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“Benzazoles, Benzoxazole, Benzthiazole And Benzimidazole Derivatives

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Patent Information

Application #
Filing Date
20 May 2005
Publication Number
0
Publication Type
INA
Invention Field
GENERAL ENGINEERING
Status
Email
remfry-sagar@remfry.com
Parent Application
Patent Number
Legal Status
Grant Date
2008-01-21
Renewal Date

Applicants

SYNGENTA LIMITED
EUROPEAN REGIONAL CENTRE, PRIESTLEY ROAD, SURREY RESEARCG PARK, GUILDFOR, SURREY GU2 7YH, ENGLAND

Inventors

1. CHRISTOPHER JOHN MATHEWS
C/O JEALOTTS HILL INTERNATIONAL RESEARCH CENTRE, BRACKNELL, BERKSHIRE RG42 6ET, UNITED KINGDOM
2. PATRICIA SUSAN BARNETT
c/o Jealotts Hill International Research Centre, Bracknell, Berkshire RG42 6ET
3. STEPHEN CHROSTPHER SMITH
c/o Jealotts Hill International Research Centre, Bracknell, Berkshire RG42 6ET
4. NIGEL JOHN BAENES
c/o Jealotts Hill International Research Centre, Bracknell, Berkshire RG42 6ET
5. WILLIAM GUY WHITTINGHAM
c/o Jealotts Hill International Research Centre, Bracknell, Berkshire RG42 6ET
6. JOHN WILLIAMS
c/o Jealotts Hill International Research Centre, Bracknell, Berkshire RG42 6ET
7. BRIAM LESLIE PILKINGTON
c/o Jealotts Hill International Research Centre, Bracknell, Berkshire RG42 6ET
8. ERIC DANIEL CLARKE
c/o Jealotts Hill International Research Centre, Bracknell, Berkshire RG42 6ET
9. ALAN JOHM WHITTLE
c/o Jealotts Hill International Research Centre, Bracknell, Berkshire RG42 6ET
10. DAVID JOHN HUGHES
c/o Jealotts Hill International Research Centre, Bracknell, Berkshire RG42 6ET
11. SARAH ARMSTRONG
c/o Jealotts Hill International Research Centre, Bracknell, Berkshire RG42 6ET
12. RUSSELL VINER
c/o Jealotts Hill International Research Centre, Bracknell, Berkshire RG42 6ET
13. CHRISTOPHER JOHN URCH
c/o Jealotts Hill International Research Centre, Bracknell, Berkshire RG42 6ET
14. PATRICK JELF CROWLEY
V
15. STEPHEN PAULHEANEY
c/o Jealotts Hill International Research Centre, Bracknell, Berkshire RG42 6ET
16. TORQUIL EOGHAN FRASER
c/o Jealotts Hill International Research Centre, Bracknell, Berkshire RG42 6ET

Specification

FORM 2
THE PATENTS ACT 1970
[39 OF 1970]
&
THE PATENTS RULES, 2003
COMPLETE SPECIFICATION
[See Section 10; rule 13] "A ISOTHIAZOLE COMPOUND"
SYNGENTA LIMITED, European Regional Centre, Priestley Road, Surrey Research Park, Guildfor, Surrey GU2 7YH, Germany,
The following specification particularly describes the invention and the manner in which it is to be performed:
ORIGINAL
GRANTED
7/11/2006


The present invention relates to isothiazole derivatives, to processes for preparing them, fungicidal, insecticidal, acaricidal, molluscicidal and nematicidaJ compositions comprising them, to methods of using them to combat fungal diseases (especially fungal diseases of plants) and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
Isothiazole derivatives are disclosed in WO 95/31448, WO 97/18198, WO 98/02424 and WO 98/05670.
The present invemion provides a compound of formula (I):

whereinX is O or S; n is 0 or 1; Y is O, S or NR7;R' is hydrogen, halogen, C1-6 alkyl, C1-6
■■fiialo'allwi;:C1-6alk63^,,-C1-6 haloalkoxy, C1-6 alkylthid, C1-6 haloalkylthio, C1-6 cycloalkyl, C1-6
alkb^fC1-6aJ^^prSjFj; R2 is hydrogen, halogen,C1-6alkyl^C1-6 alkoxy, C1-6 haloalkoxy, C1-6
alk^lthidl e^^halpalkylthio, C1-6 alkylsulfinyl;*C1-6;halba^ C1-6 alkylsulfonylj C1-6,
halpalk^lsti]&nyl, C1-6 haloalkyl, cyano, nitro, CHO, GH=NOR5, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl or SFS; or together R1 and R2 form a five or six membered saturated or tmsaturatedearbocyclic ring, optionally substituted by one or two-G.1-6 alkyl groups; R3 is hydrogen,1-6 aBcyl, CH2(C1-6 haloalkyl), C1-6 cyanoalkyl, C1-6 alkenyl, C1-6 alkynyl, C1-6 alkTOcy(C1-6)alkyl, C1-6 alkylthio(C1-6alkyl, C1-6 alkoxyC1-6alkoxyC1-6alkyl, C1-6 alkylcarbonyl,, C1-6alkoxycarbonyl, formyl, C1-6 alkylcarbonyl(C1-6)alkyl, C1-6 alkoxycarbonyl(C1-6)alkyl, C1-6alkylaminocarbonyl, di(C1-6)alkylaminocarbonyl, optionally substituted phenoxycarbonyl, optionally substituted phenyl(C1-6)alkyl or S(0)qR6; R4 is hydrogen, halogen, cyano, C1-6 alkyl, C1-6 haloalkyl, C1-6 cyanoalkyl, C1-6 alkenyl, C1-6
alkynyl, C1-6 cycloalkyl, C1-6 halocycloaUcyl, C1-6 cyanocycloalkyl, C1-6 alkyl(C1-6)cycloalkyl,
C1-6alkyl(C1-6)halocycloalkyl, C1-6 cycloalkyl(C, Jalkyl, C1-6 cycloalkenyl, C1-6
cycloalkenyl(C1-6)alkyl, C1-6 haloalkenyl, C1-6cyanoalkenyl, C1-6 alkoxy(C1-6)alkyl, formyl, C1-6
6 carboxyalkyl, C1-6 alkylcarbonyl(C1-6alkyl, C1-6 alkoxycarbonyl(C1-6)alkyl, C1-6 alkylthio(C1-6

