-dichloro-1-[1-(chlorodifluorofluoromethyl)ethenyl] benzene in 3 ml of 1,2-dimethoxyethane, 0.43 g of potassium hydrogen carbonate and a small amount of water were added, and stirred at room temperature for 15 hours. After the completion of the reaction, the reaction mixture was filtered and thereby solid substance was excluded, and the filtrate was concentrated under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (2:3) to obtain 0.28 g of the aimed product as yellow oily substance. 'H NMR (CDCI3, Me4Si, 300MHz) 57.35-7.65 (m, 6H), 6.06 (t, J=6.1Hz, 1H), 4.0-4.25 (m, 3H), 3.72 (d, J=17.1Hz, 1H), 2.47 (s, 3H). Synthetic Example 28 4-[5-(3,5-Dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazol-3-yl]-2-methyl-N-methoxycarbonyl-N-(2-pyridylmethyl) benzoic acid amide (Compound of the present invention No. 6-043) Step 1: Production of 5-(3,5-dichlorophenyl)-3-(3-methyl-4-nitrophenyl)¬ 5-trifluoromethyl-4,5-dihydroisoxazole [0246] In a solution of 1.31 g of 3,5-dichloro-1-(1-trifluoromethylethenyl) benzene synthesized in Step 1 of Synthetic Example 3 and 1.17 g of a-chloro-3-methyl¬4-nitrobenzaidoxime in 10 ml of tetrahydrofuran, 1.15 g of potassium hydrogen carbonate and 1.50 g of water were added, and stirred at room temperature for 18 hours. After the completion of the reaction, tetrahydrofuran was removed from the reaction mixture, 3 mi of water was added, and stirred under colloing with ice for further 30 minutes. Precipitated crystal was filtered off, washed with 5 ml of water and then 5 ml of diisopropyl ether to obtain 1.29 g of the aimed product as white crystal. • Melting point 135.0 to 136.0°C M NMR (CDCI3, Me^Si, 300MHz) 58.03 (d, J=7.5Hz, 1H), 7.6-7.75 (m, 2H), 7.51 (bs, 2H), 7.44 (t, J=1.8Hz, 1H), 4.11 (d, J=17.4Hz, 1H), 3.73 (d, J=17.4Hz,JH), 2.64 (s, , 3H). Step 2: Production of 3-(4-amino-3-methylphenyl)-5-(3,5-dichlorophenyl)¬5-trifluoromethyl-4,5-dihydroisoxazole [0247] In a solution of 1.23 g of 5-(3,5-dichlorophenyl)-3-(3-methyl¬4-nitrophenyl)-5-trifluoromethyl-4,5-dihydroisoxazole in 10 ml of ethyl acetate, 5.0 ml of water, 5.0 ml of acetic acid and 0.66 g of reduced iron were added and stirred at 100°C for 2 hours. After the completion of the reaction, the reaction mixture was filtered through Celite, 20 ml of water was added in the filtrate, extracted with ethyl acetate (20 ml x 2). The organic phases together were washed with 10 mi of saturated sodium hydrogen carbonate aqueous solution, and then with 10 ml of water, thereafter dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure to obtain 1.05 g of crude aimed product as red-brown oily substance. The resulting product was used as such without purification for the next step. ^H NMR (CDCI3, Me^Si, 300MHz) 57.52 (s, 2H), 7.35-7.5 (m, 2H), 7.31 (dd, J=8.0, 2.0Hz, 1H), 6.65 (d, J=3.4Hz, 1H), 4.05 (d, J=17.1Hz, 1H), 3.93 (bs, 2H), 3.64 (d, J=17.1Hz, 1H), 2.17(s, 3H). Step 3: Production of 3-(4-bromo-3-methylphenyl)-5-(3,5-dichlorophenyl)¬5-trifluoromethyl-4,5-dihydroisoxazole [0248] in a solution of 0.50 g of ,3-(4-amino-3-methylphenyl)-5¬(3,5-dichlorophenyi)-5-t^ifluoromethyl-4,5-dihydroisoxazoIe in 1.0 ml of 1,4-dioxane and 2.0 ml of water, 1.0 ml of 47% hydrobromic acid was added, and stirred under reflux with heat for 1 hour. Then, the reaction mixture was cooled with ice, and a solution of 0.10 g of sodium nitrite in 1.0 ml of water was slowly added dropwise with stirring at a temperature of 5°C or less, after the completion of the addition dropwise, continued to stir at the same temperature for further 1 hour. The diazo mixture was slowly added dropwise in a mixture of 1.0 ml of 47% hydrobromic acid and 0.28 g of copper (1) bromide at 60°C with stirring, after the completion of the addition dropwise, continued to stir at 60°C for further 2 hours. After the completion of the reaction, 10 ml of water was added in thereaction mixture, extracted with ethyl acetate (20 ml x 2), the organic phases together were washed with water, then dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluated with ethyl acetate-hexane (1:10) to obtain 0.43 g of the aimed product as pale yellow crystal. Melting point 105.0 to 108.0°C 'H NMR (CDCI3, Me4Si, 300MHz) 57.59 (d, J=8.4Hz, 1H), 7.45-7.55 (m, 3H), 7.42 (t, J=1.8Hz, 1H), 7.33 (dd, J=8.4, 2.1Hz, 1H), 4.07 (d, J=17.1Hz, 1H), 3.68 (d, J=17.1Hz, 1H), 2.43(s, 3H). Step 4: Production of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-methylbenzoic acid ethyl ester [0249] in a solution of 15.0 g of 3-(4-bromo-3-methylphenyl)-5-(3,5¬dichlorophenyl)-5-trifluoromethyl-4,5-dihydroisoxazole in 60 ml of ethanol in an autoclave, 3.26 g of sodium acetate, 0.37 g of 1,1'-bis(diphenylphosphino) ferrocene and 0.08 g of palladium (II) acetate were added, and stirred under 2.0 MPa carbon monoxide atmosphere at 110°C for 3 hours. After the completion of the reaction, the reaction mixture was left and cooled to room temperature, 200 ml of water was added and extracted with ethyl acetate (200 ml x 2), the organic phase was washed with water, dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate and the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluted with ethyl acetate-hexane (1:8) to obtain 10:8 g of the aimed product as colorless clear liquid. Refractive index rio^^-^'^ = 1.5474 'H NMR (CDCI3, Me4Si, 300MHz) 67.95 (d, J=8.4Hz, 1H), 7.45-7.65 (m, 4H), 7 .43 (t, J=1.8Hz, 1H), 4.37 (q, J=7.2Hz, 2H), 4.10 (d, J=17.4Hz, 1H), 3.71 (d, J=17.1Hz, 1H), 2.62 (s, 3H), 1.40 (t, J=7.2Hz, 3H). Step 5: Production of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-methyl benzoic acid [0250] In a solution of 10.79 g of 4-[5-(3,5-dichIorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazo!-3-yl]-2-methylbenzoic acid ethyl ester in 50 ml of ethanol and 10 mi of water, a solution of 2.0 g of sodium hydroxide in 10 ml of water was slowly added with stirring at room temperature. Then, the reaction mixture was stirred at SOX for 2 hours, after the completion of the reaction, ethanol was distilled off under reduced pressure. The residue was adjusted to pH 1-2 with concentrated hydrochloric acid with stirring at SOX, then continued to stir at the same temperature • for 1 hour and then at 5 X for 1 hour. Presipitated crystal was filtered off, washed with water and dried to obtain 9.36 g of the aimed product as white crystal. Melting point 146.0 to 148.5X 'H NMR (CDCI3, Me4Si, 300MHz) 58.12 (d, J=8.7Hz, 1H), 7.5-7.7 (m, 21H), 7.52 (d, J=1.5Hz, 2H), 7.43 (d, J=1.5Hz, 1H), 4.11 (d, J=16.8Hz, 1H), 3.73 (d, J=17.4Hz, 1H), 2.69 (s, 3H). Sti^p 6: Production of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-methyl-N-methoxycarbonyl-N-(2-pyridylmethyl) benzoic acid amide [0251] In a solution of 1.00 g of 4-[5-(3,5-dichlorophenyl)-5-trifluoromethyl¬4,5-dihydroisoxazol-3-yl]-2-methyl benzoic acid in 30 ml of toluene, 0.43 g of thionyl chloride and 3 drops of N,N-dimethylformamide were added, and stirred at 90 X for 1 hour. After the completion of the reaction, the solvent was distilled off under reduced pressure, and the resudue was dissolved in 5 ml of tetrahydrofuran. In a solution of 0.40 g of N-(2-pyridylmethyl) carbamic acid methyl ester in 5 ml of tetrahydrofuran, 0.27 g of t-butoxy potassium was added at room temperature with stirring, and stirred at the same temperature for 3 minutes. Then, the above-mentioned solution of acid chloride in tetrahydrofuran was added dropwise in the reaction mixture, after the completion of the addition dropwise, continued to stir at the same temperature for further 1 hour. After the completion of the reaction, the reaction mixture was diluted with 60 ml of ethyl acetate, washed with 50 ml of water, then dehydrated with saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate and the solvent was distilled off under reduced pressure. The residue was purified with silica gel column chromatography that was eluted with ethyl acetate-hexane (1:2 to 1:1) to obtain 0.75 g of the aimed product as yellow resinous substance. ^H NMR (CDCI3, Me^Si, 300MHz) 88.56 (d, J=4.8Hz, 1H), 7.65-7,7 (m, 1H), 7.5-7.55 (m, 4H), 7.35-7.45 (m, 2H), 7.15-7.3 (m, 2H), 5.21 (s, 2H), 4.09 (d, J=17.4Hz, 1H), 3.70 (d, J=17.4Hz, 1H), 3.58 (s, 3H), 2.40 (s, 3H). [0252] The compounds of the present invention can be produced according to the above-mentioned production methods and working examples. The examples of the compounds produced similarly to Synthetic Examples 1 to 28 are shown in Tables 7 to 20 to which the present invention is not limited. In the meantime, in Tables, the indication "Et" means ethyl, hereinafter similarly thereto, "n-Pr" and "Pr-n" mean normal propyl, "i-Pr" and "Pr-i" mean isopropyl, "c-Pr" and "Pr-c" mean cyclopropyl, "n-Bu" and "Bu-n" mean normal butyl, "s-Bu" and "Bu-s" mean secondary butyl, "i-Bu" and "Bu-i" mean isobutyl, "t-Bu" and "Bu-t" mean tertiary butyl, "c-Bu" and "Bu-c" mean cyclobutyl, c-Pen" and "Pen-c" mean c^clopentyl, "n-. Hex" and "Hex-n" mean normal hexyl, "c-Hex" and "Hex-c" mean cycTohexyl, "Ph" means phenyl, "TMS" means trimethylsilyl, and in Tables, aromatic heterocyclic rings of D-1a to D-54b are the following structures, respectively j O O ^^ S o J^ ' RJ^ Z D-6c : ^A 3 ^-^^ • .-X~}o D-8b : ^,JC~)) ^ ^ N N ~ Z Z D-lOb : ,J^^ D-lla : ,,J^S D'Hb • .^C} s •S O N N Z ^^~^^ fni r=\ D-llc : J / X D-13b : Jl N D-14a : ^ N x) 1[ R^^ Z NO2 N-N \=N D-15a : ^JiJ D-16b : ^k.^^ ^ CI RJ^ /=N . \= N N-N D-I6C : ^k.cH 3 °""' ' ^ -^^-CH , "-l' " ^ ^ ^ Z CI CH3 Z iSf-N N—ry N ^ D-17b : ^J<^^ D-21a : ^ J D-llb : ^ J CHj D-21C . J^ ^ B-2W : ^^cH 3 D-21e : J[)^ , ^'^^^ • -^S/^ ^ CI D-21g : ^"3-^ »-21h ^ > V N N \ OCH3 D-21i : ^ > ^ D-21J : ^~>J^NO, ^.^ N S N N ^ S CI CI ^ N /=A^ y=( D-23b : ^ ^ ^ D-24a : ^N^.N D-24b : ^N^ .N CI CI R^^ CH3 Z D-24C : ^N /N D-25a : _ ^ J^ D-25c : ^ } "^ Y N N CH3 y;:^ R'' RJ' N—<( \ ^N N-^ D-25d : ^ }^ D-26a : ^ ^ D-27a : ^ ^ .^ N N ^^ Z /T"^ VN N=A D-28a : ^ , N D-29b : ^ > I>-30a : ^ > N' S N N-T\ N-N N-N D-31a : J ^k D-34a : ^ > D-34b : ^ ^^^ N—N N—N Nr=^ D-35a : ^Jj^ } D-35b : ^ ^ JL.^ D'^Sa : ^N^^ N S S z RJ^ D-39C : ^ ^ NH D-42a : ^ ^ ^N N ' N D-47a • I D-47b : | D-47d : | _ AN ^ -^N^ -^N^ D-47e : I D-47f: D-47h : /^^ N Z -^ N -^ N O D-47i : D-48a : I D-48e : | I ri^^ N N' ^ N" ^ D-49a : I D-50a : || D-50b : || OCH3 Z I ^ x D-50d : II D-51a : || | D-51b : || | / ^ /N . /N . ,Z D-51c : II I D-53a : . D-53b : D-54b : I -^ N 316 in Tables, saturated heterocyclic rings of E-4a to E-43a are the following structures, respectively, '• E-4a : ^A \ E-Sa : ^A o E-5b : ^A n n o r-\ ^-\ R^^o-x E-9b : „X^N-^j^23 E-lOa : , ^ ^ E-lOb : ^^ ) E-llc : ^JZX"^^" E-17a : .X^XQ ^-ISa : ^ 3 , " CH3 " ^ O2S—\ O"^ S''^ E-18c : ^^J. J> E-32a : 1 E-43a : 1 S ^^^^ /A.g/^ In Tables, partially saturated heterocyclic ring of M-5a is the following structure M-5a : (II In Tables, T-4 to T-'43 are the following structures, respectively o T-4 : <^ T-9>: / T-13 : —/ \ HO T-17 : -U ) T-21 : -^ J T-22 : ^ ^ /^^«3 ^OCH3 T-28 : —N J T-29a : —N J T-29b : __p^/^ ' /^S / \ / \ T-32 : —N I T-34 : —N ) T-35 : —N O o T-37 : —N N-CH3 T-39 : •"'\^>v^ T-40 : —N 1 ^ •^H3^cH3 r^ OH ^ _ / T-41 : —N==( )) T-42.: / N—^ /C-NH T-43 : ( ^C-NH O' \—CF3 In addition, in Tables, the number showing the substitution position of substituents (X)m and (Y)r, correspond to he position number indicated in the following strutural formulae. The indication "-" means no-substitution. Further, in Tables, the indication of "Mw" shows the calculated velue of molecular weight, the indication of "M+H" shows the measured value of molecular ion peak, and "*1" , "*2" or "*3" means "resinous", "oily" or "decomposition", respectively. Table 7 V ^ ^-^^^e' -R^ 5 O ' No. (X)^ R^ R' 1-001 - C(0)0CH3 CH2CF31-002 - C(0)0CH3 CH2Ph1-003 2-F C(0)0CH3 CH2CF31-004 2-CI CPpCHg CH2CF31-005 3-Br CF3 CHsPh1-006 4-Br CF3 CH2CF31-0D7 4-Br CF3 CH2Ph1-008 3-CH3 CF3 CH2CF31-009 3-CH3 CF3 CHsPh1-010 4-CH3 CF3 CH2CF31-011 4-CH3 CF3 CHzPh1-012 4-Bu-t CF3 CH2CF31-013 4-Bu-t CF3 CH2Ph1-014 2-CF3 C(0)0CH3 CH2CF31-015 3-CF3 CF3 CH2CF31-016 3-CF3 CF3 CHaPh1-017 4-CF3 CF3 CH2CF31-018 4-CF3 CF3 CHgPh1-019 2-OCH3 C(0)0CH3 CH2CF31-020 3-OCH3 CF3 CH2CF31-021 3-OCH3 ' CF3 CHsPh1-022 4-OCH3 CF3 CH2CF31-023 4-OCH3 CF3 CH2Ph1-024 4-OCH3 C(0)0CH3 CH2CF31-025 3-OCF3 CF3 CH2CF3.1-026 3-OCF3 CF3 CH2Ph1-027 4-OCF3 CF3 CH2CF31-028 4-OCF3 CF3 CHgPh1-029 4-OPh CF3 CH2CF31-030 4-OPh CF3 CH2Ph1-031 4-SCH3 CF3 CH2CF31-032 4-SCH3 CF3 CH2Ph1-033 4-SO2CH3 CF3 CH2CF31-034 3-NHC(0)CH3 CF3 CH2CF31-035 3-NHC(0)CH3 CF3 CHgPh1-036 4-NHC(0)CH3 CF3 CH2CF3 Mw M++H 406.36 407.00 414^16 415.07 ' 424.35 424.99 440.81 440.94 503.31 502.75 495.21 494.68 503.31 502.74 ^ 430.34 430.91 438.44 438.95 430.34 430.92 438.44 438.91 472.42 472.94 480.52 480.99 474.36 474.87 484.32 484.78 492.41 492.82 484.32 484.80 492.41 492.85 436.39-436.99 446.34 446.89 454.44 454.94 446.34 446.89 454.44 454.91 436.39 437.00 500.31 500.76 508.41 508.80 500.31 500.76 508.41 508.82 508.41 508.85 516.51 516.88 462.41 462.84 470.51 470.88 494.41494.86 473.37 473.90 481.47 481.93 473.37 473.81 1-037 4-NHC(0)CH3 1-038 4-N(CH3)2 1-039 4-N(CH3)2 1-040 3-NO2 1-041 3-NO2 1-042 3-TMS 1-043 3-CN 1-044 4-CN 1-045 3-CHO 1-046 3-C(0)CH3 1-047 3-C(0)CH3 1-048 4-C(0)CH3 1-049 4-C(0)CH3 1-050 3-C(0)0Et 1-051 3-C(0)0Et 1-052 4-Ph 1-053 3,4-F2 1-054 3,4-F2 1-055 3,5-F2 1-056 3,5-F2 1-057 3-CW-F 1-058 3-CW-F 1-059 2,5-Cl2 1-060 2,5-Cl2 1-061 2,5-Cl2 1-062 3,4-Cl2 1-063 3,4-Cl2 1-064 3,4-Cl2 1-065 3,4-Cl2 1-066 3,4-Cl2 1-067 3,4-Cl2 1-068 3,4-Cl2 1-069 3,4-Cl2 1-070 3,4-Cl2 1-071 3,4-Ci2 1-072 3,4-Cl2 1-073 3,4-Cl2 1-074 3,4-Cl2 1-075 3,4-Cl2 1-076 3,4-Cl2 1-077 3,4-Cl2 1-078 3,4-Cl2 1-079 3,4-Cl2 1-080 3,4-Cl2 1-081 3,4-Cl2 1-082 3,4-Cl2 Cf, CF3 CF,3 CF'3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 QF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CHaPh CH2CF3 CH^Ph CH2CF3 CHgPh CH2CF3 CH2Ph CHzPh CH2CF3 CH2CF3 CHgPh CH2CF3 CHsPh CH2CF3 CHaPh CH2CF3 CH2Pr-c CHgPh CH2CF3 CHaPh CH2CF3 CHaPh CH2CF3 CHgPh CH2(D-47a) Et n-Pr i-Pr n-Bu CHgPr-c s-Bu t-Bu c-Bu n-Pen CH2BU-S CH2Bu-t CH(CH3)Pr-n c-Pen n-Hex c-Hex CHgHex-c CH2(T-39) CH2CH2CI CH2CF3 CH2CF2CF2CF3 CH2CH(CH3)OH(R) 481.47 481.94 459.38 459.90 467.48 467.94 461.31 461.82 469.41 469.86 488.50 488.87 449.42 449.89 449.42 449.89 444.33 444.89 458.35 458.82 466.45 466.81 _458.35 458.80 466.45 466.86 488.38 488.89 496.48 496.92 492.41 492.81 424.36 424.91 460.40 460.87^ 452.30 452.84 460.40 460.89 468.75 468.76 476.85 476.80 485.21 484.79. 1 492.82 2 493.84 431.24 430.93 445.27 444.94 445.27 444.94 459.29 458.97 457.28 456.94 459.29 458.93 459.29 458.92 457.27 456.79 473.32 473.02 473.32 472.82 473.32 472.94 473.32 472.94 471.31 470.99 487.35 486.96 485.33 484.93 499.35 498.88 539.42 538.88 465.69 464.73 485.21 484.85 585.23 584.65 461.26 460.78 1-083 3,4-Cl2 CFg CH2CH(CH3)OH(S) 461.26 460.82 1-084 3,4-Cl2 CFg CH2CH(CH3)OC(0)NHEt(S) 532.34 531.78 1-085 3,4-C!2 CF3 CH(CH3)CH20CH3 475.29 474.94 1-086 3,4-Cl2 CFg' CH2CH(Et)OH 475.29 474.82 1-087 3,4-C!2 CF3 CH(Et)CH20CH3 489.32 488.95 1-088 3,4-Cl2 CF:, CH2CH(OCH3)2 491.29 490.80 1-089 3,4-Cl2 CF3 CH2CH2CH2OH 461.27 460.97 1-090 3,4-Cl2 CFg CH2CH2CH2OCH3 475.29 474.98 • 1-091 3,4-Cl2 CF3 CH2(T-13) 515.35 514.80 1-092 3,4-Cl2 CFg CH2(E-11c) 517.33 516.79 1-093 3,4-Cl2 CF3 CH2CH2SCH3 477.33 476.75 1-094 3,4-Cl2 CF3 CHsCHgSBu-t 5J9.41 518.96, 1-095 3,4-Cl2 CFg CHsCHsCHgSCHg 491.35 490.92' 1-096 3,4-Cl2 CFg CH2CH2NHC(0)OBu-t 546.37 545.75 1-097 3,4-Cl2 CF3 CH2CH2CH2Si(OCH3)3 565.44 564.77 1-098 3,4-Cl2 CFg CH2CH2CH2Si(CH3)(OEt)2 577.49 576.79 1-q99 3,4-Cl2 CFg CH2C(0)OCH3 475.25 474.89 1-100 3,4-Cl2 CFg CH2CH2C(0)OCH3 489.28 488.80 1-101 3,4-Cl2 CF3 CH2C(0)NH2 460.24 459.74 1-102 3,4-Cl2 CF3 .CH2CH=CH2 443.25 442.81 1-103 3,4-Cl2 CF3 CH2CH2(T-17) 511.36 510.76 1-104 3,4-Cl2 CF3 CHgC^CH 441.24 440.91 1-105 3,4-Cl2 CF3 CHaPh 493.31 492.86 1-106 3,4-Ci2 CFg CH2(Ph-2-F) 511.30 510.80 1-107 3,4-Cl2 CFg CH2(Ph-3-F) 511.30 510.81 1-108 3,4-Cl2 CFg CH2(Ph-2-CI) 527.75 526.74 1-109 3,4-Cl2 CFg CH2(Ph-3-CI) 527.75 526.75 1-110 3,4-Cl2 CF3 CH2(Ph-2-CH3) 507.33 506.78 1-111 3,4-Cl2 CFg CH2(Ph^-CH3) 507.33 506.73 1-112 3,4-Cl2 CFg CH2(Ph-4-Bu-t) 549.41 548.77 1-113 3,4-Cl2 . CFg CH2(Ph-2-CF3) 561.30 560.72 1-114 •3,4-Cl2 CFg CH2(Ph-3-CF3) 561.30 560.69 1-115 3,4-Cl2 CFg CH2(Ph-4-CF3) 561.30 560.97 1-116 3,4-Cl2 CFg CH2(Ph-2-OCH3) 523.33 522.77 1-117 3,4-Cl2 CFg CHgCPh-S-OCHg) 523.33 522.74 1-118 3,4-Cl2 CFg CHglPh^-OCHg) ' 523.33 522.68 1-119 3,4-Cl2 CFg CH2(Ph-3-OCF3) 577.30 576.69 1-120 3,4-Cl2 CFg CH2(Ph^-S02CH3) 571.40 570.71 1-121 3,4-Cl2 CFg CH2[Ph-*-N(CH3)2] 536.37 535.81 1-122 3,4-Cl2 CF3 CH2(Ph-3-N02) 538.30 537.64 1-123 3,4-Cl2 CF3 CH2(Ph-4-N02) 538.30 537.66 1-124 3,4-Cl2 CF3 CH2[Ph^-C(0)OCH3] 551.34 550.74 1-125 3,4-Ci2 CF3 CH2(Ph-2,5-F2) 529.29 528.72 1-126 3,4-Cl2 CF3 CH2(Ph-2,6-F2) 529.29 528.81 1-127 3,4-Cl2 CF3 CH2(Ph-3,5-F2) 529.29 528.73 1-128 3,4-Cl2 CF3 CH2(Ph-3-CW-F) 545.74 544.67 1-129 3,4-Cl2 CF3 CH2(Ph-2,3-C!2) 1-130 3,4-C!2 CF3 CH2(Ph-2,4-Cl2) 1-131 3,4-Cl2 CF3 CH2(Ph-2,5-Cl2) 1-132 3,4-Cl2 CF3 '. CH2(Ph-2,6-Cl2) 1-133 3,4-Cl2 CF3. CH2(Ph-3,5-Ci2) 1-134 3,4-Cl2 CF3 CH2(Ph-3-CF3^-F) 1-135 3,4-Cl2 CF3 " CH2[Ph-3,4-(OCH3)2] 1-136 3,4-Cl2 CF3 CH2(Ph-3-OCH20-4) 1-137 3,4-Cl2 CF3 CH2(1-Naph) 1-138 3,4-Cl2 CF3 CH(CH3)Ph 1-139 3,4-Cl2 CF3 CH(CH3)(Ph-3-CI) 1-140 3,4-C!2 CF3 C(CH3)2Ph 1-141 3,4-Cl2 CF3 CHaCHjPh 1-142 3,4-Cl2 CF3 CH2CH2(Ph^OPh) 1-143 3,4-Cl2 CF3 CH2CH(CH3)Ph 1-144 3,4-Cl2 CF3 CHgCHPhs 1-145 3,4-C(2 CF3 CH(CH3)CH2(Ph^-CI) 1-146 3,4-Cl2 CF3 T-9 1-147 3,4-Cl2 CF3 CHgCHjCHgPh 1-148 3,4-Cl2 CF3 CH2CH2SCH2Ph 1-149 3,4-Cl2 CF3 CHsCCOKPh^-OCHg) 1-150 3,4-Cl2 CF3 CH2(D-1c)CH3 1-151 3,4-Cl2 CF3 CH2(D-3a) 1-152 3,4-Cl2 CF3 CH2(D-3b)CH3 1-153 3,4-Cl2 CF3 CH2(D^7a) 1-154 3,4-Cl2 CF3 CH^iDAlf) 1-155 3,4-Cl2 CF3 CH2(D-48a) 1-156 3,4-Cl2 CF3 CH2(D^9a) 1-157 3,4-Cl2 CF3 CH2(D-53b)CH3 1-158 3,4-Cl2 CF3 CH2CH2(D-3a) 1-159 3,4-Cl2 CF3 CH2CH2(D-47a) 1-160 3,4-Cl2 CF3 CH2CH2(D^8a) 1-161 3,4-Cl2 CF3 CH2CH2CH2(D-24a) 1-162 3,4-Cl2 CF3 T-21 1-163 3,4-Cl2 CF3 T-22 1-164 3,4-Cl2 CF3 (D-8b)CH3 ' 1-165 3,4-Cl2 CF3 D-llc 1-166 3,4-Cl2 CF3 D-21a 1-167 3,4-Cl2 CF3 (D-21b)CH3 1-168 3,4-Cl2 CF3 (D-21c)CH3 1-169 3,4-Cl2 CF3 (D-21c)N02 1-170 3,4-Cl2 CF3 D-25d 1-171 3,4-C!2 CF3 D^8a 1-172 3,4-Cl2 CF3 D-49a 1-173 3,4-Cl2 CF3 OPr-n 1-174 3,4-Cl2 CF3 N(CH3)2 562.20 560.72 562.20 560.72 562.20 560.72 562.20 560.73 562.20 560.64 579.29 578.70 553.36 552.76 537.31 536.73 543.36 542.80 507.34 506.88 541.78 540.70 52J.37 520.99 5Q7.34 507.01' 599.44 598.95 521.37 520.93 583.43 582.79 555.81 554.78 519.35 518.88 521.37 520.97 553.43 552.75 551.34 550.66 497.29 496.80 499.33 498.70 513.36 512.74 494.29 493.84 596.74 595.79 494.29 493.84 494.29 493.86 509.31 508.78 513.36 512.71 508.32 507.76 508.32 507.77 .511.32 510.84 472.24 471.77 488.31 487.72 484.25 483.75 581.35 580.66 486.29 485.70 500.32 499.70 500.32 499.70 531.29 530.60 533.33 532.73 480.27 479.76 480.27 479.76 461.27 460.94 446.26 445.92 1-175 3,5-Cl2 CF3 CH^Pr-c 1-176 3,5-Cl2 CF3 CH2CH2CF3 1-177 3,5-Ci2 CF3, CHaCHsOEt 1-178 35-CI2 CF3 '. CH2CH2OCH2CH2OH 1-179 * 3,'5-C!2 CF3 CH2CH(CH3)OH 1-180 3,5-Cl2 CFV CH2CH2CH20Et 1-181 3,5-Cl2 CF3 ' CH2CH2CH20Pr-i 1-182 3,5-Cl2 CF3 CH2CH2SEt 1-183 3,5-Cl2 CF3 CH2(Ph-3-Br) 1-184 3,5-Cl2 CF3 CH2(Ph-3-OCH3) 1-185 3,5-Cl2 CF3 CH2(Ph^-OCH3) 1-186 3,5-Cl2 CF3 CHsCPh^-OCFg) 1-187 3,5-Cl2 CF3 CH2(Ph-4-S02NH2) 1-188 3,5-Cl2 CF3 CH2(Ph-3-N02) 1-189 3,5-Cl2 CF3 CH2(Ph^-N02) 1-190 3,5-Cl2 CF3 CH2CH2(Ph-3-CI) 1-191 3,5-Cl2 CF3 CH2CH2(Ph^-OCH3) 1-1^2 3,5-Cl2 CF3 CH2CH2(Ph-3,4-Cl2) 1-193 3,5-Cl2 CF3 CH2CH2[Ph-3,4-(OCH3)2] 1-194 3,5-Cl2 CF3 CH2CH20Ph 1-195 3,5-Cl2 CF3 Ph-4-OCH3 1-196 3,5-Cl2 CF3 (D-21b)CH2C(0)OEt 1-197 3,5-Cl2 CF3 (D-21c)Br 1-198 3,5-Ci2 CF3 (D-21c)S02(Ph^-N02) 1-199 3,5-Cl2 CF3 D-21d 1-200 3,5-Cl2 CF3 D-21e 1-201 3,5-Cl2 CF3 D-21f 1-202 3,5-Cl2 CF3 D-21g 1-203 3,5-Cl2 CF3 D-21h 1-204 3,5-Cl2 CF3 D-21i 1-205 3,5-Cl2 . CF3 D-21J 1-206 3,5-Cl2 CF3 NHPh 1-207 3,5-Br2 • CF3 CH2CF3 1-208 3,5-Br2 CF3 CHgPh 1-209 S-CHg^-F CF3 CH2Ph 1-210 3,4-(CH3)2 CF3 CH2CF3 1-211 3,4-(CH3)2 CF3 CHzPh 1-212 3,5-(CH3)2 CF3 CH2CF3 1-213 3,5-(CH3)2 CF3 CHsPh 1-214 3,5-(CF3)2 CF3 , CH2CF3 1-215 3,5-(CF3)2 CF3 •CH2Ph 1-216 3-OEt-4-CI CF3 CH2CF3 1-217 3-OEt-4-Cl CF3 CHgPh 1-218 3,4-(OCH3)2 CF3 CH2CF3 1-219 3,4-(OCH3)2 CF3 CHaPh 1-220 3-OCH20^ CF3 CHzPr-c 457.27 456.83 499.23 498.79 475.29 474.86 491.29 490.78 461.27 460.88 489.31 488.90 503.34 502.86 491.35 490.99 572.20 570.68 523.33 522.80 523.33 522.74 5Z7.30 576.75 ^ 572.38 571.78 538.30 537.76 538.30 537.76 541.78 540.71 537.36 536.79 576.22 574.60 567.38 566.77 523.33 522.85 509.30 508.75 572.38 571.70 565.19 563.59 671.45 670.55 514.35 513.72 536.35 535.70 570.80 569.68 570.80 569.68 566.38 565.71 566.38 565.76 581.35 580.69 494.29 493.81 574.11 572.49 582.21 580.61 456.43 456.87 444.37 444.89 452.47 452.94 444.37 444.86 452.47 452.95 552.31 552.72 560.41 560.76 494.81 494.76 502.91 502.81 476.37 476.83 484.47 484.90 432.39 432.89 1-221 3-OCH20^ CF3 CH2Ph 468.42 468.86 1-222 3,5-(CHO)2 CF3 CH2CF3 472.34 472.92 1-223 3-CH=CHCH=CH^ CF3 CH2CF3 466.38 466.83 1-224 3-CH=CHCH=CH^ CF3 CH2Ph 474.47 474.86 1-225 3,4,5-F3 CF3, CH2CF3 470.29 470.77 1-226 3,4,5-F3 CF. CHgPh 478.39 478.82 Table 8 4 c 2 " No. (XL (Y)„ R' R' Mw M++H ; _-__ J 2-001 3,4-F2 - CH3 CH2Ph 474.42 474.88 2-002 3,4-Cl2 - CH3 CH3 431.24 430.91 2-003 3,4-Cl2 - Et Et 459.29 458.94 2-004 3,4-Cl2 - CH3 n-Bu 473.32 472.97 2-005 3,4-Cl2 - CH3 i-Bu 473.32 472.89 2-006 3,4-Cl2 - -CH2CH2CH2CH2- 457.28 456.85 2-007 3,4-C!2 - -CH2CH2CH2CH2CH2- 471.31 470.84 2-008 3,4-Cl2 - -CH2CH2CH2CH2CH(CH3)- 485.33 484.83 2-009 3,4-Cl2 - -CH2CH2CH2CH(CH3)CH2- 485.33 484.82 2-010 3,4-Cl2 - -CH2CH(CH3)CH2CH(CH3)CH2- 499.35 498.82 2-011 3,4-Cl2 - -CH2CH2OCH2CH2- 473.28 472.75 2-012 3,4-Cl2 - -CH2CH(CH3)OCH(CH3)CH2- 501.33 500.77 2-013 3,4-Cl2 - -CH2CH2SCH2CH2- 489.34 488.74 2-014 3,4-Cl2 - -CH2CH2N(CHO)CH2CH2- 500.30 .499.76 2-015 3,4-Cl2 - CH3 CH2CH=CH2 457.27 456.87 2-016 3,4-Cl2 - CH2CH=CH2 CH2CH=CH2 483.31 482.85 2-017 3,4-Cl2 - CH3 CH2C=CH 455.26 454.86 2-018 3,4-Cl2 - CH3 CH2P.h 507.34 506.93 2-019 3,4-Cl2 - Et CH2(D^8e)CI 556.79 555.73 2-020 3,5-Ci2 - Et Et 459.29 458.85 2-021 3,5-Cl2 " CH3 CH2Ph 507.33 506.79 2-022 3,5-Cl2 - Et CH2Ph 521.36 520.79 2-023 3,5-Cl2 - CHjPh CHgPh 583.43 582.79 2-024 3,5-Cl2 2-CH3 H CH2CH2OH 461.26 460.99 2-025 3,5-Cl2 2-CH3 H CH2CH20Fr-n 503.34 502.99 2-026 3,5-Cl2 2-CH3 H CHsCHgOPr-i 503.34 502.98 2-027 3,5-Cl2 2-CH3 H CH2CH2OCH2CH2OH 505.31 504.95 2-028 3,5-Cl2 2-CH3 H CH2CH20Ph 537.36 536 94 2-029 3,5-Cl2 2-CH3 H CH(CH3)CH20CH3 489.31 488.98 2-030 3,5-Cl2 2-031 3,5-Cl2 2-032 3,5-Cl2 2-033 3,5-Cl2 2-034 3,5-Cl2 2-035 3,5-Cl2 2-036 3,5-Cl2 2-037 3,5-Cl2 • 2-038 3,5-Cl2 2-039 3,5-Cl2 2-040 3,5-Cl2 2-041 3,5-Cl2 2-042 3,5-Cl2 2-043 3,5-Cl2 2-044 3,5-Cl2 2-045 3,5-Cl2 2-046 3,5-Cl2 2-ci47 3,5-CI, 2-048 3,5-C!2 2-049 3,5-Cl2 2-050 3,5-Cl2 2-051 3,5-Cl2 2-052 3,5-Cl2 2-053 3,5-Cl2 2-054 3,5-Cl2 2-055 3,5-Cl2 2-056 3-OCH20^ 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 , H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H 2-CH3 H ¬ CH3 CH2CH2N(CH3)2 488.33 487.98 CH(Ph)C(0)0CH3(R) 565.37 564.84 CH(Ph)C(0)0CH3(S) 565.37 564.92 CH2CH2C(0)OCH3 503.30 502.91 CH2(Ph^-OCH3) CH2(Ph-4-CN) CH2CH2(D^7a) T-29b NHCH2C(0)0Et NHCHO NHC(0)CH2(D-3a) N(CH3)C(S)NH2 N(CH3)C(S)NHCH3 T-40 NH(Ph-2-F) NH(Ph-3-F) NH(Ph^-F) NH(Ph^-Br) NH(Ph^-CH3) NH(Ph-4-Pr-i) NH(Ph-4-OCF3) NH(Ph-4-CN) N(CH3)(D-47d)CF3 N=CHC(CH3)=CHPh D-47a D-49a 537.36 536.98 532.34 531.94 522.35 521.94 562.32 559.80* 518.31 517.93 460.23 457.86* 556.38 553.71* 505.34 504.82 , 519.37 518.88 530.37 529.98 526.31 525.92 526.31 525.92 526.31 523.89* 587.22 585.91 ^ 522.35 521.93 550.40 549.94 592.32 591.97 533.33 533.01 591.33 590.99 560.39 559.95 494.29 493.94 494.29 493.