6)alkyl, C1-6 alkylsulfinyl(C1-6)alkyl, C1-6 alkylsulfonyl(C1-6)alkyl, aininocarbonyl(C1-6)alkylT C1-6alkylaniinocarbonyl(C1-6)alkyl, di(C1-6)alkylaminocarbonyl(C1-6)aIkyl, C1-6 alkoxycarbonyl, C1-6alkylcarbonyl, arninocarbonyl, C1-6 alkylaminocarbonyl, di(C,. 6)alkylaminocarbonyi, optionally substituted phenyl, optionally substituted phenyl(C1-6)alkyl, optionally substituted phenyl(C1-6)alkenyl, optionally substituted heteroaryl, optionally substituted heteroaryl(C1-6)alkyl, optionally substituted heterocyclyl, optionally substituted heterocyclyl(C1-6)alkyl, a group OR8, a group SH, a group S(0)pR9, a group NR,0Rn or a group C(R12)=NOR13; R5 is hydrogen, C1-6alkyl, optionally substituted phenyl or optionally substituted phenyl(C1-6)alkyl; R6 is C1-6 alkyl, C1-6 haloalkyl or optionally substituted phenyl; R7 is hydrogen, cyano, C1-6 alkyl, C1-6 haloalkyl, C1-6 cyanoalkyl, C1-6 alkenyl, C1-6 alkynyl, C1-6 cycloalkyl, C1-6 haloalkenyl, C1-6 cycloalkyl(C1-6)alkyl, CI-6 alkoxy(C, Jalkyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyl, C1-6alkylaminocarbonyl, di(C1-6)alkylaminocarbonyl, optionally substituted phenyl or optionally substituted heteroaryl; R8 is hydrogen, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkenyl, C1-6 cyanoalkyl, C1-6 alkoxycarbonyl(C1-6)alkyl, optionally substituted phenyl, optionally substituted pbenyl(C1-6)alkyl, optionally substituted heteroaryl, N=C(eH3)2; R9 is C1-6 alkyl, C1-6 haloalkyl, C1-6 alkenyl, cyano, C1-6 cyanoalkyl, 1-6 alkoxycarbonyl(G,^)alkyl, optionally substituted phenyl, optionally substituted phenyl(C,. 4)alkyl or optionally substituted heteroaryl; R'° and R1' are, independently, hydrogen, C1-6 alkyl, C1-6 cycloalkyl, C1-6 alkenyl, C1-6 alkynyl, C1-6 haloalkyl, C1-6 alkoxy(C1-6)alkyl, C1-6 alkoxycarbonyl, optionally substituted phenoxycarbonyl, fonnyl, C1-6 alkylcarbonyl, C1-6 alkylS02, optionally substituted phenylS02 or optionally substituted phenyl(CM)alkyl; R'2 is C1-6 alkyl; R13 is C1-6 alkyl, optionally substituted phenyKC1-6alkyl; and p and q are, independently, 0,1 or 2.
The compounds of formula (I) may exist in different isomeric or tautomeric forms. This invention covers all such isomers and tautomers and mixtures thereof in all proportions.
In a further aspect the present invention provides a compound of formula (I) wherein X is O or S; n is 0 or 1; Y is O, S or NR7; R1 is hydrogen, halogen, C1-6 alkyl, C1-6haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6 alkylthio, C1-6 cycloalkyl or C1-6 alkoxy(C, Jalkyl; R2 is hydrogen, halogen, C1-6 alkyl, C1-6 haloalkyl, cyano, nitro, CHO, CH=NO5, C1-6 alkylcarbonyl, C1-6alkoxycarbonyl or C1-6 alkylS(0)x; or together R1 and R2 form a five or six membered saturated or unsaturated carbocyclic ring, optionally substituted by one or two C1-6

alkyl groups; R3 is hydrogen, C1-6 alkyl, CH2(C1-6 haloalkyl), C1-6 alkenyl, C1-6 alkynyl, C1-6 alk| (C1-6)alkyl, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, formyl, optionally substituted phenoxycarbonyl, optionally substituted phenyl(C1-6)alkyl or S(0)yR25; R4 is hydrogen, halogen, cyano, optionally substituted alkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6 alkylthio, C1-6 alkenyl, C1-6 alkynyl, C1-6 cycloalkyl (optionally substituted with halogen or C1-6alkyl), C1-6 cycloalkenyl (optionally substituted with halogen or C1-6 alkyl), C1-6 haloalkenyl, NHS02R24 NHCOR24 CONR20R21, NR2R21, COR24, C02R20, optionally substituted phenyl, optionally substituted heteroaryl or a group ZR26; R5 is hydrogen, C1-6 alkyl, optionally substituted phenyl or optionally substituted phenyl(C1-6)alkyl; R25 is C1-6 alkyl, C1-6 haloalkyl or optionally substituted phenyl; Z is O, S, SO, S02 or NR27; R7 is hydrogen, cyano, C1-6 alkyl, C1-6 haloalkyl, C1-6 cyanoalkyl, Q1-6 alkenyl, Q1-6 alkynyl, C1-6 cycloalkyl, C1-6 haloalkenyl, C3. 6 cycloalkyl(C1-6)alkyl, C1-6 alkoxy(C1-6)alkyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyl, C1-6 alkylaminocarbonyl, m(Cw)alkylaminocarbonyl, optionally substituted phenyl or optionally substituted heteroaryl; R26 and R27 are, independently, hydrogen, C1-6 alkyl, C1-6 alkenyl, C1-6 alkynyl, C1-6 alkoxy(C1-6)alkyl, C1-6 alkoxycarbonyl, optionally substituted phenoxycarbonyl, C1-6 alkylcarbonyl or optionally substituted pheriyl(C1-6)alkyl, or R26 and R27 join to form a 5-or 6-membered saturated or ur^aturated ring optionally containing another hetefoatorri selected from oxygen, sulfur an]l nitrogen; R20 and R2' are, mdepoidently, hydrogen or C1-6 alkyl; R24 is C1-6 alkyl or phenyl; and x and y are, independently, 0,1 or 2.
Alkyl is straight or branched chain and is, for example, methyl, ethyl, n-propyl, n-butyl, n-pentyl, /j-hexyl, iso-propyl, n-butylj sec-butyl, wo-butyl, ter/-butyl or neo-pentyl.
Halogen is fluorine, chlorine, bromine or iodine.
Haloalkyl groups are alkyl groups which are optionally substituted with one or more of the same or different halogen atoms and are, for example, CF3, CH2CF3 or CH2CHF2.
Phenyl(C1-6)alkyI is, for example, 1-phenyleth-l-yl, 2-phenyleth-l-yl, 2-phenylprop-2-yl, 3-phenylprop-l -yl, but is preferably benzyl.
The term heteroaryl refers to an aromatic ring containing one or more heteroatoms (preferably one or two heteroatoms) selected from 0, S and N. Examples of such rings include pyridine, pyrimidine, furan, quinazoline, thiophene, thiazole, oxazole and isoxazole.
The term heterocyclyl refers to a non-aromatic ring containing one or more (preferably one or two) heteroatoms selected from O, S and N. Examples of such rings

include 1,3-dioxolanyl, tetrahydrofuryl and morpholinyl. It is preferred that heterocyclyl is cgfconally substituted by C1-6 alkyl.
Cycloalkenyl includes cyclopentenyl, cyclohexenyl and cyclohexadienyl.
It is preferred that phenyl moieties and heteroaryl groups are optionally substituted by one or more substituents independently selected from halogen, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy(C1-6)alkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6 alkylthio, C1-6 haloalkylthio, C1-6 alkylsulfinyl, C1-6 haloalkylsulfinyl, C1-6 alkylsulfonyl, C1-6 haloalkylsulfonyl, C1-6 alkenyl, C2_6 haloalkenyl, C2-6 alkynyl, C3-6 cycloalkyl, nitro, cyano, C02H, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, R14R,5N or R,6R,7NC(0); wherein R14 R15, R16 and R'7 are, independently, hydrogen or C1-6 alkyl.
It is preferred that R1 is C1-2 alkyl, especially, methyl.
It is preferred that R2 is hydrogen, cyano or halogen, especially, halogen (especially bromo or chloro).
It is preferred that R3 is hydrogen, C1-6 alkyl or C1-6 alkoxy(C1-6)alkyl.
It is further preferred that R3 is hydrogen, ethyl or ethoxymethyl.
It is preferred that R4 is C1-6 alkoxy(C1-6)alkyl, C1-6 haloalkyl, (C1-6 alkyl)amino, di-(C1-6 alkyl)airnno (swhas N(C2H5)2 orN(C2H5) (CH[CH2]CH3)), morpholinb, C1-6 alkyl or C1-6 alkoxy, especially morpholino, C1-6 alkyl or C1-6alkoxy.
It is prefeiredthat n is 0.
It is preferred that X is oxygen.
It is preferred that Y is oxygen or sulphur.
It is preferred that the compounds of the invention are of formula (la).
In one particular aspect the present invention provides a compound of formula (la) wherein R1 is C1-6 alkyl (especially methyl or ethyl); R2 is hydrogen, halogen (especially chloro or bromo) or cyano; or R1 and R2 together form a cyclopentyl, cyclohexyl or phenyl ring; R3 is hydrogen, C1-6 alkyl (especially methyl or ethyl), C1-6 alkenyl (especially allyl), C,. 6 alkynyl (especially propargyl), or C1-6 alkoxy(C1-6)alkyl (especially methoxymethyl and ethoxymethyl); n is 0; X and Y are both oxygen; and R4 is C1-6 alkyl [optionally substituted with halogen, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkylthio, alkylamino, dialkylamino (wherein the alkyl groups may form part of a five or six-membered ring, optionally containing one heteroatom such as oxygen or nitrogen), phenyl (itself optionally substituted

with halogen), C1-4 cycloalkyl, C1-4 alkenyl, C1-4 alkynyl, C1-4 cycloalkyl, phenyl [optionally su^tuted with halogen, C1-4 haloalkyl (especially CF3), nitro, CO2H, or cyano] or heteroaryl (especially pyridyl or pyrimidinyl) [optionally substituted with C1-4 alkyl or C1-4 haloalkyl]].
In one particular aspect the present invention provides a compound of formula (la) wherein R1 is C1-4 alkyl (especially methyl or ethyl); R2 is hydrogen, halogen (especially chloro or bromo) or cyano; or R1 and R2 together form a cyclopentyl, cyclohexyl or phenyl ring; R3 is hydrogen, C1-4 alkyl (especially methyl or ethyl), phenyl(C1-4)alkyl (especially benzyl), C1-4alkylcarbonyl (especially acetyl) or C1-4 alkylsulfonyl (especially methanesulfonyl); n is 0; X is oxygen; Y is oxygen or sulphur (especially oxygen); R4 is hydrogen, C1-4 alkyl [optionally substituted with halogen, C1-4 alkoxy, C1-4alkylS(0)m, phenyl (itself optionally substituted with halogen), phenoxy, NR20R21, C02H, CONR22R23, cyano, C3-6 cycloalkyl or CO(C1-6 alkoxy)], C1-4 alkoxy (optionally substituted with halogen), C1-4 alkylthio, C1-4 alkenyl (optionally substituted with halogen), NHS02R21 NHCOR24, NR20R21 COR24, COjR20, GM alkynyl, CM cycloalkyl (optionally substituted with halogen or C14j alkyl), C1-4 cycloalkenyl, phenyl [optionally substituted with halogen, C1-4 haloalkyl (especially CF3), C1-4 alkoxy, nitro, C02R20 or cyano] or heteroaryl (especially pyridyl, pyrimidinyl, furanyl or thiophenyl) [optionally substituted with Cj^ alkyl, nitro or CM haloalkyl]; R20, R21, R22 and R23 are, independently,hydrogen or C1-4-alkyl; R24 is C1-4 alkyl or phenyl; and m is 0,1 or 2.
The physical parameter K1- 2 concerns the relative solubility of a compound in n-octahol and water and, for a compound [A]:
K_-. = (solubility of compound TA1 in »-octanolt (solubility of compound [A] in water)
In a further aspect the present invention provides a compound of formula (I) wherein logio^Srfw (calculated using the CLOGP3 program, available from BioByte Corp.,201 West 4th Street, Suite 204, Claremont, CA 91711, USA) of the compound is in the range zero to 8, preferably in the range 1 to 6 and more preferably in the range 1.2 to 5.2.
It will readily be seen that the side chain portion of formula (XIX):


is a portion of a compound of formula (I). The longest bond path of the side chain portion of formula (XIX) is the path involving the minimum number of bonds from the carbon labelled # to the furthest atom of the side chain, having an atomic weight greater than 10 Daltons. If there is more than one longest bond path, each involving the same minimum number of bonds, there is a set of longest bond paths.
In a further aspect of the present invention it is preferred that R* is hydrogen, SH,.CM alkyl, C3.4 cycloalkyl, C^ alkenyl, C2.5 alkynyl, Cw haloalkyl, CM cyanoalkyl, C^ haloalkenyl, optionally substituted heterocyclyl(CM)alkyl, C2^ cyanoalkenyl (such as 1-cyano-2-methylpropenyI), phenyl (optionally substituted with fluoro, chloro, bromo, nitro, cyano, Cw alkyl, C,_2 alkoxy, CM haloalkyl (such as trifiuoromethyl), CM haloalkoxy (such as trifluoromethoxy), methanesulfonyl, methylenedioxy or di(CM alkyl)amirio (such as dimethylamino)), phenyl(C,.3)alkyl (phenyl optionally substituted with halogen^ nitro, cyano, CM alkyl, C,.2 alkoxy, CM haloalkyl (such as trifiuoromethyl), CM haloalkoxy (such as trifluoromethoxy), methanesulfonyl, or methylenedioxy), formyl, optionally substituted heterocyclyl, optionally substituted heterbaryl, optionally substituted heteroaryl(CM)alkyl, Cj.2 alkylcarbonyl, Cw alkoxycarbonyl, C,.5 alkoxycarbonyl(Cw)alkyl, a group NR10!^', a group ORs, CM alkoxymethyl, chlorine, a group SR\ or a group C(R,2)=NORn; R* is hydrogen, C,.5 alkyl, CM haloalkyl (such as 2,2,2-trifluoroethyl), C^, alkenyl (such as allyl), phenyl (optionally substituted with fluoro, chlorOj bromo, nitro, cyano, Cw alkyl, C,_2 alkoxy, CM haloalkyl (such as trifiuoromethyl), CM haloalkoxy (such as trifluoromethoxy), methanesulfonyl, or methylenedioxy), phenylfCHj) (phenyl optionally substituted with fluoro, chloro, bromo, nitro, cyano, C,^ alkyl, C,_2 alkoxy, CM haloalkyl (such as trifiuoromethyl), C,^ haloalkoxy (such as trifluoromethoxy), methanesulfonyl, or methylenedioxy), N=C(CH3)2; R9 is C,_5 alkyl, phenyl (optionally substituted with fluoro, chloro, bromo, nitro, cyano, C,^ alkyl, C,_2 alkoxy, CM haloalkyl (such as trifiuoromethyl),