&7 CHgPh 482.45 482.86 In Table above, the indication of "*"shows the measured value of molecular ion peak of M+H measured with negative mode. Table 9 ^VCX II I H 4 r II 5 O No. (X)„ R' R' m.p.fC) 3-001 - CF3 CH2CF3 172.0-173.0 3-002 3-CI CF3 CH2CF3 157.0-158.0 3-003 3-CI CF3 CH2Ph 168.0-169.0 3-004 4-CI CF3 CH2CF3 190.0-191.0 3-005 4-Cl CF3 CH2Ph 212.0-214.0 325 3-006 3-Br CF3 CH2CF3 132.0-135.0 3-007 3-OCF3 CF3 CH2(D-47a) 145.0-147.0 3-008 3-OCH2Ph CF3 CH2CF3 146.0-149.0 3-009 3-OCH2(Ph-2-CI) CFgl CH2CF3 158.0-159.0 3-010 3-OCH2(Ph-2-CI) CF3 CH2(D-47a) *1 3-011 3-SEt Ce^ CH2CF3 105.0-106.0 3-012 3-CN CFg" CH2CF3 93.0-96.0 3-013 4-CN CF3 CH2CF3 149.0-151.0 3-014 3-CH=N0H CF3 CH2CF3 168.0-169.0 3-015 3-CH=NOCH3 CF3 CH2CF3 *1 3-016 4-C(CH3)=NOCH3(E)CF3 CH2CF3 160.0-162.0 3-017 4-C(CH3)=NOCH3(Z)CF3 CH2CF3 ^ *1 3-018 3,4-F2 CF3 CH2CF3 -150.0-152.0 3-019 2,4-Cl2 CF3 CH2CF3 149.0-151.0 3-020 3,4-Cl2 H CH2CF3 161.0-162.0 3-021 3,4-Cl2 H CH2Ph 147.0-148.0 3-022 3,4-Cl2 CH3 CHaPr-c 157.0-158.0 3-023 3,4-Cl2 CH3 CH2CF3 120.0-122.0 3-024 3,4-Cl2 CH3 CH2ph 153.0-155.0 3-025 3,4-Cl2 CF3 CH3 139.0-140.0 3-026 3,4-Cl2 CF3 c-Pr 193.0-194.0 3-027 3,4-Cl2 CF3 i-Bu 158.0-159.0 3-028 3,4-Cl2 CF3 CH2BU-C 177.0-179.0 3-029 3,4-Cl2 CF3 CH2CH(Et)Bu-n 125.0-127.0 3-030 3,4-Cl2 CF3 CH2CF2CF3 171.0-173.0 3-031 3,4-Cl2 CF3 CH2(E-4a) 136.0-138.0 3-032 3,4-Cl2 CF3 CH(CH3)CH2SCH3 145.0-147. 3-033 3,4-Cl2 CF3 C(CH3)2CH2SCH3 150.0-152.0 3-034 3,4-Cl2 CF3 C(CH3)2CH2S(0)CH3 *1 3-035 3,4-Cl2 CF3 C(CH3)2CH2S02CH3 161.0-163.0 3-036 3,4-Cl2 CF3 CH2CH2CH2C(0)OEt 105.0-107.0 3-037 3,4-Cl2 CF3 CH2(Ph-4-F) 155.0-156.0 3-038 3,4-Cl2 CF3 CH2(Ph^-CI) 191.0-193.0 3-039 3,4-Cl2 CF3 CH2(Ph-3-CH3) 198.0-200.0 3-040 3,4-Cl2 CF3 CH2(Ph-3,4-Cl2) 161.0-162.0 3-041 3,4-Cl2 CF3 CH2CH(Ph)0H ' 211.0-213.0 3-042 3,4-Cl2 CF3 CHgCpXPh^-Br) 193.0-195.0 3-043 3,4-Cl2 CF3 CH2(D-1a) ¬ 179.0-180.0 3-044 3,4-Cl2 CF3 CH2(D^8e)Cr 154.0-157.0 3-045 3,4-Cl2 CF3 CH2(D-50d) 183.0-186.0 3-046 3,4-Cl2 CF3 CH2CH2(D^9a) 113.0-116.0 3-047 3,4-Cl2 CF3 NHPh 160.0-162.0 3-048 3,4-Cl2 CF3 Ph 208.0-210.0 3-049 3,4-Cl2 CF3 Ph-2-CH3^-C! 237.0-238.0 3-050 3,4-Cl2 CF3 D-35a 238.0-241.0 3-051 3,4-Cl2 CF3 D^7a 167.0-169.0 326 3-052 3,4-Cl2 CN CHgCFg 162.0-164.0 3-053 3,4-C!2 Ph CHgPr-c 153.0-154.0 3-054 3,4-Cl2 Ph CH2CF3 157.0-158.0 3-055 3,4-Cl2 Ph ' CHgPh 173.0-175.0 3-056 3,5-Cl2 c-Pr CH2CF3 144.0-145.0 3-057 3,5-Cl2 CF^_ • H 256.0-258.0 3-058 3,5-Cl2 CF3 " i-Bu 167.0-170.0 3-059 3,5-Cl2 CF3 CH2CI *1 •3-060 3,5-Cl2 CF3 CH2CF3 94.0-96.0 3-061 3,5-Cl2 CF3 CH2(T-4) 84.0-87.0 3-062 3,5-C(2 CF3 CH2OH 254.0-260.0 3-063 3,5-Ci2 CF3 CH2CH(OCH3)2 _ 198.0-200.0 3-064 3,5-Cl2 CF3 CH2CH(OEt)2 ~ *1 3-065 3,5-Cl2 CF3 CH2CH(CH3)OC(0)NHEt 127.0-129.0 3-066 3,5-Cl2 CF3 CH2CH(CH3)OC(0)NH(Ph-4-F) 162.0-165.0 3-067 3,5-Cl2 CF3 CH2CH(OH)CH20H *1 3-0§8 3,5-Cl2 CF3 CH2(E^a) 123.5-126.0 3-0o9 3,5-Cl2 CF3 CH2(E-5a) *1 3-070 3,5-Cl2 CF3 CH2(E-10a) 152.0-153.0 3-071 3,5-Cl2 CF3 CH2(E-10b)CH3 151.0-153.0 3-072 3,5-Cl2 CF3 CH2(E-32a) *1 3-073 3,5-Cl2 CF3 C(CH3)2CH2SCH3 91.0-92.0 3-074 3,5-Cl2 CF3 C(CH3)2CH2S02CH3 *1 3-075 3,5-Cl2 CF3 CH2(E-18a) 124.0-126.0 3-076 3,5-Cl2 CF3 CH2(E-18c) 253.0-255.0 3-077 3,5-Cl2 CF3 CH2CHO *1 3-078 3,5-Cl2 CF3 CH2CH=N0H *1 3-079 3,5-Cl2 CF3 CH2CH=NOCH3 *1 3-080 3,5-Cl2 CF3 CH2C(CH3)=NOCH3 71.0-75.0 3-081 3,5-Cl2 CF3 CH2CN 145.0-151.0 3-082 3,5-Cl2 CF3 CH2C(0)0H *1 3-083 3,5-Cl2 CF3 CH2C(0)OCH3 *1 3-084 3,5-Cl2 = CF3 CH2C(0)NH2 . 100.0-107.0 3-085 3,5-Cl2 CF3 CH2C(0)NHCH2CH2CI 161.5-165.0 3-086 3,5-Cl2 CF3 CH2C(0)NHCH2CF3 108.0-114.0 3-087 3,5-Cl2 CF3 CH2C(S)NH2 ' *1 3-088 3,5-Ci2 CF3 CH2C(=NOH)NH2 • HCI 140.0-144.5 3-089 3,5-Cl2 CF3 CH2CH=CH2¬ *1 3-090 3,5-Cl2 CF3 CH2C(CH3)=CH2 133.0-136.0 3-091 3,5-Cl2 CF3 CH2CCNCH2 121.0-123.0 3-092 3,5-Cl2 CF3 CH2CH=CCl2 118.0-120.0 3-093 3,5-Cl2 CF3 CH2CC1=CHC1 153.0-154.0 3-094 3,5-Cl2 CF3 CH2C=CH 144.0-146.0 3-095 3,5-Ci2 CF3 CH2Ph 174.0-177.0 3-096 3,5-Cl2 CF3 CH2(Ph-4-Br) 203.0-205.0 3-097 3,5-C!2 CF3 CH2(Ph-4-SCH3) 182.0-184.0 327 3-098 3,5-Cl2 CFg CH2[Ph-4-S(0)CH3] 170.0-174.0 3-099 3,5-Cl2 CF3 CH^iPh-ASO^CHs) 214.0-216.0 3-100 3,5-Cl2 CFg CH2(Ph-2-N02) 165.0-167.0 3-101 3,5-Cl2 CF3 • CH2(D-1a) 178.5-181.0 3-102 3,5-C!2 CF3 CH2(D-3a) 201.0-202.0 3-103 3,5-Cl2 CFg CH2(D-3d)CI 144.0-146.0 3-104 3,5-Cl2 CF3 ~ CH2(0-1 Ob)CI 87.0-95.0 3-105 3,5-Cl2 CF3 CH2(D-15a)CH3 154.0-155.0 3-106 3,5-Cl2 CF3 CH 2(0-16b)CI 224.0-225.0 3-107 3,5-Cl2 CF3 CH2(0-16c)CI *1 3-108 3,5-Cl2 CF3 CH2(D-16d) *1 3-109 3,5-C!2 CF3 CH2(0-17a)CH3 _^ 59.0-61.0 3-110 3,5-Cl2 CF3 CH2(D-17b)CI ~ *1 3-111 3,5-Cl2 CF3 CH 2(0-21 a) 178.0-179.0 3-112 3,5-Cl2 CF3 CH2(D-22a) 156.0-158.0 3-113 3,5-Cl2 CF3 CH2(D-22b)CI 94.0-96.0 3-1,14 3,5-Cl2 CF3 CH2(D-22b)CH3 *1 3-115 3,5-Cl2 CF3 CH2(0-23a) 191.0-193.0 3-116 3,5-Cl2 CF3 CH2(D-23b)Cl 165.0-167.0 3-117 3,5-Cl2 CF3 CH2(0-24b) 218.0-220.0 3-118 3,5-Cl2 CF3 CH2(D-24c) *1 3-119 3,5-02 CF3 CH2(D-25a)CH3 *1 3-120 3,5-Cl2 CF3 CH2(0-27a)CH3 *1 3-121 3,5-Cl2 CF3 CH2(0-29b)CH3 *1 3-122 3,5-Cl2 CF3 CH2(0-34a) *1 3-123 3,5-Cl2 CF3 CH2(D-35a) 157.5-161.0 3-124 3,5-Ci2 CF3 CH2(D-38a) 224.5-226.0 3-125 3,5-Cl2 CF3 CH2(D-47a) 150.0-151.0 3-126 3,5-Cl2 CF3 CH2(0-47c)CI 124.0-126.0 3-127 3,5-Cl2 CF3 CH2(D-47e)CH3 *2 3-128 3,5-Cl2 „ CF3 CH2(D^7i) 121.0-124.0 3-129 3,5-Cl2 CF3 CH2(D-48e)Cl 159.5-163.0 3-130 3,5-Cl2 CF3 CHsP-SOd) 250.0-255.0 3-131 3,5-Cl2 CF3 CH2(D-53b)CH3 *1 3-132 3,5-Cl2 CF3 CH(CH3)Ph 137.5-141.0 3-133 3,5-Cl2 CF3 C(0)(D-47a) *1 3-134 3,5-Cl2 CF3 OCH3 *1 3-135 3,5-Cl2 CF3 NH(0-47a) *1 3-136 3,5-Cl2 CF3 NH(O-50a) 202.0-204.0 3-137 3,5-Cl2 CF3 NH(O-50b)CF3 146.0-149.0 3-138 3,5-Cl2 CF3 NH(D-54b)CI 124.0-130.0 3-139 3,5-Cl2 CF3 N(CH3)Ph 174.0-178.0 3-140 3,5-Cl2 CF3 D-21a 268.0-273.0 3-141 3-CH3-i-F CF3 CH2CF3 151.0-152.0 ^ 3-142 3-CI-5-CH3 CF3 CH2CF3 74.0-76.0 3-143 3-CI-5-CH3 CF3 CH 2(0-473) *1 328 3-1443-145162.0 3-1463-1473-148 3-C!-4-OCH3 3-CF3-5-OCH3 3-OCH20^ 2-F-3-CH3-5-CI 3,5-Cl2 CF , CF3 CFl CF3 CF3 ^ CH2CF3 CH2CF3 CH2CF3 CH2CF3 CH2(D-34b)CH3 135.0-138.0 161.0¬ 149.0-151.0 *1 143.0-144.5 Table 10 \L^ \-^^C R^ 5 No, (XL R^ 4-001 3,4-Cl2 CF3 4-002 3,4-Cl2 CF3 4-003 3,5-Cl2 CF3 4-004 3,5-Ci2 CF3 4-005 3,5-C!2 CF3 4-006 3,5-Cl2 CF3 4-007 3,5-Cl2 CF3 4-008 3,5-Cl2 CF3 4-009 3,5-Cl2 CF3 4-010 3,5-Cl2 CF3 4-011 3,5-Ci2 CF3 Table 11 O R^ R^ m.p. (°C) -CH2CH2CH(CH3)CH2CH2- 132.0-134.0 -CH2CH2CH2CH2CH2CH2- 160.0-163.0 CH2OCH3 CH2(D-47a) *1 CHsOEt CH2(D-47a) *1 CH2SO2CH3 CH2(D-47a) *1 CH2CH=CH2 CH2(D-47a) *1 CH(C'H=CH2)CH2CH=CH2 CH2(D-47a) *1 CHsPh C(0)0CH3 Et CH3 R!/^"N C (Y) \l_j/ J ^-^^C R^ 5 ^ O No. (XL R' (Y)„ 5-001 3-Cl CF3 2-CH3 5-002 3-Br CFg 2-CH3 5-003 3-Br CF3 2-CH3 5-004 3-1 CF3 2-CH3 5-005 3-1 CF3 2-CH3 5-006 4-1 CF3 2-CH3 329 CH2(D-47a) *1 CH2(D^7a) *1 CH2(D^8e)CI *1 OCH3 *1 R^ m.p.(°C) CH2(D-47a) *1 CH2CF3 158.5-161.0 CH2(D-47a) *1 CH2CF3 168.0-172.5 CH2(D-47a) 135.5-138.0 CH2CF3 134.0-135.0 5-007 4-1 CFg 2-CH3 CH2(D^7a) *1 5-008 3-CF3 CF3 2-CH3 CH2CF3 135.5-137.5 5-009 3-CF3 CF3 2-CH3 CH2(D^7a) *1 5-010 3-(T-4) CF3 2-CH3 CH2CF3 *2 5-011 3-(T-4) CF3 2-CH3 CH2(D-47a) *2 5-012 3-OCF3 CF3 ,. 2-CH3 CH2CF3 *2 5-013 3-OCF3 CF3 2'CH3 CH2(D^7a) *1 5-014 S-OCFaBr CF3 2-CH3 CH2CF3 *1 5-015 3-OCF2Br CF3 2-CH3 CH2(D^7a) *2 5-016 3-OCF2CHFOCF2CF2CF3 CF3 2-CH3 CH2CF3 *1 5-017 3-OCF2CHFOCF2CF2CF3 CF3 2-CH3 CH2(D-47a) *1 5-018 3-OCH2(Ph-2-Cl) CF3 2-CH3 CH2(D-47a) _ *1 5-019 3-0(D^7f) CF3 2-CH3 CH2CF3 ~ *1 5-020 3-O(D^70 CF3 2-CH3 CH2(D-47a) *1 5-021 3-SEt CF3 2-CH3 CH2(D^7a) *1 5-022 3-SCF3 CF3 2-CH3 CH2CF3 *1 5-023 3-SCF3 CF3 2-CH3 CH2(D-47a) *1 5-024 3-N(CH3)C(0)CF3 CF3 2-CH3 CH2CF3 *1 ' 5-025 3-N(CH3)C(0)CF3 CF3 2-CH3 CH2(D^7a) *1 5-026 3-N(CH3)S02CF3 CF3 2-CH3 CH2CF3 *1 5-027 3-N(CH3)S02CF3 CF3 2-CH3 CH2(D-47a) *1 5-028 3-Ph CF3 2-CH3 CH2(D^7a) *1 5-029 3,5-F2 CF3 2-CH3 CH2(D^7a) *1 5-030 3,5-Cl2 CH3 2-CH3 CH2CF3 *1 5-031 3,5-Cl2 i-Pr 2-CH3 CH2CF3 *1 5-032 3,5-Cl2 c-Pr 2-CH3 CH2CF3 157.0-158.0 5-033 3,5-Cl2 c-Pr 2-CH3 CH2(D^7a) *1 5-034 3,5-Cl2 CH2CI 2-CH3 CH2CF3 117.0-119.0 5-035 3,5-Cl2 CH2CI 2-CH3 CH2(D^7a) *1 5-036 3,5-Cl2 CHF2 2-CH3 CH2CF3 94.0-97.5 5-037 3,5-Cl2 > CHF2 2-CH3 CH2(D^7a) *1 5-038 3,5-Cl2 CF3 2-F CH2CF3 *1 5-039 3,5-Cl2 CF3 2-F CHzPh . 172.0-176.0 5-040 3,5-Cl2 CF3 2-F CH2(D-22a) *1 5-041 3,5-Cl2 CF3 2-F CH2(D-47a) 126.0-129.0 5-042 3,5-C!2 CF3 3-F CH2CF3 ' *1 5-043 3,5-Cl2 CF3 3-F CHgPh 178.0-181.0 5-044 3,5-Cl2 CF3 3-F CH2(D^7a) 125.0-127.0 5-045 3,5-Cl2 CF3 2-CI CHaPr-c" 132.0-134.0 5-046 3,5-Cl2 CF3 2-CI CH2CF3 124.0-125.0 5-047 3,5-Cl2 CF3 2-CI CHgPh 57.0-58.0 5-048 3,5-Cl2 CF3 2-CI CH2(Ph-1-N02) *1 5-049 3,5-Cl2 CF3 2-CI CH2(D-21a) *1 5-050 3,5-Cl2 CF3 2-CI CH2(D-22a) *1 5-051 3,5-Cl2 CF3 2-CI CH2(D-22b)Cl *2 5-052 3,5-Cl2 CF3 2-CI CH2(D-28a) *1 5-053 3,5-Ci2 CFg 2-Ci CH2(D-47a) *1 5-054 3,5-Cl2 CF3 3-Cl CH^CFg 149.0-150.0 5-055 3,5-Cl2 CF3 3-Cl CHgPh 119.0-121.0 5-056 3,5-Cl2 CF3 • 3-Ci CHalD^Ta) *1 5-057 3,5-Cl2 CF3 2-Br CH2CF3 145.0-147.0 5-058 3,5-Cl2 CF3 -_ 2-Br CH2(D-47a) *1 5-059 3,5-Cl2 CF3 2-1 CH2CF3 128.0-130.0 5-060 3,5-Cl2 CF3 2-1 CH2CH20Et *1 '5-061 3,5-Cl2 CF3 2-1 CH2CH(OCH3)2 *1 5-062 3,5-Cl2 CF3 2-1 CH2C(0)NHCH3 *1 5-063 3,5-Cl2 CF3 2-1 CH2C(0)NHCH2CH2C1 68.0-70.0 5-064 3,5-Cl2 CF3 2-1 CH2CH=CH2 ^ 97.0-100.0 . 5-065 3,5-Cl2 CF3 2-1 CH2(D-47a) ~ *1 5-066 3,5-Cl2 CF3 2-CH3 H *1 5-067 3,5-Cl2 CF3 2-CH3 Et 129.5-133.0 5-068 3,5-Cl2 CF3 2-CH3 c-Pr 84.0-86.0 5-0p9 3,5-Cl2 CF3 2-CH3 i-Bu 138.0-140.0 5-070 3,5-Cl2 CFg 2-CH3 CHsPr-c *1 5-071 3,5-Cl2 CF3 2-CH3 c-Bu 139.0-141.0 5-072 3,5-Cl2 CF3 2-CH3 CH2BU-C *1 5-073 3,5-Cl2 CF3 2-CH3 c-Pen 155.0-158.0 5-074 3,5-Cl2 CF3 2-CH3 CH2CH2CI 161.5-164.5 5-075 3,5-Cl2 CF3 2-CH3 CH2CF3 155.5-157.0 5-075(+) 99%e.e. [a]D''°+74.38° (EtOH, c=0.621) *1 5-075(-) 99%e.e. [a]D'^'-70.98° (EtOH, c=0.648) *1 5-076 3,5-Cl2 CF3 2-CH3 CH2CH2OCH3 115.0-117.0 5-077 3,5-Cl2 CF3 2-CH3 CH2CH20Et *1 5-078 3,5-Cl2 CF3 2-CH3 CH2CH2OCH2CH2CI 140.0-142.0 5-079 3,5-Cl2 CF3 2-CH3 CH2CH20C(0)CH3 *2 5-080 3,5-Cl2 CF3 2-CH3 CH2CH20C(0)NHEt *2 5-081 3,5-Cl2 CFg 2-CH3 CH2CH(CH3)DH 67.0-70.0 5-082 3,5-Cl2 CF3 2-CH3 CHaCHCCHaPCHa 179.0-181.0 5-083 3,5-Cl2 CF3 2-CH3 CH2CH(0CH3)2 *1 5-084 3,5-Cl2 CF3 2-CH3 CH2CH(OEt)2 *2 5-085 3,5-Cl2 CF3 2-CH3 CH(CH3)CH20C(0)NHEt *1 5-086 3,5-Cl2 CF3 2-CH3 CH2(E-4a) *1 5-087 3,5-Cl2 CF3 2-CH3 CH2(E-5a) , *2 5-088 3,5-Cl2 CF3 2-CH3 CH2(E-10a) 158.5-160.5 5-089 3,5-Cl2 CF3 2-CH3 CH2(E-"10b)CH3 153.0-154.0 5-090 3,5-Ci2 CF3 2-CH3 CH2(E-32a) *1 5-091 3,5-Cl2 CF3 2-CH3 CH2CH2SCH3 121.0-127.0 5-092 3,5-Cl2 CF3 2-CH3 CH2CH2S(0)CH3 *1 5-093 3,5-Cl2 CF3 2-CH3 CHgCHgSEt 106.0-109.0 5-094 3,5-Cl2 CF3 2-CH3 CH2CH2S02Et *1 5-095 3,5-Cl2 CF3 2-CH3 CH2CH,SCH2Ph *1 5-096 3,5-Cl2 CF3 2-CH3 CH2CH2S02CH2Ph *1 5-097 3,5-CI, CF3 2-CH3 5-098 3,5-Cl2 CF3 2-CH3 5-099 3,5-Cl2 CF3 2-CH3 5-100 3,5-Cl2 CF3 ' 2-CH3 5-101 3,5-Ci2 CF3 2-CH3 5-102 3,5-Cl2 CF3 :., 2-CH3 5-103 3,5-C!2 CF3 2-CH3 5-104 3,5-Cl2 CF3 2-CH3 •5-105 3,5-Cl2 CF3 2-CH3 5-106 3,5-Cl2 CF3 2-CH3 5-107 3,5-Cl2 CF3 2-CH3 5-108 3,5-Ci2 CF3 2-CH3 5-109 3,5-Cl2 CF3 2-CH3 5-110 3,5-Cl2 CF3 2-CH3 5-111 3,5-Cl2 CF3 2-CH3 5-112 3,5-Cl2 CF3 2-CH3 5-1,13 3,5-Cl2 CF3 2-CH3 5-114 3,5-Cl2 CF3 2-CH3 5-115 3,5-Cl2 CF3 2-CH3 5-116 3,5-Cl2 CF3 2-CH3 5-117 3,5-Cl2 CF3 2-CH3 5-118 3;5-Cl2 CF3 2-CH3 5-119 3,5-Cl2 CF3 2-CH3 5-120 3,5-Ci2 CF3 2-CH3 5-121 3,5-Cl2 CF3 2-CH3 5-122 3,5-Cl2 CF3 2-CH3 5-123 3,5-Cl2 CF3 2-CH3 5-124 3,5-Cl2 CF3 2-CH3 5-125 3,5-Cl2 CF3 2-CH3 5-126 3,5-Cl2 CF3 2-CH3 5-127 3,5-Cl2 ' CF3 2-CH3 5-128 3,5-Cl2 CF3 2-CH3 5-129 3,5-Cl2 CF3 2-CH3 5-130 3,5-Cl2 CF3 2-CH3 5-131 3,5-Cl2 CF3 2-CH3 5-132 3,5-Cl2 CF3 2-CH3 5-133 3,5-Cl2 CF3 2-CH3 5-134 3,5-Cl2 CF3 2-CH3 5-135 3,5-Cl2 CF3 2-CH3 5-136 3,5-Cl2 CF3 2-CH3 5-137 3,5-Cl2 CF3 2-CH3 5-138 3,5-Cl2 CF3 2-CH3 5-139 3,5-Cl2 CF3 2-CH3 5-140 3,5-Cl2 CF, 2-CH3 5-141 3,5-Cl2 CF3 2-CH3 5-142 3,5-Cl2 CF3 2-CH3 CHsCHsSCHaCD-la) *1 CHzCHaSOsCHsCD-la) *1 CH2CH(CH3)SCH3 *1 CH2CH(CH3)S(0)CH3 *1 CH2CH(CH3)S02CH3 *1 CH(CH3)CH2SCH3 *1 CH(CH3)CH2S02CH3 *1 C(CH3)2CH2SCH3 *1 C(CH3)2CH2S02CH3 167.0-169.0 CH2(E-18a) ' ' 204.0-206.0 CH2(E-18c) 249.0-251.0 CH2(E-43a) ^199.0-201.0 CH2CH2NHC(0)CF3 ~ 81.0-84.0 CH2CH2NHC(0)CH2CF3 143.0-146.0 CH2C(0)CH3 155.0-160.0 CH2CH=N0H *1 CH2CH=NOCH3 *2 CH2CH=NOCH2Pr-c *1 CH2CH=NOCH2(Ph-4-CI) *2 CH2CH=NOCH2CH2-TMS *1 CH2C(CH3)=NOCH3 101.0-105.0 CH2(M-5a)CH3 *1 CH2CN 186.5-189.0 CH(OCH2CF3)CN *1 CH(Ph)CN 165.5-167.0 CH(D-1a)CN *1 CH(D-3a)CN *1 CH(D-14a)CN 192.0-194.5 CH(D-38a)CN 185.0-189.5 CH(D^7a)CN *'1 CH2C(0)0H *1 CH2C(0)OCH3 *2 CH2C(0)0CH2CF3 157.0-158.0 CH(CH3)C(0)OCH3(D) *1 CH(CH3)C(0)0Et(L) *1 CH(CH3)C(0)OCH2CF3 *1 CH(0H)C(0)0CH3 *1 CH(OCH3)C(0)OCH3 *1 CH(D-14a)C(0)OCH3 93.5-97.0 CH2CH2C(0)OEt *1 CH2C(0)NH2 87.0-91.0 CH2C(0)NHCH3 *1 CH2C(0)N(CH3)2 *1 CH2C(0)NHEt 137.5-141.0 CH2C(0)NHPr-n *1 CH2C(0)FvJHPr-i 152.0-155.0 5-143 3,5-Cl2 CF3 5-144 3,5-Cl2 CF3 5-145 3,5-Cl2 CF3 5-146 3,5-C!2 CF3 5-147 3,5-Cl2 CF3 5-148 3,5-Cl2 CF3 5-149 3,5-Cl2 CF3 5-150 3,5-Ci2 CF3 •5-151 3,5-Cl2 CF3 5-152 3,5-Cl2 CF3 5-153 3,5-Cl2 CF3 5-154 3,5-Ci2 CF3 5-155 3,5-Cl2 CF3 5-156 3,5-Cl2 CF3 5-157 3,5-Cl2 CF3 5-158 3,5-Cl2 CF3 5-159 3,5-Cl2 CF3 5-lfe0 3,5-Cl2 CF3 5-161 3,5-Cl2 CF3 5-162 3,5-Cl2 CF3 5-163 3,5-Cl2 CF3 5-164 3,5-Cl2 CF3 5-165 3,5-Ci2 CFg 5-166 3,5-Ci2 CF3 5-167 3,5-Cl2 CFg 5-168 3,5-Cl2 CFg 5-169 3,5-Cl2 CF3 5-170 3.5-Ci2 CF3 5-171 3,5-Cl2 CFg 5-172 3,5-Cl2 CF3 5-173 3,5-Cl2 . CF3 5-174 3,5-Cl2 CF3 5-175 3,5-Cl2 CF3 5-176 3,5-Cl2 CF3 5-177 3,5-Cl2 CF3 5-178 3,5-Cl2 CF3 5-179 3,5-Cl2 CF3 5-180 3,5-Cl2 CF3 5-181 3,5-Cl2 CF3 5-182 3,5-Cl2 CF3 5-183 3,5-Cl2 CF3 5-184 3,5-Ct2 CF3 5-185 3,5-Cl2 CF3 5-186 3,5-Cl2 CF3 5-187 3,5-Cl2 CF3 5-188 3,5-Ci2 CF3 2-CH3 2-CH3 2-CH3 •'• 2-CH3 ^ . 2-CH3 :. 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 2-CH3 CH2C(0)NHBu-i *1 CH2C(0)NHBu-c 174.0-177.0 CH2C(0)NHBu-t *1 CH2C(0)NHCH2Bu-t *1 CH2C(0)NHCH2CH2F *1 CH2C(0)NHCH2CH2CI 109.0-112.0 CH2C(0)N(CH3)CH,CH2CI *2 CH2C{0)NHCH2CH2Br *1 CH2C(0)NHCH2CF3 173.5-175.5 CH2C(0)NHCH2CH2CH2C1 *1 CH2C(0)NHCH2(T-4) *1 CH2C(0)NHCH2CH20ti *1 CH2C(0)N(CH3)CH2CH-20H *1 CH2C(0)NHCH2CH20CH3 146.0-149.0 CH2C(0)NHCH2CH20Et *1 CH2C(0)NHCH2CH2SCH3 138.0-143.0 CH2C(0)NHCH2CH2S02CH3 *1 CH2C(0)NHCH2CH=CH2 76.0-79.0 CH2C(0)N(CH3)CH2CH=CH2 *1 CH2C(0)N(CH2CH=CH2)2 *1 CH2C(0)NHCH2CCI=CH2 *1 CH2C(0)NHCH2CH=CCl2 188.0-192.0 CH2C(0)NHCH2C^CH *1 CH2C(0)NHCH2ph 187.0-191.0 CH2C(0)NHCH2(D-22a) *1 CH2C(0)NHCH2(D-47a) *1 CH2C(0)NHPh 181.0-183.0 CH2C(0)(T-32) 118.0-121.0 CH2C(0)(T-35) *1 CH2C(0)NHNHCH2CF3f 118.0-120.0 CH2C(0)NHN(CH3)Ph *1 CH(CH3}C(0)NHCH2CH2C1146.0-149.0 CH(Ph)C(0)NHCH3(R) 118.0-121.0 CH(Ph)C(0)NHCH3(S) *1 CH2CH2C(0)NHCH2CH2CI 153.0-157.0 CH2(T-21) ' *1 CH2C(S)NH2 *1 CH(Ph)C{S)NH2 *1 CH2-TMS *1 CH2CH=CH2 *1 CH2CC1=CH2 *1 CH2CH=CCl2 *1 CH2CCI=CHC1 *1 CH2C=CH *1 CHgPh 142.0-144.5 CH(CH3)Ph 121.5-123.5 5-189 3,5-Cl2 CF35-189(+) 99%d.e.5-189(-) 99%d.e.5-190 3,5-Cl2 CF35-190(+) 99%d.e.5-190(-) 99%d.e.5-191 3,5-Cl2 CF35-192 3,5-Cl2 CF3 -5-193 3,5-Cl2 CF35-194 3,5-Cl2 CF35-195 3,5-Cl2 CF35-196 3,5-Cl2 CF35-197 3,5-Cl2 CF35-198 3,5-Cl2 CF35-199 3,5-Cl2 CF35-200 3,5-Cl2 CF35-201 3,5-Cl2 CF35-202 3,5-Cl2 CF35-203 3,5-Cl2 CF35-204 3,5-Cl2 CF35-205 3,5-Cl2 CF35-206 3,5-Cl2 CF35-207 3,5-Cl2 CF35-208 3,5-Cl2 CF35-209 3,5-Cl2 CF35-210 3,5-Cl2 CF35-211 3,5-Cl2 CF35-212 3,5-Cl2 CF35-213 3,5-Cl2 CF35-214 3,5-Cl2 CF35-215 3,5-Cl2 > CF35-216 3,5-Cl2 CF35-217 3,5-Cl2 CF35-218 3,5-Cl2 CF35-219 3,5-Cl2 CF35-219(+) 97%e.e.5-219(-) 99%e.e.5-220 3,5-Cl2 CFg 5-221 3,5-Cl2 CF35-222 3,5-Cl2 CF35-223 3,5-Cl2 CF35-224 3,5-Cl2 CF35-225 3,5-Cl2 CF35-226 3,5-Cl2 CF35-227 3,5-Cl2 CF35-228 3,5-Cl2 CF3 2-CH3 CH(CH3)Ph(R) *1 [a]D^'+59.13° (EtOH, c=0.262) *1 [aL''°-86.72° (EtOH, c=0.250) *1 :• 2-CH3 CH(CH3)Ph(S) *1 ^ fa]D^°+89.06° (EtOH, c=0.466) *1 JQ;JD''°-117.66 ° (EtOH, C=0.322) * 1 2-CH3 CH(Et)Ph *1 2-CH3 C(CH3)2Ph 91.0-93.5 2-CH3 CH(CF3)Ph 175.5-180.0 2-CH3 CH(OEt)Ph ' *2 2-GH3 CH2(Ph-2-F) 151.0-153.0 2-CH3 CH2(Ph-3-F) ^134.0-136.0 2-CH3 CH2(Ph-4-F) -153.0-155.0 2-CH3 CH2(Ph-2-Cl) 147.0-149.0 2-CH3 CH2(Ph-3-CI) 160.0-162.0 2-CH3 CH2(Ph-4-CI) 164.0-166.0 2-CH3 CH2(Ph-3-N02) 198.0-200.0 2-CH3 CH2(Ph^-N02) 204.0-206.0 2-CH3 CH2(Ph-2,5-F2) 153.0-155.0 2-CH3 CH2(Ph-3,5-F2) 146.0-149.0 2-CH3 CH2(D-1a) *1 2-CH3 CH2(D-3a) 147.0-148.5 2-CH3 CH2(D-3d)CI *1 2-CH3 CH2(D-8b)CH3 *1 2-CH3 CH 2(0-1 Ob)CI *1 2-CH3 CH2(D-15a)CH3 147.0-148.0 2-CH3 CH 2(0-16b)CI 237.0-238.0 2-CH3 CH2(0-16c)CI *1 2-CH3 CH 2(0-16d) *1 2-CH3 CH2(0-17a)CH3 76.0-77.0 2-CH3 CH2(0-17b)CI 157.0-158.0 2-CH3 CH2(D-21a) *1 2-CH3 CH(Ph)(D-21a) *1 2-CH3 CH 2(0-21 b)CF 3 *1 2-CH3 CH2(0-22a) 135.0-136.5 [a]D^'+56.54° (EtOH, c=0.384)" *1 [ah'^'-58.G5° (EtOH, c=0.393) *1 2-CH3 CH2(D-22b)CI *1 2-CH3 CH2(D-22b)CH3 *1 2-CH3 CH2(D-23a) *1 2-CH3 CH2(0-23b)CI *1 2-CH3 CH2(D-25a)CH3 *1 2-CH3 CH2(D-27a)CH3 *1 2-CH3 CH2(0-28a) *1 2-CH3 CH2(D-29b)CH3 *1 2-CH3 CH2(O-30a) 120.0-123.5 5-229 3,5-Ci2 CF3 2-CH3 CH2(D-31a) 122.0-125.0 5-230 3,5-Cl2 CF3 2-CH3 CH2(D-34a) *1 5-231 3,5-Cl2 CF3 2-CH3 CH2(D-34b)CH3 *1 5-232 3,5-Cl2 CF3 • 2-CH3 CH2(D-35a) *1 5-233 3,5-Cl2 CF3 2-CH3 CH2(D-38a) *1 5-234 3,5-Cl2 CF3 .... 2-CH3 CH2(D^7a) 131.0-135.5 5-235 3,5-Cl2 CF3 2-CH3 CH(CH3)(D^7a) *1 5-236 3,5-Cl2 CF3 2-CH3 CH2(D^7c)Cl 164.0-166.0 •5-237 3,5-Cl2 CF3 2-CH3 CH2(D47c)N02 129.0-131.0 5-238 3,5-Cl2 CF3 2-CH3 CH2(D-47e)C|¬ *1 5-239 3,5-Cl2 CF3 2-CH3 CH2(D^7h) *1 5-240 3,5-Ci2 CF3 2-CH3 CH2(D48a) ^ *1 5-241 3,5-Cl2 CF3 2-CH3 CH2{D-48e)Cl ~200.5-202.0 5-242 3,5-Cl2 CF3 2-CH3 CH2(D^9a) *1 5-243 3,5-Cl2 CF3 2-CH3 CH2(D-50a) *1 5-244 3,5-Cl2 CF3 2-CH3 CH2(D-50d) 58.0-65.0 5-245 3,5-Cl2 CF3 2-CH3 CH2(D-51a) *1 5-2^6 3,5-Cl2 CF3 2-CH3 CH2(D-53a) *1 5-247 3,5-Cl2 CF3 2-CH3 CH2(D-53b)CH3 *1 5-248 3,5-Cl2 CF3 2-CH3 NH2 87.0-89.0 5-249 3,5-Cl2 CF3 2-CH3 N(CH3)2 79.0-84.0 5-250 3,5-Cl2 CF3 2-CH3 NHBu-t 71.0-76.0 5-251 3,5-Cl2 CF3 2-CH3 NHCH2CF3 158.0-159.0 5-252 3,5-Cl2 CF3 2-CH3 NHCH2CH2OH 61.0-70.0 5-253 3,5-Cl2 CF3 2-CH3 T-29a 59.0-63.0 5-254 3,5-Cl2 CF3 2-CH3 T-35 95.0-105.0 5-255 3,5-Cl2 CF3 2-CH3 T-37 155.0-157.0 5-256 3,5-Cl2 CF3 2-CH3 NHC(0)CH3 117.0-118.0 5-257 3,5-Cl2 CFg 2-CH3 N(Ph)C(0)CH3 89.0-99.0 5-258 3,5-Cl2 CF3 2-CH3 NHC(0)Pr-n 109.0-111.0 5-259 3,5-Cl2 • CF3 2-CH3 NHC(0)CH2CH2CI 109.0-110.0 5-260 3,5-Cl2 CF3 2-CH3 NHC(0)CH2CN 121.0-125.0 5-261 3,5-Cl2 CF3 2-CH3 NHC(0)0CH3 86.0-93.0 5-262 3,5-Cl2 CF3 2-CH3 N(CH3)C(0)OCH3 131.0-132.0 5-263 3,5-Cl2 CF3 2-CH3 N(Ph)C(0)0CH3 98.0-106.0 5-264 3,5-Cl2 CF3 2-CH3 NHC(0)OEt 75.0-84.0 5-265 3,5-Cl2 CF3 2-CH3 NHC(0)OBu-t *1 5-266 3,5-Cl2 CF3 2-CH3 NHC(0)0CH2Ph 155.0-156.0 5-267 3,5-Cl2 CF3 2-CH3 NHC(0)NHPh 212.0-214.0 5-268 3,5-Cl2 CF3 2-CH3 NHC(0)Ph 213.0-214.0 5-269 3,5-Cl2 CF3 2-CH3 NHC(0)(D-1a) 230.0-232.0 5-270 3,5-Cl2 CF3 2-CH3 NHC(0)(D-47a) 116.0-117.0 5-271 3,5-Cl2 CF3 2-CH3 NHC(S)NHCH3 143.0-145.0 5-272 3,5-Cl2 CF3 2-CH3 NHC(S)N(CH3)2 179.0-182.0 5-273 3,5-Cl2 CF3 2-CH3 NHPh 88.0-96.0 5-274 3,5-Cl2 CF3 2-CH3 N(CH3)Pli 158.0-160.0 5-275 3,5-Cl, CF3 2-CH3 N(CH2CH=CH2)Ph 78.0-86.0 5-276 3,5-C!2 CF3 2-CH3 NCCH^PhjPh 58.0-60.0 5-277 3,5-Ci2 CF3 2-CH3 NH(Ph-2-C!) *1 5-278 3,5-Cl2 CF3 1 2-CH3 NH(Ph-3-CI) *1 5-279 3,5-Cl2 CF3 , 2-CH3 NH(Ph-4-Cl) *1 5-280 3,5-Cl2 CF3 .2-CH3 NH(Ph-4-CF3) *1 5-281 3,5-Ci2 CF3 " 2-CH3 NH(Ph-2-N02) 89.0-95.0 5-282 3,5-Cl2 CF3 2-CH3 NH(Ph-3-N02) 104.0-109.0 ,5-283 3,5-Cl2 CF3 2-CH3 NH(Ph-4-N02) 120.0-126.0 5-284 3,5-Cl2 CF3 2-CH3 N(CH3)(D-21a) 181.0-185.0 5-285 3,5-Cl2 CF3 2-CH3 NH(D47a) 213.0-217.0 5-286 3,5-C!2 CF3 2-CH3 N(CH3)(D-47a) 202.0-203.0 5-287 3,5-Cl2 CF3 2-CH3 NH(D^7b)CI J 02.0-103.0 ' 5-288 3,5-Cl2 CF3 2-CH3 NH(D-47d)CI 91.0-92.0 5-289 3,5-Cl2 CF3 2-CH3 NH(D^7e)CI 89.0-90.0 5-290 3,5-Cl2 CF3 2-CH3 NH(D47f) 137.0-140.0 5-291 3,5-Cl2 CF3 2-CH3 NH(D-50a) 209.0-211.0 5-2b2 3,5-Cl2 CF3 2-CH3 NH(D-50b)CF3 95.0-100.0 5-293 3,5-Cl2 CF3 2-CH3 NH(D-50d) 91.0-98.0 5-294 3,5-Cl2 CF3 2-CH3 N(CH3)(D-50a) 194.0-196.0 5-295 3,5-Cl2 CF3 2-CH3 N(Et)(D-50a) 60.0-67.0 5-296 3,5-Cl2 CF3 2-CH3 NH(D-51b)SCH3 *1 5-297 3,5-Cl2 CF3 2-CH3 NH(D-51b)S(0)CH3 156.0-152.0 5-298 3,5-Cl2 CF3 2-CH3 NH(D-51b)S02CH3 147.0-151.0 5-299 3,5-Cl2 CF3 2-CH3 NH(D-51c)CI *1 5-300 3,5-Cl2 CF3 2-CH3 NH(D-53a) 111.0-112.0 5-301 3,5-Cl2 CF3 2-CH3 NH(D-54b)Cl *1 5-302 3,5-Cl2 CF3 2-CH3 N=C(CH3)Ph 134.0-135.0 5-303 3,5-Cl2 CF3 2-CH3 N=CH(D^7a) *1 5-304 3,5-Cl2 CF3 2-CH3 T-41 146.0-148.0 5-305 3,5-Cl2 .. CF3 2-CH3 D-8a 127.5-129.0 5-306 3,5-Cl2 CF3 2-CH3 (D-13b)CH3 271.0-275.0 5-307 3,5-Cl2 CF3 2-CH3 D-21a " 281.0-284.0 5-308 3,5-Cl2 CF3 2-CH3 D-48a 188.0-190.0 5-309 3,5-Cl2 CF3 2-CH3 D-50a 98.0-100.0 5-310 3,5-Cl2 CF3 2-CH3 D-51a 90.0-91.0 5-311 3,5-Cl2 CF3 3-CH3 CH2CF3 *1 5-312 3,5-Cl2 CF3 2-Et CH2CF3¬ *1 5-313 3,5-Cl2 CF3 2-Et CH2(D^7a) *1 5-314 3,5-Cl2 CF3 2-CF3 CH2CF3 70.0-72.0 5-315 3,5-Cl2 CF3 2-CF3 CH2(D^7a) 69.0-70.0 5-316 3,5-Cl2 CF3 2-CH2OH CH2CF3 *1 5-317 3,5-Ci2 CF3 2-OCH3 CH2CF3 *1 5-318 3,5-Cl2 CF3 2-OCH3 CHgPh *1 5-319 3,5-Cl2 CF3 2-OCH3 CH2(D^7a) 173.5-176.0 5-320 3,5-Cl2 CF3 2-OCF3 CH2CF3 *2 336 5-321 3,5-C!, CF3 2-OCF3 CH2(D^7a) 145.0-148.5 5-322 3,5-C! 2 CF3 2-SCH3 CH2CF3 *2 5-323 3,5-Ci2 CF3 2-SCH3 CH2(D-47a) *2 5-324 3,5-Cl2 CF3 I 2-S(0)CH3 CH2CF3 *2 5-325 3,5-Cl2 CF3 2-S(0)CH3 CH2(D-47a) *1 5-326 3,5-Cl2 CF3 . 