C1-4 haloalkoxy (such as trifluoromethoxy), methanesulfonyl, methylenedioxy or di(C1-4 alk^fctmino (such as dimethylamino)), C1-4 haloalkyl, cyano, cyanomethyl or C1-4 alkoxycarbonylmethyl; R10 and R11 are, independently, hydrogen, C1-4 alkyl, C1-4 cycloalkyl, formyl, C1-4 alkylcarbonyl, phenoxycarbonyl, C1-4 alkylS02 or phenylS02; R12 is C1-4 alkyl; R 13 is C1-4 alkyl or benzyl; heterocyclyl is, for example, tetrahydroruryl, 1,3-dioxolanyl or morpholinyl; an example of an optional substituent for heterocyclyl is C1-4 alkyl; heteroaryl is, for example, thienyl, furyl, pyridyl, quinazolinyl, pyrazolyl or isoxazolyl; and examples of optional substituents for heteroaryl include C1-4 alkyl, C1-4 haloalkyl and phenoxy.
In a further aspect the present invention provides a compound of formula (I) wherein the side chain portion of formula (XIX) is such that each atom having an atomic weight greater than 10 Daltons in the side chain portion is no more than four bond lengths away from any of the atoms present in the longest bond path or one of the longest bond paths.
In another aspect the present invention provides a compound of formula (la) or (lb) wherein R1 is C,.2 alkyl, chloro, CF3, OCH3 or SCH3; R2 is hydrogen, halogen (such as fluorine, chlorine or bromine), cyano, nitro, CMalkyl (such as methyl), CuaIkoxy (such methbxy) or SCH3; or R' and R2 join to form a C1-4 cycloalkyl (such as cyclopentyl or cyclohexyl) or phenyl ring; R3 is hydrogen, G1-4 alkyl optionally substituted with cyano, halogen, (Cualkoxy, (G1-4)alkoxy(G1-4)alkoxy, C1-4alkoxycarbonyl, phenyl or C1-4alkylthib (such as methyl, ethyl, w-propyl, iso-piopyl, cyanomethyl, 2,2,2-trifluoroethyl, (C,. 2)alkoxymethyl, methoxyethoxymethyl, methoxycarbonylmethyl, phenylmethyl or methylthiomethyl), C1-4 alkenyl {such as allyl), C1-4, alkynyl (such as propargyl), carbonyl substituted with G1-4 alkoxy, C1-4alkylamino or di(C1-4alkyl)amino (such as C1-4 alkoxycarbonyl, memylaminocarbonyl or dimemylaminocarbonyl), CMalkylthio (such as methylthio) or phenyllhio; X is oxygen or sulphur; Y is oxygen, sulphur or NR7; n is 0; R4 is hydrogen, SH, C1-4 alkyl, C1-4 cycloalkyl, C1-4alkenyl, C1-4 alkynyl, C1-4 haloalkyl, C1-4 cyanoalkyl, C1-4 haloalkenyl, optionally substituted heterocyclyl(C1-4)alkyl, l-cyano-2-methylpropenyl, phenyl (optionally substituted with fluoro, chloro, bromo, nitro, cyano, C1-4 alkyl, fer/-butyl, C1-4 alkoxy, trifluoromethyl, trifluoromethoxy, methanesulfonyl, methylenedioxy or dimethylamino), phenyl(C1-4)a]kyl (phenyl optionally substituted with fluorine), formyl, optionally substituted heteroyclyl, optionally substituted heteroaryl, optionally substituted heteroaryl(C1-4)alkyl, C1-4 alkylcarbonyl, C1-4 alkoxycarbonyl, C1-4

alkoxycarbonyl(CM)alkyl, a group NR10R", a group OR', C1-4 alkoxymethyl, chlorine, a @gp SR', or a group C(R,2)=NOR13; R7 is hydrogen or C1-4alkyl (such as methyl); R8 is hydrogen,.C1-4 alkyl, 2,2,2-trifluoroethyl, allyl, phenyl (optionally substituted with chloro), phenyl(CH2) (phenyl optionally substituted with fluoro, chloro), N=C(CH3)2; R9 is C,.s alkyl, phenyl, C1-4 haloalkyl, cyano, cyanomethyl or C1-4 alkoxycarbonylmethyl; R10 and R11 are, independently, hydrogen, C1-4 alkyl, C1-4 cycloalkyl, fonnyl, C1-4 alkylcarbonyl, phenoxycarbonyl, C1-4 alkylS02 or phenylS02; R12 is C1-4 alkyl; R13 is C1-4 alkyl or benzyl; heterocyclyl is, for example, tetrahydrofuryl, 1,3-dioxolanyl or morpholinyl; an example of an optional substituent for heterocyclyl is C1-4 alkyl; heteroaryl is, for example, thienyl, furyl, pyridyl, quinazolinyl, pyrazolyl or isoxazolyl; and examples of optional substituents for heteroaryl include C1-4 alkyl, C1-4 haloalkyl and phenoxy. Specific preferred values of R4 are recited in Table Al.
The compounds in the following Tables illustrate compounds of the invention. Table Al provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is hydrogen; X and Y are each oxygen; n is 0; and R4 is as defined in the Table.
TABLE Al


350 6-tnfiuoromethyl-2-pyridyl
351 OH
352 SH
TABLE A2 Table A2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A3 Table A3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A4 Table A4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A5 Table A5 provides 352 compounds of formula (la) wherein R' is methyl; R2 is cyano; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A6 Table A6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A7 Table A7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A8 Table A8 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is chloro; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE A9
^ Table A9 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is bromo; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A10 Table A10 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE All Table Al 1 provides 352 compounds of formula (Ia) wherein R1 is methyl; R2 is hydrogen; R3 is hydrogen; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A12
Table A12 provides 352 compounds of formula (Ia) wherein R1 is methyl; R2 is
fluoro; R3 is hydrogen; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of
the correspondingly numbered compounds of Table Al.
TABLE A13
Table A13 provides 352 compounds of formula (la) wherein Rl is methyl; R2 is chloro; R3 is hydrogen; Xis oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A14 Table A14 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is hydrogen; X is oxygen; Y is sulphur, n is 0; and the values of R4 ihatch those of the correspondingly numbered compounds of Table A1.
TABLE A15 Table A15 provides 352 compounds of formula (Ia) wherein R1 is methyl; R2 is cyano; R3 is hydrogen; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A16


Table A16 provides 352 compounds of formula (la) wherein R1 is ethyl; R: is h^rogen; R3 is hydrogen; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A17 Table Al 7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is hydrogen; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A18 Table Al 8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is hydrogen; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A19
Table A19 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo;
R3 is hydrogen; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the
correspondingly numbered compounds of Table Al.
- I TABLE A20
Table A20 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is hydrogen; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the co^espohdihglyTiumbered compounds of Table Al.
TABLE A21 Table A21 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A22 Table A22 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A23 Table A23 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE A24 Tibte A24 provides 152 compounds of formula (lb> vfherevn. R,1 is. toe&y V, R2 is, bromo; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A25 Table A25 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is cyano; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE A26 Table A26 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; K3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE, an
Table A27 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A28 Table A28 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A29 Table A29 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A30 Table A30 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is cyano; R3 is hydrogen; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A31


Table A31 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hwlrogen; R3 is hydrogen; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A32 Table A32 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is hydrogen; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A33 Table A33 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is hydrogen; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A34 Table A34 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is hydrogen; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE A35 Table A35 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is hydrogen; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A36 Table A36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is hydrogen; Xis oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A37 Table A37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is hydrogen; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A38 Table A38 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is hydrogen; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE A39
Table A39 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is hydrogen; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A40 Table A40 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is hydrogen; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A41 Table A41 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is hydrogen; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A42 Table A42 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is hydrogen; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A43 TableA43.proyides 352i compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is hydrogen; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A44 Table A44 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is hydrogen; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A45 Table A45 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is hydrogen; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A46
-^2-—

Table A46 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is ogen; R3 is hydrogen; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A47 Table A47 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is hydrogen; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A48 Table A48 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is hydrogen; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A49 Table A49 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is hydrogen; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE ASO Table A50 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is hydrogen; X is oxygen; Y isNR7; R7 is hydrogen; n is 0; andthe values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A51 Table A51 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; arid the values of R4 match thoseof the correspondingly numbered compounds of Table Al.
TABLE A52 Table A52 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A53 Table A53 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE A54
Table A54 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE ASS Table A55 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A56 Table A56 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al,
TABLE A57 Table A57 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of me correspondingly numbered compounds of Table Al.
TABLE AS8 Table A58 provides 352 compounds of formula (lb) wherein Rl is^thyl; R2 is chlbro; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE A59 Table A59 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A60 Table A60 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE A61


Table A61 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of K" match those of the correspondingly numbered compounds of Table Af.
TABLE A62 Table A62 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A63 Table A63 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A64 Table A64 provides 352 compounds of formula (la) wherein R' is methyl; R2 is bromo; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE A65 Table A65 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A66 Table A66 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE A67 Table A67 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A68 Table A68 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compound's of Table Al.


TABLE A69
Table A69 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE A70 Table A70 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is cyano; R3 is hydrogen; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Bl Table Bl provides 352 compounds of formula (la) wherein R' is methyl; R2 is hydrogen; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE B2 Table B2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B3 Table B3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B4 Table B4 provides 352 compounds of formula (la) wherein R' is methyl; R2 is bromo; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B5 Table B5 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE B6


Table B6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B7 Table B7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B8 Table B8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B9 Table B9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE BIO Table BIO provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Bll Table Bll provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is methyl; X is oxygen; Y is sulphur; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE B12 Table B12 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is methyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B13 Table B13 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is methyl; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE B14
Affable B14 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is methyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B15 Table B15 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is methyl; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B16 Table B16 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is hydrogen; R3 is methyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B17 Table B17 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is methyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the coiTespondmglyiiumbered compounds,of Table Al.
TABLE B18
Tal)le^l^MPOvides 3 52 impounds of fbnniiia^(Ia) wherein^^
R3 &meftyl^^^xygen; Y is sulphur, n is 0; and the values of R4 match(those of the
conespondmglyiiiumbCTed compounds of Table Al. ' -
TABLE B19 TableBlP^rovides.SSJZcompounds of formula (la) wheremR^ethyt-R-as bromo; R3 is methyl; X is oxygen; Y is sulphur; n is 0; and the values of R4inaifcK'tKosebf the correspondingly numbered compounds of Table Al.
TABLE B20 Table B20 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R is methyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B21

Table B21 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R* match those of the Jprespondingly numbered compounds of Table A1.
TABLE B22 Table B22 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE B23 Table B23 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE B24 Table B24 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is bromo; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE B25
table B25 provides 352 compounds of formula (lb) wherein Rl is methyl; R2 is
cyano;;E^}mtf^ 0; and me values of R^naatch those of the
corre^p^na^glyatimbeTed compounds of Table Al.
TABLE B26 Table B26 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R* match those of the coiresppndihgly numbered compounds ofTable Al.
TABLE B27 Table B27 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table A1.
TABLE B28 Table B28 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE B29
Table B29 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B30 Table B30 provides 352 compounds of formula (lb) wherein R1 is ethyl; R: is cyano; R3 is methyl; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE B31 Table B31 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is methyl; X is oxygen; Y is sulphur, n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE B32 Table B32 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is methyl; X is oxygen; Y is sulphur, n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE B33 '.[ Table,B33 provides 352 compounds offormula (lb) wherein-R' is methyl; R2is chloro; R3 is methyl; X is oxygen; Y is sulphur, n is 0; and the values df R* match those of the correspondingly numbered compounds of Table Al.
TABLE B34 Table B34 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is methyl; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B35 Table B35 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is methyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B36


Table B36 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is hydrogen; R3 is methyl; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of thd^rrespondingly numbered compounds of Table Al.
TABLE B37 Table B37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is methyl; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B38 Table B38 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is chloro; R3 is methyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B39 Table B39 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is bromo; R3 is methyl; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLEB4Q Table B40 provides 352 compounds offonnula (lb) wherein R1 is ethyl; R2 is cyano; R3 is methyl; X is oxygen; Y is sulphur; n isiO; ahdftiie Rvalues of R* match those of the correspondingly numbered compounds of Table -Al.
TABLE B41 Table B41 provides 352 compounds of formula (lb) wheTein R1 is methyl; R2 is hydrogen; R3 is methyl; X is oxygen; Y is NR7; R7 is hydrogen; his 0; and the values of R4 rnatcii those of the correspondingly numbered compounds of Table Al.
TABLE B42 Table B42 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is methyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B43 Table B43 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is methyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE B44
^ Table B44 provides 352 compounds of formula (lb) wherein R* is methyl; R2 is bromo; R3 is methyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE B45 Table B45 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is methyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE B46 Table B46 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is methyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE B47 Table B47 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 isiluoro; R3 is methyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the corre^iohdingly numbered1 compounds of Table Al. ^TABLE^B48
Table:B4^provides 352 compounds ofibnihila(lb) wherein R1 is efhyfc'&Sschloro; R3 is methyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B49 Table B49 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is bromo; R is methyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of TabJe A1.
TABLE B50 Table B50 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R is methyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B51


Table B51 provides 352 compounds oi lormula (lb) wnerein K' is methyl; R- is hydrogen; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 matchthose of the correspondingly numbered compounds of Table Al.
TABLE B52 Table B52 provides 352 compounds of formula (lb) wherein R1 is methyl; R- is fiuoro; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B53 Table B53 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B54 Table B54 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE B55
Table B55 provides 352 compounds of formula(lb) wherein R1 is methyl; R2 is
(^ano;^^^ethyl;X.isoxygen; YisNR^T^is^nethyl;nis0;l^^e^aluesoM4match
those of the wirespondirigl|y numbered compounds of Table Ak -
TABLE B56 Table B56 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 matchthoseof the correspondingly numbered compounds ofTable AL-
TABLE B57 Table B57 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fiuoro; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is Orand the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B58 Table B58 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE B59
^Table B59 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B60 Table B60 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B61 Table B61 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B62 Table B62 provides 352 compounds of formula (la) wherein Rl is methyl; R2 is fluoro; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds ofTable At;
TABLE B63
. otTable B63 provides 352 impounds offdimula(Ia) whrein R1 is methy; R2 is
chloro; R3 is methyl; X is oxygen; Y is NR7;-R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLEB64 Tabje B64 provides 352 compounds ofibrmula (la) wherein R1 is methyl; R2 is bromo; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B65 Table B65 provides 352 compounds of formula (Ib)Avherein R1 is methyl; R2 is cyano; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B66


Table B66 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 ma^ those of the correspondingly numbered compounds of Table Al.
TABLE B67 Table B67 provides 352 compounds of formula 0a) wherein R1 is ethyl; R2 is fluoro; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE B68 Table B68 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLEB69 Table B69 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is methyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLEB70 Table B70 provides 352 compoundsbf iformula (la) wherein R1 is ethyl; R2 is cyano; R3 is methyl; X is oxygen; Y is NR7;:R7 is mekhyl^nisOiand the values of R4 matcnt&Mfelof ^' zthe correspondingly numbered compounds "of Table Al. ~
TABLE CI Table CI provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is ethyl; X and Y are each oxygen; n is 6; and the values of R4 match those of the correspondingly numbered compounds: of Table A1
TABLE C2 Table C2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al."
TABLE C3 Table C3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R is ethyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE C4
^ Table C4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C5 Table C5 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C6 Table C6 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is hydrogen; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C7 Table C7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al. TABLE C8
Table G8 provides 352 compounds of formula (la) wherein R1 Is ethyl; R3 is chlorb; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE C9 Table C9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C10 Table C10 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE CI 1