2-SO2CH3 CH2CF3 *1 5-327 3,5-Cl2 CF3 "2-SO2CH3 CH2(D^7h) 120.0-121.0 5-328 3,5-Cl2 CF3 2-S(0)CH2CI CH2CF3 *2 5-329 3,5-Cl2 CF3 2-NH2 CH2CF3 78.0-79.0 5-330 3,5-Cl2 CF3 2-NH2 CH2(D-47a) *2 5-331 3,5-Cl2 CF3 2-NHCH3 CH2CF3 156.0-158.0 5-332 3,5-C!2 CF3 2-NHCH3 CH2(D-47a) _ *1 5-333 3,5-Cl2 CF3 2-NHC(0)CH3' CH2CF3 ~ *2 5-334 3,5-Cl2 CF3 2-N(CH3)2 CH2CF3 *2 5-335 3,5-Cl2 CF3 2-N(CH3)2 CH2(D-47a) *1 5-336 3,5-Cl2 CF3 2-N(CH3)CHO CH2(D^7a) *1 5-337 3,5-Cl2 CF3 2-N(CH3)C(0)CH3 CH2(D^7a) *1 5-338 3,5-Cl2 CF3 2-NO2 CH2CF3 180.0-181.0 5-339 3,5-Cl2 CF3 2-NO2 CH2(D^7a) *2 5-340 3,5-Cl2 CF3 2-CN CH2CF3 *1 5-341 3,5-Cl2 CF3 2-CN CH2(D-47a) *1 5-342 3,5-Cl2 CF3 2-CsC-TMS CH2CF3 *1 5-343 3,5-Cl2 CF3 2-Ph CH2CF3 *1 5-344 3,5-Cl2 CF3 2-Ph CH2(D-47a) 194.0-198.0 5-345 3,5-C! 2 CF3 2-(D-38a) CH2(D-47a) *2 5-346 3,5-Cl2 CF3 2,3-F2 CH2CF3 *1 5-347 3,5-Cl2 CF3 2,3-F2 CH2Ph *1 5-348 3,5-Cl2 CF3 2,3-F2 CH2(D^7a) *1 5-349 3,5-Cl2 CF3 2,6-F2 CH2CF3 140.0-141.0 5-350 3,5-Cl2 CF3 2,6-Cl2 CH2(D-47a) 131.0-132.0 5-351 3,5-Cl2 n CF3 2,6-(CH3)2 CH2CF3 125.0-129.0 5-352 3,5-Cl2 CF3 2,6-(CH3)2 CH2(D^7a) *1 5-353 3,5-Cl2 . CF2CI 2-CI CH2(D-22a) *1 5-354 3,5-C!2 CF2CI 2-CI CH2(D-47a) *1 5-355 3,5-Cl2 CF2CI 2-CH3 CH2CF3 *1 5-356 3,5-Cl2 • CF2C! 2-CH3 CH-zCHzOEt ' *1 5-357 3,5-Ci2 CF2CI 2-CH3 CH2CH(OCH3) *1 5-358 3,5-Cl2 CF2CI 2-CH3 CH2CH=CH2 *1 5-359 3,5-Cl2 CF2Ci 2-CH3 CH2(D-22a) *1 5-360 3,5-Cl2 CF2CI 2-CH3 CH2(D-47a) *1 5-361 3,5-Cl2 CF2CF3 2-CH3 CH2CF3 *1 5-362 3,5-Ci2 CF2CF3 2-CH3 CH2(D^7a) *1 5-363 3,5-Cl2 CF2CF3 2-CH3 C(0)(D-47a) *1 5-364 3,5-Cl2 CH2OCH2CF3 2-CH3 CH2CF3 *1 5-365 3,5-Cl2 CH2OCH2CF3 2-CH3 CH2(D^7a) *1 5-366 3,5-C!2 CF2SCH3 2-CH3 CH2CF3 *2 5-367 3,5-Cl2 CF2SCH3 2-CH3 CH2(D47a) 51.0-52.0 5-368 3,5-Cl2 CHg-TTvlS 2-CH3 CH^CFa *1 5-369 3,5-Cl2 CH2-TMS 2-CH3 CH2(D-47a) *1 5-370 3,5-Cl2 TMS '•' 2-CH3 CH2CF3 *1 5-371 3,5-Cl2 TMS , 2-CH3 CH,(D^7a) *1 5-372 3,5-Cl2 D^7a 2-CH3 CH2CF3 *1 5-373 3,5-Cl2 D-47a ' ~2-CH3 CH2(D-47a) *1 5-374 3-CI-5-Br CF3 2-CH3 CH2CF3 *1 .5-375 3-CI-5-Br CF3 2-CH3 CH2(D-47a) *1 5-376 3,5-Br2 CF3 2-Cl CH2(D-22a) 63.0-64.0 5-377 3,5-Br2 CF3 2-CI CH2(D-47a) *2 5-378 3,5-Br2 CF3 2-CH3 CH2CF3 *1 5-379 3,5-Br2 CF3 2-CH3 CH2CH2OCH3 ^ *2 ' 5-380 3,5-Br2 CF3 2-CH3 CH2CH20Et *2 5-381 3,5-Br2 CF3 2-CH3 CH2CH(OCH3)2 *2 5-382 3,5-Br2 CF3 2-CH3 CH2C(0)OCH3 *2 5-383 3,5-Br2 CF3 2-CH3 CH2C(0)NHCH2CH2Ci 69.0-70.0 5-3S4 3,5-Br2 CF3 2-CH3 CH2C(0)NHCH2CF3 173.0-175.0¬5-385 3,5-Br2 CF3 2-CH3 CH2CH=CH2 *2 5-386 3,5-Br2 CF3 2-CH3 CH2(D-22a) *1 5-387 3,5-Br2 CF3 2-CH3 CH2(D-47a) *1 5-388 3-CI-5-CH3 CF3 2-CH3 CH2(D-47a) *2 5-389 3,5-(CF3)2 CF3 2-CH3 CH2CF3 *1 5-390 3,5-(CF3)2 CF3 2-CH3 CH2(D-47a) *1 5-391 3-F-5-SCH3 CF3 2-CH3 CH2(D^7a) *1 5-392 3-Ci-5-SCH3 CF3 2-SCH3 CH2(D-47a) *2 5-393 3-CF3-5-OCH3 CF3 2-CH3 CH2(D^7a) *1 5-394 3,5-{SCH3)2 CF3 2-CH3 CH2(D^7a) *1 5-395 3-CF3-5-CN CF3 2-CH3 CH2CF3 72.0-73.0 5-396 3-CF3-5-CN CF3 2-CH3 CH2(D-47a) 63.0=64 0 5-397 3A5-CI3 , CF3 2-CH3 CH2CF3 194.0-197 0 5-398 3,4,5-Cl3 CF3 2-CH3 CH2(D-47a) *1 5-399 3,5-Cl2 CF3 2-CH3 CH2CH2CF3 *1 5^00 3,5-Cl2 CF3 2-CH3 CH{CF3)0H *1 5^01 3,5-Cl2 CF3 2-CH3 CH(CF3)0CH, *1 5^02 3,5-Cl2 CF3 2-CH3 E-5b ^^ 197.0-199.0 5-403 3,5-Cl2 CF3 2-CH3 CH2CH2(T-28) *1 5-404 3,5-Cl2 CF3 2-CH3 CH2CH2(T-34) *1 5-405 3,5-Cl2 CF3 2-CH3 (E-9b)CH2CF3 *2 5^06 3,5-Cl2 CF3 2-CH3 (E-17a)H *1 5-407 3,5-Cl2 CF3 2-CH3 CH[C(0)OCH3]2 *2 5^08 3,5-Cl2 CF3 2-CH3 CH2C(0)NH0Et 141.0-145 0 5-409 3,5-Cl2 CF3 2-CH3 CH2C(0)NHOCH2CH=CH2 *1 5-410 3,5-Cl2 CF3 2-CH3 CH(CH3)C(0)NHEt *1 5411 3,5-Cl2 CF3 2-CH3 CH(CH3)C(0)NHPr-i 172.0-1740 5^12 3,5-C!2 CF3 2-CH3 CH(CH3)C(0)NHCH2CF3 161.0-163.0 5-413 3,5-Cl2S414 3,5-Cl25-415 3,5-Cl25^16 3,5-Cl25-417 3,5-Cl25-418 3,5-Cl25-419 3,5-CI,5-420 3,5-Ci;5-421 3,5-Cl25-422 3,5-Cl25^23 3,5-Cl25-424 3,5-Ci25-425 3,5-Cl25^26 3,5-Cl25-427 3,5-Cl2 •5^28 3,5-Cl25-429 3,5-Cl25^30 3,5-Cl25-431 3,5-Cl25^32 3,5-Cl25^33 3,5-Cl25-434 3,5-Cl25^35 3,5-Cl25^36 3,5-Ci25^37 3,5-Cl25^38 3,5-Cl25439 3,5-Cl25-440 3,5-Cl25^ 1 3,5-Cl25442 3,5-Ci25443 3,5-Cl2 5.444 3,5-C!25-445 3,5-Cl25446 3,5-Cl25^W7 3,5-Cl25448 3,5-Cl25449 3,5-Cl25450 3,5-Cl25451 3,5-Br2 5452 3-CF3-5-NO2 CF3 5453 3-CF3-5-NO2 CF3 5454 3,5-Cl24-NH2 5455 3,5-Cl24-NH2 5456 3,5-Cl24-NHC(0)OBu-t 5457 3,5-Cl24-NHC(0)OBu-t 5458 3,5-Cl2 CF3 CF3 CF3 CF3 CF3 CF3 CF3 \, CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 CF3 :. CF3 CF3 CF3 CF3 CF3 CF3 CF3 CH(0Et)2 CF3 2-CH3 CH(CH3)C(0)NHCH2CH=CH2 175.0-178.0 2-CH3 T-42 *2 2-CH3 T43 *2 ' 2-CH3 CH[C(0)NHCH3]2 146.0-149.0 2-CH3 CH(0CH3)Ph *1 2-CH3 CH(CH3)(D-1a) 142.0-144.0 2-CH3 CH2(D-6c)CH3 155.0-157.0 2-CH3 CH(CF3)(D-6c)H *1 2-CH3 CH2(D-11a) *1 2-CH3 CH(CF3)(D-14a) 114.0-118.0 2-CH3 CH(CH3)(D-21a) *2 2-CH3 CH(CF3)(D-24a) ^ *1 2-CH3 CH2(D-26a)CH3 - *1 2-CH3 CH(CH3)(D-38a) *1 2-CH3 CH(CF3)(D-38a) *1 2-CH3 CCOpCHgCFa *1 2-CH3 C(0)NHCH2CF3 81.5-83.0 2-CH3 C(S)NHCH2CF3 137.5-140.0 2-CH3 C(D-49a)=C(CN)2 122.0-1240 2-CH3 NHC(0)NHCH2CH2CI 105.0-108.0 2-CH3 N(CH2C=CH)Ph 76.0-84.0 2-CH3 Ph-4-CN *1 2-CH3 Ph-4-C(0)0H 248.0-251.0 2-CH3 Ph^C(0)OEt 230.0-232.0 2-CH3 Ph^-C(0)NHCH2CH2CI 188.0-195.0 2-CH3 Ph-4-C(0)NHCH2CF3 110.0-120.0 2-CH3 (D-8b)CH3 163.0-165.0 2-CH3 (D-15a)CH3 96.0-110.0 2-CH3 (D-17a)CH3 95.0-101.0 2-CH3 (D-17b)Cl 100.0-108.0 2-CH3 (D-21b)CH3 110.0-1140 . 2-CH3 (D-21c)CI 288.0-292.0 2-CH3 (D-21c)CH3 . 271.0-273.0 2-CH3 D-35a 117.0-126.0 2-CH3 (D-35b)CH3 , 227.0-230.0 2-CH3 (D-39c)SCH3 188.0-190.0 2-CH3 (D42a)H 109.0-112.0 2-CH3 CH2(D47a) *1 2-CH3 CHgCpp H 102.0-106.0 2-CH3 CH2CF3 *1 2-CH3 CH2(D47a) *1 CF3 2-CH3 CH2CF3 153.0-154.0 CF3 2-CH3 CH2(D47a) *1 CF3 2-CH3 CHgCFg *1 CF3 2-CH3 CH2(D47a) *1 2-CH3 CH2CHF2 *1 339 S459 3,5-Cl2 CF3 2-CH3 CH(CH3)C(0)NHCH2CH2C1(D) 162.0-164.0 5^ 0 3,5-CI, CF3 2-CH3 CH(CH3)C(0)NHCH2CH2CI(L) 149.0-151.0 5^161 3,5-Cl2 CF3 , 2-CH3 CH(CH3)C(0)NHCH2CF3(D) 188.0-190.0 5-462 3,5-Cl2 CF3 ' 2-CH3 CH(CH3)C(0)NHCH2CF3(L) 181.0-183.0 Table 12 .(x).2 Xji ^r¬ 4 5 2 H ^ ^ No. (XL R' (Y)„ R^ R' m.p.rC) 6-001 3,5-Cl2 CF3 2-CI Et Et *1 6-002 3,5-Cl2 CF3 2-CH3 NH2 CH3 138.0-139.0^ 6-003 3,5-Cl2 CF3 2-CH3 Et Et *1 6-004 3,5-Cl2 CF3 2-CH3 NH2 Et 76.0-78.0 6-005 3,5-Cl2 CF3 2-CH3 NHC(0)CH3 Et *1 6-006 3,5-Cl2 CF3 2-CH3 N=C(CH3)2 Et *1 6-007 3,5-Cl2 CF3 2-CH3 CH2CN n-Bu *1 6-008 3,5-Cl2 CF3 2-CH3 CH2CN CH2CN *1 6-009 3,5-Cl2 CF3 2-CH3 OH CHsPh 175.0-177.0 6-010 3,5-Cl2 CF3 2-CH3 OCH3 CHgPh *1 6-011 3,5-Cl2 CF3 2-CH3 0C(0)CH3 CHsPh *1 6-012 3,5-Cl2 -CF3 2-CH3 0C(0)0CH3 CHsPh *1 6-013 3,5-Cl2 CF3 2-CH3 OSO2CH3 CHgPh *1 6-014 3,5-Cl2 CF3 2-CH3 NH2 CH2Ph 135.0-136.0 6-015 3,5-Cl2 CF3 2-CH3 CH2CN CH^(D-22a) *1 6-016 3,5-Cl2 CF3 2-CH3 CHgC^CH CH2(D-22a) *1 6-017 3,5-Cl2 CF3 2-CH3 C(0)CH3 CH2(D-22a) *1 6-018 3,5-Cl2 CF3 2-CH3 C(0)Et CH2(D-22a) *1 6-019 3,5-Cl2 CF3 2-CH3 C(0)0CH3 CH2(D-22a) *1 6-020 3,5-Cl2 CF3 2-CH3 CH3 CH2lD^7a) *1 6-021 3,5-Cl2 CF3 2-CH3 Et CH2(D-47a) *1 6-022 3,5-Cl2 CF3 2-CH3 n-Pr CH2(D^7a) *1 6-023 3,5-Cl2 CF3 2-CH3 i-Pr GH2(D-47a) *1 6-024 3,5-Cl2 CF3 2-CH3 c-Pr CH2(D^7a) *1 6-025 3,5-C!2 CF3 2-CH3 t-Bu CH2{D^7a) *1 6-026 3,5-Cl2 CF3 2-CH3 CH2CF3 CH2(D^7a) *1 6-027 3,5-Cl2 CF3 2-CH3 CH2OCH3 CH2(D-47a) *1 6-028 3,5-Ci2 CF3 2-CH3 CH2CH2OCH3 CH2(D47a) *1 6-029 3,5-Cl2 CF3 2-CH3 CH2SCH3 CH2(D-47a) *1 6-030 3,5-Cl2 CF3 2-CH3 CH2C(0)OCH3 CH2(D^7a) *1 6-031 3,5-Cl2 CF3 2-CH3 CH2CN CH2(D-47a) *1 6-032 3,5-Cl2 CF3 2-CH3 CH2CH=CH2 CH^iDAla) *1 6-033 3,5-C!2 CF3 2-CH3 CH2C=CH CH2(D^7a) *1 6-034 3,5-C!2 CF3 2-CH3 C(0)CH3 CH2(D^7a) *1 6-035 3,5-CU CF3 2-CW3 C(0)Et CH2(D-47a) *1 5-036 3,5-C!2 CF3 ?>dH3 C(0)Pr-n CH2(D^7a) *1 6-037 3,5-Cl2 CF3 2-CH3 C(0)Pr-i CH2(D^7a) *1 6-038 3,5-Cl2 CF3 2-CH3 C(0)Pr-<; CH2(D^7a) *1 6-039 3,5-Cl2 CF3 2-CH3 C(0)Bu-t CH2(D^7a) *1 6-040 3,5-Cl2 CF3 2-CH3 C(0)CH20CH3 CH2(D^7a) 53.0-55.0 6-041 3,5-Cl2 CF3 2-CH3 C(0)CH=CH2 CH2(D-47a) *1 6-042 3,5-Cl2 CF3 2-CH3 C(0)Ph CH2(D-47a) *1 6-043 3,5-Cl2 CF3 2-CH3 C(0)0CH3 CH2(D-47a) ^ *1 6-044 3,5-Cl2 CF3 2-CH3 C(0)OEt CH2(D-47a) ¬ *1 6-045 3,5-Cl2 CF3 2-CH3 C(0)OPr-i CH2(D^7a) *1 6-046 3,5-Cl2 CF3 2-CH3 C(0)OBu-i • CH2(D^7a) *1 6-047 3,5-Cl2 CF3 2-CH3 CppCHaCHgCI CH2(D-47a) *1 6-048 3,5-Cl2 CF3 2-CH3 C(0)OCH2CH20CH3 CH2(D-47a) *1 6-0^9 3,5-Cl2 CF3 2-CH3 C(0)OCH2CH=CH2 CH2(D-47a) *1 6-050 3,5-Cl2 CF3 2-CH3 C(0)SCH3 CH2(D^7a) *1 6-051 3,5-Cl2 CF3 2-CH3 SO2CH3 CH2(D-47a) *1 6-052 3,5-Cl2 CF3 2-CH3 NH2 CH2(D^7a) 126.0-130.0 6-053 3,5-Cl2 CF3 2-CH3 N(CH3)2 CH2(D-47a) *1 6-054 3,5-Ci2 CF3 2-CH3 Et CH2(D-48e)CI *1 6-055 3,5-Cl2 CF3 2-CH3 c-Pr CH2(D-49a) *1 6-056 3,5-Cl2 CF3 2-CH3 C(0)Et CH2(D-50a) *1 6-057 3,5-Cl2 CF3 2-CH3 -CH2CH2SCH2CH2¬ 209.5-211.5 6-058 3,5-Cl2 CF3 2-CH3 CH3 N(CH3)Ph 153.0-154.0 6-059 3,5-Cl2 CF3 2-CH3 Et N(CH3)Ph 78.0-79.0 6-060 3,5-Cl2 CF3 2-CH3 CH2OCH3 N(CH3)Ph 72.0-73.0 6-061 3,5-Cl2 CF3 2-CH3 CH2CH=CH2 N(CH3)Ph 76.0-77.0 6-062 3,5-Cl2 ,CF3 2-CH3 CHaC^CH N(CH3)Ph 83.0-84.0 6-063 3,5-Cl2 CF3 2-CH3 CH2CN N(CH3)Ph 69.0-70.0 6-064 3,5-Cl2 CF3 2-CH3 C(0)CH3 N(CH3)Ph 82.0-83.0 6-065 3,5-Cl2 CF3 2-CH3 C(0)0CH3 N(CH3)Ph 70.0-71.0 6-066 3,5-Cl2 CF3 2-CH3 CH3 NH(D.50a) 107.0-109.0 6-067 3,5-Cl2 CF3 2-CH3 Et NH(D-50a) 185.0-187.0 6-068 3,5-Cl2 CF3 2-CH2¬H 234.0-236.0 6-069 3,5-Cl2 CF3 2-CH2¬ CH3 *1 6-070 3,5-Cl2 CF3 2-CH2¬ CH2(D-47a) *1 6-071 3,5-Cl2 CF3 2-N(CH3)CH2¬ CH2(D-47a) *1 6-072 3,5-Cl2 CF3 2-N=CH¬H 249.0-251.0 6-073 3,5-Cl2 CF3 2-N=CH¬ CH2(D^7a) *1 6-074 3,5-Cl2 CF2CI 2-CH3 C(0)CH3 CH2CF3 *1 6-075 3,5-Br2 CF3 2-CH3 C(0)CH3 CH2CF3 *1 6-076 3,5-Br2 CF3 2-CH3 CpjCHg CH2(D-47a) *1 6-077 3,5-Cl2 CF3 2-CH3 C(0)0CH3 CH2CF3 *2 341 6-078 3,5-Cl2 CFg 2-CH3 CH2OCH3 CH2(D-22a) *1 6-079 3,5-Cl2 CF3 2-CH3 CHaOEt CH2(D-47a) *1 6-080 3,5-Cl2 CF3 2-CH3 C(0)0CH3 CH(CH3)(D-47a) *2 6-080(+)* 98%e.e. [^a]D^'+35.40° (CHCI3, c=0.397) *2 6-080(-)* 99%e.e. .[a]D^-'-37.20° (CHCI3, c=0.473) *2 6-081 3,5-Cl2 CF3 2-etH3 C(0)CH3 N(CH3)(D-47a) *1 6-082 3,5-Cl2 CF3 2-CH; C(0)0CH3 N(CH3)(D^7a) *1 6-083 3,5-Cl2 CF3 2-CH3 C(0)CH3 N(CH3)(D-50a) *2 6-084 3,5-Cl2 CF3 2-CH 3 CppCH g N(CH3)(D-50a) *1 6-085 3,5-Cl2 CF3 2-CH 3 -CH2CH2CH2C(0)- *1 5-086 3,5-Cl2 CF3 2-CH3 -C(0)CH2CH2C(0)- *1 6-087 3,5-C!2 CF3 2-CH 3 -CH2CH2N(Ph)CH2CH2-_ 84.0-88.0 6-088 3,5-Cl2 CF3 2-CH 3 -CH2CH2N(D-47a)CH2CH2--^ 87.0-92.0 ' 6-089 3,5-Cl2 CFg 2-C(=CH2)- CH^CFg 141.0-144.0 6-090 3,5-Cl2 CF3 2-CH 3 -CH2CH2CH2CH[C(0)NHCH2CF3]- *1 In Table above, the Indications of "(+)*" and "(-)*" show optically active forms of only 1-(2-pyridyl) ethylamine moiety. Table 13 (x).2 Xi '/^ , 4 c 7 I' 5 ^ S No. (XL R' (Y), R' R^ m.p.ro 7-001 3,5-Cl2 CF3 -H H 227.0-232.0 7-002 3,5-Cl2 CF3 -H CH2CF3 *1 7-003 3,5-Cl2 CF3 -H CH2(D-22a) *1 7-004 3,5-Cl2 CF3 -H CH2(D^7a) 165.0-167.0 7-005 3,5-Cl2 CF3 2-F H CH2(D-22a) 171.0-173.0 7-006 3,5-Cl2 CF3 2-CI H CH2(D-22a) 90.0-92.0 7-007 3,5-Cl2 CF3 2-CH3 H CH2CF3 *1 7-008 3,5-Cl2 CF3 2-CH 3 H CH2(D-22a) *1 7-009 3,5-Cl2 CF3 2-CH3 H CH2(D-47a) *1 7-010 3,5-Cl2 CF3 2-CH 3 H N(CH3)Ph 100.0-111.0 Table 14 5 ^ O- - R^^ No. (XL R^ COn R'^ R'^ m.p.rC) 8-001 3,5-Cl2 CFg - -N(CH3)CH=CHS- *1 8-002 3,5-Cl2 CFg 2-CH3 -N(CH3)CH=CHS- *1 8-003 3,5-Cl2 CF3 2-CH3 -N(Pr-n)CH=CHS-- *1 8-004 3,5-Cl2 CF3 2-CH3 -N(CH3)N=CHCH2S-~ *1 Table 15 Ry^-N 3 (Y)„ Substituent G in the above-mentioned formula is tiie structure of G-3, G-6, G-18 or G-20mentionecl below. "'ti' "'ti^ "•¥. ":^ ^-—XT ^ ^ N ^^ 6 CH3 ^ G-3 ., G-6 G-18 G-20 No. G (XL R' (Y)„ R^ R^ . m.p. (°C) 9-001 G-3 6-F CF3 -H CHgCFg 175.0-177.0 9-002 G-3 6-CI CF3 -H CH2C;F3 192.0-195.0 9-003 G-3 5-Br CF3 2-CH3 H CH2CF3 *1 9-004 G-3 6-OCH3 CF3 -H -CH2CF3 150.0-152.0 9-005 G-6 4,6-Cl2 CF3 -H CHaCFg 140.0-142.0 9-006 G-6 4,6-Cl2 CF3 2-CH3 H CH2CF3 131.0-134.0 9-007 G-18 - CF3 -H CH2CF3 156.0-157.0 9-008 G-20 4-CF3 CF3 2-CH3 H CH2CF3 *1 9-009 G-20 4-CF3 CF3 2-CH3 H CH2(D^7a) *1 Table 16 , ^V^!? 5 (Y)„ T / \ \ ll I 5 2 o._ No. (X)^ A^ A^ A^ (Y)„ R^ m.p. (X ) 10-001 3,5-Cl2 N C C ¬ CH2CF3 ' *1 10-002 3,5-Cl2 N C C ¬ CH2(D-47a) *1 10-003 3,5-Ci2 N(0) C C ¬ CH2CF3 ^ *1 10-004 3,5-Cl2 C N C ¬ CH2CF3 ~ *1 10-005 3,5-Cl2 C N C ¬ CH2(D-47a) *1 Table 17 4 5 2 No. (XL R' (Y)„ R m.p. CO 11-001 3-CI CFg ¬ C(0)OH 220.0-225.0 11-002 3-CI CF3 ¬ C(0)0CH3 100.0-101.0 11-003 4-Cl CF3 ¬ C(0)OH 255.0-257.0 11-004 4-CI CF3 ¬ CppCH s *1 11-005 3-1 CF3 2-CH3 C(0)OH , 169.0-172.0 11-006 3-1 ' CF3 2-CH3 C(0)0CH3 *1 11-007 3-NO2 CF3 2-CH3 C(0)0CH3 *1 11-008 3,4-F2 CF3 ¬ C(0)OH 246.0-248.0 11-009 3,4-F2 CF3 ¬ C(0)0CH3 132.0-133.0 11-010 2,4-Cl2 CF3 ¬ .C(0)OH ^ 104.0-106.0 11-011 2,4-Cl2 CF3 ¬ C(0)0CH3 103.0-106.0 11-012 2,5-Cl2 CF3 ¬ C(Q)OH 97.0-100.0 11-013 2,5-Cl2 CF3 ¬ C(0.)0CH3 163.0-165.0 11-014 3,4-Cl2 H ¬ C(0)0CH3 115.0-117.0 11-015 3,4-Cl2 CH3 ¬ C(0)0CH3 98.0-100.0 11-016 3,4-C!2 CF3 ¬ C(0)OH 215.0-217.0 11-017 3,4-Cl2 CF3 ¬ C(0)0CH3 95.0-97.0 11-018 3,4-Cl2 CF3 ¬ C(0)OBu-t 94.0-95.0 11-019 3,4-Cl2 CF3 ¬ C(0)0CH2Ph 94.0-95.0 11-020 3,4-Cl2 Ph ¬ C(0)0CH3 143.0-145.0 11-021 3,5-Cl2 CF3 ¬ CH2OH 108.0-110.0 11-022 3,5-Ci2 CF3 ¬ OH 153.0-155.5 11-023 3,5-Cl2 CF3 ¬ OCH3 93.0-96.5 11-024 3,5-Cl2 CF3 ¬ NO2 161.0-162.0 11-025 3,5-Cl2 CF3 I ¬ NH2 98.0-99.0 11-026 3,5-Cl2 CF3' ¬ CN 140.0-142.0 11-027 3,5-Cl2 CF3: ¬ C(0)OH 237.0-240.0 11-028 3,5-Cl2 CF3 ¬ C(0)0CH3 94.0-96.0 11-029 3,5-Cl2 CF3 2-F CH2Br *2 11-030 3,5-Cl2 CF3 2-F CH20C(0)CH3 *2 11-031 3,5-Cl2 CF3 2-F CH2OH *1 11-032 3,5-Cl2 CF3 2-F C(0)OH 172.0-174.0 11-033 3,5-Cl2 CF3 3-F Br J36.0-138.0 11-034 3,5-Cl2 CF3 3-F C(0)OH ¬ *1 11-035 3,5-Cl2 CF3 3-F C(0)OEt 94.0-96.0 11-036 3,5-Cl2 CF3 2-CI OSO2CF3 154.0-157.5 11-037 3,5-Cl2 CF3 2-CI C(0)OH 150.0-151.0 11-038 3,5-Cl2 CF3 2-Cl C(0)0CH3 *2 11-039 3,5-Cl2 CF3 3-CI Br *2 11-040 3,5-Cl2 CF3 3-CI C(0)OH 187.0-188.0 11-041 3,5-Cl2 CF3 3-CI C(0)OEt *1 11-042 3,5-Cl2 CF3 2-Br C(0)0CH3 83.0-86.0 11-043 3,5-Cl2 CF3 2-1 CH3 130.0-132.0 11-044 3,5-Cl2 CF3 2-1 CHgBr *1 11-045 3,5-Cl2 CF3 2-1 CH20C(0)CH3 *1 11-046 3,5-Cl2 CF3 2-1 CH2OH *1 11-047 3,5-Cl2 CF3 2-1 C(0)OH *1 11-048 3,5-Cl2 CF3 2-1 C{0)0CH3 *2 11-049 3,5-Cl2 CF3 2-CH3 NO2 135.0-136.0 11-050 3,5-Cl2 CF3 2-CH3 NH2 *1 11-051 3,5-Cl2 CF3 2-CH3 F 67.0-68.0 11-052 3,5-Cl2 .. CF3 2-CH3 Br 105.0-108.0 11-053 3,5-Cl2 CF3 2-CH3 C(0)OH 146.0-148.5 11-054 3,5-Cl2 CF3 2-CH3 C(0)0CH3 96.0-99.5 11-055 3,5-Cl2 CF3 2-CH3 C(0)OEt nD'^'^^l .5474 11-056 3,5-Cl2 CF3 2-CH3 C(0)OCH-2(0^73) *2 11-057 3,5-Cl2 CF3 2-CH3 • C(0)(D-14a) *1 11-058 3,5-Cl2 CF3 2-CH3 C(0)(D-38a) 58.0-59.0 11-059 3,5-Cl2 CF3 2-Et C(0)0CH3 *2 11-060 3,5-Cl2 CF3 2-CH2Br C(0)0CH3 *2 11-061 3,5-Cl2 CF3 2-CF3 F *1 11-062 3,5-Cl2 CF3 2-CF3 CN *1 11-063 3,5-Cl2 CF3 2-CF3 C(0)0CH3 . *2 11-064 3,5-Cl2 CF3 2-OH NO2 110 0-113 0 11-065 3,5-C[2 CF3 2-OH NH2 178.0-181.0 11-066 3,5-Ci2 CF3 2-OCH3 OSO2CF3 *1 11-067 3,5-Cl2 CF3 2-OCH3 C(0)OH *1 345 11-068 3,5-C!2 CF3 2-OCH3 C(0)OEt 142.0-144.0 11-069 3,5-Cl2 CF3 2-OCF3 NH2 81.5-84.0 11-070 3,5-Ci2 CF3 2-OCF3 i *1 11-071 3,5-Ci2 CF3 ' 2-OCF3 CppCH g *1 11-072 3,5-Ci2 CFg¬ 2-SCH3 C(0)OH 151.0-152.0 11-073 3,5-Ci2 CF3 ; 2-SCH3 C(0)OCH3 *2 11-074 3,5-Cl2 CF3 " 2-NO2 Br 179.0-181.0 11-075 3,5-Ci2 CF3 2-NO2 C(0)OEt 160.0-162.0 11-076 3,5-Cl2 CF3 2-NH2 Br *2 11-077 3,5-Cl2 CF3 2-NH2 C(0)OH *2 11-078 3,5-Cl2 CF3 2-NH2 C(0)OEt *2 11-079 3,5-Ci2 CF3 2-Ph C(0)OH _ *1 11-080 3,5-Cl2 CF3 2-Ph C(0)0CH3 . ~ *1 11-081 3,5-Cl2 CF3 2,3-F2 CH3 *1 11-082 3,5-Cl2 CF3 2,3-F2 CHaBr *1 11-083 3,5-C!2 CF3 2,3-F2 CH2OH *1 11-084 3,5-Cl2 CF3 2,6-Cl2 C(0)OEt *2 11-085 3,5-Cl2 CF3 2-CI-6-CH3 NH2 *1 11-086 3,5-Cl2 CF3 2,6-(CH3)2 OH 209.0-214.0 11-087 3,5-Cl2 CF3 2,6-(CH3)2 OSO2CF3 nD'''°^1.5194 11-088 3,5-Cl2 CF3 2,6-(CH3)2 C(0)OH 128.5-130.5 11-089 3,5-Cl2 CF3 2,6-(CH3)2 CCOpCHg 135.0-138.0 11-090 3,5-Cl2 CF2CI 2-CI C(0)OH 100.0-104.5 11-091 3,5-Cl2 CF2CI 2-CH3 C(0)OH 76.0-80.0 11-092 3,5-Cl2 CF2CI 2-CH3 C(0)OEt *1 11-093 3,5-Br2 CF3 2-CI C(0)OH 144.5-147.0 11-094 3,5-Br2 CF3 2-CH3 C(0)OH 135.0-138.5 11-095 3,5-Br2 CF3 2-CH3 C(0)OEt *1 11-096 3-OCH2O-* CF3 ¬ C(0)OH 208.0-210.0 11-097 3-OCH20^ CF3 ¬ C(0)0CH3 172.0-173.0 Table 18 4 5 2 No. (XL R' A^ A' (Y)„ R m.p.(°C) 12-001 3,5-Cl2 CF3 N C ¬ CI 139.0-140.0 12-002 3,5-Cl2 CF3 N C ¬ Br 147.0-148.0 12-003 3,5-Cl2 CF3 N C ¬ C(0)OH 118.0-120 0 12-004 3,5-Cl2 CF3 N C ¬ C(0)OEt 154.0-155 0 12-005 3,5-Cl2 CF3 C N ¬ C(0)OH 195.5-198.5 12-006 3,5-Cl, CF3 C N - CppCHg 147.0-151.5 Table 19 HO, 2 a No. A^ (Y)„ R" R^ J „. m.p.(°C) 13-00113-00213-00313-00413-00513-00613-00713-00813-00913-010 C C C C C C C C C C ¬¬¬¬¬ 2-CH3 2-CH3 2-CH3 2-CH3 3-CH3 H H H H H H H H H H CH2CF3 CH2CF3 CHaPh CHsPh CH2(D^7a) CH2CF3 CH2CF3 CH2(D^7a) CH2(D^7a) CH2CF3 H CI H CI H H CI H CI H 153.0-154.0 158.0-160.0 191.0-192.0 131.0-133.0 166.0-168.0 190.&-194.0 134.0-137.0 163.0-164.0 174.0-176.0 163.0-168.0 Table 20 4 y y 6 (X')„,i No. X^ (X^Li R^ n^/b.p. r o 14-0014-0014-0014-0014-0014-0014-0014-0014-0014-01014-01114-012 CI CI CI CI CI CI CI CI CI CI CI CI 5-CI 5-CI 5-Ci 5-CI 5-CI 5-CI 5-CI 5-CI 5-Br 5-CH3 5-CH3-6-F 4,5-Cl2 Pr-i CHF2 CF3 CF2CI CF2CF3 CH2OCH2CF3 CH2TMS L-47a CF3 CF3 CF3 CF3 = 00^^^=1.5472 nD^^1.5370 64.0-66.0y2mmHg *2 *2 *2 *2 *2 *2 *2 nD^^"^1.4895 *1 347 14-013 CI 4-NHC{0)OBu-t-5-Cl CF3 67.068.0 14-014 Br - CF3 nD^^I.5258 14-015 Br 5-Br CF3 *2 144316 CF3 r- CF3 nD^^^I.4228 14-017 CF3 . 5-NO2 CF3 nD^^"^1.4553 14-018 T-4 ; ~ CF3 *2 14-019 OCF2CHFOCF2CF2CF3 - CF3 *2 14-020 0CH2ph - CF3 *2 •14-021 OCH2(Ph-2-CI) - CF3 *2 14-022 0(D^7f) - CF3 *2 14-023 SCF3 - CF3 *2 14-024 NO2 - CF3 ^ *2 Among the compounds of the prsent invention, ^H NMR data of the compounds that the measured value of molecular ion peak, melting point or refractive index is not shown are shown in Table 21. •i in the meantime, the indication of" (A)" in the table shows a condition in which tetramethylsilane is used as standard substance in chloroform-d solvent and measurement is carried out at 300MHz (CDCI3, Me4Si, 300MHz), hereinafter, the indication "(B)" shows the measurement condition of (CDCI3, Me4Si, 400MHz), the indication of "(C)" shows the measurement condition of (CDCIa-DMSO-dg, Me4Si, 300MHz), and the indication of "(D)" shows the measurement condition of (CDCI3¬DMSO-de, Me^Si, 400MHz). Table 21 No. 'H NMR 3-010 (A) 5 8.55-8!fe (m, 1H), 7.15-8.05 (m, 15H), 6.95-7.1 (m, 1H), 5.20 (s, 2H), 4.76 (d, J=4.4Hz, 2H), 4.10 (d, J=17.2Hz, 1H), 3.78 (d, J=17.2Hz, 1H). 3-034 (A) 8 7.2-7.5 (m, 7H), 4.55-4.7 (m, 2H), 4.06 (d, J=17.1 Hz, 1H), 3.67 (d, J=17.1Hz, 1H),2.38(s,3H). 3-059 (B) 5 7.9-7.95 (m, 2H), 7.8-7.9 (m, 1H), 7.7-7.8 (m, 2H), 7.51 (s, 2H), 7.4-7.45 (m, 1H), 5.02 (d, J=7.0Hz, 2H), 4.12 (d, J=17.0Hz, 1H), 3.73 (d,J=17.0Hz, 1H). 3-064 (A) 5 7.84 (d, J=8.4Hz, 2H), 7.74 (d, J=8.4Hz, 2H), 7.51 (bs, 2H), 7.43 (bs, 1H), 6.42 (bs, 1H), 4.63 (t, J=5.1Hz, 1H), 4.11 (d, J=17.4Hz, 1H), 3.65-3.85 (m, 3H), 3.5-3.65 (m, 4H), 1.24 (t, J=6.8Hz, 6H). 3-067 (A) 5 7.6-7.8 (m, 3H), 7.54 (d, J=7.8Hz, 2H), 7.44 (bs, 2H), 7.38 (bs, 1H), 3.4^.25 (m, 7H), 4.04 (d, J=17.7Hz, 1H), 3.69 (d, J=17.4Hz, 1H). 3-069 (A) 5 7.82 (d, J=8.7Hz, 2H), 7.71 (d, J=8.7Hz, 2H), 7.51 (bs, 2H), 7.42 (bs, 1H), 6.71 (bs, 1H), 4.11 (d, J=17.4Hz, 1H)„ 3.6-3.95 (m, 4H), 3.74 (d, J=17.1Hz, 1H), 3.48 (t, J=6.3Hz, 2H), 2.55-2.7 (m, 1H), 2.0-2.15 (m, 1H), 1.6-1.75 (m,1H). 3-072 (A) 6 7.85 (d, J=8.4Hz, 2H), 7.73 (d, J=8.4Hz, 2H), 7.51 (bs, 2H), 7.4¬ 7.5 (m, 1H), 6.44 (bs, 1H), 4.75 (t, J=4.8Hz, 1H), 4.1^.2 (m, 2H), 4.10 (d, J=17.4Hz, 1H), 3.75-3,9 and 3.6-3.65 (m, 2H), 3.72 (d, J=17.4Hz, 1H), 3.6-3.65 (m, 2H), 2.0-2.15 (m, 1H), 1.35-1.45 (m, 1H). 3-074 (A) 5 7.82 (d, J=8.4Hz, 2'H), 7.72 (d, J=8.4Hz, 2H), 7.51 (bs, 2H), 7.4¬ 7.45 (m, 1H), 6.53 (bs, 1H),~4:09 (d, J=17.4Hz, 1H), 3.72 (s, 2H), 3.71 (d, J=17.4Hz, 1H), 2.92 (s, 3H), 1.72 (s, 6H). .3-077 (A) 5 9.79 (s, 1H), 7.89 (d, J=8.4Hz, 2H), 7.76 (d, J=8.4Hz, 2H), 7.61 (bs, 2H), 7.51 (bs, 1H), 6.91 (bs, 1H), 4.46 (d, J=4.5Hz, 2H),,4.11 (d, J=17.4Hz, 1H), 3.72 (d, J=17.1Hz, 1H). 3-078 (A) 5 9.27 (bs, 1H), 7.85 (d, J=8.5Hz, 2H), 7.74 (d, J=8.7Hz, 2H), 7.60 and 6.93 (t, J=4.4Hz, 1H), 7.51 (bs, 2H), 7.44 (bs, 1H), 6.71 (bs, 1H), ¬ 4.37 and 4.26 (d, J=4.7Hz, 2H), 4.11 (d, J=16.8Hz, 1H), 3.72 (d, J=17.4 Hz, 1H). 3-079 (A) 5 7.8-7.9 (m, 2H), 7.7-7.8 (m, 2H), 7.45-7.55 (m, 2H), 7.45-7.55 and 6.82 (t, J=4.4Hz, 1H), 7.43 (t, J=2.0Hz, 1H), 6.71 and 6.60 (bs, 1H), ' 4.31 and 4.24 (t, J=4.5Hz, 2H), 4.11 (d, J=17.4Hz, 1H), 3.94 and 3.88 (s,3H),3.72(d,J=17.4Hz, 1H). 3-082 (A) 5 7.90 (d, J=8.7Hz, 2H), 7.73 (d, J=8.7Hz, 2H), 7.52 (s, 2H), 7.43 (s , 1H), 7.10 (t, J=4.8Hz, 1H), 4.21 (d, J=4.8Hz, 2H),4.12 (d, J=17.4Hz, 1H), 3.74 (d,J=17.4Hz, 1H). 3-083 (A) 5 7.87 (d, J=8.1Hz, 2H), 7.74 (d, J=8.1Hz, 2H), 7.52 (s, 2H), 7.43 (s , 1H), 6.73 (bs, 1H), 4.26 (d, J=5.1Hz, 2H), 4.11 (d, J=17.4Hz, 1H), 3.82 (s, 3H), 3.73 (d, J=17.4Hz, 1H). 3-087 (A) 5 8.52 (bs, 1H), 7.97 (bs, 1H), 7.88 (d, J=8.4Hz, 2H), 7.7-7.8 (m, 3H), 7.51 (s, 2H), 7.43 (s, 1H), 4.45 (d, J=4.8Hz, 2H), 4.11 (d, J=17.4 Hz, 1H), 3.74 (d, J=17.4Hz, 1H). 3-089 (A) 5 7.84 (d, J=8.5Hz, 2H), 7.73 (d, J=8.5Hz, 2H), 7.51 (bs,.2H), 7.43 (bs, 1H), 6.18 (bs, 1H), 5.85^.05 (m, 1H), 5.2-5.35 (m, 2H), 4.05-4.15 (m, 3H),3.72,(d,J=17.4Hz, 1H). 3-107 (A) 57.82 (d, J=8.1Hz, 2H), 7.72 (d, J=8.4Hz, 2H), 7.55 (s, 1H), 7.51 (bs, 2H), 7.43. (bs, 1H), 6.27 (bs, 1H), 4.48 (d, J=5.1Hz, 2H), 4.10 (d, J=17.1Hz, 1H), 3.79 (s, 3H), 3.71 (d, J=17.4Hz, 1H). 3-108 (A) 57.82 (d, J=8.1Hz, 2H), 7.72 (d, J=8.4Hz, 2H), 7.51 (bs, 2H), 7.4¬ 7.45 (m, 1H), 6.34 (bs, 1H), 4.48 (d, J=5.4Hz, 2H), 4.10 (d,'U=17.1Hz, 1H), 3.81 (s, 3H), 3.71 (d, J=17.4Hz, 1H). 3-110 (A) 5 7.82 (d, J=8.1Hz, 2H), 7.74 (d, J=8.7Hz, 2H), 7.51 (bs, 2H), 7.43 (bs, 1H), 6.36 (bs, 1H), 6.17 (s, 1H), 4.65 (d, J=5.7Hz, 2H), 4.08 (d, J=17.1Hz, 1H), 3.85 (s, 3H), 3.69 (d, J=17.4Hz, 1H). 3-114 (A) 5 7.86 (d, J=8.1Hz, 2H), 7.71 (d, J=8.4Hz, 2H), 7:51 (bs, 2H), 7.4¬ 7.45 (m, 2H), 7.08 (s, 1H), 6.98 (bs, 1H), 4.68 (d, J=5.4Hz, 2H), 4.07 (d, J=17.4Hz, 1H), 3.68 (d, J=17.4Hz, 1H), 2.72 (s, 3H). 3-118 (D) 5 7.95-8.0 (m, 2H), 7.75-7.8 (m, 2H), 7.35-7.55 (m, 4H), 5.45-5.5 (m, 2H), 4.15-4.2 (m, 1H), 3.8-3.85 {m, 1H), 2.57 (s, 3H). 3-119 (B) 5 8.55-8.65 (m, 1H), 7.91 (d, J=8.2Hz, 2H), 7.65 (d, J=8.2Hz, 2H), 349 7.50 (s, 2H), 7.42 (s, 1H), 6.91 (s, 1H), 6.86 (s, 1H), 4.67 (d, J=5.3 Hz, 2H), 4.08 (d, J=17.0Hz, 1H), 3.77 (s, 3H), 3.70 (d, J=17.0Hz, 1H). 3-120 (B) 5 7.35-8.0 (m, 8H), 6.95 (m, 2H), 6.6-6.75 (m, 2H), 4.08 (d, J=17.0 Hz, 1H), 3.70 (d, J=17.0H2,1H), 3.63 (s, 3H). 3-121 (B) 5 8.1-8.2 (m, 1H), 7.65-7.9 (m, 3H), 7.4-7.6 (m, 3H), 7.1-7.2 (m, 1H) , 4.86 (d, J=5.8Hz, 2H), 4.05-4.15 (m, 1H), 3.65-3.8 (m, 1H), 2.72 (s, 3H). 3-122 (A) 5 8.43 (s, 1H), 7.88 (d, J=8.1 Hz, 2H), 7.72 (d, J=8.1 Hz, 2H), 7.51 (s , 2H), 7.44 (s, 1H), 7.30 (t, J=5.4Hz, 1H), 4.93 (d, J=5.4Hz, 2H), 4.10 (d, J=17.1Hz, 1H), 3.72 (d, J=17.1Hz, 1H). 3-127 (B) 5 7.93 (d, J=8.2Hz, 2H), 7.82 (t, J=4.8Hz, 1H), 7.74 (d, J=8.2Hz, 2H) , 7.58 (t, J=7.7Hz, 1H), 7.5-7.55 (m, 2H), 7.43 (t, J=1.8Hz, 1H), 7.16 ... (d, J=7.7Hz. 1H), 7.09 (d, J=7.7Hz, 1H), 4.71 (d, J=4.8Hz, 2H), 3.93 ¬(d, J=17.2Hz, 1H), 3.74 (d, J=17.4Hz, 1H), 2.57 (s, 3H). 3-131 (A) 5 8.55 (s. 1H), 8.40 (s, 1H), 7.91 (d, J=8.2Hz, 2H), 7.72 (d, J=8.2Hz , 2H), 7.53 (s, 3H), 7.42 (s, 1H), 4.7-4.8 (m, 2H), 4.13 (d, J=17.0Hz, i 1H), 3.74 (d, J=17.0Hz, 1H), 2.57 (s, 3H). 3-134 (A) 6 9.64 (bs, 1H), 7.81 (d, J=8,1Hz, 2H), 7.69 (d, J=8.1Hz, 2H), 7.50 (s, 2H), 7.43 (s, 1H), 4.10 (d, J=17.4Hz, 1H), 3.86 (s, 3H), 3.73 (d, J= 17.4Hz, 1H). 3-135 (A) 5 8.19 (d, J=4.2Hz, 1H), 7.95 (d, J=8.4Hz, 2H), 7.76 (d, J=8.4Hz, 2H) , 7.5-7.6 (m, 4H), 7.44 (s, 1H), 7.10 (bs, 1H), 6.84 (t, J=8.4Hz, 1H), 6.78 (d, J=8.4Hz, 1H), 4.11 (d, J=17.4Hz, 1H), 3.73 (d, J=17.4Hz, 1H). 3-143 (A) 5 8.57 (d, J=5.1 Hz, 1H), 8.21 (bs, 1H), 7.85-8.05 (m, 2H), 7.6-7.8 (m, 3H), 7.15-7.45 (m, 5H), 4.72 (d, J=5.1Hz, 2H), 4.10 (d, J=17.4Hz, 1H), 3.76 (d, J=17.4Hz, 1H), 2.38 (s, 3H). 