Table CI 1 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is ethyl; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the Mrrespondingly numbered compounds of Table Al.
TABLE C12 Table C12 provides 352 compounds of formula (la) wherein R1 is methyl; R: is fluoro; R3 is ethyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C13 Table CI 3 provides 352 compounds of formula (la) wherein R' is methyl; R3 is chloro; R3 is ethyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C14 Table CI 4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is ethyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
l^BLECIS Table C15 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is ethyl^X-k oxygen; Y is sulphur, n island the^values of R4 matchlhose of the correspondingly numbered compounds ofltable Al.
TABLE C16 Table CI 6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is ethyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered impoundsof Table Al.
TABLE CI 7 Table CI 7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is ethyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C18 Table Cl 8 provides 352 compounds of formula (la) wherein Rl is ethyl; R2 is chloro; R is ethyl; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE C19
Table CI 9 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is bromo; R3 is ethyl; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C20 Table C20 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is ethyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C21 Table C21 provides 352 compounds of formula 0b) wherein R1 is methyl; R2 is hydrogen; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C22
Table C22 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is
fiuoro; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the
corresponcHngly numbered .compounds of Table A1.
TABLEC23
Table C23 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is chloro; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE €24 Table C24 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is ethyl; X and Y are each oxygen; h is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C25 Table C25 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is cyano; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C26

Table C26 provides 352 compounds of fonnula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R* match those of th4Borrespondingly numbered compounds of Table Al.
TABLE C27 Table C27 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE C28 Table C28 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is chloro; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C29 Table C29 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is ethyl; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table A1.
TABLE C30 Table C30 provides 352 compounds; ppfohnula (lb) wherein R1 is ethyl; R2 is cyano; R3 is ethyl; X and Y areeach .oxygen; ni^jiand the; values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE €31 Table C31 provides 352 compounds of fonnula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is ethyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compoundsof-Table Al:
TABLE C32 Table C32 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is ethyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C33 Table C33 provides 352 compounds of fonnula (lb) wherein R1 is methyl; R2 is chloro; R3 is ethyl; X is oxygen; Y is sulphur; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.


TABLE C34
Table C34 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is brort^ R3 is ethyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C35 Table C35 provides 352 compounds of formula (lb) wherein R1 is methyl; R3 is cyano; R3 is ethyl; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C36 Table C36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is ethyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C37 Table C37 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is ethyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C38 TableC38pipVides 352 compounds of formula (lb) wherein R1 is ethyl^rischlbrb; R3 is ethyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of ihe correspondingly numbered compounds of Table Al.
TABLE C39 Table C39 provides 352 compounds of formula (lb) wherein R1 is ethyl; R3 is bromo; R3 is ethyl; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C40 Table C40 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is ethyl; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C41


Table C41 provides 352 compounds of formula (lb) wherein R1 is methyl; R3 is hydrogen; R3 is ethyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 ,- match those of the correspondingly numbered compounds of Table Al.
TABLE C42 Table C42 provides 352 compounds of formula (lb) wherein R1 is methyl; R: is fluoro; R3 is ethyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE C43 Table C43 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is ethyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C44 Table C44 provides 352 compounds of formula (lb) wherein R* is methyl; R2 is bromo; R3 is ethyl; X is oxygen; Y isNR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C45 Table C45 provides 352 compounds of formula (lb) wherein Rl is methyl; R2 is cyano; R3 is ethyUJX is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C46 Table C46 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is ethyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and me values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C47 Table C47 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is ethyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C48 Table C48 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R is ethyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE C49
Table C49 provides 352 compounds of formula 0b) wherein R1 is ethyl; R2 is bromo; RJi#hyI;X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE C50 Table C50 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is cyano; R3 is ethyl; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C51 Table C51 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C52 Table C52 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly Su1nbcred;compdunds of Table Al.
TABLE C53 Table C53 provides 352 compounds^of formum (lb) wherein R1 is methyl; R2 is chloro; R3 is ethyl; X is oxygen; Y is NR7; R7 is methylfn is 6; and the" values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C54 Table C54 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is ethyl; X is oxygen; Y is NR7; R7 is memyljn is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE CSS Table C55 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is cyano; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C56


Table C56 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C57 Table C57 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fiuoro; R3 is ethyl; X is oxygen; Y is NR1; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C58 Table C58 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C59 Table C59 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C60 Table G60 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is ethyl; X*« oxygei^ ^isiNR7; R7 is diethyl; n is 0;«and the values of R4 matcbrthose of the correspondmgly numbered compounds of Table Al.
TABLE C61 Table C61 provides 352 compounds of formula (la) wherein R" is methyl; R2 is hydrogen; R3 is ethyl; X is oxygen; Y is NR7;R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE C62 Table C62 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fiuoro; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C63 Table C63 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE C64
Table C64 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C65 Table C65 provides 352 compounds of formula (lb) wherein R* is methyl; R2 is cyano; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C66 Table C66 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is hydrogen; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C67 Table C67 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of/Table Al.
^ TABLE C68
Table C68 provides352 compounds of formula (la) wherein*R,;is emyl^3 ischlorb; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match Ihose of the correspondingly numbered compounds of Table Al.
TABLE C69 Table C69 provides .352 compounds of formula (la) wherein R1 is ethyl; R2 isT)romo; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE C70 Table C70 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is ethyl; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Dl


Table Dl provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match thos^f the correspondingly numbered compounds of Table Al.
TABLE D2 Table D2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D3 Table D3 provides 352 compounds of formula (la) wherein R1 is methyl; R*is chloro; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D4 Table D4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2CH2GH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P5 Table D5 provides 352 compounds of formula (la) wherein RJ is methyl; R2 is cyano; R3 isCH2CH2CH3; X and Y,are each oxygen; n is 0; and the values of R-ifiatch those bfthe correspondingly numbered compounds of Table Al.
TABLE D6
Table D6 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is
hydrogen; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the vah^rif R4 match
those of the correspondingly numbered compounds of Table Al.
TABLE D7 Table D7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D8 Table D8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH3CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE l>9
Table D9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE DIP Table D10 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Dll Table Dl 1 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D12
Table D12 provides 352 compounds of formula (la) wherein R' is methyl; R2 is
fluoro; R3 is CH2CHjCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those
i5ff%e rorresp^na^^ Al.
TABLEP13
TableDl3 provides 352 compound chloro; R3 is CH2CH2CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondinjgly numbered compounds of Table A1.
TABLE D14 Table D14 provides 352 compounds of formula (la) wherein R' is methyl; R2 is bromo; R3 is CH2CH2CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D15 Table D15 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is CH2CH2CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D16
-t/C-

Table Dl 6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2CH2CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Dl 7 Table Dl 7 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is fluoro; R3 is CH2CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D18 Table Dl 8 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is chloro; R3 is CH2CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Dl 9 Table Dl 9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2CH2CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D2Q Table D20 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is cyano; R3 is iGKjCTjd^Xis .Oxygen; Y is siilphur, n is 0; and the values.-.of R4 iDatcti'thbse of the correspbndmgly Numbered compounds of Table Al.
TABLE D21 Table D21 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D22 Table D22 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D23 Table D23 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE D24
Table D24 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D25 Table D25 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D26 Table D26 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D27
Table D27 provides 352 compounds of formula (lb) wherein R* is ethyl; R1 is fluoro;
R3 is CHjGHiCIV, X and Y are each oxygen; n is 0; and the values of R4 match those of the
correspondnigly numbered compounds of Table Al.
TABLEIP28
Table D28 provides 352 compounds of formula (lb) wlierem^R-is ethyl; R2 is chloro; R3 is CH2GH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLED29 Tablg D29 provides 352 compounds of formula (lb) wherein Rlis ethyl; R1 is bromo; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the Valiieitif R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D30 Table D30 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is cyano; R3 is CH2CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D31