3-147 (A) 5 7.86 (d, J=8.5Hz, 2H), 7.77 (d, J=8.5Hz, 2H), 7.55-7.65 (m, 1H), 7.2-7.3 (m, 1H), 4.05-4.25 (m, 3H), 3.86 (d, J=17.0Hz, 1H), 2.30 (s, 3H). 4-003 (A) 5 8.5-8.7 (m, 1H), 7.35-7.9 (m, 9H), 7.1-7.3 (m, 1H), 4.5-5.1 (m, 4H) , 4.0-4.2 (m, 1H), 3.6-3.8 (m, 1H), 3.15-3.55 (m, 3H). 4-004 (A) 5 8.55-8;.65 (m, 1H), 7.35-7.8 (m, 9H), 7.1-7.3 (m, 1H), 4.6-5.15 (m, 4H), 3.3A2 (m, 4H), 1.1-1.35 (m, 3H). 4-005 (A) 5 8.2-8.3 (m, 1H), 7.15-7.8 (m, 10H). 4.75-5.35 (m, 4H), 4.08 (d, J= 17.0Hz, 1H), 3.70 (d,J=17.0Hz, 1H), 3.04 and 2.84 (bs, 3H). 4-006 (B) 5 8.5-8.6 (m, 1H), 7.1-7.75 (m, 10H), 5.65-5.95 (m, 1H), 5.1-5.3 (m, 2H), 4.85 and 4.53 (s, 2H), 3.6-4.2 (m, 4H). 4-007 (B) 5 8.5-8.7 (m, 1H), 6.95-7.75 (m, 10H), 5.65-6.1 (m, 2H), 5.1-5.45 (m, 4H), 4.4^.9 (m, 4H), 3.75-4.2 (m, 3H). 4-008 (A) 5 8.50 (bs, 1H), 7.0-7.75 (m, 15H), 4.35^.9 (m, 4H), 4.05 (d, J=17.0 Hz, 1H), 3.68 (d,J=17.0Hz, 1H). 4-009 (A) 6 8.5-8.55 (m, 1H), 7.65-7.75 (m, 5H), 7.51 (s, 2H), 7.42 (s, 1H), 7.25-7.3 (m, 1H), 7.15-7.25 (m, 1H), 5.17 (s, 2H), 4.10 (d, J=17.0Hz, 1H), 3.71 (d, J=17.0Hz, 1H), 3.60 (s, 3H). 4-010 (A) 8 8.37 (bs, 1H), 7.65-7.8 (m, 3H), 7.3-7.55 (m, 6H), 4.4-4.9 (m, 2H), 4.10 (d, J=17.0Hz, 1H), 3.70 (d, J=17.0Hz, 1H), 3.1-3.65 (m, 2H), 1.12 (bs, 3H). 4-011 (B) 5 7.7-7.8 (m, 4H), 7.52 (s, 2H), 7.43 (s, 1H), 4.10 (d, J=17.0Hz, 1H) , 3.72 (d, J=17.0Hz, 1H), 3.53 (s, 3H), 3.37 (s, 3H). 5-001 (A) 5 8.51 (d, J=4.8Hz, 1H), 7.69 (t. J=5.1Hz, 1H), 7.62 (s, 1H), 7.45¬ 7.55 (m, 2H), 7.25-7.4 (m.'iiH), 7.22 (dd, J=6.9,2.5Hz, 1H), 4.73 (d, J= 5.1Hz, 2H), 4.09 (d, J=1&8Hz, 1H), 3.73 (d, J=16.8Hz, 1H), 2.48 (s, 3H). 5-003 (A) 8 8.51 (d, J=4.8Hz, A H), 7.77 (s, 1H), 7.68 (t, J=4.5Hz, 1H), 7.45¬ 7.6 (m, 5H), 7.25-7.35 (m, 3H), 7.22 (dd, J=7.5,1.8Hz, 1H), 4.73 (d, J= 4.5Hz, 2H), 4.09 (d, J=17.4Hz, IN), 3.73 (d, J=17.4Hz, 1H), 2.49 (s, 3H). • 5-007 (A) 5 8.52 (d, J=4.2Hz, 1H), 7.78 (d, J=9.3Hz, 2H), 7.67 (t, J=5.1 Hz, 1H) , 7.51 (bs, 3H), 7.3-7.4 (m, 4H), 7.15-7.25 (m, 1H), 4.73 (d, J=5.1Hz, 2H), 4.07 (d, J=17.4Hz, 1H), 3.70 (d, J=17.4Hz, 1H), 2.48 (s, 3H). 5-009 (A) 8 8.51 (d, J=4.5Hz, 1H), 7.89 (bs, 1H), 7.82 (d, J=7.8Hz, 1H), 7.65¬ 7.75 (m, 2H), 7.60 (t, J=7.8Hz, 1H), 7.5-7.55 (m, 3H), 7.33 (bs, 1H), ~ 7.32 (d, J=7.8Hz, 1H), 7.21 (dd, J=7.2,1.5Hz, 1H), 4.73 (d, J=5.1Hz, 2H), 4.15 (d, J=17.4Hz, 1H), 3.77 (d, J=17.4Hz, 1H), 2.49 (s, 3H). 5-010 (A) 6 7.25-7.6 (m,7H), 6.37 (bs, 1H), 4.0-4.15 (m,2H), 4.11 (d, J=17.4 Hz, 1H), 3.77 and 3.75 (d, J=17.4Hz, 1H), 2.95 (dd, J=10.2, 8.7Hz, 1H), 2.41 (s, 3H), 2.03 (dd, J=10.2, 3.3Hz, 1H), 1.90 (dd, J=8.7, 3.3Hz, 1H). 5-011 (A) 5 8.51 (d, J=4.2Hz, 1H), 7.69 (t, J=4.8Hz, 1H), 7.15-7.6 (m, 10H), 4.72 (d, J=4.8Hz, 2H), 4.10 (d, J=17.1Hz, 1H), 3.77 (dd, J=17.1, 3.0Hz, 1H), 2.95 (dd, J=10.2, 8.4Hz, 1H), 2.48 (s, 3H), 2.02 (dd, J=10.2, 3.0Hz , 1H), 1.89 (dd, J=8.4, 3.0Hz, 1H). 5-012 (A) 6 7.25-7.5 (m, 7H), 7.16 (bs, 1H), 4.0-4.2 (m, 3H), 3.75 (d, J=17.2Hz ,1H),2.42(s,3H). 5-013 (A) 8 8.5-8.6 (m, 1H), 7.65-7.8 (m, 1H), 7.15-7.6 (m, 10H), 4.72 (d, J= 5.2Hz, 2H), 4.12 (d, J=17.3Hz, 1H), 3.74 (d, J=17.3Hz, 1H), 2.46 (s, 3H). 5-015 (B) 8 8.5-8.55 (m, 1H), 7.72 (td, J=6.8,4.8Hz, 1H), 7.45-7.6 (m, 5H), 7.2-7.4 (m, 5H), 4.75 (d, J=4.8Hz, 2H), 4.11 (d, J=17.2Hz, 1H), 3.74 (d, J=17.2Hz,1H), 2.50(3, 3H). 5-016 (A) 8 7.35-7.6 (m, 6H), 7.2-7.3 (m, 1H), 6.10 (d, J=53.4Hz, 1H), 6.06 (bs , 1H), 4.0-4.2 (m, 3H), 3.72 (d, J=16.8Hz, 1H), 2.47 (s, 3H). 5-017 (A) 8 8.54 (d, J=4.8Hz, 1H), 7.65-7.75 (m, 1H), 7.35-7.6 (m, 6H), 7.2¬ 7.35 (m, 4H),-6.10 (d, J=53.1Hz, 1H), 4.75 (d, J=5.1Hz, 2H), 4.11 (d, J= 17.4Hz, 1H), 3.73 (d, J=17.4Hz, 1H), 2.50 (s, 3H). 5-018 (A) 5 8.45-8.55 (m, 1H), 7.15-7.75 (m, 14H), 6.95-7.05 (m, 1H), 5.19 (s, 2H), 4.74 (d, J=4.4Hz, 2H), 4.07 (d, J=16.8Hz, 1H), 3.75 (d, J=16.8Hz, 1H),2.49(s,3H). 5-019 (A) 5 8.24 (s, 1H), 8.00 (s, 1H), 7.2-7.6 (m, 6H), 7.2-7.3 (m, 1H), 6.44 (t, J=6.5Hz, 1H), 3.95^.15 (m, 2H), 4.09 (d, J=17.1Hz, 1H), 3.78 (d, J= 17.1Hz, 1H), 2.40 (s,3H). 5-020 (A) 5 8.52 (d, J=4.8Hz, 1H), 8.25 (s, 1H), 8.00 (s, 1H), 7.45-7.75 (m, 7H), 7.15-7.35 (m, 4H), 4.74 (d, J=4.8Hz, 2H), 4.10 (d, J=17.4Hz, 1H), 3.78 (d, J=17.4Hz, 1H), 2.49 (s, 3H). 5-021 (A) 8 8.51 (d, J=4.5Hz, 1H), 7.69 (t, J=5.1Hz, 1H), 7.5-7.6 (m, 4H), 7.25 -7.4 (m, 5H), 7.21 (dd, J=7.2,1.5Hz, 1H), 4.73 (d, J=5.1 Hz, 2H), 4.08 (d, J=17.4Hz, 1H), 3.74 (d, J=17.4Hz, 1H), 2.98 (q, J=7.2Hz, 2H), 2.48 (s,3H), 1.33(t,J=7.2Hz,3H). 5-022 (A) 5 7.89 (s, 1H), 7.7-7.8 (m, 2H), 7.5-7.6 (m, 3H), 7.45 (d, J=8.0Hz, 1H), 6.06 (t, J=6.2Hz, 1H), 4.0-4.2 (m, 3H), 3.73 (d, J=16.6Hz, 1H), 2.47 (s, 3H). 5-023 (A) 6 8.55 (d, J=4.7Hz, 1H), 7.90 (s, 1H), 7.65-7.8 (m, 3H), 7.5-7.6 (m, 4H), 7.3-7.45 (m, 2H), 7.2r7.3,(m, 1H), 4.74 (d, J=5.0Hz, 2H), 4.12 (d, J=17.1Hz, 1H), 3.73 (d, J=17.1Hz, 1H), 2.49 (s, 3H). 5-024 (B) 5 7.65 (d, J=8.1 Hz, 1H), 7.45-7.6 (m, 4H), 7.40 (d, J=7.9Hz, 1H),' 7.34 (d, J=7.7Hz, 1H), 6.35 (bs, 1H), 4.0^.15 (m, 3H), 3.73 (d, J=17.2 Hz, 1H), 3.37 (s, 3H), 2.43 (s, 3H). 5-025 (B) 5 8.5-8.55 (m, 1H), 7.71 (td, J=7.7,1.6Hz, 1H), 7.3-7.7 (m, 7H), 7.28 (d, J=4.6Hz, 1H), 7.26 (t, J=4.8Hz, 1H), 7.23 (dd, J=7.5, 5.9Hz, ^ 1H), 4.75 (d, J=4.8Hz, 2H), 4.12 (d, J=17.2Hz, IN), 3.73 (d, J=17.2Hz,~ 1H), 3.39 (s,3H), 2.50 (s,3H). 5-026 (B) 5 7.4-7.65 (m, 6H), 7.36 (d, J=7.9Hz, 1H), 6.34 (t, J=6.1 Hz, 1H), 4.11 (d, J=17.2Hz, 1H), 4.08 (qd, J=9.6, 6.6Hz, 2H), 3.73 (d, J=17.4Hz, ,, 1H), 3.50 (d, J=0.9Hz, 3H), 2.41 (s, 3H). 5-027 (B) 8 8.53 (ddd, J=4.9,1.6, 0.9Hz, 1H), 7.70 (td, J=7.7,1.8Hz, 1H), 7.6 -7.65 (m,-2H), 7.5-7.55 (m, 4H), 7.44 (ddd, J=7.9, 2.0,1.3Hz, 1H), 7.33 (d, J=7.7Hz, 1H), 7.26 (t, J=4.8Hz, 1H), 7.22 (ddd, J=7.5,4.8,1.1Hz, 1H), 4.75 (d, J=4.8Hz, 2H), 4.12 (d, J=17.2Hz, 1H), 3.74 (d, J=17.2Hz, 1H), 3.51 (s,3H), 2.49 (s,3H). 5-028 (B) 8 8.5-8.55 (m, 1H), 7.83 (bs, 1H), 7.2-7.75 (m, 15H), 4.76 (d, J=4.8 Hz, 2H), 4.13 (dd, J=17.2,1.8Hz, 1H), 3.82 (d, J=17.2Hz, 1H), 2.51 (s, 3H). 5-029 (A) 5 8.51 (d, J=4.5Hz, 1H), 7.69 (t, J=5.1 Hz, 1H), 7.51 (bs, 2H), 7.50 (bs, 1H), 7.15-7.4 (m, 5H), 6.8-6.95 (m, 1H), 4.74 (d, J=4.8Hz, 2H), 4.07 (d, J=17.4Hz, 1H), 3.72 (d, J=17.4Hz, 1H), 2.48 (s, 3H). 5-030 (A) 8 7.2-7.45 (m, 6H), 6.49 (bs, 1H), 4.0-4.15 (m, 2H), 3.46 (s, 2H), 2.40 (s,3H), 1.79 (s,3H). 5-031 (A) 8 7.25-7.5 (m, 6H), 6.50 (bs, 1H), 4.0-4.15 (m, 2H), 3.60 (d, J=16.8 Hz, 1H), 3.39 (d, J=16.8Hz, 1H), 2.38 (s, 3H), 2.15-2.3 (m, 1H), 0.98 (d, J=6.6Hz, 3H), 0.90 (d, J=6.9Hz, 3H). 5-033 (A) 5 8.51 (d, J=4.8Hz, 1H), 7.69 (t, J=4.5Hz, 1H), 7.45-7.5 (m, 3H), 7.41 (bs, 2H), 7.15-7.4 (m, 4H), 4.73 (d, J=4.5Hz, 2H), 3.57,(d, J=16.8 Hz, 1H), 3.47 (d, J=16.8Hz, 1H), 2.48 (s, 3H), 1.35-1.5 (m, 1H), 0.45¬ 0.7 (m, 4H). 5-035 (B) 8 8.5-8.55 (m, 1H), 7.72 (td, J=7.6,1.8Hz, 1H), 7.5-7.55 (m, 4H), 7.43 (d, J=1.8Hz, 2H), 7.35-7.4 (m, 2H), 7.2-7.25 (m, 1H), 4.76 (d, J= 4.8Hz, 2H), 3.93 (d, J=16.8Hz, 1H), 3.85 (dd, J=18.6,11.8Hz, 2H), 3.53 (d,J=16.8Hz, 1H),2.50(s,3H). 5-037 (A) 8 8.53 (d, J=5.0Hz, 1H), 7.65-7.75 (m, 1H), 7.15-7.6 (m, 9H), 5.89 (t J=55.2Hz, 1H), 4.74 (d, J=4.7Hz, 2H), 4.00 (d, J=17.0Hz, 1H), 3.55 (d, J=17.0Hz, 1H),2.50(s,3H). 5-038 (B) 5 8.17 (t, J=7.0Hz, 1H), 7.45-7.6 (m, 4H), 7.44 (t, J=1.8Hz, 1H), 7.0 -7.1 (m, 1H), 4.05-4.25 (m, 3H), 3.73 (d, J=17.4Hz, 1H). 5-040 (A) 5 8.82 (s, 1H), 8.19 (t, J=7.8Hz, 1H), 7.4-7.6 (m, 6H), 7.31 (s, 1H), 4.84 (d, J=5.4Hz, 2H), 4.08 (d, J=17.4Hz, 1H), 3.69 (d, J=17.1Hz, 1H). 5-042 (B) 5 8.03 (m, 1H), 7.64'(d, J=1.1 Hz, 1H), 7.58 (d, J=0.8Hz, 1H), 7.50 (s, 2H), 7.43 (bs, 1H), 6.39 (bs, 1H), 4.18 (d, J=16.0Hz, 1H), 4.1-4.2 (m,2H), 3.80(d,J=16:.0Hz, 1H). 5-048 (A) 8 8.22 (d, J=8.7Hz;2H); 7.81 (d, J=7.8Hz, 1H), 7.74 (d, J=1.2Hz, 1H) , 7.63 (dd, J=8.4,1.8Hz, 1H), 7.54 (d, J=8.7Hz, 2H), 7.50 (bs, 2H), 7.44 (d, J=2.1 Hz, 1H), 6.72 (bs, 1H), 4.77 (d, J=6.3Hz, 2H), 4.04 (d, J= 17.1Hz, 1H), 3.66 (d, J=17.1Hz, 1H). 5-049 (A) 5 7.81 (d, J=8.1Hz, 1H), 7.7-7.75 (m, 2H), 7.63 (dd, J=8.1, 1.8Hz, 1H), 7.50 (bs, 2H), 7.44 (bs, 1H), 7.34 (d, J=3.3H2,1H), 7.16 (bs, Ihf), • 5.00 (d, J=5.4Hz, 2H), 4.06 (d, J=17.1Hz, 1H), 3.69 (d, J=17.1Hz, 1H). 5-050 (A) 8 8.79 (s, 1H), 7.75 (dd, J=8.4, 3.0Hz, 1H), 7.70 (bs, 1H), 7.60 (bs, 1H), 7.50 (bs, 2H), 7.44 (bs, 1H), 7.33 (s, 1H), 7.01 (bs, 1H), 4.82 (d, J=5.1Hz, 2H), 4.07 (d,'J=17.4Hz, 1H), 3.69 (d, J=17.1Hz, 1H). 5-051 (A) 8 7.7-7.8 (m, 2H), 7.61 (dd, J=8.1,1.5Hz, 1H), 7.50 (bs, 2H), 7.44 ) (bs, 1H), 7.19 (s, 1H), 6.84 (bs, 1H), 4.69 (d, J=5.7Hz, 2H), 4.07 (d, J=17.4Hz, 1H), 3.69 (d, J=17.4Hz, 1H). 5-052 (B) 8 8.63 (s, 1H), 7.25-7.75 (m, 7H), 5.10 (d, J=5.8Hz, 2H), 4.07 (d, J= 17.0Hz, 1H), 3.71 (d, J=17.0Hz, 1H). 5-053 (A) 8 8.54 (d, J=4.2Hz, 1H), 7.77 (d, J=7.8Hz, 1H), 7.6-7.8 (m, 3H), 7.62 (d, J=7.8Hz, 1H), 7.50 (bs, 2H), 7.44 (bs, 1H), 7.34 (d, J=7.5Hz, 1H), 7.23 (dd, J=7.5, 2.4Hz, 1H), 4.78 (d, J=4.5Hz, 2H), 4.08 (d, J=18.0Hz, 1H), 3.71 (d,J=18.0Hz, 1H). 5-056 (A) 5 8.55 (d, J=4.5Hz, 1H), 8.08 (t, J=4.5Hz, 1H), 7.96 (s, 1H), 7.78 (d, J=8.4Hz, 1H), 7.72 (d, J=8.4Hz, 1H), 7.69 (dd, J=4.5, 2.4Hz, 1H), 7.50 (bs, 2H), 7.43 (bs, 1H), 7.33 (d, J=7.2Hz, 1H), 7.23 (dd, J=7.2, 2.4Hz, 1H), 4.73 (d, J=4.5Hz, 2H), 4.28 (d, J=18.0Hz, 1H), 3.87 (d, J= 18.0Hz, 1H). 5-058 (B) 8 8.54 {0, J=3.9Hz, 1H), 7.89 (bs, 1H), 7.74 (td, J=7.8,' 1.8Hz, 1H), 7.6-7.7 (m, IH), 7.50 (bs, 3H), 7.44 (t, J=1.8Hz, 1H), 7.38 (d, J=7.8Hz, 1H), 7.2-7.3 (bs, 1H), 4.79 (d, J=4.7Hz, 2H), 4.07 (d, J=17.2Hz, IH), 3.70 (d,J=17.2Hz, IH). 5-060 (B) 5 8.01 (bs, 1H), 7.65-7.75 (m, 2H), 7.50 (bs, 2H), 7.4-7.45 (m, 1H), 6.25-6.3 (m,'1H), 4.06 (d, J=17.2Hz, 1H), 3.55-3.75 (m, 3H), 3.45-3.6 (m ,4H), 1.20(t,J=7.0Hz,3H). 5-061 (B) 5 8.10 (bs, IH), 7.69 (d, J=8:0Hz, IH), 7.50 (bs, 2H), 7.4-7.45 (m, 2H), 6.09 (bs, IH), 4.54 (t, J=5.2Hz, IH), 4.06 (d, J=-17.2Hz, IH), 3.69 . (d, J=17.2Hz, IH), 3.60 (t, J=5.2Hz, 2H), 3.44 (s, 6H). 5-062 (B) 5 8.13 (bs, 1H), 7.71 (d, J=8.0Hz, 1H), 7.4-7.5 (m, 4H), 6.7-6.9 (br, IH), 6.05-6.3 (br, IH), 4.054.15 (m, 2H), 4.06 (d, J=17.2Hz, IH), 3.69 (d,J=17.2Hz, 1H),2.88(bs,3H). 5-065 (B) 8 8.5-8.55 (m, 1H), 8.13 (d, J=1.8Hz, 1H), 7.7-7.5 (m, 2H), 7.50 (d, J=1.8Hz, 2H), 7.44 (t, J=1.8Hz, 1H), 7.37 (d, J=8.0Hz, 1H), 7.2-7.3 (m, 3H), 478 (d, J=4.8Hz, 2H), 4.06 (d, J=17.2Hz, IH), 3.68 (d, J=17.2Hz, 1H). 5-066 (B) 8 7.45-7.55 (m, 6H), 6.40 (bs, 1H), 6.00 (bs, 1H), 4.09 (d, J=17.0Hz, 1H),3.71 (d,J=17.0Hz, 1H),2.49 (s, 3H). 5-070 (A) 57.35-7.55 (m, 6H), 6,02 (bs, 1H), 4.09 (d, J=17.4Hz, 1H), 3.71 (d, J=17.4Hz, 1H), 3.25-3.35 (m, 2H), 2.45 (s, 3H), 1.0-1.15 (m, 1H), 0.55¬ 0.65 (m, 2H), 0.2^0.35 (m, 2H). 5-072 (A) 8 7.35-7.55 (m, 6H), 5.78 (bs, 1H), 4.08 (d, J=17.0Hz, 1H), 3.69 (d, J=17.0Hz, 1H), 3.47 (t, J=7.1Hz, 2H), 2.45-2.65 (m, 1H), 2.44 (s, 3H), 1.65-2.2 (m,6H). 5-077 (A) 67.4-7.5 (m, 6H), 6.19 (bs, 1H), 4.08 (d, J=16.8Hz, 1H), 3.5-3.75 (m , 7H), 2.47 (s, 3H), 1.20 (t, J=6.9Hz, 3H). 5-079 (B) 5 7.45-7.55 (m, 4H), 7.43 (t, J=1.8Hz, 1H), 7.39 (d, J=8.4Hz, 1H), 6.28 (bs, 1H), 4.27 (t, J=5.1Hz, 2H), 4.08 (d, J=17.2Hz, 1H), 3.65-3.75^^ (m, 3H), 2.44 (s, 3H), 2.08 (s, 3H). 5-080 (B) 8 7.45-7.55 (m, 4H), 7.35-7.45 (m, 2H), 6.48 (bs, 1H), 4.80 (bs, 1H), 4.28 (t, J=5.0Hz, 2H), 4.08 (d, J=17.2Hz, 1H), 3.70 (d,>17.2Hz, 1H), 3.65-3.7 (m, 2H), 3.15-3.25 (m, 2H), 2.46 (s, 3H), 1.13 (t, J=7.2Hz, 3H) • i 5-083 (A) 8 7.4-7.55 (m, 6H), 5.95 (bs, 1H), 4.48 (t, J=5.4Hz, 1H), 4.05 (d, J= 17.4Hz, 1H), 3.66 (d, J=17.4Hz, 1H), 3.59 (t, J=5.4Hz, 2H), 3.44 (s, 6H) , 2.48 (s, 3H). 5-084 (A) 8 7.4-7.55 (m, 6H), 6.02 (bs, 1H), 4.63 (t, J=5.1 Hz, 1H), 4.08 (d, J= 16.8Hz, 1H), 3.5-3.8 (m, 7H), 2.48 (s, 3H), 1.22 (t, J=6.6Hz, 6H). 5-085 (B) 8 7.45-7.55 (m, 4H), 7.43 (t, J=1.8Hz, 1H), 7.39 (d, J=8.4Hz, 1H), 6.31 (d, J=8.1Hz, 1H), 4.81 (bs, 1H), 4.35^.45 (m, 1H), 4.22 (dd, J=: 11.5, 6.8Hz, 1H), 4.10 (dd, J=11.5, 3.7Hz, 1H), 4.08 (d, J=17.2Hz, 1H), 3.70 (d, J=17.2Hz, 1H), 3.15-3.25 (m, 2H), 2.45 (s, 3H), 1.27 (d, J=7.1 Hz,3H), 1.13(t,J=7.2Hz,3H). 5-086 (A) 8 7.35-7.6 (m, 6H), 6.24 (bs, 1H), 4.0-4.15 (m, 2H), 3.65-3,9 (m, 4H) , 3.25-3.35 (m, 1H), 2.46 (s, 3H), 1.85-2.1 (m, 3H), 1.55-1.7 (m, 1H). 5-087 (A) 8 7.35-7.55 (m, 6H), 5.97 (bs, 1H), 4.08 (d, J=17.4Hz, 1H), 3.55-4.0 (m, 4H), 3.69 (ci, J=17.1Hz, 1H), 3.45-3.5 (m, 2H), 2.55-2.65 (m, 1H), 2.47 (s, 3H), 2.05-2.15 (m, 1H), 1.6-1.75 (m, 1H). 5-090 (A) 5 7.4-7.55 (m.6H), 6.14 (bs, 1H), 4.75 (t, J=4.5Hz, 1H), 4.14.2 (m, 2H), 4.08 (d, J=174Hz, 1H), 3.75-3.9 (m, 2H), 3.71 (d, J=174Hz, 1H), 3.5-3.65 (m, 2H), 2.47 (s, 3H), 2.0-2.15 (m, 1H), 13-1.45 (m, 1H). 5-092 (A) 8 7.35-7.6 (m, 6H), 7.05 (bs, 1H), 4.08 (d, J=17.1Hz, 1H), 3.94.05 (m, 2H), 3.70 (d, J=17.1Hz, 1H), 3.1-3.25 (m, 1H), 2.8-:2.95 (m, 1H), 2.66 (s, 3H), 2.47 (s, 3H). 5-094 (A) 8 7.4-7.6 (m, 6H), 6.73 (bs, 1H), 4.08 (d, J=17.1 Hz, 1H), 3.9-4.05 (m , 2H), 3.70 (d, J=17.1Hz, 1H), 3.28 (t, J=5.7Hz, 2H), 3.08 (q, J=7.5Hz, 2H), 2.47 (s, 3H), 143 (t, J=7.5Hz, 3H). 5-095 (A) 8 7.2-7.6 (m, 11H), 6.09 (bs, 1H), 4.08 (d, J=17.1 Hz, 1H), 3.75 (s, 2H), 3.70 (d, J=17.1Hz, 1H), 3.5-3.6 (m, 2H), 2.68 (t, J=6.3Hz, 2H), 2.45 (s, 3H). 5-096 (A) 8 7.35-7.55 (m, 11H), 6.62 (t, J=6.0Hz, 1H), 4.30 (s, 2H), 4.07 (d, J=174Hz, 1H), 3.85-3.95 (m, 2H), 3.69 (d, J=174Hz, 1H), 3.1-3.2 (m, 2H), 2.41 (s, 3H). 5-097 (A) 6 7.35-7.55 (m, 6H), 7.32 (s, 1H), 6.30 (bs, 1H), 6.22 (d, J=2.7Hz, 1H), 6.13 (bs, 1H), 4.08 (d, J=17.4Hz, 1H), 3.77 (s, 2H), 3.70 (d, J= 17.4Hz, 1H), 3.55-3.65 (m, 2H), 2.78 (t, J=6.3Hz, 2H), 2.47 (s, 3H). 5-098 (A) 8 7.4-7.55 (m, 7H), 6.55-6.6 (m, 2H), 6.45 (dd, J=3.0,1.8Hz, 1H), 4.39 (s, 2H), 4.07 (d, J=^7:4Hz, 1H), 3.85-3.95 (m, 2H), 3.69 (d, J=17.4 Hz, 1H), 3.25-3.3 (m, 2H), 2.45 (s, 3H). . 5-099 (A) 6 7.4-7.6 (m, 6H), 6.22 (t, J=5.4Hz, 1H), 4.08 (d, J=17.0Hz, 1H), 3.6 -3.75 (m, 2H), 3.35-3.5 (m, 1H), 2.85-3.05 (m, 1H), 2.49 (s, 3H), 2.11 (s,3H), 1.35(d,J=6.9Hz,3H). 5-100 (A) 5 7.4-7.6 (m, 6H), 7.15-7.25 and 6.9-7.0 (m, 1H), 3.9^.2 (m, 2H), 3.6-3.85 (m, 2H), 2.85-3.2 (m, 1H), 2.68 and 2.56 (s, 3H), 2.49 (s, 3flX 1.32(d,J=6.9Hz,3H). 5-101 (A) 57.4-7.6 (m, 6H), 6.65 (t, J=5.8Hz, 1H), 4.08 (d, J=17.3Hz, 1H), 3.75-4.0 {m, 2H), 3.69 (d, J=17.3Hz, 1H), 3.25-3.45 (m, 1H), 2.94 (s, 3H), 2.49 (s, 3H), 1.50 (d, J=6.9Hz, 3H). 5-1102 (A) 5 7.35-7.65 (m, 6H), 6.08 (bs, 1H), 4.3-^.45 (m, 1H), 4.09 (d, J=17.4 Hz, 1H), 3.71 (d, J=17.4Hz, 1H), 2.71 (d, J=5.7Hz, 2H), 2.44 (s, 3H), 2.17 (s, 3H), 1.34 (d, J=6.6Hz, 3H). 5-103 (A) 5 7.4-7.6 (m, 6H), 6.46 (d, J=8;iHz, 1H), 4.6-4.75 (m, IN), 4.08 (d, J=17.1Hz, 1H), 3.70 (d, J=174Hz, 1H), 3.42 (dd, J=14.4, 6.3Hz, 1H), 3.26 (dd, J=144, 5.1Hz, 1H), 3.03 (s, 3H), 2.45 (s, 3H), 1.53 (d, J=6.9 Hz, 3H). - 5-104 (A) (5 745-7.55 (m, 4H), 7.4-7.45 (m, 2H), 5.75 (bs, 1H), 4.07 (d, J=174 Hz, 1H), 3.69 (d, J=174Hz, 1H), 3.07 (s, 2H), 2.48 (s, 3H), 2.18 (s, 3H), 1.51 (s,6H). 5-112 (A) 8 745-7.65 (m, 6H), 7.43 and 6.93 (t, J=4.8Hz, 1H), 6.29 (bs, 1H), 4.33 and 4.25 (t, J=4.7Hz, 2H), 4.08 (d, J=17.1Hz, 1H), 3.70 (d, J=174 Hz, 1H),2.48(s,3H). 5-114 (A) 8 7.4-7.6 (m, 6H), 7.43 and 6.85 (bs, 1H), 6.30 (bs, 1H), 4.25-4.35 and 4.2-4.25 \m, 2H), 4.08 (d, J=174Hz, 1H), 3.93 and 3.86 (d, J=7.2Hz, 2H), 3.70 (d, J=17.4Hz, 1H), 2.49 (s, 3H), 1.1-1.3 (m, 1H), 0.5-0.6 (m, 2H), 0.2-0.3 (m, 2H). 5-115 (A) 8 7.57 and 6.86 (t, J=44Hz, 1H), 7.25-7.55 (m, 10H), 6.26 (bs, 1H), 5.10 and 5.02 (s, 2H), 4.28 and 4.20 (t, J=5.3Hz, 2H), 4.08 (d, J=17.1 Hz, 1H), 3.70 (d, J=17.1Hz, 1H), 2.44 (s, 3H). 5-116 (A) 8 7.4-7.5 (m, 6H), 7.39 and 6.79 (t, J=4.5Hz, 1H), 6.25 and 6.15 (bs, 1H), 4.0-4.3 (m, 4H), 4.05 (d, J=17.4Hz, 1H), 3.67 (d, J=174Hz, 1H), 2.46 and 245 (s, 3H), 0.9-1.25 (m, 2H), 0.01 (s, 9H). 5-118 (A) 8 7.45-7.55 (m, 4H), 7.35-7.45 (m, 2H), 6.19 (bs, 1H), 4.7^.85 (m, 1H), 4.08 (d, J=17.4Hz, 1H), 3.7-3.8 (m, 1H), 3.70 (d, J=174Hz, 1H), 3.5-3.6 (m, 1H), 3.0-3.15 (m, 1H), 2.7-2.85 (m, 1H), 2.47 (s, 3H), 2.00 (s, 3H). 5-120 (A) 8 7.4-7.6 (m, 6H), 7.11 (d, J=9.6Hz, 1H), 6.30 (d, J=9.6Hz, 1H), 4.0¬ 4.25 (nn, 3H), 3.70 (d, J=17.0Hz, 1H), 2.50 (s, 3H). 5-122 (A) 6 7.4-7.6 (m, 7H), 6.61 (d, J=3.3Hz, 1H), 6.49 (d, J=84Hz, 1H), 6.44 355 (dd,J=3.3, 2.1Hz, 1H), 6.33 (d, J=8.4Hz, 1H),4.08(d, J=:17.3Hz, 1H), 3.70 (d, J=17.3Hz, 1H), 2.48 (s, 3H). ^123 (A) § 7.3-7.6 (m, 8H), 7.0-7.1 (m, 1H), 6.49 (d, J=8.8Hz, 1H), 6.42 (d, J=8.8Hz, 1H), 4.08 (d, Jf 17.0Hz, 1H), 3.69 (d, J=17.0Hz, 1H), 2.50 (s, 3H), 5-126 (A) 5 8.62 (d, J=5.0Hz, lH),-7.85 (td, J=8.1, 2.1Hz, 1H), 7.35-7.65 (m, 9H), 6.15 (d, J=6.9Hz, 1H), 4.09 (d, J=17.0Hz, 1H), 3.71 (d, J=17.0Hz, 1H),2.52(s, 3H). 5-128 (A) 5 7.45-7.65 (m, 6H), 6.33 (bs, 1H), 4.23 (d, J=5.1Hz, 2H), 4.09 (d, J=17.4Hz, 1H), 3.81 (s, 3H), 3.70 (d, J=17.4Hz, 1H), 2.49 (s, 3H). 5-130 (B) 8 7.4-7.55 (m, 6H), 6.33 (d, J=6.6Hz, 1H), 4.75-4.85 (m, 1H), 4.08 (d , J=17.2Hz, 1H), 3.81 (s, 3H), 3.70 (d, J=17.2Hz, 1H), 2.49 (s, 3H), 1.55 (s,3H). 5-131 (B) 5 7.4-7.55 (m, 6H), 6.34 (d, J=7.6Hz, 1H), 47-4.8 (m, 1H), 4.2-^.3 (m, 2H), 4.08 (d, J=174Hz, 1H), 3.70 (d; J=174Hz, 1H), 2.49 (s, 3H), 1.54 (t, J=7.0Hz, 3H), 1.32 (t, J=7.2Hz, 3H). 5-132 (A) 5 7.4-7.55 (m, 6H), 6.36 (bs, 1H), 4.75^.9 (m, 1H), 4.6^.75 (m, 1H) , 4.4-4.55 (m, 1H), 4.18 (d, J=174Hz, 1H), 3.71 (d, J=17.4Hz, 1H), 2.45 (s,3H), 1.57(d,J=7.2Hz, 3H). 5-133 (A) 5 7.4-7.6 (m, 6H), 7.06 (d, J=6.6Hz, 1H), 5.76 (t, J=6.6Hz, 1H), 4.27 (d, J=6.6Hz, 1H), 4.08 (d, J=17.1Hz, 1H), 3.89 (s, 3H), 3.70 (d, J=17.1 Hz, 1H),2.49(s,3H). 5-134 (A) 8 7.4-7.6 (m, 6H), 6.79 (d, J=9.4Hz, 1H), 5.72 (d, J=9.4Hz, 1H), 4.09 (d, J=17.3Hz, 1H), 3.87 (s, 3H), 371 (d, J=17.3Hz, 1H), 3.59 (s, 3H), 2.51 (s, 3H). 5-136 (A) 8 7.35-7.55 (m, 6H), 6.44 (bs, 1H), 4.05-4.25 (m, 3H), 3.6-3.8 (m, 3H), 2.66 (t, J=6.0Hz, 2H), 2.46 (s, 3H), 1.27 (t, J=7.2Hz. 3H). 5-138 (A) 5 7.45-7.6 (m, 6H), 7.09.(bs, 1H), 6.69 (bs, 1H), 4.05-4.15 (m, 3H), 3.72 (d, J=174Hz, 1H), 2.83 (d, J=4.8Hz, 3H), 2.44 (s, 3H). 5-139 (A) 8 7.5-7.6 (m, 5H), 743 (s, 1H), 6.98 (bs, 1H), 4.23 (d, J=3.9Hz, 2H) , 4.09 (d, J=17.*hHz, 1H), 3.71 (d, J=17.1Hz, 1H), 3.04 (s, 3H), 3.02 (s, 3H), 2.50 (s, 3H). 5-141 (B) 8 7.4-7.55 (m, 6H), 7.05-7.1 (m, 1H), 6.62 (bs, 1H), 4.05-4.15 (m," 3H), 3.72 (d, J=17.2Hz, 1H), 3.23 (dd, J=13.8, 7.2Hz, 2H), 2.45 (s, 3H), 1.5-1.6 (m, 2H), 0.91 (t, J=74Hz, 3H). 5-143 (B) 5 7.4-7.55 (m, 6H), 6.9-7.05 (m, 1H), 6.45-6.55 (m, 1H), 4.05^.2 (m, 3H), 3.70 (d, J=17.2Hz, 1H), 3.1-3-. 15 (m, 2H), 2.45-2.5 (m, 4H), 0.9¬ 1.0(m,6H). 5-145 (B) 8 7.4-7.55 (m, 6H), 6.78 (bs, 1H), 5.93 (bs, 1H), 4.0^.15 (m, 3H), 3.70 (d, J=16.8Hz, 1H), 2.48 (s, 3H), 1.38 (s, 9H). 5-146 (B) 8 7.4-7.55 (m, 6H), 7.01 (bs, 1H), 6.53 (bs, 1H), 4.05-4.2 (m, 3H), 3.71 (d, J=17.4Hz, 1H), 3.05-3.1 (m, 2H), 2.46 (s, 3H), 0.91 (s, 9H). 5-147 (B) 8 7.4-7.55 (m, 6H), 6.89 (bs, 2H), 4.56 (t, J=5.0Hz, 1H), 4.44 (t, J= 5.0Hz, 1H), 4.16 (d,J-5.0Hz,2H), 4.19 (d,J=17.2Hz,1H), 3.71 (d, J= 17.2Hz, 1H), 3.5-3.7 (m, 2H), 2.46 (s, 3H). 5-149 (A) 8 7.45-7.6 (m, 5H), 7.42 (s, 1H), 7.27 (bs, 1H), 4.25-44 (m, 2H), 4.09 (d, J=17.4Hz, 1H), 3.6-3.8 (m, 5H), 3.17 (s, 3H), 2.49 (s, 3H). 5-150 (B) 6 7.4-7.55 (m, 6H), 6.8-7.2 (m, 2H), 4.16 (d, J=5.0Hz, 2H), 4.09 (d, J=17.2Hz, 1H), 3.5-3.75 (m'j 3H), 3.48 (t, J=5.8Hz, 2H), 2.48 (s, 3H). 5-152 (A) 8 7.4-7.55 (m, 6H), 7.05 (bs, 1H), 6.90 (bs, 1H), 4.0-4.2 (m, 3H), 3.71 (d, J=17.0Hz, 1H), 3.-5-3.6 (m, 2H), 3.4-3.5 (m, 2H), 2.45 (s, 3H), 1.9-2.1 (m,2H). "' ~ 5-153 (B) 5 7.4-7.55 (m, 6H), 6.7-7.05 (m, 2H), 4.15-4,2 (m, 2H), 4.09 (d, J= • 17.2Hz, IN), 3.75-3.9 (m, 1H), 3.71 (d, J=17.2Hz, 1H), 3.05-3.2 (m, 1H), 2.47 (s, 3H), 1.49 (bs, 1H), 1.6-1.7 (m, 1H), 1.2-1.3 (m, 1H)., 5-154 (A) 5 7.45-7.55 (m, 5H), 7.43 (s, 1H), 6.86 (bs, 1H), 6.77 (bs, 1H), 4.05 ^.15 (m, 3H), 3.65-3.8 (m, 3H), 3.45-3.55 (m, 2H), 2.46 (s, 3H), 1.69 (bs, 1H). 5-155 (B) 5 7.5-7.55 (m, 5H), 7.43 (t, J=1.8Hz, 1H), 6.9-7.0 (m, 1H), 4.25^.4 (m, 2H), 4.19 (d, J=17.4Hz, 1H), 3.8-3.9 (m, 2H), 3.70 (d, J=17.4Hz, 1H) , 3.63 (t, J=5.2Hz, 1H), 3.49 (t, J=5.2Hz, 1H), 3.13 and 3.04 (s, 3H), 2.50 (s, 3H). 5-159 (B) 5 7.4-7.55 (m,6H), 7.25-7.35 (m, 1H), 7.0-7.05 (m, 1H),4.10 (d, J= 17.2Hz, 1H), 4.06 (bs, 2H), 3.77 (bs, 2H), 3.73 (d, J=17.2Hz, IN), 3.25 (t, J=5.6Hz, 2H), 2.96 (s, 3H), 2.42 (s, 3H). 5-161 (B) 57.4-7.55 (m, 6H), 6.96 (bs, 1H), 5.7-5.85 (m, 1H), 5.15-5.35 (m, 2H), 4.2-4.3 (m, 2H), 4.05-4.15 (m, 2H), 3.92 (bs, 1H), 3.71 (d, J=17.2 Hz, 1H), 3.01 and 2.99 (s, 3H), 2.50 (s, 3H). 5-162 (B) 5 7.45-7.55 (m, 5H), 7.4-7.45 (m, 1H), 6.97 (bs, 1H), 5.7-5.85 (m, 2H), 5.15-5.3 (m, 4H), 4.27 (d, J=4.0Hz, 2H), 4.10 (d, J=17.2Hz, 1H), 4.05 (d, J=5.8Hz, 2H), 3.91 (d, J=5.8Hz, 2H), 3.72 (d, J=17.2Hz, 1H), 2.50 (s, 3H). 5-163 (A) 57.4-7.6 (m, 6H), 6.9-7.2 (m, 2H), 538 (s, 1H), 5.30 (s, 1H), 4.0¬ 4.3 (m, 5H), 3.70 (d, J=17.0Hz, 1H), 2.44 (s, 3H). 5-165 (B) 5 7.4-7.55 (m, 6H), 7.00 (bs, 2H), 4.05^.2 (m, 5H), 3.72 (d, J=17.2 Hz, 1H), 2.54 (s, 3H), 2.22 (s, 1H). 5-167 (B) 58.78 (d, J=1.8Hz, 1H), 7.45-7.55 (m, 6H), 7.43 (t, J=1.8Hz, 1H), 6.65-6.8 (m, 2H), 4.65 (d, J=7.4Hz, 2H), 4.05^.2 (m, 3H), 3.70 (d, J= 17.2Hz, 1H), 2.46 (s,3H). 5-168 (B) 8 8.52 (d, J=4.1Hz, 1H), 7.67 (td, J=7.8,1.8Hz, 1H), 7.4-7,55 (m, 8H), 7.2-7.25 (m, 1H), 6.83 (bs, 1H), 4.59 (d, J=5.0Hz, 2H), 4.22 (d, J= 5.0Hz, 2H), 4.08 (d, J=17.2Hz, 1H), 3.70 (d, J=17.2Hz, 1H), 2.47 (s, 3H) 5-171 (B) 5 7.45-7.55 (m, 6H), 6.94 (bs, 1H), 4.25 (d, J=3.8Hz, 2H), 4.08 (d, J=17.2Hz, 1H), 3.65-3.75 (m, 7H), 3.48 (t, J=4.4Hz, 2H), 2.50 (s, 3H). 5-173 (B) 5 7.2-7.6 (m, 7H), 6.6-7.1 (m, 6H), 4.0-4.6 (m, 3H), 3.70 (d, J=17.0 Hz, 1H), 3.33 (s, 3H), 2.49 (s, 3H). 5-176 (B) 5 7.3-7.55 (m, 12H), 6.37 (bs, 1H), 5.71 (d, J=7.0Hz, 1H), 4.08 (d, J=17.2Hz, 1H), 3.71 (d, J=17.2Hz, 1H), 2.75 (d, J=4.9Hz, 3H), 2.41 (s, 3H). 5-178 (A) 5 7.45-7.6 (m, 5H), 7.43 (s, 1H), 6.62 (bs, 1H), 4.37 (t, J=9.3Hz, 2H), 4.23 (d, J=4.5Hz, 2H), 4.09 (d, J=17.1Hz, 1H), 3.86 (t, J=9.3Hz, 357 2H), 3.71 (d, J=17.1Hz, 1H), 2.48 (s, 3H). 5-179 (A) 8 8.10 (bs, 1H), 7.4-7.65 (m, 7H), 7.06 (bs, 1H), 4.43 (d, J=5.1Hz, 2H), 4.09 (d, J=17.1Hz, IH), 3.71 (d, J=17.1Hz, 1H), 2.49 (s, 3H). 5-180 (A) 5 7.65-7.8 (m, 2H), 7.1-7.6 (m, 12H), 6.03 (d, J=7.4Hz, IH), 4.08 (d, J=17.0Hz, 1H), 3.70 (d, J=17.0Hz, IH), 2.45 (s, 3H). 5-181 (A) 5 7.51 (bs, 4H), 7.4-7.45 (m, 1H), 7.38 (d, J=8.5Hz, 1H), 5.5-5.6 (m, IH), 4.08 (d, J=17.1Hz, 1H), 3.69 (d, J=:17.1Hz, IH), 2.97 (d, J=6.1Hz, 2H), 2.46 (s,3H), 0.13 (s,9H). 5-182 (A) 8 7.51 (bs, 4H), 7.4-7.45 (m, 2H), 5.85-6.05 (m, 1H), 5.81 (bs, 1H), 5.15-5.35 (m, 2H), 4.05^.15 (m, 3H), 3.69 (d, J=17.4Hz, IH), 2.49 (s, 3H). 5-183 (A) <5 7.4-7.75 (m, 5H), 7.33 (d, J=7.8Hz, 1H), 4.04 (d, J=17.1Hz, 1H)r 3.75 (m, IH), 3.66 (d, J=17.4Hz, IH), 3.37 (m, 1H), 3.08 (m, 2H), 1.25 (t, J=7.4Hz, 3H), 1.04 (t, J=7.2Hz, 3H). 5-184 (A) 87.51 (bs, 4H), 7.4-7.5 (m, 2H), 6.10 (t, J=6.9Hz, IH), 5.95 (bs, IH), 4.17 (t, J=6.6Hz, 2H), 4.08 (d, J=17.1Hz, IH), 3.69 (d, J=17.4Hz, J 1H),2.48(s,3H). 5-185 (A) 5 7.4-7.55 (m, 6H), 6.58 and 6.34 (s, 1H), 6.10 and 5.99 (bs, IH), 4.49 and 4.30 (d, J=6.0Hz, 2H), 4.08 (d, J=17.1Hz, IH), 3.69 (d, J=17.1 Hz, IH), 2.50 and2.48(5, 3H). 5-186 (A) 8 7.35-7.55 (nn, 6H), 6.03 (bs, 1H), 4.27 (q, J=2.4Hz, 2H), 4.08 (d, J=17.4Hz, IH), 3.70 (d, J=^17.4Hz, IH), 2.47 (s, 3H), 2.30 (t, J=2.4Hz, IH). 5-191 (A) 5 7.2-7.6 (m, 11H), 6.09 (bs, 1H), 5.06 (q, J=7.5Hz, 1H), 4.06 (d, J= 17.1Hz, IH), 3.68 (d, J=17.1Hz, IH), 2.40 (s, 3H), 1.85-2.0 (m, 2H), 0.97 (t, J=7.2Hz, 3H). 5-194 (B) 5 7.3-7.6 (m, 11H), 6.42 (d, J=9.6Hz, 1H), 6.26 (d, J=9.6Hz, 1H), 4.07 (d, J=17.2Hz, IH), 3.85-3.95 (m, IH), 3.7-3.8 (m, 1H), 3.69 (d, J= 17.2Hz, IH), 2.50 (s, 3H), 1.33 (t, J=7.2Hz, 3H). 5-205 (A) 8 7.35-7.55 (m, 7H), 6.25-6.35 (m, 2H), 6.10 (bs, 1H), 4.62 (d', J=5.4 Hz, 2H), 4.07 (d, J=17.1Hz, IH), 3.69 (d, J=17.1Hz, IH), 2.46 (s, 3H). 5-207 (A) 5 7.3-7.55 (m, 6H), 6.7-6.8 (m, 2H), 6.39 (bs, 1H), 4.64 (d, J=6.0Hz, 2H), 4.07 (d, J=17.4Hz, IH), 3.69 (d, J=17.4Hz, IH), 2.43 (s, 3H). 5-208 (A) 5 7.4-7.6 (m, 6H), 6.37 (bs, 1H), 6.04 (s, 1H), 4.66 (d, J=5.7Hz, 2H) , 4.08 (d, J=17.4Hz, IH), 3.69 (d, J=17.4Hz, IH), 2.49 (s, 3H), 2.43 (s, 3H). 5-209 (A) 5 7.35-7.6 (m, 6H), 6.57 (t, J=6.0Hz, 1H), 6.31 (s, 1H), 4.70 (d, J= 6.0Hz, 2H), 4.09 (d, J=17.4Hz, IH), 3.71 (d, J=17.4Hz, 1H), 2.43 (s, 3H). 5-212 (A) 8 7.56 (s, IH), 7.35-7.55 (m, 6H), 5.90 (bs, 1H), 4.46 (d, J=5.4Hz, 2H), 4.07 (d, J=17.1Hz, IH), 3.85 (s, 3H), 3.68 (d, J=17.1Hz, IH), 2.47 (s, 3H). 5-213 (A) 8 7.3-7.55 (m, 6H), 6.19 (bs, IH), 4.43 (d, J=5.4Hz, 2H), 4.07 (d, J= 17.4Hz, 1H), 3.78 (s, 3H), 3.72 (d, J=17.1 Hz, 1H), 2.43 (s, 3H). 5-216 (A) 8 7.74 (d, J=3.3Hz, 1H), 7.45-7.55 (m, 5H), 7.43 (bs, 1H), 7.40 (d, J=3.3Hz, IH), 6.66 (bs, IH), 4.95 (d, J=5.4Hz, 2H), 4.08 (d, J=16.8Hz, IH), 3.70 (d, J=17.4Hz, IH), 2.50 (s, 3H). 5-217 (A) 67.75 (d. J=3.3Hz, 1H), 7.3-7.6 (m, 13H), 6.59 (d, J=7.4Hz, 1H), 4.08 (d, J=17.3Hz, 1H), 3.69 (d, J=17.3Hz, 1H), 2.46 (s, 3H). 5-218 (A) 5 7.76 (s, 1H), 7.4-7.75(m, 6H), 6.78 (bs, 1H), 4.93 (d, J=3.6Hz, 2H), 4.09 (d,J=17.4Hz, IH), 3.70(d, J-17.4Hz, 1H).2.47 (s, 3H). 5-219 (A) 5 8.79 (s, 1H), 7.4-7.55 (m, 6H), 7.32 (s, 1H), 6.53 (bs, 1H), 4.77 (d, J=5.4Hz, 2H), 4.05 (drJ=17.4Hz, 1H), 3.66 (d, J=17.4Hz, 1H), 2.47 (s, 3H). 5-220 (A) 8 7.4-7.55 (m, 6H), 7.17 (s, 1H), 6.40 (bs, 1H), 4.64 (d, J=5.7Hz, 2H),4.08(d, J=17.1Hz, 1H), 3.73(d, J-17.1Hz, 1H),2.46 (s,.3H). 5-221 (A) 5 7.4-7.55 (m, 6H), 7.07 (s, 1H), 6.42 (bs, 1H), 4.66 (d, J=5.4Hz, 2H), 4.05 (d, J=17.4Hz, 1H), 3.66 (d, J=17.4Hz, 1H), 2.70 (s, 3H), 2.47^ (s, 3H). 5-222 (A) 5 8.76 (s, 1H), 7.81 (s, 1H), 7.50 (bs, 4H), 7.35-7.45 (m, 2H), 6.36 (bs, 1H), 4.83 (d, J=6.0Hz, 2H), 4.07 (d, J=17.4Hz, 1H), 3.69 (d, J=17.1 Hz, 1H),2.46(s, 3H). 5-223 (A) 8 7.45-7.55 (m, 4H), 7.35-7.45 (m, 3H), 6.27 (t, J=6.0Hz, 1H), 4.71 I (d, J-6.0HZ, 2H), 4.08 (d, J=17.4Hz, 1H), 3.69 (d, J=17.4Hz, 1H), 2.48 (s, 3H). 5-224 (B) 8 7.91 (bs, 1H), 7.4-7.55 (m, 6H), 6.84 (s, 1H), 6.79 (s, 1H), 4.66 (d, J=4.9Hz, 2H), 4.07 (d, J=17.0Hz, 1H), 3.80 (s, 3H), 3.77 (d, J=17.0 Hz, 1H),2.45(s,3H). 5-225 (B) 8 7.25-7.55 (m, 7H), 6.9-7.0 (m, 1H), 6.84 (s, 1H), 4.57 (d, J=5.5Hz, 2H), 4.07 (d, J=17.0Hz, 1H), 3.70 (d, J=17.0Hz, 1H), 3.63 (s, 3H), 2.42 (s,3H). 5-226 (B) 8 8.62 (s, 1H), 7.35-7.65 (m, 6H), 6.8-6.9 (m, 1H), 5.07 (d, J=6.1 Hz, 2H), 4.06 (d, J=17.0Hz, 1H), 3.69 (d, J=17.0Hz, 1H), 2.42 (s, 3H). 5-227 (B) 8 7.45-7.55 (m, 5H), 7.35-7.4 (m, 1H), 6.9-6.95 (m, 1H), 4.80 (d, J= 5.8Hz, 2H), 4.08 (d, J=17.0Hz, 1H), 3.71 (d, J=17.0Hz, 1H), 2.68 (s, 3H) ,2.41(s,3H). 5-230 (A) 5 8.43 (s, 1H), 7.45-7.55 (m, 5H), 7.43 (s, 1H), 6.68 (t, J=5.7Hz, 1H), 4.90 (d, J=5.7Hz, 2H), 4.09 (d, J=17.1Hz, 1H), 3.71 (d, J=17.1Hz, 1H),2.48(s,3H). 5-231 (A) 5 7.45-7.55 (m, 5H), 7.43 (s, 1H), 6.78 (t, J=5.7Hz, 1H), 4.80 (d, J= 5.7Hz, 2H), 4.09 (d, J=17.1Hz, 1H), 3.72 (d, J=17.1Hz, 1H), 2.54 (s, 3H) ,2.47(s,3H). • 5-232 (A) 5 9.14 (s, 1H), 7.45-7.55 (m, 6H), 6.85 (t, J=5.7Hz, 1H), 5.09 (d, J= 5.7Hz, 2H), 4.08 (d, J=17.4Hz, 1H),-3.70 (d, J=17.4Hz,- 1H), 2.48 (s, 3H). 5-233 (B) 8 8.42 (s, 1H), 8.05-8.15 (m, 1H), 7.87 (s, 1H), 7.35-7.55 (m, 6H), 5.70 (d, J=6.4Hz, 2H), 4.08 (d, J=17.0Hz, 1H), 3.72 (d, J=17.0Hz, 1H), 2.32 (s, 3H). 5-235 (A) 5 8.52 (d, J=4.8Hz, 1H), 7.65-7.75 (m, 1H), 7.15-7.55 (m, 9H), 5.32 (dq, J=6.9Hz, 1H), 4.09 (d, J-16.8Hz, 1H), 3.70 (d, J=16.8Hz, 1H), 2.48 (s, 3H), 1.59(d,J=6.9Hz, 3H). 5-238 (B) 8 7.66 (t, J=7.7Hz, 1H), 7.45-7.55 (m, 5H), 7.43 (t, J=1.8Hz, 1H), 7.25-7.35 (m, 2H), 7.02 (t, J=5.3Hz, 1H), 4.69 (d, J=5.3Hz, 2H), 4.10 (d , J-17.2HZ, 1H), 3.72 (d, J=17.4Hz, 1H), 2.47 (s, 3H). 359 5-239 (B) 6 8.2-8.3 (m, 1H), 7.55-7.65 (m, 2H), 7.45-7.55 (m, 3H), 7.4-7.5 (m, 3H), 7.25-7.4 (m, 2H), 4.79 (d, J=6.2Hz, 2H), 4.07 (d, J=17.2Hz, 1H), 3.69 (d, J=17.2Hz, 1H), 2,41 (s, 3H). 5-240 (A) 5 8.58 (d, J=1.8Hz, 1H), 8.53 (dd, J=4.8,1.8Hz, 1H), 7.72 (d, J=7.8 Hz, 1H), 7.4-7.55, (m, 6H)„7.30 (dd, J=7.8,4.8Hz, 1H), 6.40 (t, J=6.0 Hz, 1H), 4.63 (d, J=6.0'Hz,-2H), 4.08 (d, J=17.4Hz, 1H), 3.70 (d, J=17.4 Hz, 1H),2.46(s,3H). 5-242 (A) 8 8.57 (d, J=6.0Hz, 2H), 7.4-7.55 (m, 6H), 7.26 (d, J=6.0Hz, 2H), 6.42 (t, J=6.0Hz, 1H), 4.64 (d, J=6.0Hz, 2H), 4.08 (d, J=17.4Hz, 1H), 3.70 (d, J=17.4Hz, 1H), 2.48 (s, 3H). 5-243 (A) 5 8.73 (d, J=5.4Hz, 2H), 7.5-7.6 (m, 5H), 7.43 (s, 1H), 7.24 (t, J=^ 5.4Hz, 1H), 7.19 (bs, 1H), 4.89 (d, J=5.2Hz, 2H), 4.10 (d, J=17.0Hz, 1JH). , 3.72 (d, J=17.0Hz, 1H), 253 (s, 3H). 5-245 (A) 5 9.18 (bs, 1H), 8.73 (d, J=5.2Hz, 1H), 7.56 (s, 3H), 7.52 (bs, 2H), 7.4-7.45 (m, 1H), 7.35-7.4 (m, 1H), 7.04 (bs, 1H), 4.77 (d, J=4.8Hz, 2H) , 4.10 (d, J=17.2Hz, 1H), 3.72 (d, J=17.2Hz, 1H), 2.52 (s, 3H). 5-246 (B) 5 8.69 (s, 1H), 8.53 (s, 2H), 7.5-7.55 (m, 5H), 7.4-7.45 (m, 1H), 6.95-7.0 (m, 1H), 4.81 (d, J=5.3Hz, 2H), 4.09 (d, J=17.0Hz, 1H), 3.71 (d,J=17.0Hz, 1H),2.49(s, 3H). 5-247 (B) 5 8.55-8.6 (m, 1H), 8.35-8.4 (m, 1H), 7.4-7.55 (m, 6H), 6.95-7.05 (m, 1H), 4.75^.8 (m, 2H), 4.08 (d, J=17.0Hz, 1H), 3.72 (d, J=17.0Hz, 1H), 2.57 (s, 3H), 2.46 (s, 3H). 5-265 (B) 5 7.5-7.55 (m, 5H), 7.4-7.45 (m, 1H), 6.70 (bs, 1H), 4.08 (d, J=19.0 Hz, 1H), 3.70 (d, J=19.0Hz, 1H), 2.51 (s, 3H), 1.51 (s, 9H). 5-277 (C) 8 7.45-7.65 (m, 6H), 7.44 (s, 1H), 7.33 (d, J=7.8Hz, 1H), 7.21 (t, J= 7.8Hz, 1H), 7.00 (d, J=7.8Hz, 1H), 6.89 (t, J=7.8Hz, 1H), 6.69 (s, 1H), 4.08 (d, J=174Hz, 1H), 3.61 (d, J=174Hz, 1H), 2.53 (s, 3H). 5-278 (C) 5 7.45-7.65 (m, 6H), 7.44 (s, 1H), 7.20 (t, J=84Hz, 1H), 6.85-6.95 (m,2H),6.81 (d, J=8.4Hz, 1H),6.33(s, 1H),4.10 (d, J=17.1Hz, 1H), 3.71 (d, J=17.1Hz, 1H), 2.52 (s, 3H). 5-279 (A) 6 7.95 (s,' 1H), 7.35-7.55 (m, 6H), 7.17 (d, J=84Hz, 2H), 6.79 (d, J= 84Hz, 2H), 6.42 (bs, 1H), 4.09 (d, J=174Hz, 1H), 3.71 (d, J=17.4Hz, 1H),2.43(s,3H). 5-280 (A) 8 7.4-7.65 (m, 10H), 6.98 (d, J=84Hz, 2H), 4.10 (d, J=1.7.3Hz, 1H), 3.72 (d, J=17;3Hz, 1H), 2.52 (s, 3H). 5-296 (A) 8 8.76 (bs, 1H), 8.12 (bs, 1H), 8.02 (d, J=5.4Hz, 1H), 7.35-7.5 (m, 6H), 6.26 (d, J=5.4Hz, 1H), 4.10(d, J=17.4Hz, 1H), 3.73 (d, J=17.4Hz, 1H), 2.45 (s,3H), 2.43 (s,3H). 5-299 (C) 5 10.15 (bs, 1H), 9.37 (bs, 1H), 8.40 (s, 1H), 7.5-7.6 (m, 5H), 7.46 (s, 1H), 6.69 (s, 1H), 4.17 (d, J=174Hz, 1H), 3.86 (d, J=174Hz, 1H), 2.59 (s, 3H). 5-301 (A) 8 7.4-7.65 (m, 7H), 7.34 (d, J=9.3Hz, 1H), 7.01 (d, J=9.3Hz, 1H), 4.10 (d, J=174Hz, 1H), 4.13 (d, J=174Hz, 1H), 3.71 (d, J=17.4Hz, 1H), 2.52 (s, 3H). 5-303 (B) 5 10.38 (bs, 1H), 7.2-8.65 (m, 11H), 4.05^.2 (m, 1H), 3.7-3.85 (m, 1H), 2.44 and 2.37 (s,3H). 5-311 (A) 5 7.3-7.75 (m, 6H), 6.52 (t, J=6.3Hz, 1H), 4.05-4.2 (m, 3H), 3.77 (d, J=17.4Hz, 1H),2.60(s,3H). 5-312 (A) 5 7.25-7.65 (m, 6H), 6'>54 (t, J=6.3Hz, 1H), 3.9-4.15 (m, 2H), 4.10 (d, J=17.7Hz, 1H), 3.73.(d, J=17.7Hz, 1H), 2.74 (q, J=7.2Hz, 2H), 1.19 (t, J=7.2Hz, 3H). 5-313 (A) 5 8.50 (d, J=4.8Hz, 1H), 7.70 (t, J=4.5Hz, 1H), 7.5-7.6 (m, 3H), 7.49 (bs, 2H), 7.42 (bs, 1H), 7.15-7.35 (m, 3H), 4.73 (d, J=4.5Hz, 2H), 4.11 (d, J=17.4Hz, 1H), 3.73 (d, J=17.4Hz, 1H), 2.84 (q, J=7.5Hz, 2H), 1.23 (t, J=7.5Hz, 3H). 5-316 (B) 5 7.72 (bs, 3H), 7.51 (bs, 2H), 7.45 (t, J=1.8Hz, 1H), 7.15-7.25 (m, 1H), 4.71 (d, J=6.0Hz, 2H), 4.15^.2 (m, 3H), 3.73 (d, J=17.2Hz, 1H), _^ 3.34(t, J=6.0Hz, 1H). 5-318 (A) 6 8.30 (d, J=8.4Hz, 1H), 8.18 (bs, 1H), 7.51 (s, 2H), 7.48 (s, 1H), 7.25-7.45 (m, 6H), 7.16 (d, J=8.4Hz, 1H), 4.68 (d, J=5.7Hz, 2H), 4.11 (d, J=17.4Hz, 1H), 3.97 (s, 3H), 3.73 (d, J=17.4Hz, 1H). 5-320 (B) 6 8.11 (d, J=8.0Hz, 1H), 7.70 (s, 1H), 7.64 (d, J=8.0Hz, 1H), 7.51 I (s, 2H), 7.45 (s, 1H), 6.86 (t, J=6.0Hz, 1H), 4.0-4.25 (m, 3H), 3.71 (d, J=17.6,1H). 5-322 (A) 5 8.14 (t, J=7.8Hz, 1H), 7.54 (d, J=7.8Hz, 1H), 7.50 (d, J=7.8Hz, 1H) , 7.34 (s, 1H), 7.31 (s, 1H), 7.23 (s, 1H), 7.09 and 7.05 (t, J=6.3Hz, 1H), 4.18 (qd, J=18.5, 6.3Hz, 2H), 4.08 (d, J=17.4Hz, 1H), 3.74 (d, J= 17.4Hz, 1H), 2.52 (s,3H). 5-325 (A) 5 8.59 (bs, 1H), 8.32 (s, 1H), 8.11 (bs, 1H), 8.03 (d, J=8.1Hz, 1H), 7.85 (d, J=8.1Hz, IN), 7.73 (t, J=8.1Hz, 1H), 7.51 (bs, 2H), 7.43 (bs, 1H), 7.2-7.4 (m, 2H), 4.73 (bs, 2H), 4.23 and 4.21 (d, J=17.4Hz, 1H), 3.86 and 3.85 (d, J=17.4Hz, 1H), 2.96 and 2.93 (s, 3H). 5-328 (A) 6 8.16 (t, J=8.0Hz, 1H), 7.6-7.8 (m, 3H), 7.56 (d, J=8.0Hz, 1H), 7.52 (d, J=8.1Hz, 1H), 7.08 and 7.03 (t, J=6.5Hz, 1H), 4.35^.55 (m, 2H), 4.05-4.25 (m, 2H), 4.14 (d, J=174Hz, 1H), 3.79 (d, J=174Hz, 1H). 5-330 (B) 5 8.57 (d, J=4.8Hz, 1H), 7.71 (td, J=7.7,1.8Hz, 1H), 7.62 (t, J=4.6 Hz, 1H), 7.54 (d, J=8.6Hz, 1H), 7.50 (d, J=1.6Hz, 2H), 7.42 (t, J=1.8Hz, 1H), 7.33 (d, J=7.9Hz, IN), 7.24 (dd, J=7.5, 5.0Hz, 1H), 6.9-7.0 (m, 2H), 5.73 (bs, 2H), 4.72 (d, J=4.8Hz, 2H), 4.04 (d, J=17.2Hz, 1H), 3.66 (d,J=17.4Hz, 1H). 5-332 (A) 5 8.57 (d, J=4.2Hz, 1H), 7.65-7.75 (m, 2H), 745-7.6 (nn: 4H), 7.43 (bs, 1H), 7.33 (d, J=7.8Hz, 1H), 7.2-7.3 (m, 1H), 6.93 (bs, 1H), 6.85 (d , J=7.8Hz, 1H), 4.71 (d, J=4.8Hz, 2H), 409 (d, J=17.1Hz, 1H), 3.69 (d, J=17.1Hz, 1H), 2.90 (d, J=3.6Hz, 3H). 5-335 (A) 5 10.29 (bs, IN), 8.56 (d, J=6.0Hz, 1H), 8.18 (d, J=8.1Hz, 1H), 7.15¬ 7.75 (m, 8H), 479 (d, J=54Hz, 2H), 410 (d, J=17.1Hz, 1H); 3.71 (d, J= 17.1Hz, 1H), 2.75 (s,6H). 5-336 (A) 5 8.45-8.6 (m, 1H), 8.23 and 8.29 (s, 1H), 7.15-7.9 (m, 10H), 4.65¬ 4.75 (m, 2H), 40^. 2 (m, 1H), 3.6-3.8 (m, 1H), 3.25 and 3.34 (s, 3H). 5-337 (A) 6 8.45-8.6 (m, 1H), 7.15-8.05 (m, 10H), 4.65^.75 (m, 2H), 4.0-4.2 (m , 1H), 3.65-3.8 (m, 1H), 3.33 and 3.22 (s, 3H), 2.19 and 1,87 (s, 3H). 5-340 (B) 5 7.95-8.0 (m, 1H), 7.89 (dd, J=8.0,2.6Hz, 1H), 7.79 (dd, J=7.8,1.6 361 Hz, 1H), 7.52 (bs, 2H), 7.44 (t, J=1.8Hz, 1H), 5.51 (s, 1H), 4.45^.55 (m, 1H), 4.14 (dd, J=20.2, 7.6Hz, 1H), 3.9^.05 (m, 1H), 3.77 (dd, J= 17.4,5.2Hz, 1H). 5-342 (B) 5 7.9-7.95 (bs, 2H), 7-53 (d, J=1.8Hz, 1H), 7.44 (dd, J=8.2,1 .BHz, 1H), 7.21 (bs, 2H), 7.14 (t, J=1.8Hz, 1H), 3.75-3.9 (m, 3H), 0.30 (s, 9H). ••-• ¬ 5-343 (B) 6 7.25-7.8 (m, 11H), 5.65 (t, J-^O.OHz, 1H), 4.10 (d, J=17.2Hz, 1H), 3.7-3.85 (m, 3H). 5-345 (A) 8 8.47 (s, 1H), 8.43 (d, J=4.8Hz, 1H), 7.95 (s, 1H), 7.6-7.85 (m, 5H) , 7.50 (bs, 2H), 7.43 (bs, 1H), 7.15-7.25 (m, 2H), 4.55 (d, J-54Hz, 2H) ,4.13(d, J=17.7Hz, 1H),3.77(d, J=17.7Hz, 1H). 5-346 (B) 8 7.91 (ddd, J=8.6, 6.8,1.8Hz, 1H), 7.78 (ddd, J=8.6, 6.8, 1.8Hz, ^„ 1H), 7.49 (d, J=1.6Hz, 2H), 7.45 (t, J=2.0Hz, 1H), 6.84 (bs, 1H), 4.15¬ 4.25 (m,3H), 3.80 (bs,1H). 5-347 (B) 5 7.85-7.95 (m, 1H), 7.7-7.8 (m, 1H), 7.25-7.5 (m, 8H), 6.90 (bs, 1H) , 4.68 (d, J=54Hz, 2H), 4.16 (bs, 1H), 3.78 (bs, 1H). 5-348 (B) 8 8.59 (bs, 1H), 8.11 (bs, 1H), 7.89 (bs, 1H), 7.71 (bs, 2H), 7.2-7.5 ' (m, 5H), 4.80 (bs, 2H), 4.18 (d, J=17.8Hz, 1H), 3.80 (d, J=17.8Hz, 1H). 5-352 (A) 5 849 (d, J=4.5Hz, 1H), 7.65-7.75 (m, 1H), 7.51 (s, 2H), 7.42 (s, 1H), 7.3-74 (m, 3H), 7.22 (dd, J=7.5,4.5Hz, 1H), 7.10 (bs, 1H), 4.76 (d, J=4.5Hz, 2H), 4.07 (d, J=17.4Hz, 1H), 3.69 (d, J=174Hz, 1H), 2.33 (s, 6H). 5-353 (A) 8 8.77 (d, J=24Hz, 1H), 7.73 (d, J=8.1 Hz, 1H), 7.70 (s, 1H), 7.60 (d , J=8.1 Hz, 1H), 7.52 (bs, 2H), 7.43 (bs, 1H), 7.33 (d, J=2.4Hz, 1H), 7.10(t, J=5.4Hz, 1H),4.81 (d, J=5.4Hz,2H),4.12(d, J=17.4Hz, 1H), 3.72 (d,J=17.4Hz, 1H). 5-354 (A) 5 8.53 (d, J=4.5Hz, 1H), 7.55-7.8 (m, 5H), 7.53 (bs, 2H), 743 (bs, 1H), 7.2-74 (m, 2H), 4.77 (d, J=4.8Hz, 2H), 4.13 (d, J=17.4Hz, 1H), 3.74 (d,J=17.4Hz, 1H). 5-356 (A) 8 7.4-7.6 (m, 6H), 6.17 (bs, 1H), 4.12 (d, J=17.6Hz, 1H), 3.72 (d, J= 17.6Hz, 1H), 3.55-3.7 (m, 4H), 3.53 (q, J=7.1Hz, 2H), 2.47 (s, 3H), 1.20 (t,J=7.1Hz,3H). 5-357 (A) 8 7.4-7.6 (m, 6H), 5.97 (t, J=5.6Hz, 1H), 4.50 (t, J=5.6Hz, 1H), 4.12 (d, J=17.6Hz, 1H), 3.72 (d, J=17.6Hz, 1H), 3.60 (t, J=5.6Hz, 2H), 3.43 (s, 6H), 2.48 (s, 3H). 5-358 (A) 5 7.4-7.6 (m, 6H), 5.75-6.0 (m, 2H), 5.27 (d, J=17.1 Hz, 1H), 5.21 (d, J=10.2Hz, 1H), 4.0-^.2 (m, 3H), 3.72 (d, J=17.3Hz, 1H), 2.48 (s, 3H). 5-359 (A) 8 8.79 (d, J=2.1 Hz, 1H), 7.3-7.6 (m, 7H), 6.54 (t, J=5.4Hz, 1H), 4.77 (d, J=5.4Hz, 2H), 4.12 (d, J=17.6Hz, 1H), 3.72 (d, J=17.6Hz, 1H), 2.47 (s, 3H). 5-360 (A) 8 8.54 (d, J=5.0Hz, 1H), 7.65-7.8 (m, 1H), 7.15-7.6 (m, 9H), 4.74 (d, J=5.0Hz, 2H), 4.08 (d, J=17.6Hz, 1H), 3.72 (d, J=17.6Hz, 1H), 2.50 (s, 3H). 5-361 (B) 8 7.5-7.55 (m, 4H), 7.43 (d, J=5.0Hz, 1H), 7.42 (d, J=1.8Hz, 1H), 6.07 (t, J=64Hz, 1H), 4.27 (d, J=17.4Hz, 1H), 4.05-4.15 (m, 2H), 3.68 (dd, J=174, 1.8Hz, 1H), 2.46 (s, 3H). 5-362 (B) 5 8.5-8.55 (m, 1H), 7.71 (td, J=7.6,1.6Hz, 1H), 7.5-7.55 (m, 4H), 7.42 (t, J=1.6Hz, 1H), 7.34 (d, J=7.8Hz, 1H), 7.2-7.3 (m, 3H), 4.75 (d, . J=4.8Hz, 2H), 4.27 (d, J=^17.2Hz, 1H), 3.68 (d, J=17.2Hz, 1H), 2.50 (s, 3H). 5-364 (A) 67.3-7.6 (m, 6H),'6.07 (t, J=6.3Hz, 1H), 3.8^.25 (m, 7H), 3.41 (d, J=16.8Hz, 1H), 2.46(sr3H). 5-365 (A) 5 8.52 (d, J=3.8Hz, 1H), 7.65-7.75 (m, 1H), 7.15-7.6 (m, 9H), 4.75 (d, J=4.6Hz, 2H), 3.8-^.2 (m, 5H), 3.41 (d, J=16.8Hz, 1H), 2.50 (s, 3H). 5-366 (A) 8 7.3-7.55 (m, 6H), 6.83 (t, J=6.5Hz, 1H), 4.20 (d, J=17.4Hz, 1H), 4.0-4.15 (m, 2H), 3.62 (d, J=17.4Hz, 1H), 2.40 (s, 3H), 2.30 (s, 3H). 5-368 (B) 5 7.5-7.6 (m, 2H), 7.4-7.5 (m, 4H), 6.0-6.5 (m, 1H), 4.1-4.2 (m, 2H), 3.53 (d, J=3.2Hz, 2H), 2.50 (s, 3H), 1.64 (d, J=3.2Hz, 2H), 0.04 (s, \ . 9H). 5-369 (B) 8 8.55-8.6 (m, 1H), 7.7-7.8 (m, 1H), 7.5-7.55 (m, 3H), 7.35-7.45 (m, 3H), 7.2-7.3 (m, 3H), 4.79 (d, J=4.8Hz, 2H), 3.53 (d, J=3.2Hz, 2H), 2.55 (s, 3H), 1.64 (d, J=5.8Hz, 2H), 0.04 (s, 9H). 5-370 (A) 5 7.47 (s, 1H), 7.45 (d, J=7.8Hz, 1H), 7.34 (d, J=7.8Hz, 1H), 7.15¬ 7.3 (m, 3H), 6.28 (t, J=6.5Hz, 1H), 4.07 (qd, J=18.5, 6.5Hz, 2H), 3.61 (d, J=16.2Hz, 1H), 3.53 (d, J=16.2Hz, 1H), 2.40 (s, 3H), 0.11 (s, 9H). 5-371 (A) 8 8.50 (d, J=5.1Hz, 1H), 7.45-7.75 (m, 4H), 7.15-7.35 (m, 6H), 4.72 (d, J=5.1Hz, 2H), 3.63 (d, J=16.2Hz, 1H), 3.54 (d, J=16.2Hz, 1H), 2.48 (s,3H),0.11(s,9H). 5-372 (A) 5 8.60 (d, J=4.7Hz, 1H), 7.15-7.75 (m, 9H), 6.05 (t, J=6.0Hz, 1H), 4.77 (d, J=16.8Hz, 1H), 4.0^.2 (m, 2H), 3.69 (d, J=16.8Hz, 1H), 2.45 (s ,3H). 5-373 (A) 8 8.60 (d, J=4.9Hz, 1H), 8.53 (d, J=5.1Hz, 1H), 7.15-7.8 (m, 13H), 4.7^.85 (m, 3H), 3.69 (d, J=16.7Hz, 1H), 2.48 (s, 3H). 5-374 (A) 8 7.3-7.75 (m, 6H), 6.0-6.5 (br, 1H), 3.95-4.25 (m, 3H), 3.70 (d, J= 17.1Hz, 1H), 2.42 (s,3H). 5-375 (A) 8 8.55 (d, J=4.8Hz, 1H), 745-7.75 (m, 7H), 7.3-745 (m, 2H), 7.15¬ 7.3 (m, 1H), 4'.74 (d, J=5.1Hz, 2H), 4.09 (d, J=17.4Hz, 1H), 3.70 (d, J= 17.4Hz, 1H), 2.49 (s,3H). 5-377 (A) 8 8.53 (d," J=4.5Hz, 1H), 7.55-7.8 (m, 8H), 7.15-74 (m, 2H), 4.77 (d, J=4.5Hz, 2H), 4.08 (d, J=174Hz, 1H), 3.71 (d, J=17.4Hz, 1H). 5-378 (A) 8 7.65-7.8 (m, 3H), 7.4-7.6 (m, 3H), 6.04 (t, J=6.3Hz, IH), 4.0^.2 (m, 3H), 3.70 (d, J=17.0Hz, IN), 2.47 (s, 3H). 5-379 (A) 8 7.73 (bs, 1H), 7.71 (bs, 2H); 7.51 (s, 1H), 7.49 (d, J=8.7Hz, 1H), 7.42 (d, J=8.7Hz, 1H), 6.2-6.3 (m, 1H), 4.08 (d, J=174Hz, 1H), 3.71 (d, J=174Hz, 1H), 3.5-3.65 (m, 4H), 3.38 (s, 3H), 2.45 (s, 3H). 5-380 (A) 5 7.74 (bs, 1H), 7.71 (bs, 2H), 7.51 (s, 1H), 7.50 (d, J=8.4Hz, 1H), 7.42 (d, J=84Hz, 1H), 6.2-6.3 (m, 1H), 4.08 (d, J=174Hz, 1H), 3.71 (d, J=174Hz, 1H), 3.55-3.65 (m, 4H), 3.53 (q, J=7.2Hz, 2H), 2.46 (s, 3H), 1.20(t,J=7.2Hz, 3H). 5-381 (A) 8 7.73 (bs, 1H), 7.70 (bs, 2H), 7.51 (s, 1H), 7.50 (d, J=8.4Hz, 1H), 7.41 (d, J=84Hz, 1H), 6.06 (t, J-54Hz, 1H), 4.50 (t, J=5.4Hz, 1H), 4.08 (d, J=16.8Hz, 1H), 3.70 (d, J=16.8Hz, 1H), 3.59 (t, J=54Hz, 2H), 363 3.43 (s, 6H), 2.46 (s, 3H). 5-382 (A) 5 7.73 (bs, 1H), 7.71 (bs, 2H), 7.50 (s, 1H), 7.49 (d, J=8.7Hz, 1H), 7.45 (d, J=8.7H2, 1H), 6.47 (t, J=5.4Hz, 1H), 4.20 (d, J=5.4Hz, 2H), 4.09 (d, J-17.4Hz. IH), 3.80 (s, 3H), 3.72 (d, J=17.4H2, 1H), 2.46 (s, 3H). 5-385 (A) 8 7.74 (bs, 1H), 7.7tf (bs; 2H), 7.49 (s, 1H), 7.48 (d, J=8.7Hz, 1H), 7.39 (d, J=8.7Hz, 1H), 6.06 (t, J=5.4Hz, 1H), 5.92 (ddd, J=15.9, 10.2; 5.4Hz, 1H), 5.26 (d, J=15.9Hz, 1H), 5.19 (d, J-10.2Hz, 1H), 4.08 (d, J= 17.4Hz, 1H), 4.05 (t, J=5.4Hz, 2H), 3.71 (d, J=17.4Hz, 1H), 2.45 (s, 3H) 5-386 (A) 5 8.76 (d, J=2.1 Hz, 1H), 7.73 (bs, 1H), 7.70 (bs, 2H), 7.49 (s, 1H), 7.48 (d, J=8.1Hz, 1H), 7.42 (d, J=8.1Hz, IN), 7.29 (d, J=2.1Hz, 1H), . 6.75 (t, J=5.4Hz, 1H), 4.76 (d, J=5.4Hz, 2H), 4.08 (d, J=17.4Hz, 1H), 3.70 (d, J=17.4Hz, 1H), 2.44 (s, 3H). 5-387 (A) 8 8.53 (d, J=5.1Hz, 1H), 7.65-7.8 (m, 4H), 7.53 (s, 3H), 7.33 (d, J= 8.1Hz, 1H), 7.15-7.3 (m, 2H), 4.75 (d, J=4.8Hz, 2H), 4.08 (d, J=17.1Hz, ! 1H), 3.70 (d, J=17.1Hz, 1H), 2.51 (s, 3H). 5-388 (A) 8 8.5-8.55 (m, 1H), 7.65-7.75 (m, 1H), 7.5-7.6 (m, 3H), 7.2-7.45 (m, 6H), 4.75 (d, J=4.8Hz, 2H), 4.07 (d, J=17.2Hz, 1H), 3.72 (d, J=17.2Hz, 1H), 2.51 (s,3H), 2.39 (s,3H). 5-389 (A) 8 8.09 (s, 2H), 7.98 (s, 1H), 7.45-7.55 (m, 2H), 7.38 (d, J=84Hz, 1H), 6.35 (bs, 1H), 4.21 (d, J=174Hz, 1H), 4.0A15 (m, 2H), 3.77 (d, J=17.4Hz, 1H),2.42(s,3H). 5-390 (A) 8 8.53 (d, J=4.2Hz, IN), 8.10 (s, 2H), 7.97 (s, 1H), 7.65-7.8 (m, 1H) , 7.54 (bs, 3H), 7.2-7.35 (m, 3H), 4.75 (d, J=4.5Hz, 2H), 4.22 (d, J= 17.1Hz, 1H), 3.77 (d, J=17.1Hz, 1H), 2.50 (s, 3H). 5-391 (A) 8 8.52 (d, J=5.1Hz, 1H), 7.72 (t, J=4.8Hz, 1H), 7.52 (bs, 3H), 7.15¬ 7.35 (m, 4H), 7.07 (d, J=9.3Hz, 1H), 6.96 (d, J=9.3Hz, 1H), 4.73 (d, J= 4.8Hz, 2H), 4.10 (d, J=17.4Hz, 1H), 3.72 (d, J=174Hz, 1H), 2.51 (s, 3H) . ,2.50(s,3H). 5-392 (A) 8 8.53 (d, J=4.8Hz, IN), 7.6-7.75 (m, 4H), 7.3-74 (m, 4H), 7.15-7.35 (m, 2H), 4.77 (d, J=5.1Hz, 2H), 4.08 (d, J=17.1Hz, 1H), 3.72 (d, J=17.1 Hz, 1H), 2.52 (s, 3H), 2.50 (s, 3H). 5-393 (A) 5 8.52 (d, J=4.5Hz, 1H), 7.70 (t, J=4.8Hz, 1H), 7.53 (bs, 1H), 7.52 (bs, 2H), 7.15-7.45 (m, 6H), 4.74 (d, J=4.8Hz, 2H), 4.12 (d, J=174Hz, 1H), 3.89 (s, 3H), 3.75 (d, J=174Hz, 1H), 2.50 (s, 3H). 5-394 (A) 5 8.52 (d, J=5.1 Hz, 1H), 7.70 (t, J=4.8Hz, 1H), 7.52 (bs, 3H), 7.15¬ 7.35 (m, 5H), 7.13 (bs, 1H), 4.74 (d, J=4.8Hz, 2H), 4.07 (d, J=174Hz, 1H), 3.73 (d, J=17.4Hz, 1H), 2.51 (s, 6H), 2.50 (s, 3H). 5-398 (A) 5 8.56 (d, J=4.5Hz, 1H), 7.72 (td, J=7.5,1.5Hz, 1H), 7.65 (s, 2H), 745-7.6 (m, 4H), 7.39 (d, J=7.8Hz, 1H), 7.15-7.3 (m, 1H), 4.72 (d, J= 5.1Hz, 2H), 4.10 (d, J=17.4Hz, 1H), 3.71 (d, J=17.4Hz, 1H), 2.46 (s, 3H). 5-399 (6)5 7.35-7.55 (m, 6H), 6.12 (bs, 1H), 4.18 (d, J=17.2Hz, 1H), 3.65-3.75 (m, 3H), 2.4-2.55 (m, 5H). 5^00 (6)6 7.4-7.6 (m, 6H), 6.87 (d, J=9.2Hz, 1H), 59-6.0 (m, 1H), 4.08 (dd, J=17.2Hz, 1H), 3.71 (d, J-17.2Hz, 1H), 2.48 (s, 3H). 5-401 (6)57.4-7.6 (m, 6H), 6.27 (d, J=10,4Hz, 1H), 5.6-5.8 (m, 1H), 4.08 (d, J=17.6Hz, 1H), 3.71 (d, J=17.6Hz, 1H), 3.61 (s, 3H), 2.50 (s, 3H). 5^03 (A) 6 7.35-7.7 (m, 6H), ,6.8 (s, 1H), 4.09 (d, J=17.4Hz, 1H), 3.73 (d, J=: 17.4Hz, 1H), 3.55 (q, J=5.4Hz, 2H), 2.74 (t, J=5.7Hz, 2H), 2.60 (bs, 4H) , 2.45 (s, 3H), 1.79 (bs, 4H). 5404 (A) 6 7.35-7.6 (m, 6H): 6.77 (s, 1H), 4.10 (d, J=17.4Hz, 1H), 3.73 (d, J= 17.4Hz, 1H), 3.53 (q, J=5.7Hz, 2H), 2.57 (t, J=6.0Hz, 2H), 2.47 (bs, 7H) , 1.55-1.65 (m, 4H), 1.35-1.5 (m, 2H). 5405 (6)6 7.45-7.55 (m, 5H), 7.43 (t, J=1.8Hz, 1H), 6.56 (d, J=5.7Hz, 1H), 4.58 (ddd, J=10.6, 8.4, 5.7Hz, 1H), 4.09 (d, J=17.2Hz, 1H), 3.954.05 (m , 1H)._ 3.8-3.9 (m, 1H), 3.71 (d, J=17.2Hz, 1H), 3.5-3.65 (m, 2H)^ 2.85¬ 2.9 (m, 1H), 2.48 (s, 3H), 2.0-2.15 (m, 1H). ^ . 5-406 (6) 6 7.4-7.55 (m, 6H), 6.52 (t, J=6.0Hz; 1H), 5.35 (bs, 1H), 4.84.95 (m , 1H), 4.09 (d, J=174Hz, 1H), 3.6-3.95 (m, 3H), 3.75 (d, J=174Hz, 1H), 3.4-3.5 (m, 1H), 2.45 (s, 3H). 5407 (6)6 7.5-7.55 (m, 5H), 7.43 (t, J=1.8Hz, 1H), 6.84 (d, J=7.0Hz, 1H), 5.37 (d, J=7.1Hz, IN), 4.09 (d, J=17.2Hz, 1H), 3.87 (s, 6H), 3.72 (d, J= 17.2Hz, 1H), 2.49 (s, 3H). 5409 (A) 6 9.80 and 8.65 (bs, 1H), 7.4-7.6 (m, 6H), 7.1 and 6.64 (bs, 1H), 5.94 (bs, 1H), 5.2-5.5 (m, 2H), 3.95445 (m, 5H), 3.73 (d, J=17.0Hz, 1H), 2.42 (s, 3H). 5410 (6)6 7.4-7.55 (m, 6H), 6.72 (bs, 1H), 6.37 (bs, IN), 4.65 (q, J=74Hz, 1H), 4.08 (d, J=174Hz, 1H), 3.70 (d, J=17.4Hz, IN), 3.25-3.35 (m, 2H), 2.45 (s, 3H), 1.47 (d, J=74Hz, 3H), 1.16 (t, J=74Hz, 3H). 5414 (6) 6 8.19 (t, J=6.0Hz, 1H), 7.45-7.55 (m, 5H), 7.43 (t, J=1.8Hz, 1H), 7.21 (d, J=7.5Hz, 1H), 4.93 (ddd, J=11.9, 7.5, 4.2Hz, 1H), 4.31 (bs, 1H) , 4.09 (d, J=17.2Hz, 1H), 4.04.1 (m, 1H), 3.65-3.9 (m, 3H), 3.72 (d, J= 17.2Hz, IN), 2.47 (s, 3H), 2.15-2.25 (m, 1H), 1.8-1.9 (m, 1H). 5415 (6)6 7.67 (t, J-6.6Hz, 1H), 7.3-7.55 (m, 6H), 7.11 (d, J=8.1Hz, 1H), 4.9 -5.0 (m, IN), 4.34.45 (m, 2H), 4.09 (d, J=17.2Hz, 1H),.3.8-3.9 (m, 2H), 1 (d, J=17.2Hz, 1H), 3.03 (s, 3H), 2.33 (s, 3H), 2.2-24 (m, 2H). 5417 (6)6 7.3-7.6 (m, 11H), 6.32 (d, J=9.6Hz, 1H), 6.24 (d, J=9.6Hz, 1H), 2 (d, J=17.2Hz, 1H), 3.69 (d, J=17.2Hz, 1H), 3.59 (s, 3H), 2.51 (s, 3H). 5420 (A) 6 8.77 (bs, 1H), 7.35-7.55 (m, 6H), 6.81 .(s, 1H), 6.37 (d, J=9.3Hz, 1H), 6.31 (s, 1H), 6.15-6.25 (m, 1H), 5.9-6.05 (m, 1H), 4.07 (d, J=17.3 Hz, 1H), 3.69 (d, J=17.3Hz, 1H), 2.43 (s, 3H). ¬ 5421 (A) 6 8.69 (d, J=4.8Hz, 1H), 7.51 (s, 5H), 7.43 (s, 1H), 7.25 (d, J=4.8Hz , 1H), 6.86 (t, J=5.7Hz, 1H), 4.82 (d, J=5.7Hz, 2H), 4.09 (d, J=17.1Hz, 1H), 3.70 (d, J=17.1Hz, 1H), 2.50 (s, 3H). 5423 (6) 5 7.72 (d, J=3.3Hz, 1H), 7.45-7.55 (m, 5H), 7.43 (t, J=1.8Hz, 1H), 7.31 (d, J=3.3Hz, 1H), 6.78 (d, J=7.7Hz, 1H), 5.55-5.65 (m, 1H), 4.08 (d , J=17.2Hz, 1H), 3.71 (d, J=17.2Hz, 1H), 2.47 (s, 3H), 1.72 (d, J=6.8Hz, 3H). 5424 (A) 5 8.29 (d, J=9.6Hz, 1H), 7.4-7.6 (m, 7H), 7.12 (s, 1H), 7.01 (s, 1H), 6.7-6.85 (m, 1H), 4.08 (d, J=17.3Hz, 1H), 3.70 (d, J=17.3Hz, 1H), 2.38 (s, 3H).. 5425 (6)6 7.45-7.55 (m, 6H), 7.34 (bs, 1H), 6.89 (bs, 1H), 6.58 (t, J=4.8Hz, 1H), 4.52 (d, J=15.8Hz, 2H), 4.07 (d, J=17.2Hz, 1H), 3.69 (d, J=17.2Hz, 1H), 3.67 (s, 3H), 2.46. (s, 3H). 5-426 (6)6 8.33 (s, 1H), 7.92 (s.,,1HX 7.45-7.55 (m, 4H), 7.42 (t, J=1.8Hz, 1H), 7.25-7.35 (m, 2H); 6.45-6.55 (m, 1H), 4.07 (d, J=17.2Hz, 1H), 3.71 (d, J=17.2Hz, 1H), 2.29 (s, 3H), 1.87 (d, J=6.6Hz, 3H). 5-427 (A) 5 8.40 (s, 1H), 8.07 (s, 1H), 7.2-7.6 (m, 7H), 6.9-7.1 (m, 1H), 4.08 (d, J=16.5Hz, 1H), 3.70 (d, J=16.5Hz, 1H), 2.44 (s, 3H)., 5-434 (A) 57.4-7.85 (m, 11H), 4.09 (d, J=17.2Hz, 1H), 3.72 (d, J=17.2Hz, 1H), 2.53 (s, 3H). 5450 (A) 6 8.52 (d, J=4.5Hz, 1H), 7.69 (t, J=7.8Hz, 1H), 7.4-7.6 (m, SHT), 7.15 -7.35 (m, 4H), 4.73 (d, J=4.8Hz, 2H), 4.49 (s, 1H), 3.99 (d, J=16.8Hz, 1H), 3.65-3.85 (m, 3H), 3.3-3.65 (m, 1H), 3.33 (d, J=16.8Hz, 1H), 2.48 (s, 3H), 1.20 (t, J-6.9HZ, 3H), 1.16 (t, J=6.9Hz, 3H). 5452 (A) 6 8.68 (s, 1H), 8.59 (s, 1H), 8.25 (s, 1H), 7.4-7.6 (m, 3H), 6.06 (t, •1 J=6.2Hz, 1H), 4.24 (d, J=17.1Hz, 1H), 4.0-4.2 (m, 2H), 3.79 (d, J=17.1 Hz, 1H), 2.47 (s, 3H). 5453 (A) 6 8.69 (s, 1H), 8.58 (s, 1H), 8.55 (d, J=4.9Hz, 1H), 8.26 (s, 1H), 7.71 (td, J=7.5, 1.5Hz, 1H), 7.2-7.55 (m, 6H), 4.74 (d, J=4.9Hz, 2H), 4.25 (d, J=17.3Hz, 1H), 3.79 (d, J=17.3Hz, 1H), 2.50 (s, 3H). 