Table D31 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is CH2CH2CH3; X is oxygen; Y is sulphur, n is 0; and the values of R' match those of the correspondingly numbered compounds of Table Al.
TABLE D32 Table D32 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2CH3CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D33 Table D33 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is chloro; R3 is CH2CH2CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D34 Table D34 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is bromo; R3 is CH2CH2CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D35 Table 035 provides. 352 comrxiunds pf€6nnula (lb) wherein R1 is methyl; R2 is cyano; R3is CH2CH3CH3; X is oxygen; Yds stilphuryii is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al-1
TABLEP36 Table D36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2CH2CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match % those of the correspondingly numbered compoundVbfrTableAl.
TABLE D37 Table D37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2CH2CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D38 Table D38 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is chloro; R3 is CH2CH2CH3-, X is oxygen; Y is sulphvsr, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE D39
Table D39 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3*CH2CH2CH3; X is oxygen; Y is sulphur, n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE D40 Table D40 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE D41 Table D41 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE D42 Table D42 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R" match those of the correspond^gly nuinbered compounds of Table Al.
TABLE D43 Table D43 provides 352 comr^unaVbffo^ chloro; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D44 Table D44 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2CH2CH3; X is oxygen; Y is'NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D45 Table D45 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D46


Table D46 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of Riwatch those of the correspondingly numbered compounds of Table A1.
TABLE D47 Table D47 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D48 Table D48 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is chloro; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of RA match those of the correspondingly numbered compounds of Table Al.
TABLE D49 Table D49 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is bromo; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Bio Table D50 provides 352 compounds of forixiula (lb) wherein R is ethyl; R is cyano; R3 is CH2CH2CH3; X is oxygen; YjsNR7; R7 is hydrogen; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE D51 Table D51 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D52 Table D52 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE D53 Table D53 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cmoro; R1 is CH2CH2CH3; X is oxygen; V ism7; R7 is methyl; n is t>; and 1he values of R* match those of the correspondingly numbered compounds of Table Al.

TABLE D54
Table D54 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D55 Table D55 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2CH3CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P56 Table D56 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is hydrogen; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D57 Table D57 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE3)58
Table D58 provides 352 compounds of formula (Ib) wherein R1 is ethy R2 is fluoro R3 is CH2GH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; arid the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D59 . _ Table D59 provides 352 compounds of formula (lb) whereiriR1 is ethyl; R2 is bromo; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; ami the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D60 Table D60 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D61


Table D61 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D62 Table D62 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D63 Table D63 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D64 Table D64 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2CH2CH3; X is oxygen; Y is NR7;R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLEP65 Table D65 provides 352 compounds; of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CHjCH2CH3; X is oxygen^js NR^R7 is methyl; n is 0; and the values of R4 match those of the correspondihgly numbered compounds of Table Al.
TABLE P66 Table D66 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of ■R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P67 Table D67 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D68 Table D68 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is chloro; R3 is CHrCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE P69
Table D69 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE D70 Table D70 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CHXH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE El Table El provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E2 Table E2 provides 352 compounds of formula (la) wherein Rl is methyl; R2 is fluoro; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E3 Table E3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is;chldro; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds pf Table Al.
TABLE E4 Table E4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E5 Table E5 provides 352 compounds of formula (la) wherein R1 is methyl; R3 is cyano; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E6


Table E6 provides 352 compounds of formula (la) wherein R is ethyl; R2 is hydrogen; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E7 Table E7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E8 Table E8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE E9 Table E9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2CH=CH2; X and Y arc each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E10 Table El 0 provides 352 compounds of formula Qa) wherein R' is ethyl; R2 is cyano; R3 is CHjCH^H^ X and Y are each oxygen; nis 0; and the values of R4 match thoseof the correspondingly numbered compounds of Table Al.
TABLE Ell Table El 1 provides 352 compounds of formula (la) wherein R' is methyl; R2 is hydrogen; R3 is CH2CH=CH2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E12 Table El 2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2CH=CH2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E13 Table E13 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2CH=CH2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE El 4
Table El 4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2CH=CH2; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E15 Table El 5 provides 352 compounds of formula (la) wherein R} is methyl; R2 is cyano; R3 is CH2CH=CH2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE El 6 Table El 6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2CH=CH2; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E17 Table El 7 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is fluoro; R3 is CH,CH=CH2; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the con-espon^ingly numbered compoundsi of Table Al.
TABLE EI 8 Table El 8 provides352 compounds of formula (la) whereiriR1 is ethyl; R2 is chloro; R3 is CH2CH=CH2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE E19 Table El 9 provides 352 compounds of formula (la) wherein R1 is ethyl; R?is bromo; R3 is CH2CH=CH2; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E20 Table E20 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2CH=CH2; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E21


Table E21 provides 352 compounds of formula (lb) wherein R is methyl; R2 is hydrogen; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E22 Table E22 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E23 Table E23 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E24 Table E24 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is bromo; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E25 Table E25 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2GH=CH2; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE E26 Table E26 provides 352 compounds of formula (lb) wherein R! is ethyl; R2 is hydrogen; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE E27 Table E27 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E28 Table E28 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is chloro; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE E29
Table E29 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2CH=CH2; X and Y arc each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E30 Table E30 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2CH=CH2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E31 Table E31 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is CH2CH=CH2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E32 Table E32 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2CH=CH2; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of mVcorrespondhfgly numberedcompounds of Table Al.
. . TABLE E33
Table E33 provides 352 compounds of formula (lb) wherein R* is;memyl*R?ls3 chloro; R3 is CH2CH=€H2; X is oxygen; Y is-sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E34 Table E34 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is -bromo; R3 is CH2CH=CH2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E35 Table E35 provides 352 compounds of formula (lb) wherein Rl is methyl; R2 is cyano; R3 is CH2CH=CH2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E36


Table E36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2CH=CH2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match iSlfee of the correspondingly numbered compounds of Table Al.
TABLE E37 Table E37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R- is fluoro; R3 is CH2CH=CH2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E38 Table E38 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2CH=CH2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E39 Table E39 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2CH=CH2; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLEE40 Table E40 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2CH=CHj; X is oxygen; Y is sulphur, nis 0; and the;values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E41 Table E41 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E42 Table E42 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is iluoro; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E43 Table E43 provides 352 compounds of formula (lb) wherein Rl is methyl; R2 is chloro; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE E44
Table E44 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is bromo; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of RA match those of the correspondingly numbered compounds of Table Al.
TABLE E45 Table E45 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is cyano; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E46 Table E46 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is hydrogen; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E47
Table E47 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro;
R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match
those of the correspondingly numbered compounds of Table A1.
^ TABLE E48
Table E48 provides 352 compounds of formula (lb) -wherein R1 irethyl; R2 is chloro; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE E49 Table E49 provides 352 compounds of formula (lb) wherein R1 is ethyl; R is bromo; R3 is CH2CH=CH2; X is oxygen; Y isNR7;.R7 is hydrogen; n is 0; and the values of RA match those of the correspondingly numbered compounds of Table Al.
TABLE E50 Table E50 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E51