5455 (6)5 8.54 (ddd, J=4.9, 1.6, 0.9Hz, 1H), 7.70 (td, J=7.7, 1.8Hz, 1H), 7.5 -7.55 (m, 3H), 7.43 (s, 2H), 7.33 (d, J=7.7Hz, 1H), 7.2-7.3 (m, 2H), 4.74 (d, J=4.9Hz, 2H), 4.63 (bs, 2H), 4.02 (d, J=17.2Hz, 1H), 3.69 (d, J=17.2Hz, 1H), 2.49 (s, 3H). 5456 (6)5 7.61 (s, 2H), 7.45-7.55 (m, 2H), 7.39 (d, J=7.9Hz, 1H), 6.28 (t, J= 6.6Hz, 1H), 6.24 (bs, 1H), 4.04.15 (m, 2H), 4.07 (d, J=17.2Hz, 1H), 3.69 (d, J=17.2Hz, 1H), 2.43 (s, 3H), 1.50 (s, 9H). 5457 (6)6 8.5-8.55 (m, 1H), 7.71 (td, J=7.7, 1.7Hz, 1H), 7.62 (s, 2H), 745¬ 7.55 (m, 3H), 7.34 (d, J=7.9Hz, 1H), 7.29 (t, J=4.8Hz, 1H), 7.2-7.25 (m, 1H), 6.37 (bs, 1H), 4.75 (d, J=5.0Hz, 2H), 4.07 (d, J=17.2Hz, 1H), 3.70 (d, J=17.2Hz, 1H), 2.50 (s, 3H), 1.50 (s, 9H). 6-001 (A) 6 7.4-7.55 (m, 6H), 6.06 (bs, 1H), 5.39 (d, J=28.6Hz, 2H), 4.24 (d; J=6.0Hz, 2H), 4.05 (d, J=17.0Hz, 1H), 3.67 (d, J=17.3H2, 1H), 2.49 (s, 3H). 6-003 (A) 5 7.45-7.55 (m, 4H), 743 (s, 1H), 7.23 (d, J=7.8Hz, 1H), 4.09 (d, J= 17.1Hz, 1H), 3.71 (d, J=17.1Hz, 1H), 3.43 (bs, 2H), 3.10 (bs, 2H), 2.32 (s, 3H), 1.26 (t, J=6.9Hz, 3H), 1.03 (t, J=6.9Hz, 3H). ¬ 6-005 (6) 5 7.98 (m, 1H), 7.2-7.6 (m, 6H), 4.09 (d, J=17.0Hz, 1H), 3.18 (bs, 1H), 3.71 (d, J=17.0Hz, 1H), 3.40 (bs, 1H), 2.43 and 2.33 (s, 3H), 2.12 and 1.66 (s, 3H), 1.23 and 1.08 (bs, 3H). 6-006 (6) 5 7.2-7.6 (m, 6H), 4.054.15 (m, 1H), 3.75-3.9 and 3.35-3.5 (m, 2H), 3.7 and 3.8 (m, 1H), 241 and 2.38 (s, 3H), 2.23 and 1.80 (s, 3H), 2.00 and 1.77 (s, 3H), 1.25-1.3 and 1.05-1.1 (m, 3H). 6-007 (6) 6 7.5-7.6 (m, 4H), 74-7.45 (m, 1H), 7.2-7.25 (m, 1H), 3.24.7 (m, 4H), 4.10 (d, J=17.0Hz, 1H), 3.72 (d, J=17.0Hz, 1H), 2.35 and 2.33 (s, 3H), 1.65-1.8 and 1.5-1.6 (m, 2H), 1.4-1,5 and 1.1-1.25 (m, 2H), 1.0¬ 1.05 and 0.75^.85 (m,3H). 6-008 (B) 6 7.6-7.65 (m, 2H), 7.5-7.55 (m, 2H), 7.4-7.45 (m, 1H), 7.3-7.35 (m, 1H), 4.65 (bs, 2H), 4.19 fbs, 2H), 4.09 (d, J=17.0Hz, 1H), 3.71 (d, J= 17.0Hz, 1H), 2.37 (s,3H). 6-010 (B) 5 7.5-7.55 (m, 4H), 7.3-7.5 (m, 7H), 4.85 (bs, 2H), 4.08 (d, J=17.0Hz , 1H), 3.69 (d, J=17.0Hz, 1H), 3.35 (bs, 3H), 2.27 (s, 3H). 6-011 (B) 6 7.4-7.55 (m, 5H), 7.25-7.4 (m, 6H), 4.90 (bs, 2H), 4.07 (d, J=17.0 Hz, 1H), 3.68 (d, J=17.0Hz, 1H), 2.40 (s, 3H), 1.88 (bs, 3H). , 6-012 (B) 5 7.4-7.55 (m, 5H), 7.25-7.4 (m, 6H), 4.43 (bs, 2H), 4.07 (d, J=17.0 Hz, 1H). 3.78 (bs, 3H), 3.68 (d, J=17.0Hz, 1H), 2.38 (s, 3H). 6-013 (B) 8 7.5-7.6 (m, 4H), 7.4-7.45 (m, 1H), 7.3-7.4 (m, 4H), 7.15-7.25 (m,^. 2H), 4.93 (bs, 2H), 4.08 (d, J=17.0Hz, 1H), 3.69 (d, J=17.0Hz, 1H), 3.05 (bs, 3H), 2.28 (s, 3H). 6-015 (A) 5 8.82 (s, 1H), 7.35-7.6 (m, 6H), 7.08 (s, 1H), 4.75-5.2 (m, 2H), 4.56 (bs, 2H), 4.08 (d, J=17.4Hz, 1H), 3.79 (d, J=17.4Hz, 1H), 2.36 and • 2.29 (s,3H). 6-016 (A) 8 8.80 and 8.77 (d, J=7.8Hz, 1H), 7.45-7.55 (nn, 4H), 7.3-7.45 (m, 3H) , 4.85-5.2 (m, 1H), 4.2-4.7 (m, 2H), 4.07 and 4.08 (d, J=17.4Hz, 1H), 3.754.0 (m, 1H), 3.69 (d, J=17.4Hz, 1H), 2.31 and 2.36 (s, 3H), 2.25¬2.3(m, 1H). 6-017 (B) 5 8.72 (s, 1H), 7.5-7.6 (m, 4H), 7.48 (s, 1H). 7.4-7.45 (m, 1H), 7.18 (s, 1H), 5.03 (s, 2H), 4.07 (d, J=17.0Hz, 1H), 3.68 (d, J=17.0Hz, 1H), 241 (s, 3H), 2.35 (s, 3H). 6-018 (A) 8 8.72 (s, 1H), 745-7.55 (m, 4H), 7.4-7.45 (m, 1H), 7.31 (d, J=7.8Hz , 1H), 7.20 (s, 1H), 5.04 (s, 2H), 4.07 (d, J=17.4Hz, 1H), 3.68 (d, J= 174Hz, 1H), 2.75 (q, J=7.2Hz, 2H), 2.34 (s, 3H), 1.12 (t, J=7.2Hz, 3H). 6-019 (B) 8 8.80 (s, 1H), 7.55-7.6 (m, 4H), 7.42 (s, 1H), 7.25-7.3 (m,'2H), 5.26 (s, 2H), 4.07 (d, J=17.0Hz, 1H), 3.68 (d, J=17.0Hz, 1H), 3.62 (s, 3H), 2.33 (s, 3H). 6-021 (B) 5 8.5-8.6 (m, 1H), 7.65-7.75 (nn, 1H), 7.4-7.5 (m, 5H), 7.1-7.35 (m, 3H), 3.0-5.3 (m, 4H), 4.04.15 (m, 1H), 3.65-3.8 (m, 1H), 2.37 and 2.34 (s, 3H), 1.25-1.35 and 1.0-1.1 (m, 3H). 6-022 (B) 5 8.55-8.6 (m, 1H), 7.65-7.75 (m, 1H), 7.05-7.55 (m, 8H), 4.3-5.3 (m, 2H), 4.04.15 (m, 1H), 2.94.1 (m, 2H), 3.65-3.75 (nn, 1H), 2:37 and 2.32 (s, 3H), 1.65-1.75 and 1.45-1.55 (m, 2H), 0.95-1.0 and 0.65-0.75 (m , 3H). 6-023 (B) 5 8.55-8.6 and 845-8.5 (m, 1H), 7.4-7.7 (m, 7H), 7.25-7.35 (m, 1H), 7.1-7.2 (m, 1H), 490 (d, J=16.0Hz, 1H), 4.76 (d, J=16.0Hz, 1H), 4.0¬ 4.15 (m, 1H), 3.6-3.85 (m, 2H), 2.42 and 2.34 (s, 3H), 1.23 and 1.06 (bs ,6H). 6-024 (B) 8 8.5-8.6 (m, 1H), 7.05-7.7 (m, 9H), 483 and 4.39 (s, 2H), 4.04.15 (m, 1H), 3.65-3.8 (m, 1H), 2.75-2.85 and 2.65-2.7 (m, 1H), 2.36 and 2.33 (s, 3H), 0.75-0.9 and 0.45-0.6 (m, 4H). 6-025 (B) §8.5-8.55 (m, 1H), 7.55-7.7 (m, 1H), 7.15-7.5 (m, 8H), 4.45 and 416 (bs, 2H), 4.02 (d, J=17.0Hz, 1H), 3.63 (d, J=17.0Hz, 1H), 2.38 (s, 3H), 1.54 (s,9H). 6-026 (B) 8 8.55-8.6 (m, 1H), 7.2-7.75 (m, 8H), 6.92 (d, J=7.7Hz, 1H), 3.7-5.25 (br, 4H), 4.1-4.15 (m, 1^), 3.65-3.7 (m, 1H), 2.04 and 2.26 (s, 3H). 6-027 (A) 6 8.55 (bs, 1H), 6.95-7.75 (m, 9H), 5.07 and 4.93 (bs, 2H), 4.53 and 4.48 (bs, 2H), 4.09 and 4.05 (d, J=17.1Hz, 1H), 3.70 and 3.66 (d, J=17.4 Hz, 1H), 3.47 and 3.14'ls,-3H), 2.38 and 2.33 (s, 3H). 6-028 (B) 6 8.5-8.6 (m, 1H), 7.6-7.75 (m, 1H), 7.05-7.55 (m, 8H), 3.25-5.2 (m, 8H), 3.37 and 3.17 (s, 3H), 2.28 and 2.34 (s, 3H). 6-029 (A) 5 8.5-8.6 (m, 1H), 6.95-7.75 (m, 9H), 4.98 (bs, 2H), 4.58 and 4.37 (bs, 2H), 4.09 and 4.05 (d, J=17.2Hz, 1H), 3.70 and 3.67 (d, J=17.2Hz, 1H), 2.38 and 2.31 (s, 3H), 2.29 and 1.99 (s, 3H). 6-030 (B) 5 8.5-8.65 (m, 1H), 7.15-7.8 (m, 8H), 7.0-7.05 (m, 1H), 3.5-5.3 (rh, 6H), 3.77 and 3.65 (s, 3H), 2.45 and 2.32 (s, 3H). 6-031 (B) 8 8.5-8.65 (m, 1H), 7.2-7.8 (m, 8H), 6.9-7.0 (m, 1H), 4.0-5.2 (m, 5H) , 3.6-3.8 (m,1H), 2.35 (s,3H). 6-032 (B) 8 8.5-8.65 (m, 1H), 7.0-7.8 (m, 9H), 5.8^.0 and 5.55-5.75 (m, 1H), i 3.6-5.55 (m, 8H), 2.37 and 2.34 (s, 3H). 6-033 (B)8 8.5-8.65 (m, 1H), 7.05-7.75 (m, 9H), 3.5-5.3 (m, 6H), 2.37 (s, 3H), 2.28 (s,1H). 6-034 (B) 5 8.45-8.5 (m, 1H), 7.6-7.65 (m, 1H), 7.4-7.55 (m, 6H), 7.15-7.2 (m, 2H), 4.98 (s, 2H), 4.06 (d, J=17.0Hz, 1H), 3.68 (d, J=17.0Hz, 1H), 2.41 (s, 3H), 2.39 (s, 3H). 6-035 (A)8 8.45-8.55 (m, 1H), 7.6-7.7 (m, 1H), 7.35-7.55 (m, 6H), 7.1-7.25 (m, 2H), 4.99 (s, 2H), 4.06 (d, J=19.0Hz, 1H), 3.67 (d, J=19.0Hz, IN), 2.74 (q, J=8.2Hz, 2H), 2.39 (s, 3H), 1.11 (t, J=8.2Hz, 3H). 6-036 (A) 5 8.49 (d, J=4.8Hz, 1H), 7.63 (td, J=7.8,1.8Hz, 1H), 7.35-7.55 (m, 6H), 7.1-7.2 (m, 2H), 4.98 (s, 2H), 4.06 (d, J=17.4Hz, 1H), 3.67 (d, J= 17.4Hz, 1H), 2.70 (t, J=7.2Hz, 2H), 1.64 (hex, J=7.2Hz, 2H), 1.55 (s, 3H), 0.89 (t, J=7.2Hz, 3H). 6-037 (A)8 8.49 (d, J=5.1 Hz, 1H), 7.63 (td, J=7.8,1.8Hz, 1H), 7.35-7.55 (m, 6H), 7.1-7.25 (m, 2H), 4.99 (s, 2H), 4.06 (d, J=17.4Hz, 1H), 3.77 (d, J= 17.4Hz, 1H), 3.1-3.3 (m, 1H), 2.42 (s, 3H), 1.13 (d, J=6.6Hz, 6H). 6-038 (A)8 8.53 (d, J=4.8Hz, 1H), 7.64 (td, J=7.8,1 .BHz, 1H), 7.45-7.55 (m, 5H), 7.4-7.45 (m, 1H), 7.15-7.3 (m, 2H), 5.16 (s, 2H), 4.08 (d, J=17.4Hz , 1H), 3.68 (d; J=17.4Hz, 1H), 2.45 (s, 3H), 1.9-2.0 (m, IN); 0.95-1.05 (m, 2H), 0.7-0.8 (m, 2H). 6-039 (A) 5 8.50 (d, J=5.2Hz, 1H), 7.55-7.65 (m, 1H), 7.4-7.55 (m, 6H), 7.1-7.2 (m, 2H), 4.86 (s, 2H), 4.06 (d, J=19.0Hz, 1H), 3.68 (d, J=19.0Hz, 1H), 2.44 (s,3H), 1.34 (s,9H). 6-041 (B)8 8.5-8.55 (m, 1H), 7.6-7.7 (m, 1H), 7.4-7.55 (m, 6H), 7.27 (s, 1H), 7.15-7.2 (nn, 1H), 6.47 (dd, J=16.0,10.0Hz, 1H), 6.30 (d, J=16.0Hz, 1H), 5.62 (d, J=10.0Hz, 1H), 5.10 (s, 2H), 4.07 (d, J=17.0Hz, 1H), 3.69 (d, J=17.0Hz, 1H),2.44(s, 3H). 6-042 (A) 6 8.54 (d, J=0.9Hz, 1H), 8.09 (d, J=7.6Hz, 1H), 7.15-7.75 (m, 13H), 5.32 (s, 2H), 3.95 (d, J=19.0Hz, 1H), 3.58 (d, J=19.0Hz, 1H), 2.34 (s, 3H). 6-043 (A) 6 8.56 (d, J=4.8Hz, 1H), 7.65-7.7 (m, 1H), 7.5-7.55 (m, 4H), 7.3&¬ 7.45 (m, 2H), 7.15-7.3 (m, 2H), 5.21 (s, 2H), 4.09 (d, J=17.4Hz, 1H), 3.70 (d, J=17.4Hz, 1H), 3.58 (s, 3H), 2.40 (s, 3H). 6-044 (A) 58.56 (d, J=3.9Hz,,1H), 7,65 (td, J=7.8,1.8Hz, 1H), 7.35-7.55 (m, 6H), 7.15-7.3 (m, 2H), 5:21 (s, 2H), 4.09 (d, J=17.4Hz, 1H), 4.00 (q, J= 7.2Hz, 2H), 3.69 (d, J=17-.4Hz, 1H), 2.41 (s, 3H), 0.92 (t, J=7.2Hz, 3H). 6-045 (A) 8 8.55 (d, J=4.8Hz, 1H), 7.67 (td, J=7.8,1.8Hz, 1H), 7.45-7.55 (m, 4H), 7.35-7.45 (m, 2H), 7.15-7.3 (m, 2H), 5.20 (s, 2H), 4.7^.85 (m, 1H) , 4.08 (d, J=17.4Hz, 1H), 3.69 (d, J=17.4Hz, 1H), 2.54 (s, 3H), 0.91 (d, J=6.3Hz, 6H). 6-046 (B) 8 8.5-8.6 (m, 1H), 7.65-7.7 (m, 1H), 7.5-7.55 (m, 4H), 7.4-7.45 (m, 2H), 7.25-7.3 (m, 1H), 7.15-7.2 (m, 1H), 5.23 (s, 2H), 4.17 (d, J=17.0Hz , 1H), 3.75 (d, J=6.8Hz, 1H), 3.69 (d, J=17.0Hz, 1H), 2.42 (s, 3H), 1.55 -1.65 (m, 1H), 0.64 (d, J=6.8Hz, 6H). 6-047 (B) 8 8.5-8.6 (m, 1H), 7.65-7.7 (m, 1H), 7.5-7.55 (m, 4H), 7.4-7.45 (m, 2H), 7.25-7.3 (m, 1H), 7.15-7.25 (m, 1H), 5.23 (s, 2H), 4.15-4.25 (m, 2H), 4.08 (d, J=17.0Hz, 1H), 3.70 (d, J=17.0Hz, 1H), 3.3-3.4 (m, 2H), 2.42 (s, 3H). 6-048 (B) 5 8.55-8.6 (m, 1H), 7.65-7.7 (m, 1H), 7.5-7.55 (m, 4H), 7.4-7.5 (m, 2H), 7.25-7.3 (m, 1H), 7.15-7.25 (m, 1H), 5.23 (s, 2H), 4.05^.15 (m, 3H), 3.69 (d, J=17.0Hz, 1H), 3.2-3.25 (m, 2H), 3.15 (s, 3H), 2.49 (s, 3H). 6-049 (B) 8 8.5-8.6 (m, 1H), 7.65-7.7 (m, 1H), 7.45-7.55 (m, 4H), 7.4-7.45 (m, 2H), 7.25-7.3 (m, 1H), 7.15-7.2 (m, 1H), 5.45-5.6 (m, 1H), 5.23 (s, 2H), 5.0-5.1 (m, 2H), 4.4^.45 (m, 2H), 4.18 (d, J=17.0Hz, 1H), 3.69 (d, J= 17.0Hz, 1H), 2.40 (s,3H). 6-050 (B) 6 8.54 (d, J=4.8Hz, 1H), 7.6-7.7 (m, 1H), 7.35-7.55 (m, 6H), 7.15¬ 7.25 (m, 2H), 5.13 (s, 2H), 4.07 (d, J=17.0Hz, 1H), 3.68 (d, J=17.0Hz, 1H), 2.40 (s,3H), 2.27 (s,3H). 6-051 (B) 5 8.55-8.6 (m, 1H), 7.6-7.65 (m, 1H), 7.45-7.5 (m, 5H), 7.35-7.4 (m, 1H), 7.2-7.25 (rh, 1H), 7.0-7.05 (m, 1H), 4.96 (s, 2H), 4.05 (d, J=17.0Hz , 1H), 3.67 (d, J=17.0Hz, 1H), 343 (s, 3H), 2.37 (s, 3H). 6-053 (B) 8 8.65-8.7 (m, 1H), 7.65-7.8 (m, 2H), 7.5-7.55 (m, 2H), 7.3-7.45 (m, 5H), 5.17 (s, 2H), 4.05 (d, J=17.0Hz, 1H), 3.67 (d, J=17.0Hz,1H), 3.50 (s, 6H), 2.46 (s„3H). 6-054 (B) 8 8.4-8.45 (m, 1H), 7.8-7.85 (m, 1H), 7.2-7.6 (m, 7H), 4.2-5.3 (m, 2H), 4.05^.15 (m, 1H), 3.65-3.75 (m, 1H), 3.05-3.15 (m, 2H), 2.34 and 2.29 (s, 3H), 1.25-1.3 and 1.0-1.1 (m, 3H). 6-055 (A) 8 8.6-8.65 (nn, 2H), 7.5-7.55 (m, 4H), 7.43 {s, 1H), 7.25-7.3 (m, 3H), 4.76 (s, 2H), 4.11 (d, J=19.0Hz, 1H), 3.71 (d, J=19.0Hz, 1H), 2.45-2.5 (m, 1H), 2.34 (s, 3H), 1.2-1.3 (m, 4H). 6-056 (A) 8 8.6-8.75 (m, 2H), 7.4-7.6 (m, 6H), 7.15-7.25 (m, 1H), 5.12 (s, 2H), 4.06 (d, J=17.0Hz, 1H), 3.68 (d, J=17.0Hz, 1H), 2.69 (q, J=7.9Hz, 2H), 2.43 (s, 3H), 1.11 (t, J=7.9Hz, 3H). 6-069 (B) 8 7.8-7.9 (m, 2H), 7.67 (d, J=7.6Hz, 1H), 7.51 (bs, 2H), 7.4-7.45 (m, 1H), 4.42 (s,2H), 4.13 (d,J=17.4Hz, 1H), 3.77 (d, J=17.4Hz, 1H), 3.22 369 (s, 3H). 6-070 (A) 5 8.55 (d, J=4.4Hz, 1H), 7.92 (d, J=7.8Hz, 1H), 7.81 (s, 1H), 7.15¬ 7.7 (m, 7H), 4.93 (s, 2H), 4.52 (s, 2H), 4.13 (d, J=17.0Hz, 1H), 3.76 (d ,J=17.0Hz, 1H). 6-073 (A) 8 8.55 (d, J=4.7Hz, 1H), 8.37 (bs, 1H), 8.02 (d, J=8.5Hz, 1H), 7.91 (d, J=8.5Hz, 1H), 7.83 (bs, 1H), 7.69 (t, J=7.7Hz, 1H), 7.52 (bs, 2H), 7.4-7.5 (m, 2H), 7.15-7.3 (m, 1H), 5.27 (s, 2H), 4.15 (d, J=17.3Hz, 1H), 3.77(d,J=17.3Hz, 1H). ' 6-074 (B) 8 7.5-7.7 (m, 4H), 7.43 (s, 1H), 7.35-7.4 (m, 1H), 4.50 (q, J=8.4Hz, 2H), 4.16 (d, J=17.0Hz, 1H), 3.75 (d, J=17.0Hz, 1H), 2.44 (s, 3H), 2.15 (s, 3H). 6-075 (B) 5 7.7-7.8 (m, 3H), 7.55-7.65 (m, 2H), 7.35-7.4 (m, 1H), 4.50 (q, J=^ 8.6Hz, 2H), 4.10 (d, J=17.0Hz, 1H), 3.71 (d, J=17.0Hz, 1H), 2.44 (s, 3H) ,2.16(8, 3H). 6-076 (B) 8 8.45-8.5 (m, 2H), 7.7-7.75 (m, 2H), 7.6-7.65 (m, 1H), 7.69 (s, 1H), 7.4-7.45 (m, 2H), 7.15-7.2 (m, 2H), 4.97 (s, 2H), 4.06 (d, J=17.0Hz, •1 1H), 3.68 (d, J=17.0Hz, 1H), 2.41 (s, 3H), 2.40 (s, 3H). 6-077 (B) 6 7.5-7.6 (m, 4H), 7.43 (t, J=1.8Hz, 1H), 7.23 (d, J=7.9Hz, 1H), 4.62 (q, J=8.4Hz, 2H), 4.08 (d, J=17.2Hz, 1H), 3.70 (d, J=17.2Hz, 1H), 3.67 (s, 3H), 2.36 (s, 3H). 6-078 (A) 5 8.79 and 8.75 (d, J=1.8Hz, 1H), 7.3-7.55 (m, 7H), 4.85-5.2 (m, 2H), 4.53 and 4.50 (bs, 2H), 4.08 (d, J=17.1Hz, 1H), 3.69 (d, J=17.1Hz, 1H), 3.47 and 3.14 (s, 3H), 2.36 and 2.25 (s, 3H). 6-079 (A) 5 8.55 and 8.53 (d, J=4.8Hz, 1H), 7.69 and 7.59 (td, J=7.8, 1.8Hz, 1H), 7.25-7.55 (m, 8H), 4.8-5.25 (m, 2H), 4.57 and 4.49 (bs, 2H), 4.09 (d, J=17.1Hz, 1H), 3.70 (d, J=17.1Hz, 1H), 3.65 and 3.27 (q, J=6.9Hz, 2H), 2.37 and 2.34 (s, 3H), 1.26 and 1.08 (t, J=6.9Hz, 3H). 6-080 (B) 5 8.58 (ddd, J=4.9, 1.8, 0.9Hz, 1H), 7.70 (td, J=7.7, 1:8Hz, 1H), 7.35-7.55 {m, 7H), 7.18 (dd, J=7.5, 4.9Hz, 1H), 5.98 (q, J=7.1Hz, 1H), ¬ 4.08 (d, J=17.2Hz, 1H), 3.70 (d, J=17.2Hz, 1H), 3.42 (s„ 3H), 2.43 (s, 3H), 1.90 (d,''J=7.0Hz, 3H). 6-081 (A) 5 8.21 (d, J=4.2Hz, 1H), 7.3-7.6 (m, 7H), 6.80 (dd, J=8.1, 4.2Hz, 1H) , 6.60 (d, J=8.7Hz, 1H), 4.05 (d, J=17.1Hz, 1H), 3.66 (d, J=17.1Hz, 1H), 3.34 (s, 3H), 2.45 (s, 3H), 2.42 (s, 3H). 6-082 (A) 6 8.22 (d,.J=4.8Hz, 1H), 7.4-7.65 (m, 7H), 6.78 (dd, J=7.2, 4.8Hz, 1H), 6.63 (d, J=8.4Hz, 1H), 4.08 (d, J=16.8Hz, 1H), 3.70 (s, 3H), 3.69 (d, J=16.8Hz, 1H), 3.40 (s, 3H)' 2.46 (s, 3H). 6-083 (A) 5 8.42 (s, 2H), 7.35-7.55 (m, 6H), 6.77 (t, J=5.-1Hz, 1H), 4.06 (d, J= 18.1Hz, 1H), 3.67 (d, J=18.1Hz, 1H), 3.43 (s, 3H), 2.44 (s, 3H), 2.43 (s , 3H). 6-084 (A) 6 8.46 (bs, 1H), 8.40 (bs, 1H), 7.45-7.6 (m, 5H), 7.43 (s, 1H), 6.74 (t, J=4.8Hz, 1H), 4.09 (d, J=17.4Hz, 1H), 3.70 (d, J-17.4Hz, 1H), 3.69 (s, 3H), 3.53 (s, 3H), 2.46 (s, 3H). 6-085 (B)§ 7.4-7.55 (m, 5H), 7.2-7.3 (m, 1H), 3.85^.2 (m, 3H), 3.6-3.8 (m, 1H), 2.5-2.65 (m, 2H), 2.32 and 2.30 (s, 3H), 2.1-2.2 (m, 2H). 6-086 (A) 57.4-7.6 (m, 6H), 4.09 (d, J=17.2Hz, 1H), 3.71 (d, J=17.2Hz, 1H), 2.89 (s, 4H), 2.57 (s, 3H). 7-002 (A) 5 7.87 (bs, 1H), 7.78 (d, J=8.1Hz, 2H), 7.65 (d, J=8.1Hz, 2H), 7.50 (bs, 2H), 7.43 (bs, 1H), 4.55^.7 (m, 2H), 4.09 (d, J=17.4Hz, 1H), 3.71 (d, J=17.4Hz, 1H). ., 7-003 (A) 5 8.85 (s, 1H), 8.49 (bs, 1H), 7.86 (d, J=8.4Hz, 2H), 7.67 (d, J=8.7 Hz, 2H), 7.51 (bs, 2H), 7.43"(d, J=1.8Hz, 1H), 7.40 (s, 1H), 5.13 (d, J= 4.8Hz, 2H), 4.06 (d, J=17.4Hz, 1H), 3.67 (d, J=17.1Hz, 1H). 7-008 (A) 5 8.79 (s, 1H), 8.14 (bs, 1H), 7.35-7.5 (m, 7H), 5.11 (d, J=5.0Hz, 2H), 4.06 (d, J=17.4Hz, 1H), 3.67 (d, J=17.1Hz, 1H), 2.37 (s, 3H). 7-009 (A) 5 9.06 (bs, 1H), 8.50 (d, J=4.5Hz, 1H), 7.75 (t, J=7.2Hz, 1H), 7.2¬ 7.6 (m, 8H), 5.04 (d, J=4.2Hz, 2H), 4.08 (d, J=17.4Hz, 1H), 3.70 (d, J= 17.4Hz, 1H),2.44(s, 3H). . . 8-001 (A) 5 8.40 (d, J=8.2Hz, 2H), 7.74 (d, J=8.2Hz, 2H), 7.53 (s, 2H), 7.43 (s , 1H), 7.04 (d, J=4.7Hz, 1H), 6.74 (d, J=4.7Hz, 1H), 4.13 (d, J=17.3Hz, 1H), 3.89 (s, 3H), 3.74 (d, J=17.3Hz, 1H). 8-002 (A) 5 8.22 (d, J=8.0Hz, 2H), 7.56 (s, 1H), 7.53 (s, 2H), 7.43 (s, IN), ' 7.03 (d, J=4.7Hz, 1H), 6.72 (d, J=4.7Hz, 1H), 4.12 (d, J=17.3Hz, 1H), 3.84 (s, 3H), 3.72 (d, J=17.3Hz, 1H), 2.74 (s, 3H). 8-003 (A) 6 8.19 (d, J=8.1Hz, 1H), 7.5-7.6 (m, 4H), 7.43 (s, 1H), 7.04 (d, J= 4.8Hz, 1H), 6.71 (d, J=4.8Hz, 1H), 4.23 (t, J=7.2Hz, 2H), 4.12 (d, J= 17.1Hz, 1H), 3.72 (d, J=17.1Hz, 1H), 2.73 (s, 3H), 1.91 (hex, J=7.2Hz, 2H), 0.99 (t, J=7.2Hz, 3H). 8-004 (A) 6 8.17 (d, J=8.1Hz, 1H), 7.45-7.65 (m, 4H), 7.41 (s, 1H), 7.36 (t, J= 4.2Hz, 1H), 4.12 (d, J=17.4Hz, 1H), 3.79 (s, 3H), 3.74 (d, J=17.4Hz, 1H) ,3.17 (d, J=4.2Hz, 2H), 2.69 (s, 3H). 9-003 (B) 8 8.75 (d, J=1.2Hz, 1H), 8.7-8.75 (m, 1H), 8.14 (t, J=1.8Hz, 1H), 7.5 -7.6 (m, 2H), 7.45 (d, J=8.6Hz, 1H), 6.0-6.05 (m, 1H), 4.05-4.2 (m, 3H), 3.74 (d, J=17.2Hz, 1H), 2.48 (s, 3H). 9-008 (A) 8 7.97 (s, 1H), 7.45-7.55 (m, 2H), 7.35-7.4 (m, 1H), 6.44 (t, J=6.3Hz , 1H), 4.40 (d„J=17.6Hz, 1H), 4.0^.15 (m, 3H), 2.42 (s, 3H). 9-009 (A) 8 8.51 (dd, J=5.1, 0.9Hz, 1H), 7.96 (s, 1H), 7.70 (td, J=7.5, 1.5Hz, 1H), 7.5-7.6 (m, 3H), 7.3-7.4 (m, 2H), 7.15-7.25 (m, 1H), 4.74 (d, J=4.8 Hz, 2H), 4.40 (d, J=17.6Hz, 1H), 4.09 (d, J=17.6Hz, 1H), 2.50 (s, 3H): 10-001 (A) 8 8.87 (d, J=2.1Hz, 1H), 8.25-8.3 (m, 2H), 8.14 (dd, J=8..1, 2.1Hz, 1H), 7.51 (bs, 2H), 7.45 (d, J=1.8Hz, 1H), 4.05^-.2 (m, 3H), 3.75 (d, J= 17.4Hz, 1H). 10-002 (A) 8 8.94 (bs, 1H), 8.88 (bs, 1H), 8.61 (d, J=5.1Hz, 1H), 8.30 (d, J=7.8 Hz, 1H), 8.12 (dd, J=8.1, 2.1Hz, 1H), 7.68 (td, J=7.8,1.8Hz, IN), 7.51 (bs, 2H), 7.45 (t, J=1.8Hz, 1H), 7.34 (d, J=7.8Hz, 1H), 7.2-7.25 (m, 1H) , 4.80 (d, J=5.4Hz, 2H), 4.12 (d, J=17.4Hz, 1H), 3.74 (d, J=17.4Hz, 1H). 10-003 (A) 8 8.53 (d, J=1.8Hz, 1H),'8.48 (d, J=8.4Hz, 1H), 7.74 (dd, J=8.4,1.8 Hz, 1H), 7.47 (bs, 3H), 4.0-4.2 (m, 2H), 4.05 (d, J=17.4Hz, 1H), 3.68 (d ,J=17.4Hz, 1H). 10-004 (A) 8 9.01 (s, 1H), 8.17 (d, J=8.4Hz, 1H), 8.10 (d, J=8.4Hz, IN), 7.51 (s , 2H), 7.43 (s, 1H), 6.77 (t, J=6.3Hz, 1H), 4.26 (d, J=18.3Hz, 1H), 4.05 -4.25 (m, 2H), 3.89 (d, J=18.3Hz, 1H). 10-005 (A) 8 9.09 (s, 1H), 8.57 (d, J=5.1Hz, 1H), 8.24 (d, J=8.4Hz, 1H), 8.12 (d , J=8.4Hz, 1H), 7.86 (bs, 1H), 7.65-7.75 (m, 1H), 7.52 (s, 2H), 7.43 (s, 1H), 7.2-7.35 (m, 2H), 4.78 (d, J=4.2Hz, 2H), 4.28 (d, J=18,3Hz, 1H), 3.90 (d,J=18.3Hz, 1H). 11^34 (A) 57.96 (t, J=7.0Hz, 1H),,7.88 (dd, J=8.2, 1.6Hz, 1H), 7.81 (dd, J= 11.8, 1.4Hz, 1H), 7.51 (bs,-2H), 7.4-7.45 (m, 1H), 4.20 (dd, J=18.2, 1.4 Hz, 1H), 3.82 (d, J=18.2Hz, 1H). 11-038 (A) 5 7.89 (d, J=8.1Hz, 1H), 7.72 (s, 1H), 7.64 (d, J=8.1Hz, 1H), 7.50 (s , 2H), 7.43 (s, 1H), 4.09 (d, J=17.1Hz, 1H), 3.95 (s, 3H), ,3.71 (d, J=: 17.1Hz, 1H). 11-056 (A) 6 8.64 (d, J=4.5Hz, 1H), 8.06 (d, J=8.4Hz, 1H), 7.75 (td, J=7.7, 1.1 Hz, 1H), 7.5-7.6 (m, 4H), 7.35-7.45 (m, 2H), 7.28 (t, J=6.2Hz, 1H), 5.48 (s, 2H), 4.11 (d, J=17.1Hz, 1H), 3.72 (d, J=17.1Hz, 1H), 2.65 (s, 3H). 11-057 (6)6 8.4-8.45 (m, 1H), 7.75 (s, 1H), 7.5-7.65 (m, 5H), 7.44 (s, 1H), 6.55 (s, 1H), 4.12 (d, J=17.0Hz, 1H), 3.73 (d, J=17.0Hz, 1H), 2.37 (s, 3H). 11-059 (A) 6 7.90 (d, J=8.4Hz, 1H), 7.4-7.7 (m, 5H), 4.11 (d, J=17.4Hz, 1H), 3.91 (s, 3H), 3.72 (d, J=17.4Hz, 1H), 3.50 (q, J=7.5Hz, 2H), 1.25 (t, J= 7.5Hz, 3H). 11-060 (A) 5 8.02 (d, J=6.3Hz, 1H), 7.75 (s, 1H), 7.67 (d, J=6.3Hz, 1H), 7.51 (s , 2H), 7.43 (s, 1H), 4.95 (s, 2H), 4.12 (d, J=17.4Hz, 1H), 3.97 (s, 3H), 3.74 (d, J=17.4Hz, 1H). 11-062 , (8)6 8.07 (t, J=0.8Hz, 1H), 7.99 (ddd, J=8.0, 1.6, 0.4Hz, 1H), 7.93 (dd, J=7.4, 0.6Hz, 1H), 7.48-7.52 (m, 2H), 7.46 (t, J=1.4Hz, 1H), 4.11 (d, J=16.8Hz, 1H), 3.74 (dd, J=17.4, 1.0Hz, 1H). 11-063 (B) 6 8.00 (s, 1H), 7.93 (d, J=8.1Hz, 1H), 7.87 (d, J=8.1Hz, 1H), 7.51 (s , 2H), 7.4-7.5 (m, 1H), 4.12 (d, J=16.7Hz, 1H), 3.96 (s, 3H), 3.74 (d, J=16.7Hz, 1H). 11-071 (B) 6 8.03 (d, J=8.0Hz, 1H), 7.6-7.7 (m, 2H), 7.51 (s, 2H), 7.4-7.5 (m, 1H), 4.09 (d, J=17.2Hz, 1H), 3.95 (s, 3H), 3.70 (d, J=17.2z, 1H). 11-073 (A) 6 7.95-8.05 (m, 1H), 7.4-7.5 (m, 2H), 7.2-7.35 (m, 3H), 4.06 (d, J= 17.1Hz, 1H), 3.95 (s, 3H), 3.70 (d, J=17.1Hz, 1H), 2.52 (s, 3H). 11-092 (A) 6 7.94 (d, J=8.8Hz, 1H), 7.4-7.6 (m, 5H), 4.37 (q, J=7.1Hz, 2H), 4.15 (d, J=17.3Hz, 1H), 3.73 (d, J=17.3Hz, 1H), 2.62 (s, 3H), 1.40 (t, J=7.1 Hz, 3H). 11-095 (A)57.94 (d, J=8.8Hz, 1H), 7.5-7.8 (m, 5H), 4.37 (q, J=7.1Hz, 2H), 4.09 (d, J=17.3Hz, 1H), 3.70 (d, J=17:3Hz, 1H), 2.62 (s, 3H), 1.40 (t, J=7.1 Hz, 3H). 14-004 (A) 6 7.40 (s, 1H), 7.35 (s, 2H), 5.99 (s, 1H), 5.65 (s, 1H). 14-005 (B) 6 7.2-7.45 (m, 3H), 6.10 (s, 1H), 5.92 (s, 1H). 14-006 (A) 6 7.40 (s, 2H), 7.33 (s, 1H), 5.63 (s, 1H), 5.45 (s, 1H), 4.47 (s, 2H), 3.84 (q, J=8.8Hz, 2H). 14-007 (B) 6 7.3-7.4 (m, 3H), 5.22 (s, 1H), 5.02 (s, 1H), 2.07 (s, 2H), 0.04 (s, 9H). 14-008 (A) 6 8.63 (d, J=5.1Hz, 1H), 7.69 (t, J=8.0Hz, 1H), 7.2-7.4 (m, 5H), 5.99 (s, 1H), 5.64 (s, 1H). 14-009 (A) 6 7.25-7.6 (m, 3H), 6.04 (s, 1H), 5.80 (s, 1H). 14-010 (B) 67.24 (s, 1H), 7.20 (s, 1H), 7.14 (s, 1H), 5.97 (s, 1H), 5.77 (s, 1H), 2.36 (s, 3H). ; 14-012 (B) 67.54 (s, 2H), 6.06 (s, 1H), 5.83 (s, 1H). 14-015 (A) 67.70 (s, 1H), 7.52.(s, 2H), 6.04 (s, 1H), 5.80 (s, 1H). 14-018 (A) 5 7.2-7.45 (m, 4H), 5.98 (s, 1H), 5.78 (s, 1H), 2.93 (dd, J=10.8, 7.8 Hz, 1H), 2.01 (dd, J=10.8, 7.8Hz, 1H), 1.87 (t, J=7.8Hz, 1H). 14-019 (B) 6 7.35-7.45 (m, 2H), 7.2-7.3 (m, 2H), 6.09 (d, J=53.2Hz, 1H), 6.03 (s , 1H), 5.82 (s, 1H). 14-020 (8)67.2-7.5 (m, 6H), 6.95-7.1 (m, 3H), 5.93 (s, 1H), 5.77 (s, 1H), 5.17 (s, 2H). 14-021 (A) 6 7.57 (d, J=2.7Hz, 1H), 7.2-7.55 (m, 4H), 6.9-7.15 (m, 3H),:5.96 (s, 1H), 5.78 (s, 1H), 5.19 (s, 2H). 14-022 (A) 5 8.27 (s, 1H), 7.99 (s, 1H), 7.15-7.6 (m, 4H), 6.00 (s, 1H), 5.83 (s , 1H). 14-023 (A) 6 7.74 (s, 1H), 7.69 (d, J=7.7Hz, 1H), 7.58 (d, J=7.7Hz, 1H), 7.46 (t i , J=7.7Hz, 1H), 6.04 (s, 1H), 5.82 (s, 1H). 14-024 (A) 5 8.34 (s, 1H), 8.25 (d, J=8.0Hz, 1H), 7.79 (d, J=8.0Hz, 1H), 7.60 (t , J=8.0Hz, 1H), 6.14 (s, 1H), 5.93 (s, 1H). (Test Examples) [0253] Next, usefulness of the compound of the present invention as a pesticide is specifically explained in the following Test Examples to which the present invention is not limited. Test Example 1: Insecticidal test against cabbage moth [0254] A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 500 ppm. To the chemical solution was dipped leaves of cabbage for about 10 seconds, and after air-drying, they were placed in a laboratory dish, then 5-cabbage moth (Plutella xylostella) in the stage of second instar larva per the dish were released therein, and the dish was covered with a lid and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 6 days was counted and a rate of dead insects was calculated by the following calculation equation. Incidentally, the test was carried out with two districts. Rate of dead insects (%) = (Number of dead insects/Number of released insects) x 100 As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. 37.3 The compounds of the present invention: No.1-005,1-006,1-015,1-016,1¬025,1-031,1-040,1-041,1-053,1-055—1-058,1-062-1-074,1-076,1-077,1-079— 1-096,1-098,1-101,1-102,1-104-1-110,1-113,1-114,1-116—1-140,1-145—1¬147,1-149—1-157,1-159—1-161,1-166—1-168,1-171,1-172,1-174,1-175,1-176 M-177M-178-1-184,1-185M-187,1-188M-189M-190,1-194,1-196,1¬199,1-206*,1-207,1-209,1-212,1-214,1-215,1-225,1-226,2-001—2-005,2-011— 2-021,2-022*,2-024—2-027,2-028* *,2-029**,2-030,2-031,2-032*,2-033,2-034* *,2-035**,2-036—2-041,2-042**,2-043,2-044**,2-045**,2-046**,2-047*,2-048* *,2-049**,2-050*,2-051*,2-052*,2-053,2-054**,2-055**,3-002—3-001,3¬006,3-007,3-012,3-018,3-023,3-025—3-028,3-030-3-035,3-037,3-038,3¬040,3-043,3-044,3-046,3-047,3-050,3-055,3-058*,3-060,3-061*,3-062—3¬067,3-068 ^3-069,3-070^3-071^3-073-3-075,3-077—3-081,3-084,3-085*,3-086 *,3-d)87—3-089,3-090*,3-091*,3-092*,3-093*,3-094-3-098,3-100*,3-102— 3-104,3-105*,3-106—3-108,3-109*,3-110*,3-1ir,3-112*,3-113*,3-114,3¬115,3-116*,3-117,3-119-3-127,3-129,3-131,3-132*,3-133-3-136,3-138— 3-141,3-143,3-146,3-148,4-002,4-003*,4-004*,4-005,4-006*,4-008—4-010,5-001 *,5-002*,5-003*,5-004*,5-005*,5-006,5-007,5-008*,5-009*,5-010*,5-011*,5-012 *,5-013*,5-014*,5-015*,5-016,5-017;5-019,5-022*,5-023*,5-029*,5-030-5¬035,5-036*,5-037*,5-038*,5-039*,5-040*,5-041*,5-042,5-043,5-044*,5-045 *,5-046*,5-047*,5-048*,5-049*,5-050*,5-051*,5-052*,5-053*,5-054-5-056,5-057 *,5-058*,5-059*,5-060*,5-061*,5-062*,5-063*,5-064*,5-065*,6-066,5-067*,5-068 *,5-069*,5-070*,5-071*,5-072*,5-073*,5-074*,5-075,5-075(+)*,5-075(-),5-076 *,5-077*,5-078*,5-079—5-082,5-083*,5-084,5-085*,5-086*,5-087*,5-088*,5-089 *,5-090**,5-091*,5-092*,5-093*,5-094*,5-095,5-097,5-098,5-099*,5-100*,5-101 *,5-102*,5-103*,5-104*,5-105*,5-106-5-108,5-109*,5-110,5-111*,5-112*,5-113 *,5-114*,5-115,5-116,5-117*,5-118*,5-119*,5-120**,5-121*,5-122*,5-123*,5-124 **,5-125,5-126*,5-127,5-128*,5-129,5-130*,5-131-5-133,5-134*,5-135— 5-137,5-138*,5-139*,5-140*,5-141*,5-142*,5-143,5-144*,5-145*,5-146,5-147 *,5-148*,5-149,5-150,5-151*,5-152-5-155,5-156*,5-158,5-159,5-160*,5-161* *,5-162*,5-163,5-164,5-165*,5-166*,5-167,5-168**,5-169*,5-170—5-172,5-173* *,5-174**,5-175,5-176*,5-177,5-178,5-179*,5-180*,5-181*,5-182*,5-183 *,5-184,5-185*,5-186*,5-187*,5-188*,5-189**,5-189(+)*,5-189(-),5-190(+) *,5-190(-),5-191*,5-i92*,5-193*,5-194*,5-195**,5-196* *,5-197**,5-198¬5-200,5-201 *,5-202*,5-203**,5-204,5-205*,5-206*,5-207,5-208**,5-209,5-210 *,5-211*,5-212*,5-213*,5-214*,5-215*,5-216*,5-217**,5-218*,5-219*,5-219(+) *,5-219(-)*,5-220*,5-221*,5-222*,5-223*,5-224*,5-225*,5-226*,5-227*,5-228 *,5-229*,5-230*,5-231 *,5-232*,5-233*,5-234*,5-235**,5-236*,5-237,5-238 *,5-239*,5-240*,5-241*,5-24^*,5-243**,5-244,5-245*,5-246*,5-247",5-248,5-249 *,5-250,5-251*,5-252,5-253.5-254^5-255,5-256*,5-257*,5-258**,5-259*,5¬260,5-261 *,5-262**,5-263**,5-264*,5-265*,5-266,5-267*,5-268*,5-270,5¬271,5-272*,5-273*,5-274*,5-275*,5-276*,5-277*,5-278*,5-279*,5-280,5¬281,5-282*,5-283*,5-284*,5-285*,5-286*,5-287,5-288*,5-289*,5-290,5-291 *,5-292,5-293,5-294*,5-295*,5-296,5-298,5-299*,5-300*,5-301*,5-302,5-303 *,5-304,5-305**,5-306*,5-307*,5-308**,5-309*,5-310**,5-311,5-3T2*,5-313 *,5-314*,5-315*,5-316,5-317*,5-318*,5-319*,5-320*,5-321,5-322,5-323*,5-324~ 5-326,5-328,5-329*,5-330*,5-331*,5-332*,5-333*,5-334*,5-335*,5-336*,5¬337,5-338*,5-339*,5-340,5-341,5-342*,5-343*,5-344*,5-345,5-346*,5-347,5-349 *,5-350~5-352,5-353*,5-354*,5-355*,5-356*,5-357*,5-358*,5-359* *,5-360 *,5-361*,5-362*,5-363,5-366,5-372,5-374*,5-375*,5-376**,5-377**,5-378*,5-379 **,5-380**,5-381**,5-383*,5-384*,5-385**,5-386**,5-387*,5-389*,5-390 *,5-391,5-392*,5-393*,5-395*,5-396**,5-397*,5-398*,5-399*,5-400*,5-401 *,5-402*,5-403-'5-407,5-408*,5-409,5-410*,5-411*,5-412*,5-413*,5-414,5-415 *,5-416,5-417*,5-418*,5-419*,5-420*,5-421 *,5-422*,5-423*,5-424*,5-425*,5-427 *,5-430*,5-431,5-432*,5-433*,5-434*,5-436,5-439*,5-440*,5-441*,5-442*,5-443 *_5-444*,5-445*,5-446*,5-447~5-449,5-452*,5-453*,5-454*,5-456,5-457,6-001 *,6-002,6-003*,6-004**,6-005,6-006**,6-007*,6-008*,6-009,6-010,6-011 *,6-012,6-013*,6-015**,6-016*,6-017*,6-018*,6-019*,6-020*,6-021*,6-022* *,6-023*,6-024**,6-025,6-026*,6-027*,6-028*,6-029*,6-030,6-031*,6-032*,6-033 *,6-034*,6-035*,6-036*,6-037*,6-038*,6-039*,6-040*,6-041*,6-042*,6-043 *,6-044*,6-045*,6-046*,6-047*,6-048*,6-049*,6-050*,6-051*,6-052,6-053,6-054 *,6-055*,6-056*,6-057,6-058*,6-059*,6-060* *,6-061,6-062**,6-063*,6-064* *,6-065**,6-066*,6-067**,6-071**,6-074*,6-075*,6-076*,6-078*,6-079*,6-080 *,6-080(+)*,6-080(-)*,6-083*,6-084*,6-085-6-088,7-001,7-002*,7-003*,7-004 *,7-005*,7-006*,7-007*,7-008*,7-009*,7-010*,8-002*,8-003*,8-004,9¬003,9-008,9-009,10-001,10-002*,10-003-10-005,11-006,11-018,11-024,11-025 *,11-026*,11-038,11-043,11-045,11-046,11-049*,11-050—11-052,11-054,11-058 -11-062,11-066,11-075,11-088,11-089,12-001,12-002. In the interim, the indication of "*" shows that the insecticida! test was carried out by use of a chennical solution of a concentration of lOOppm, and the indication "**" shows that the insecticidal test was carried out by use of a chemical solution of a concentration of 10ppm. Test Example 2: Insecticidal test against common cutworm [0255] A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 500 ppm. To the chemical solution was dipped leaves of cabbage for about 10 seconds, and after air-drying, they were placed in a laboratory dish, then S-common cutworm (Spodoptera litura) in the stage of secorTd instar larva ' per the dish were released therein, and the dish was covered with a lid and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 6 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention: No.1-005,1-015,1-016,1-057,1¬ 058,1-062,1-066,1-069,1-080,1-081,1-088,1-101,1-102,1-105—1-109,1¬118,1-122,1-123,1-125,1-127,1-129,1-130,1-132,1-153,1-156,1-157,1-166— 1-168,1-175,1-176,1-177*,1-182-1-184,1-185*,1-188*,1-189M-l94,1-206 *,1-207,1-212,1-214,1-215,1-225,2-002,2-003,2-013,2-019—2-021,2-022*,2-024~ 2-026,2-028,2-029,2-031,2-032,2-034—2-039,2-041,2-042,2-044—2-046,2-047 *,2-048,2-049,2-050*,2-05r,2-052*,2-054-2-056,3-006,3-018,3-026,3-030,3-032 —3-035,3-037,3-043,3-044,3-047,3-058,3-060—3-064,3-068*,3-069,3-070*,3-071 *,3-072,3-078,3-079,3-081,3-083-3-086,3-089,3-090*,3-091*,3-093*,3¬094,3-095,3-098,3-100*,3-102,3-103,3-105*,3-106,3-107,3-109,3-110*,3-111 *,3-112*.3-113*,3-114,3-115,3-116*,3-117,3-121,3-123—3-126,3-129,3-131,3-132 *,3-135,3-136,3-139,3-140,3-145,3-148,4-003*,4-004,4-006*,4-010,5-001*,5-002 *,5-003*,5-004*,5-005*,5-006,5-007,5-008*,5-009*,5-010,5-011,5-012*,5-013 *,5-014*,5-015*,5-016,5-017,5-019,5-022*,5-023*,5-029*,5-032,5-034,5¬ 035,5-036*,5-037*,5-038*,5-039*,5-040*,5-041 *,5-042,5-045*,5-046*,5-047 *,5-048*,5-049*,5-050*,5-051*,5-052*,5-053*,5-054,5-057*,5-058*,5-059*,5-060 —5-064,5-065*,5-066—5-068,5-069*,5-070*,5-071 *,5-072*,5-073—5¬ 075,5-075{+)*,5-076*,5-077*,5-078-5-081,5-083*,5-084,5-085,5-086*,5-087 *,5-088*,5-089*,5-090,5-091*,5-092*,5-093*,5-094*,5-099-5-101,5-102*,5-103 *,5-104*,5-105*,5-106,5-109,5-111*,5-112,5-113*,5-114*,5-115,5-116,5-117 *,5-118,5-119*,5-120,5-121 *,5T122~5-126,5-128*,5-130,5-132—5-134,5¬136,5-137,5-138*,5-139*,5-140~5-147,5-148*,5-149,5-151-5-156,5-159¬5-169,5-171—5-178,5-179*,5-180,5-181,5-182*,5-183*,5-184,5-185*,5-186 *,5-187*,5-188*,5-189,5-189(+),5-191*,5-192*,5-193-5-201,5-202*,5¬203,5-204,5-205*,5-206*,5-207-5-209,5-210*,5-211*,5-212*,5-213*,5-214 *,5-215*,5-216*,5-217,5-218*,5-219*,5-219(+)*,5-219(-),5-220*,5-221,5-222 *,5-223*,5-224*,5-225,5-226*,5-227*,5-228,5-229,5-230*,5-231,5-232*,5-233 *,5-234*,5-235,5-236*,5-237*,5-239,5-240*,5-241 *,5-242*,5-243-5^245,5-246 ' *,5-247*,5-249*,5-250,5-251,5-254*,5-256*,5-257-5-259,5-261 *,5-262,5¬263,5-264*,5-265*,5-267,5-268*,5-269,5-271,5-272*,5-273*,5-274*,5-275¬5-277,5-278*,5-279*,5-280,5-282*,5-283*,5-284,5-285*,5-286*,5-288*,5-289 *,5-291*,5-292,5-294*,5-295*,5-296,5-298,5-299*,5-300,5-301*,5-302,5¬303,5-305,5-306*,5-307*,5-308-5-311,5-312*,5-313*,5-314*,5-315*,5-316,5-317 *,5-318*,5-319*,5-320-5-322,5-323*,5-329*,5-330*,5-331*,5-332,5-333*,5-334 *,5-335-5-337,5-338*,5-339*,5-341,5-342,5-343*,5-344*,5-345,5-346,5-349 *,5-351,5-353,5-354,5-355*,5-356—5-359,5-360*,5-361*,5-362*,5-363,5-374 *,5-375*,5-376,5-377,5-378*,5-379-5-386,5-387*,5-389*,5-390*,5-392*,5-393 *,5-395,5-396,5-397*,5-398*,5-399*,5-400*,5-401 *,5-402*,5-405~5-407,5-408 *,5-409,5-410*,5-411*,5-412*,5-413*,5-415*,5-417*,5-418*,5-419*,5-420*,5-421 *,5-422*,5-423*,5-424*,5-425*,5-427*,5-430*,5-432*,5-433*,5-434*,5-439 *,5-440*,5-441*,5-442*,5-443*,5-444*,5-446*,5-447,5-452*,5-453*,5-454*,6-001 *,6-002,6-003*,6-004-6-006,6-007*,6-008*,6-010,6-012,6-013,6-015,6-016,6-017 *,6-018,6-019*,6-02.0*,6-021*,6-022~6-025,6-026*,6-027*,6-028-6-030,6-Q31 *,6-032*,6-033*,6-034*,6-035*,6-036-6-038,6-039*,6-040,6-041,6-042*,6-043 *,6-044,6-045,6-046*,6-047*,6-048*,6-049*,6-050*,6-051*,6-053,6-054*,6-055 *,6-056,6-058-6-067,6-071,6-074*,6-075*,6-076*,6-078*,6-079*,6-080*,6-080(+) *,6-080(-)*,6-083*,6-084*,6-086,6-087,7-001,7-002*,7-003*,7-004*,7-005*,7-006 *,7-007*,7-008*,7-009*,7-010*,8-002*,8-003*,8-004,9-009,10-001-10¬005,11-024,11-025*,11-026*,11-038,11-049*,11-052,11-055,11-061,11¬062,11-066,11-070,12-001,12-002. In the interim, the indication of "*" shows that the insecticidal test was carried out by use of a chemical solution of a concentration of lOOppm. Test Example 3: insecticidal test against beet armyworm 377 [0256] A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with v^/ater containing a spreading agent to prepare a chemical solution with a concentration of 100 ppm. To the chemical solution was dipped leaves of cabbage for about 10 seconds, and after air-drying, they were placed in a laboratory dish, then 5-beet armyworm (Spodoptera exigua) in the stage of second instar laPv/a per the dish were released therein, and the dish was covered with a lid and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 6 days was counted and a rate of dead insects was calculated by the caTculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention: No.1-015,1-016,1-057,1-058,1-062— 1-064,1-066,1-080,1-081,1-088,1-102,1-105,1-106,1-109,1-118,1-122,1- 123,1-125;i-127,1-151,1-153,1-155-1-157,1-166,1-175,1-189,1-207,1- 214,1-215,2-003,2-019,2-020,3-026,3-027,3-030,3-032,3-037,3-060,3-091,3- 093,3-095,3-109,3-110,3-112,3-125,5-001—5-005,5-008,5-009,5-029,5- 036,5-037,5-040,5-041,5-045,5-046,5-048,5-049,5-050,5-052,5-053,5-057— 5-059,5-061-5-065,5-067-5-069,5-071,5-073~5-075,5-075(+),5-076,5-083,5-086 —5-089,5-091,5-092,5-094,5-111,5-113,5-117-5-119,5-122,5-138—5- 142,5-147,5-148,5-151,5-160,5-165,5-174,5-182,5-183,5-185—5-188,5- 189(+),5-202,5-205,5-210-5-212,5-214-5-216,5-218,5-219,5-219(+),5- 220,5-223,5-226,5-227,5-230,5-232—5-234,5-236,5-239,5-241,5-247,5- 251,5-257,5-261,5-264,5-268,5-273-5-275,5-279,5-282,5-283,5-285,5¬286,5-288,5-291,5-294,5-295,5-301,5-306,5-307,5-309,5-310,5-312—5¬315,5-320,5-321,5-323,5-331-5-334,5-339,5-341,5-355-5-357,5-360-5¬362,5-374,5-375,5-378,5-387,5-389,5-390,5-397,5-398,5-412,5-433,5-440,6-017¬6-021,6-026,6-027,6-031,6-033—6-041,6-043—6-045,6-048,6-049,6-058,6¬059,6-063-6-066,6-074—6-076,7-002,7-003,7-005—7-009,8-002,11¬024,11-025,11-026. Test Example 4: Insecticidal test against oriental tea tortix [0257] A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 100 ppm. To the chemical solution was dipped leaves of cabbage for about 10 seconds,''and after air-drying, they were placed iri a laboratory dish, then 5-oriental tea tortix (Homona magnanima) in the stage of second instar larva per the dish were released therein, and the dish was covered with a lid and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 6 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. ¬As a result, the following compounds showed an insecticidal rate of 80°7o or more among the compounds tested. The compounds of the present invention: No.1-015,1-016,1-057,1-058,1-062,1-0 80,1-105,1-107,1-0122,1-123,1-125,1-127,1-153,1-156,1-189,1-207,1-214,1-215,2¬ 003,2-034,2-035,2-051,2-052,3-037,3-060,3-095,3-110,3-112,3-125,3-129,4-003,5¬ 001,5-003-5-005,5-008,5-009,5-012,5-013,5-022,5-029,5-037,5-040,5-041,5-045 —5-050,5-052,5-053,5-057—5-059,5-061—5-065,5-069—5-071,5-073,5-075,5-075( +),5-076,5-077,5-083,5-086-5-090,5-092-5-094,5-102,5-103,5-111,5-113,5-114,5 -117,5-119,5-121,5-122,5-138-5-142,5-147,5-148,5-151,5-156,5-160,5-161,5-165, 5-166,5-180,5-182,5-183,5-185,5-187,5-188,5-189(+),5-202,5-205,5-208,5-210-5¬212,5-214-5-216,5-218,5-219,5-219(+),5-220,5-221,5-223,5-226-5-228,5-230,5¬232-5-234,5-236,5-240-5-242,5-246,5-247,5-251,5-254,5-273-5-275,5-279,5-2 82,5-283,5-285,5-286,5-288,5-289,5-291,5-294,5-295,5-301,5-306,5-307,5-310,5-3 12,5-313,5-315,5-319,5-321,5-323,5-329,5-330,5-338,5-339,5-341,5-356,5-357,5-3 59,5-360,5-362,5-374,5-375,5-378,5-379,5-381,5-387-5-390,5-392,5-393,5-395— 5-399,5-401,5-412,5-418,5-419,5-430,5-433,5-434,5-441,6-001,6-003,6-017,6-018, 6-020,6-021,6-027,6-031,6-033—6-035,6-038—6-041,6-043,6-066,6-075,6-076,7-0 02-7-009,8-002,11-024,11-026. Test Example 5: Insecticidal test against corn earworm ^ [0258] A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 100 ppm. To the chemical solution was dipped leaves of cabbage for about 10 seconds, and after air-drying, they Vv'ere placed in a laboratory dish, then 1-corn earworm (Helicoverpa armigera) in the stage of second instar lan/a per the dish were released therein, and the dish was covered v^ith a lid and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 6 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with twelve districts. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention; No.1-066,1-153,1-156,1-207,1-214,1-2 15,2-034,2-035,2-042,2-055,3-027,3-030,3-032,3-086,3-095,3-109,3-110,3-112,5-0 08,5-009,5-022,5-040,5-046,5-047,5-049,5-050,5-052,5-053,5-057—5-059,5-061 — 5-063,5-065.5-068,5-070,5-071,5-075,5-075(+),5-076,5-077,5-083,5-086—5-1D89,5¬099-5-101,5-109,5-113,5-117,5-120-5-122,5-126,5-138,5-139,5-141,5-142,5-147 ,5-148,5J151,5-156,5-160,5-165,5-169,5-177,5-180,5-185,5-189(+),5-193,5-208,5-2 10-5-2i2,5-214~5-219,5-219(+),5-223,5-227,5-228,5-230,5-231,5-233,5-234,5-2 35,5-241,5-245,5-246,5-249,5-251,5-254,5-261,5-264,5-269,5-273-5-275,5-279,5¬284,5-286,5-291,5-294,5-295,5-306,5-307,5-309,5-310,5-312-5-315,5-319,5-323,5 -331—5-336,5-338,5-339,5-341,5-353-5-355,5-357,5-359,5-360,5-374,5-375,5-37 8-5-381,5-383,5-384,5-387,5-389,5-390,5-393,5-395,5-397-5-400,5-408-5-413, 5-415,5-420—5-424,5-427,5-433,5-434,5-440,5-443,5-446,5-452—5-454,6-003,6-0 04,6-016-6-019,6-021,6-023,6-024,6-026,6-027,6-031,6-033—6-041,6-043-6-04 5,6-048,6-049,6-056,6-066,6-074—6-076,6-078,6-079,6-080,6-080(+),6-080(-),6-08 3,6-084,7-002—7-009,8-002,11-024. Test Example 6: Insecticidal test against peach fruit moth [0259] A 10% emulsifiabie concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 100 ppm. To the chemical solution was dipped apple young fruits on which peach fruit moth (Carpociria sasakii) laid eggs (20-egg/fruit) for about 10 seconds, and after air-drying, they were placed in a laboratory dish, and the dish was covered with a lid and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 20 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention: No.5-049,5-050,5-070,5-076,5-083,5-0 88,5-111,5-148,5-219,5-219 (+y,'5-221,5-234,5-286,5-291,5-323,5-360,5-387,5-390,5 -398,6-027,6-039,7-008. Test Example 7: insecticidal test against Frankiinielia occidentaiis [0260] A wet filter paper was laid in a styrol cup having an inner diameter of 7 cm, a leaf of a common bean cut out so as to have the same diameter was laid theron, and 10-Frankiiniella occidentaiis with first instar larva per leaf was inoculated thereonr A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 500 ppm. The chemical solution was sprayed with a rotating spray-tower in an amount of 2.5 m! per styrol cup, and the styrol cups were covered with lids and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 2 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention: No.1-175,1-177~1-179,1-182,2-020,2¬022,2-028 * ,2-029* ,2-032,2-033,2-034 * ,2-035 * ,2-037* ,2-038 * ,2-039* ,2-040* ,2-04 1 * ,2-042* ,2-043* ,2-044* ,2-045* ,2-046* ,2-047,2-048* ,2-049* ,2-050—2-052,3-068 ,3-072*,3-080,3-084~3-086,3-090,3-093,3-105,3-107,3-109,3-110,3-112,3-114,3-1 22-3-125,3-132,3-i 35,3-136,4-004,4-006,5-OOi ,5-003,5-009,5-013,5-022,5-023,5¬029,5-037-5-041,5-044~5-053,5-057~5-075,5-075(+),5-076~5-078,5-081-5-08 9,5-090*,5-091-5-094,5-099-5-105,5-109,5-111-5-119,5-120*,5-121-5-123,5¬124*,5-126-5-128,5-129*,5-130,5-131*,5-134,5-137^5-142,5-143*,5-144,5-145, 5.146*,5-147,5-148,5-150,5-151,5-153*,5-154,5-156,5-158-5-160,5-161*,5-162,5 -164-5-166,5-167*,5-168*,5-169,5-171,5-172*,5-178-5-188,5-189(+),5-190(+),5¬191 -5-194,5-201,5-202,5^205-5-207,5-208* ,5-210-5-216,5-217* ,5-218,5-219,5 -219(+),5-219(-),5-220-5-234,5-236-5-242,5-244-5-247,5-249,5-251 -5-254,5-2 55*,5-256,5-257,5-258*,5-259-5-261,5-264,5-265,5-269*,5-270,5-271 * ,5-272-5-, 283,5-284-5-289,5-291,5-292,5-294,5-295,5-297,5-299,5-300,5-301,5-302*,5-303 ,5-306,5-307,5-309,5-310*,5-311-5-315,5-318,5-319,5-321-5-323,5-329-5-336, 5-338,5-339,5-341-5-346,5-348,5-349,5-353-5-358,5-360-5-362,5-374,5-375,5¬ 378,5-379*,5-380*,5-381*,5-383,5-384,5-385*,5-387~5-393,5-395,5-396*,5-397 —5-401,5-403-5-406,5-408-5-413,5-415,5-417-5-419,5-421,5-422i5-425,5-427, 5-430,5-432-5-434,5-439—5-443,5-445,5-446,5-449,5-452,5-453,6-001—6-003,6¬ 004*,6-005*,6-006*,6-007-6-6l3,6-015*,6-016-6-021,6-022*,6-023,6-024*,6-02 5*,6-026-6-050,6-054-6-056,6-058,6-059,6-063,6-066,6-070,6-071*,6-074-6-0 76,6-078-6-080,6-080(+),6-080(-),6-083-6-086,7-001,7-003—7-010,8-002,8-003, 10-002,10-005,11-024-11-026,11-043,11-045,11-054-11-056,11-059,11-070,11¬ 089,12-002. \ . ' In the interim, the indication of "*" shows that the insecticidai test was carried out by use of a chemical solution of a concentration of lOOppm. Test Example 8: Insecticidai test against Thrips palmi [0261] A wet filter paper was laid in a styrol cup having an inner diameter of 7 cm, a leaf of a common bean cut out so as to have the same diameter was laid theron, and 10-Thrips palmi in the stage of adult per leaf was inoculated thereon. A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 100 ppm. The chemical solution was sprayed with a rotating spray tower in an amount of 2.5 ml per styrol cup, and the styrol cups were covered with lids and contained at a thermostat chamber at 25°C. A number of dead insect(s) afte'r 2 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidai rate of 80% or more among the compounds tested. The compounds of the present invention: No.1-179,1-196,2-022,2-024—2-026,2¬ 028,2-029,2-033,2-035,2-039,2-044-2-048,2-050-2-052,3-079,3-085,3-086,3-091 ,3-110,3-112,3-124,3-131,3-148,4-003-4-005,4-010,5-001,5-003,5-006,5-008,5-01 2—5-015,5-022,5-023,5-029,5-036,5-037,5-040,5-045—5-053,5-057—5-063,5-065, 5-067,5-068,5-070-5-075,5-075(+),5-076-5-079,5-081-5-084,5-086-5-093,5-0 99,5-102-5-104,5-111-5-114,5-117-5-121,5-124,5-128-5-130,5-137-5-148,5¬151,5-153,5-156,5-160-5-162,5-165,5-166,5-179,5-180,5-182-5-186,5-188,5-189 (+),5-193,5-202,5-205,5-206,5-208-5-210,5-214-5-216,5-218,5-219,5-219(+),5-2 20,5-224-5-226,5-228~5-230,5-232~5-234,5-236,5-238,5-239,5-242,5-246,5-24 7,5-251,5-256-5-258,5-261,5-264,5-269,5-273-5-276,5-278,5-279,5-280,5-282,5¬ 283,5-285,5-286,5-288,5-289,5-291,5-294,5-295,5-299,5-303,5-306,5-309,5-310,5¬ 312-5-314,5-319,5-322,5-323,5-329,5-330,5-332,5-334,5-335,5-338,5-339,5-346,5 -349,5-353-5-362,5-374,5-375,5-378-5-381,5-383-5-385,5-387,5-389,5-390,5-3 95-5-401,5-408-5-413,5-415,5-418—5-424,5-427,5-430,5-432-5-434,5-439-5¬'443,5-446,5-452-5-454,6-001,6-003—6-008,6-015,6-017-6-024,6-026-6-035,6¬037-6-041,6-043-6-045,6-047-6-049,6-054-6-056,6-058,6-059,6-063,6-066,6¬070,6-073-6-076,6-078-6-080,6-080(+),6-080{-),6-083,6-084,7-003-,7-005—7-00¬9,8-002,10-002,11-025,11-026,11-054,11-056,11-059,12-002. Test Example 9: Insecticidal test against Eysarcoris lewisi [0262] A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 500 ppm. To the chemical solution was dipped leave sheaths of rice for about 10 seconds, and after air-drying, they were placed in a test tube, then 5-Eysarcoris lewisi in the stage of first instar larva per the test tube were released therein, and the test tube was covered with a sponge and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 2 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention: No.1-015,1-050,1-051,1-175,1-209,2-0 29,2-034,2-035,2-042,2-044-2-052,2-054,2-055,3-047,3-068,3-070-3-072,3-086, 3-090,3-093,3-106,3-109-3-112,3-114,3-125,3-131,5-001,5-003,5-005,5-008,5-00 9,5-013-5-015,5-017,5-022,5-023,5-026,5-029,5-037-5-041,5-045-5-053,5-058 -5-065,5-067-5-069,5-071-5-075,5-075(+),5-076-5-078,5-081,5-083,5-084-5¬094,5-099-5-105,5-111 -5-114,5-116-5-122,5-124,5-126,5-128,5-130,5-134,5-1 37-5-142,5-144,5-145,5-147,5-148,5-150,5-151,5-154,5-156,5-158-5-162,5-165, 5-166,5-168,5-169,5-171,5-173,5-174,5-179—5-189,5-189(+),5-191,5-195—5-197, 5-203,5-205,5-206,5-208-5-210,5-212-5-216,5-218,5-219,5-219(+),5-220-5-230 ,5-232,5-233,5-235,5-236,5-238-5-247,5-249,5-251,5-254,5-256-5-262,5-264,5-2 65,5-273-5-279,5-283,5-285,5-286,5-288,5-289,5-291,5-294,5-295,5-299-5-301, 5-304-5-310,5-312-5-315,5-318-5-321,5-323,5-329,5-330,5-332,5-334,5-335,5¬338,5-339,5-341-5-344,5-346,5-348,5-353-5-360,5-362,5-374—5-387,5-389,5-3 90,5-392,5-393,5-395-5-401,5-403-5-405,5-408-5-413,5-415,5-417-5-419,5-4 21,5-422,5-427,5-431 —5-434,5-440,5-443,5-445,5-446,5-448,5-452,5-453,6-001,6¬006—6-013,6-015—6-024,6-026—6-029,6-031—6-051,6-054—6-056,6-058—6-060 ,6-062—6-067,6-070,6-071,6-074—6-076,6-078,6-079,6-080,6-080(+),6-080(-),6-08 •3—6-086,7-002—7-010,11-060. Test Example 10: Insecticidal test against brown rice pianthopper [0263] A 10% emulsifiable concentrate (depending on the compounds, 10% wettabie powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 500 ppm. To the chemical solution was dipped leave sheaths of rice for about 10 seconds, and after air-drying, they were placed in a test tube, then 5-brown rice pianthopper (Nilaparvata lugens) in the second instar larva per the test tube were released therein, and the test tube was covered with a sponge and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 6 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of^the present invention: No.1-005—1-007,1-017,1-061,1-154,1¬ 175,1 -185,1 -188,1 -189,2-018,2-020,2-025-2-027,2-029,2-033,2-034,2-036,2-044,2 -046,2-051,2-052,2-054,3-013,3-068,3-070,3-072,3-075,3-109,3-112,3-125,5-001,5¬003,5-009,5-013,5-015,5-023,5-029,5-040,5-041,5-049,5-05P;5-053,5-058,5-060,5¬061,5-063,5-065-5-068,5-070—5-074,5-075(+),5-076,5-077,5-080,5-081,5-083,5¬084,5-086-5-088,5-090-5-094,5-099,5-102,5-106,5-111,5-113,5-117-5-120,5-1 30,5-138—5-148,5-151—5-156,5-160,5-161,5-163,5-170,5-173,5-174,5-182,5-186, 5-189,5-189(+),5-195,5-197,5-203,5-205,5-208,5-210,5-212,5-214,5-216,5-219,5-2 19(+),5-220,5-226,5-230-5-232,5-234-5-236,5-239,5-240,5-242,5-243,5-245,5-2 46,5-251,5-254,5-257,5-258,5-261,5-262,5-264,5-265,5-273-5-275,5-279,5-280,5¬285,5-286,5-288,5-294,5-295,5-305—5-310,5-313,5-315,5-323,5-330,5-335,5-339,5 -341,5-344,5-353-5-360,5-374-5-377,5-379-5-388,5-390,5-392,5-393,5-396,5-3 98-5-401,5-405,5-410,5-412,5-413,5-419,5-421,5-422,5-427,5-432,5-433,5-440,5¬453,6-001,6-003,6-007,6-015~6-023,6-027~6-045,6-048~6-050,6-056,6-058~6¬065,6-076,6-078,6-079,6-080,6-080(+),6-080(-),6-083,6-086,7-001—7-004,7-006,7¬008,7-009,8-003,9-009,11-039,11-041,11-054. Test Example 11: Insecticidal test against Bemisia argentifolii [0264] A wet filter paper was laid in a styrol cup having an inner diameter of 7 cm, a leaf of a tomato cut out on which Bemisia argentifolii laid eggs (10-egg/leaf) was laid theron. A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention ¬was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 500 ppm. The chemical solution was sprayed with a rotating spray tower in an amount of 2.5 ml per styrol cup, and the styrol cups were covered with lids and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 6 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention: No.1-011,1-182,2-024*,2-025*,2-026 *,2-028*,2-029*,2-033,2-034*,2-035*,2-037*,2-044*,2-047,2-050,2-051,3¬068,3-079,3-090,3-112,3-125,4-003,4-006,5-001,5-003,5-005,5-007,5-009,5¬011,5-013-5-015,5-021 -5-023,5-029,5-035,5-037-5-041,5-045-5-053,5-057¬ 5-061,5-063,5-065,5-067-5-075,5-075(+),5-076~5-078,5-079*,5-081,5-084¬ 5-089,5-090* ,5-091 -5-094,5-099—5-104,5-112-5-114,5-117,5-118,5-120 *,5-122,5-123,5-126,5-128,5-130,5-137-5-142,5-143*,5-144,5-145,5-146 *,5-148,5-151,5-153*,5-154,5-156,5-158-5-160,5-161*,5-162,5-164,5-165,5-167 * ,5-171,5-180,5-182-5-188,5-189(+),5-191,5-193,5-201,5-202,5-205-5¬207,5-208*,5-209-5-216,5-218,5-219,5-219(+),5-220-5-223,5-225-5¬234,5-236,5-238-5-242,5-245-5-247,5-249,5-254,5-2"58*,5-261,5-264,5-273¬5-275,5-277-5-279,5-281,5-285-5-288,5-291,5-292,5-294,5-295,5-297,5¬299,5-301,5-306,5-309,5-310*,5-312-5-315,5-318,5-319,5-321,5-323,5¬330,5-332,5-335,5-339,5-341,5-344,5-345,5-353—5-358,5-359*,5-360,5¬362,5-374,5-375,5-378,5-379*,5-380*,5-381 *,5-383,5-384,5-385*,5-387-5¬393,5-396*,5-397-5-401,5-405,5-409,5-410,5-412,5-417,5-418,5-421,5¬ 422,5-427,5-430,5-433,5-434,5-440,5-446,5-453,6-001,6-003,6-009,6-011 ¬385 6-013,6-016-6-018,6-020,6-021,6-022* ,6-027,6-028,6-031 -6-041,6-043,6¬044,6-048-6-050,6-056,6-074—6-076,6-078,6-079,6-083,7-001,7-003—7¬006,7-008-7-010,11-017,11-024,11-026,11-028,11-056. in the interim, the indication of "*" shows that the insecticidal test was carried out by use of a chemical solution of a concentration of lOOppm. Test Example 12: Insecticidal test against green peach aphid , [0265] A wet cotton wool was laid in a laboratory dish having an inner diameter of 3 cm, a leaf of a cabbage cut out so as to have the same diameter was- laid theron, ¬and 4-green peach aphid (Myzus persicae) in the stage of no-wing adult was left. After 1 day, a 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 500 ppm, and the chemical solution was sprayed with a rotating spray tower (2.5 mg/cm^), and the laboratory dish was covered with lids and contained at a thermostat chamber at 25°C. A number of dead in'sect(s) after 6 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention: No.1-006,1-063,1-067,1-069,1-153,1¬158,1-163,1-166,1-1,67,1-171,1-175,1-207,1-209,1-215,2-005,2-015,2-017,2-024* ,2-025*,2-026*,2-027,2-029*,2-034*,2-044*,2-046*,2-050,2-051,3-006,3-029,3¬064,3-068,3-089,3-110,3-114,3-125,3-131,3-139,3-143,4-003,5-001,5-003,5-005,5¬009,5-013,5-015,5-022,5-023,5-037-5-041,5-045-5-050,5-p52,5-053,5-056,5-058 -5-061,5-063,5-065-5-068,5-070-5-075,5-075(+),5-076,5-077,5-079*,5-081,5¬083-5-086,5-090*,5-091-5-094,5-099,5-100,5-102,5-103,5-113,5-117,5-118,5¬128,5-130,5-134,5-138-5-142,5-143*,5-144,5-145,5-l46*,5-147,5-148,5-151,5¬153*,5-154,5-156,5-158,5-160,5-161*,5-162,5-165,5-180-5-187,5-189(+),5-193,5¬ 202,5-205,5-209,5-210,5-212,5-214-5-216,5-219,5-219(+),5-220-5-223,5-226,5¬228,5-230,5-231,5-233,5-234,5-236,5-238,5-240,5-242,5-243*,5-245—5-247,5¬251,5-254,5-256,5-258*,5-259,5-261,5-264,5-272-5-275,5-277-5-280,5-282,5¬284-5-288,5-291,5-294,5-295,5-300,5-301,5-306,5-307,5-309,5-310*,5-313-5¬315,5-320,5-321,5-323,5-330,5-334,5-335,5-339,5-341,5-343,5-344,5-348,5-352,5¬ 353-5-358,5-359*,5-360,5-362,5-364,5-374,5-375,5-378,5-379*,5-380*,5-383,5¬ 384,5-385* ,5-387,5-389,5-390,5-392,5-393,5-398,5-399,5-401,5-409,5-410,5¬ 415,5-418,5-421,5-422,5-427,5-433,5-434,5-440-5-442,5-446,5-453,6-001,6¬ 003,6-005*,6-007,6-009—6-012,6-015*,6-016—6-021,6-022*,6-027,6-028,6-030— 6-033,6-035—6-044,6-048—6-050,6-054,6-056—6-059,6-063,6-066,6-074—6¬ 076,6-078—6-080,6-083,6-084,6-086,7-003-7-007,7-009,9-004,10-002,11-005,11¬ •006,11-026,12-004. In the interim, the indication of "*" shows that the insecticidai test was carried out by use of a chemical solution of a concentration of lOOppm. _ Test Example 13: Insecticidai test against Japanese mealybug [0266] A wet filter paper was laid in a styrol cup having an inner diameter of 7 cm, a le^af of a common bean cut out so as to have the same diameter was laid theron, and 10-Japanese mealybug (Planococcus kraunhiae) in the first instar larva per leaf was inoculated thereon. A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 500 ppm. The chemical solution was sprayed with a rotating spray tower in an amount of 2.5 ml per styrol cup, and the styrol cups were covered with lids and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 6 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidai rate of 80% or more among the compounds tested. The compounds of the present invention: No.1-011,1-177,1-ia2,2-020,2-028*,2-029 * ,2-033,2-034* ,2-035* ,2-037* ,2-039* ,2-040* ,2-041 * ,2-042* ,2-044* ,2-045* ,2-046 *,2-047,2-048*,2-049*,2-050-2-052,2-055*,3-065,3-069,3-085,3-086,3-091-3¬093,3-104,3-109,3-125,4-003,4-004,4-006,5-001,5-003,-5-005,5-007,5-009,5-013¬5-015,5-017,5-022,5-023,5-029,5-037,5-039-5-041,5-045-5-050,5-052,5-053,5¬057-5-061,5-063-5-065,5-067-5-075,5-075(+),5-076'^5-078,5-081,5-083-5¬089,5-090*,5-091-5-094,5-098-5-105,5-109,5-111-5-114,5-116—5-118,5¬121,5-123,5-126,5-128,5-129*,5-130,5-131 *,5-138-5-142,5-143*,5-144,5-145,5¬146*,5-147,5-148,5-151,5-153*,5-154,5-156,5-158-5-160,5-161*,5-162,5-164,5¬165,5-166,5-167*,5-168*,5-171,5-172*,5-179-5-188,5-189(+),5-190(+),5-192-5¬ 194,5-201,5-202,5-205,5-206,5-208*,5-210~5-212,5-214'-'5-216,5-219,5¬219(+),5-221,5-222,5-223,5-226-5-234,5-236-5-240,5-242,5-245-5-247,5¬249,5-251,5-253,5-254,5-255*,'5-256,5-257,5-258*,5-259,5-261,5-264,5-269*,5¬271*,5-272—5-288,5-291,5-292,5-295—5-297,5-299-5-301,5-302*,5-303,5¬306,5-307,5-309,5-310* ,5-312-5-315,5-318,5-319,5-321,5-322,5-323,5-331,5¬332,5-334-5-336,5-338,5-339,5-344,5-345,5-348,5-349,5-353-5-358,5-360-5¬ •362,5-375,5-378,5-379*,5-380*,5-381 *,5-383,5-384,5-385*,5-387,5-388,5-390,5¬392,5-393,5-395,5-396*,5-397-5-399,5-401,5-406,5-407,5-410,5-412,5-417-5¬419,5-422,5-427,5-430—5-434,5-439—5-443,5-445,5-446,5-452,5-453,6-001 —6-¬003,6-005*,6-006*,6-007—6-013,6-015*,6-016-6-021,6-022*,6-023,6-024*,6-025 *,6-026-6-050,6-054-6-056,6-058,6-059,6-063,6-066,6-074—6-076,6-078—6¬080,6-080(+),6-083—6-085,7-003—7-010,8-003,9-003,10-002,11-024—11-026,11¬043.,11-045,11-056,11-058,11-059,11-089,12-006. In the interim, the indication of "*" shows that the insecticidal test was carried out by use of a chemical solution of a concentration of lOOppm. Test Example 14: Insecticidal test against cucurbit leaf beetle [0267] A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 500 ppm. To the chemical solution was dipped leaves of cucumber for about 10 seconds, and after air-drying, they were placed in a laboratory dish, then 5-cucurbit leaf beetle (Aulacophora femoralis) in the stage of second instar larva per the dish were released therein, and the dish was covered with a lid and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 6 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention: No.1-005,1-015,1-016,1-040,1-042,1-055 -1-057,1-059,1-061-1-067,1-069-1-071,1-073,1-074,1-076,1-077,1-079—1¬081,1-083—1-085,1-087,1-088,1-090,1-092—1-095,1-098,1-099,1-102,1-104—1¬110,1-113,1-116,1-118,1-119,1-122-1-129,1-131,1-135,1-136,1-138,1-146,1¬147,1-151-1-153,1-155-1-157,1-159,1-166,1-167,1-171,1-172,1-174-1-177,1¬ 179'-1-185,1-187'-1-189,1-194,1-199,1-206,1-207,1-210,1-212,1-214,1-215,1¬220,1-225,2-001,2-004,2-006,2-011,2-013,2-019~2-022,2-025~2-029,2-031,2¬032,2-034—2-055,3-002,3-003'i3-006,3-011,3-018,3-025—3-028,3-031—3-035,3¬037,3-044,3-046,3-047,3-050,3-058,3-061—3-065,3-068-3-072,3-074,3-076,3-078 -3-081,3-084-3-087,3-089^3-095,3-097-3-116,3-118-3-125,3-127—3-132,3¬134-3-136,3-138-3-143,3-145-3-148,4-003-4-007,4-009-4-011,5-001-5¬ • 015,5-017,5-021-5-023,5-028-5-042,5-044-5-075,5-075(+),5-075(-),5-076-5¬081,5-083-5-095,5-097,5-099-5-107,5-109-5-130,5-132-5-135,5-137—5¬156,5-158-5-189,5-189(+),5-190(+),5-191 -5-219,5-219(+),5-219(-),5-220-5¬236,5-238-5-296,5-298—5-326,5-329-5-339,5-341-5-350,5-352-5-363,5¬365,5-369,5-371,5-374—5-403,5-405-5-413,5-415-5-419,5-421,5-422,5-425,5¬427,5-430-5-434,5-436,5-439—5-447,5-449,5-452,5-453,6-001—6-013,6-015-6¬02^,6-026—6-051,6-053—6-067,6-070,6-071,6-074-6-076,6-078—6-080,6¬08d(+),6-080(-),6-083—6-086,7-001—7-010,8-001—8-004,9-003,9-009,10-002— 10-005,11-005,11-015,11-017,11-020,11-023-11-026,11-038,11-043,11-045,11¬046,11-052-11-054,11-056-11-060,11-066,11-067,11-072,11-076,12-006. Test Example 15: Insecticidal test against serpentine leaf miner [0268] A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 500 ppm. To the chemical solution was dipped leaves of common bean on which serpentine leaf miner (Liriomyza trifolii) laid eggs (10 eggs/leaf) for about 10 seconds, and after air-drying, they were placed on a wet filter paper laid in a styrol cup having an inner diameter of 7 cm, and the styrol cup was covered with a lid and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 6 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention: No.1-175,1-177,2-029*,2-034*,2-035*,2¬044*,2-045*,2-050,2-051,3-060,3-068,3-069,3-071,3-072*,3-085,3-086,3-093,3¬105,3-109,3-112,3-125,3-148,5-001,5-003,5-005,5-007,5-009,5-015,5-022,5-023,5¬036,5-037,5-040,5-041,5-045—5-053,5-058-5-061,5-063-5-065,5-067,5-068,5¬ 070~5-075,5-075(+),5-076,5-077,5-081,5-083,5-085~5-089,5-090*,5-091~5¬094,5-099-5-105,5-113,5-117-5-119,5-120*,5-121~5-123,5-124*,5-126,5-129* ,5-131 *,5-133*,5-138-5-142,5-144,5-145,5-147,5-148,5-150,5-151,5-154,5-156,5¬158,5-160,5-151",5-162,5-16^-5-166,5-168*,5-169,5-171,5-172*,5-178,5-180,5¬182-5-188,5-189(+),5-201,5-202,5-208*,5-209,5-210,5-212,5-214-5-216,5-217* ,5-219,5-219(+),5-221 -5-223,5-226-5-234,5-236,5-238,5-239,5-241,5-245—5¬ •247,5-251,5-256,5-257,5-258*,5-259,5-261,5-264,5-265,5-270,5-274,5-275,5¬283,5-284,5-286,5-291,5-294,5-295,5-302*,5-303,5-306,5-309,5-310*,5-313-5¬315,5-319,5-323,5-335,5-336,5-338,5-339,5-341,5-344,5-345,5-353--5-358,5¬360,5-362,5-374,5-375,5-378,5-379*,5-380*,5-381 *,5-383,5-384,5-385*,5-387,5¬388,5-390,5-392,5-393,5-395,5-396*,5-397—5-401,5-408—5-413,5-415,5-417-5¬419,5-421,5-422,5-425,5-427,5-430,5-432,5-433,5-439-5-441,5-443,5-445,5¬446,5-452,5-453,6-001,6-004*,6-005*,6-006*,6-007,6-008,6-011 —6-013,6-015*,6- . 016-6-021,6-022*,6-024*,6-025*,6-027,6-031,6-033-6-041,6-043,6-044,6-048— 6-050,6-054-6-056,6-066,6-070,6-074—6-076,6-078,6-079,6-083,6-085,7-003,7¬005-7-009. In the interim, the indication of "*" shows that the insecticidai test was carried out by use of a chemical solution of a concentration of lOOppm. Test Example 16: Insecticidai test against two-spotted spider mite [0269] A wet filter paper was laid in a styrol cup having an inner diameter of 7 cm, a leaf of a common bean cut out so as to have the same diameter was laid theron, and 10 larvae of two-spotted spider mite (Tetranychus urticae) per leaf was inoculated thereon. A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 500 ppm. The chemical solution was sprayed with a rotating spray tower in an amount of 2.5 ml per styrol cup, and the styrol cups were covered with lids and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 6 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidai rate of 80% or more among the compounds tested. The compounds of the present invention: No.1-177,1-182,2-027,2-028*,2-029*,2¬ 034*,2-035*,2-036,2-037*,2-039*,2-040*,2-041*,2-042*,2-044*,2-045*,2-046*,2¬047,2-048*,2-049*,2-050—2-052,3-068,3-084,3-086,3-109,3-110,3-112,3-114,3¬124,3-131,5-001,5-003,5-005,5'-007—5-009,5-011,5-013,5-015,5-019,5-021,5¬022,5-023,5-028,5-029,5-035~5-037,5-040,5-041,5-045~5-053,5-057'-'5-075,5¬O75(+),5-O76~5-O78,5-O8O'-^5-089,5-O9O*,5-091-5-094,5-098—5-105,5-109,5¬112-5-114,5-117-5-119,5-121-5-123,5-126,5-128,5-129*,5-130,5^132,5-134,5¬136-5-142,5-143*,5-144,5-145,5-146*,5-147,5-148,5-150-5-152,5-153*,5-154¬5-156,5-158-5-160,5-161 *,5-162~5-166,5-167*,5-168*,5-171,5-172*,5-177-5¬180,5-182-5-188,5-189*,5-189(+),5-190(+),5-191,5-192,5-196*,5-19J*,5-199-5-, 202,5-204-5-207,5-208*,5-209—5-212,5-214-5-216,5-218,5-219,5-219(+),5¬219(-),5-220-5-234,5-235*,5-236,5-238-5-242,5-243*,5-245-5-247,5-249,5¬251,5-254,5-255*,5-256,5-257,5-258*,5-259,5-261,5-264,5-265,5-269*,5-271 *,5¬27:^-5-275,5-277-5-279i5-283-5-286,5-288,5-291,5-292,5-294,5-295,5-299-5-., 301,5-306,5-307,5-312-5-316,5-321,5-323,5-325,5-330,5-336,5-338,5-339,5¬341,5-344,5-345,5-349,5-353-5-358,5-360,5-362,5-374,5-375,5-376*,5-377*,5¬378,5-379*,5-380*,5-381 *,5-383,5-384,5-385*,5-386*,5-387—5-395,5-396*,5-397 -5-399,5-401,5-402,5-405,5-406,5-408-5-413,5-415,5-417-5-419,5-421,5-, 422,5-425,5-427,5-430,5-432,5-433,5-440,5-441,5-443,5-445,5-452,5-453,6-001,6¬003,6-007,6-008,6-011—6-013,6-015*,6-016—6-021,6-023,6-027,6-030—6-044,6¬046-6-050,6-054-6-056,6-066,6-074—6-076,6-078,6-079,6-083—6-085,7-003— 7-010,8-003,10-002,11-026,12-002. In the interim, tine indication of "*" shows that the insecticidal test was carried out by use of a chemical solution of a concentration of 10Oppm. Test Example 17: Insecticidal test against pink citrus rust mite [0270] A wet filter paper was laid in a styrol cup having an inner diameter of 7 cm, a leaf of a mandarin orange cut out so as to have the same diameter was laid theron, and 10 larvae of pink citrus rust mite (Aculops pelekassi) per leaf was inoculated thereon. A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 100 ppm. The chemical solution Was sprayed with a rotating spray tower in an amount of 2.5 ml per styrol cup, and the styrol cups were covered with lids and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 6 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentaliy, the test was carried out with two districts. As a result, the following compounds showed an insecticidai rate of 80% or more among the compounds tested. The compounds of the present invention: No.1-177,3-093,3-112,5-001—5-003,5¬005,5-008,5-009,5-022,5-023,5-036,5-037,5-040,5-041,5-046,5-047;5-049,5-050,5¬ • 053,5-057-5-059,5-061,5-063,5-065,5-066,5-069—5-071,5-074—5-077,5-081,5¬083,5-084,5-086,5-088,5-111-5-113,5-121,5-137-5-140,5-148,5-151,5-174,5¬182,5-183,5-185,5-187,5-188,5-202,5-205,5-206,5-215,5-216,5-219--5-221,5¬225,5-226,5-233-5-235,5-241,5-247,5-274,5-285,5-291,5-294,5-295,5^-301,5¬313,5-323,5-331,5-334,5-338,5-339,5-355,5-360,5-374,5-378,5-387-5-390,5¬393,5-397,5-398,6-003,6-017,6-020,6-021,6-027,6-031,6-033—6-035,6-043,6¬049^,6-054,6-064,6-070,6-076,7-003,7-007-7-009,10-002. Test Example 18: Insecticidai test against broad mite [0271] A wet filter paper was laid in a styrol cup having an inner diameter of 7 cm, a leaf of a common bean cut out so as to have the same diameter was laid theron, and 10 adults of broad mite (Polyphagotarsonemus latus) per leaf was inoculated thereon. A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution with a concentration of 100 ppm. The chemical solution was sprayed with a rotating spray tower in an amount of 2.5 ml per styrol cup, and the styrol cups were covered with lids and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 2 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidai rate of 80% or more among the compounds tested. The compounds of the present invention: No.3-093,5-009,5-036,5-037,5-040,5¬041,5-050,5-053,5-058,5-063,5-067,5-071,5-075-5-077,5-083,5-088,5-089,5¬113,5-121,5-140,5-147,5-148,5-151,5-174,5-179,5-185,5-188,5-214,5-215,5-219,5¬230,5-233-5-236,5-249,5-251,5-254,5-274,5-288,5-289,5-291,5-294,5-309,5¬ 332,5-339,5-355,5-360,5-374,5-375,5-387,5-398,6-017,6-026,6-031,6-033-6¬035,6-038,6-045,6-064,6-070,6-076,7-003,7-007—7-009. Test Example 19: Insecticidal test against Ctenocephalides felis [0272] Al^er 400 ^\ of acetone solution in which 4 mg of the compound of the present invention was dissolved in 40 ml of acetone (concentration 100 ppm) was coated on the bottom face arid side face of a laboratory dish having an inner diameter of 5.3 cm, acetone was vaporized to prepare a thin film of the compound of the present invention on the inner wall of the laboratory dish. As the surface area of the inner wall is 40 cm^, the treated dosage is 1 (ig/cml 10 adults of Ctenocephalides felis (male and female are mixed) were left in the laboratory dish, , covered with lid and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 4 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with one district. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention: No.2-029*,2-052,5-002,5-003,5-005,5¬ 007,5-008,5-012,5-013,5-023,5-029,5-037,5-058,5-071 *,5-072,5-075*,5-076*,5¬077,5-086,5-088*,5-093*,5-100*,5-.101*,5-111 *,5-117,5-121,5-130*,5-138,5¬139,5-140*,5-142*,5-148*,5-160*,5-161*,5-165*,5-182*,5-184,5-187,5-188,5¬192,5-205,5-206,5-209,5-214*,5-218,5-219*,5-223,5-229,5-230,5-232,5-234*,5¬235*,5-236,5-238,5-240,5-241 *,5-243*,5-245*,5-247,5-264,5-274,5-287,5-291,5¬294,5-312,5-313,5-323,5-354*,5-356*,5-359*,5-360,5-362,5-378*,5-379*,5-383* ,5-384*,5-387*,5-389*,5-390,5-393,6-020,6-026,6-033,6-034*,6-035*,6-043*,6¬046~6-049,6-054,6-055,6-074,7-002*,7-004,7-008,7-009. In the interim, the indication of "*" shows that the insecticidal test wascarried out with a treated dosage of 0.1 f.ig/cm^. Test Example 20: Insecticidal test against American dog tick [0273] After 400 )j,l of acetone solution in which 4 mg of the compound of the present invention was dissolved in 40 ml of acetone (concentration 100 ppm) was coated on the bottom face and side face of two laboratory dishes having an inner diameter of 5.3 cm, acetone was vaporized to prepare a thin fil.m of the compound of the present invention on the inner wall of the laboratory dish. As the surface area of the inner wall is 40 cm^ the treated dosage is 1 |ig/cml 10-American dog tick (Dermacentor variabilis) (male and female are mixed) in the stage of protonymph were left in the laboratory dishes, two laboratory dishes together were sealed with a tape so that ticks do not escape, and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 4 days was counted and a rate of dead insects was calculated by the calculation'equation similar to that in Test Example 1. Incidentally, the test was carried out with one district. As a result, the following compounds showed an insecticidal rate of 80% or more • among the compounds tested. The compounds of the present invention: No.2-029*,2-052,5-003,5-005,5-008,5¬023,5-029,5-037,5-058,5-063*,5-071 *,5-072,5-075*,5-076*,5-077,5-Q86,5-088*,5-. 093*,5-100*,5-101*,5-117,5-121,5-128,5-130*,5-138,5-139,5-140*,5-142*,5-148* ,5-160*,5-161 *,5-165*,5-182*,5-184,5-187,5-188,5-191,5-192,5-205,5-206,5¬209,5-214*,5-219*,5-223,5-229,5-230,5-232,5-233*,5-234*,5-235*,5-236,5-238,5¬24Q,5-241*,5-243*,5-245*,5-247,5-264,5-274,5-287,5-291,5-294,5-312,5-313,5¬320,5-321,5-323,5-354*,5-356*,5-359*,5-360,5-362,5-378*,5-379*,5-383*,5-384* ,5-386*,5-387*,5-390,5-393,6-020,6-026,6-033,6-034*,6-035*,6-043*,6-046~6¬049,6-054,6-055,6-074,7-004,7-008,7-009,11-056. In the interim, the indication of "*" shows that the insecticidal test was carried out with a treated dosage of 0.1 ^ig/cm^. Test Example 21: Insecticidal test against German cockroach [0274] A chemical solution having a concentration of 10 |ig/;J was prepared by diluting the compound of the present invention with acetone. The chemical solution was coated on the abdominal region of male adults of German cockroach (Blattella germanica) in an amount of 1 ii\ per cockroach, and the treated cockroaches were contained at a thermostat chamber at 25°C. A number of dead (nsect(s) after 2 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with five districts. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention: No. 5-075. Test Example 22: Insecticidal test against Musca domestica [0275] A chemical solution having a concentration of 1 ug/^l was prepared by diluting the compound of the present invention with acetone. The chemical solution was coated on the abdominal region of female adults of Musca domestica in an amount of 1 ul per fly, and the treated flies were contained at a thermostat chamber at 25°C. A number of dead insect(s) after 2 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with ten districts. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention: No. 5-234. Test Example 23: Insecticidal test against Eastern subterranean termite [0276] A 10% emulsifiable concentrate (depending on the compounds, 10% wettable powder was applied for the test) of the compound of the present invention was diluted with water containing a spreading agent to prepare a chemical solution . with a concentration of 10 ppm. 0.5 ml of the chemical solution was added dropwise in 10 g of sand and mixed. A filter paper and the sand treated with the chemical solution were placed in a laboratory dish in which 1% agar was laid. 10-Eastern subterranean termite (Reticulitermes flavipes) per dish was left and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 2 days was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention: No. 5-234. Test Example 24: Insecticidal test against rust-red flour beetle [0277] A chemical solution having a concentration of 0.1 mg/ml was prepared by diluting the compound of the present invention with' acetone. After 10 ml of the chemical solution was added dropwise in 10 g of bran, 20 adults of rust-red flour beetle (Tribolium castaneum) were left therein, and contained at a thermostat chamber at 25°C. A number of dead insect(s) after 2 months was counted and a rate of dead insects was calculated by the calculation equation similar to that in Test Example 1. Incidentally, the test was carried out with two districts. As a result, the following compounds showed an insecticidal rate of 80% or more among the compounds tested. The compounds of the present invention: No. 5-234. industrial Appiicablity [0278] The isoxazoline-substituted benzanilide compounds according to the present invention are extremely useful compounds showing an excellent pesticidal activity, particularly an insecticidal and acaricidai activity, and causing little adverse effect against non-targeted beings such as mammals, fishes and useful insects. We Claim: 1. Substituted alkenylbenzene compound of fon Formula(4): wherein X1 is halogen atom, -SF5, C1-C6haloa!kyi, hydroxy C1-C5haloalkyl, C1-C8alkoxy C1¬ C6haloalkyl, C.1-C6haloalkoxy C1-C6ha!oalkyi, C3-C8halocycloalkyt, C1-C6haioalkoxy, C1-C3haloalkoxy C1-C3haloaikoxy, C1-C6haloaikyithio,C1-C6haloaIkylsulfinyi or C1¬ C6haloaIkyisulfonyl, X3 is hydrogen atom, halogen atom, cyano, nitro, C1-C6alkyl, C1-C6haloalkyt, -OR5, -OSO2R5 or -S(O)rR5, X4 is hydrogen atom, halogen atom, cyano, nitro, C1-C6alkl, -OH, C1-C6alkoxy or C1-C6haloalkoxy, R3 is C1-C6alkyl that is arbitrarily substituted with two or more arbitrarily halogen atoms, or C3-C6halocycioalkyl with a proviso that in case where X1 is fluorine atom, chlorine atom or -CF3 and both X3 and X4 are hydrogen atom, in case where both X1 and X3 are fluorine atom, and X4 is hydrogen atom, and in case where both X1 and X3 are -CF3, and X4 is hydrogen atom, R3 is -CHF2, -CHFCl, -CHFBr, -CHCJ2, -CF2CI, -CF2Br, -CF2l, -CFCI2, -CFCIBr, -CFBr2, -CCI3, C2-C6haloalkyl or C3-CBhaIocycioalkyl, R6 is C1-C6alkyl or C1-C6haloalkyI, r is an integer of O to 2.