Table E51 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of atch those of the correspondingly numbered compounds of Table Al.
TABLE E52 Table E52 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E53 Table E53 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is chloro; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E54 Table E54 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is bromo; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E55 Table E55 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2CH=GH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E56 Table E56 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is hydrogen; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al'.
TABLE E57 Table E57 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E58 Table E58 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE E59
Table E59 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is bromo; Rjf CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E60 Table E60 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E61 Table E61 provides 352 compounds of formula (la) wherein R' is methyl; R2 is hydrogen; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E62
Table E62 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is
fluoro; R3 is CH2CH=€H3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4
match those of the correspondingly numbered compounds of Table Al.
''-^ TABLE E63
TablefE&^pvides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2GI£CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E64 Table E64 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2CH=<:H2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E65 Table E65 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E66


Table E66 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is hydrogen; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of IT match those of the correspondingly numbered compounds of Table Al.
TABLE E67 Table E67 provides 352 compounds of formula (la) wherein R" is ethyl; R2 is fluoro; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E68 Table E68 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E69 Table E69 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2CH=CH2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE E70 Table E70 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2CH=€H2; X is oxygen; Y is NR7; Rr Isimethyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Fl Table Fl provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; RJ is CH2C.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F2 Table F2 provides 352 compounds of formula (la) wherein R1 is methyl; RJ is fluoro; R3 is CH2C.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F3 Table F3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2C.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE F4
Table F4 provides 352 compounds of formula (la) wherein R1 is methyl; R3 is bromo; is CHjC.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F5 Table F5 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is CHjC.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE F6 Table F6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2C.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F7 Table F7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2CCH; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F8 Table F8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CHjC.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE F9 Table F9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CHjC.CH; X and Y are each oxygen; n is 0; and ffie values56f R4 match those of the correspondingly numbered compounds of Table A1.
TABLE F10 Table F10 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is cyano; R is CH,C.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Fll


Table Fl 1 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is
hydrogen; R3 is CH2C.CH; X is oxygen; Y is sulphur, n is 0; and the values of R4 match
those of the correspondingly numbered compounds of Table Al.
TABLE F12
Table F12 provides 352 compounds of formula (la) wherein R' is methyl; R2 is fluoro; R3 is CH2C.CH; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE F13 Table F13 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2C.CH; X is oxygen; Y is sulphur, n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE Fl 4 Table F14 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH7C.CH; X is oxygen; Y is sulphur; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table A1.
TABLE F15 Table F15 provides 352 wmppund of fonnula (la) wherein R' is methyl; R2 is cyano; R3 is CH2C.CH;X is oxygen; Y isjsulphur; n is 0; and the values of Rematch those of the correspondingly numbered compounds5pf;Table Al.
TABLE F16 Table F16 provides 352 compounds of formula (la) wherein Rl is ethyl; R2 is hydrogen; R3 is CH2CCH; X is oxygen; Y is sulphur, n is 0; and the values of R* match those of the correspondingly numbered compounds of Table A1.
TABLE F17 Table Fl 7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2C.CH; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F18 Table Fl 8 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is chloro; R3 is CHX.CH; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE Fl 9
Table Fl 9 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is bromo;
R3 is CH2C.CH; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the
correspondingly numbered compounds of Table Al.
TABLE F2Q
Table F20 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano;
R3 is CH2C.CH; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the
correspondingly numbered compounds of Table Al.
TABLE F21
Table F21 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is
hydrogen; R3 is CH2C.CH; X and Y are each oxygen; n is 0; and the values of R4 match those
of the correspondingly numbered compounds of Table Al.
TABLE F22
Table F22 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is
jfluoro; R3 is CH2C.GH; X and Y are each oxygen; n is 0; and the values of R4 match those of
the correspondingly numbered compounds ofTable Al.
' TABLE F23
;, Table ra3rjrovides-352 compounds of formula (Ib)ivherein R1 is methyl; R2 is
chloro; R3 is CH2C.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of
the correspondingly numbered compounds of Table Al.
TABLE F24
Table F24 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is
bromo; R3 is CH2C.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of
the correspondingly numbered compounds of Table Al.
TABLE F25
Table F25 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is
cyano; R3 is CH2C.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of
the correspondingly numbered compounds of Table A1.
TABLE F26


Table F26 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2CCH; X and Y are each oxygen; n is 0; and the values of R4 match those oroe correspondingly numbered compounds of Table Al.
TABLE F27 Table F27 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2C.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F28 Table F28 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2C.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F29 Table F29 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is bromo; R3 is CH2C.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F30 Table F30 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2C.CH; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE F31 Table F31 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2C.CH; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of me correspondingly numbered compounds of Table AL
TABLE F32 Table F32 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is fluoro; R3 is CH2C.CH; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F33 Table F33 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is chloro; R3 is CH2C.CH; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE F34
Table F34 provides 352 compounds of formula (lb) wherein R1 is methyl: R" is hg^no; R3 is CH2C.CH; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F35 Table F35 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2C.CH; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F36 Table F36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2C.CH; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE F37 Table F37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2C.CH; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE F38 . Table J38 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CHjC.CH; X is oxygen; Y is sulphur, a is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE F39 Table F39 provides 352 compounds of formula 0b) wherein R1 is ethyl; R2 is bromo; R3 is CHjC.CH; X is oxygen; Y is sulphur, n is 0; andlhe values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F40 Table F40 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano, R3 is CH2C.CH; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F41


Table F41 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of W match those of the correspondingly numbered compounds of Table Al.
TABLE F42 Table F42 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F43 Table F43 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE F44 Table F44 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLEF45 Table F45 provides 352 compounds of formula (lb) wherein Rl is methyl; R2 is cyano; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is hydrogen; u is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F46 Table F46 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is hydrogen; R3 is CH2C.CH; X is oxygen; Y isNR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE F47 Table F47 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CHjC.CH; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F48 Table F48 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CHjC.CH; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE F49
Table F49 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F50 Table F50 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is cyano; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE F51 Table F51 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F52 Table F52 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the conwpondmgly nimibeTed compounds of Table Al.
TABLE F53 Table F53 provides,352 compounds of formula (lb) wherem Rl is memyl;R2 is chloro; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F54 Table F54 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F55 Table F55 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is cyano; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F56


Table F56 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 ra^ch those of the correspondingly numbered compounds of Table Al.
TABLE F57 Table F57 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH,C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F58 Table F58 provides 352 compounds of formula (Tb) wherein R1 is ethyl; R2 is chloro; R3 is CHX.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F59 Table F59 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is bromo; R3 is CH2CCH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F60 Table F60 provides 352 compounds of formula (Tb) wherein Rl is ethyl; R2 is cyano; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F63 Table F61 provides 352 compounds of formula (la) wherein R' is methyl; R2 is hydrogen; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F62 Table F62 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F63 Table F63 provides 352 compounds of formula (la) wherein R' is methyl; R2 is chloro; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE F64
Table F64 provides 352 compounds of formula (la) wherein R' is methyl; R2 is bromo; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F65 Table F65 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F66 Table F66 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F67 Table F67 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2C.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the; wirespondlrjgly numtered compounds of Table Al.
TABLE F68 Table F68 provides 352icompounds of formula (la) whecin Rl Is ethy ; R2 is chloro; R3 is CH2C.CH; X is oxygen; Y is NR7; R- is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE F69 Table F69 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2C.CH; X is oxygen; Y isNR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F70 Table F70 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is cyano; R is CHjC.CH; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G

Table Gl provides 352 compounds of formula (la) wherein R' is methyl; R2 is hydrogen; R3 is CH2CN; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G2 Table G2 provides 352 compounds of formula (la) wherein R' is methyl; R2 is fiuoro; R3 is CH2CN; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G3 Table G3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2CN; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G4 Table G4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2CN; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE G5 Table G5 provides 352 compounds of formula (la) wherein RJ is methyl; R2 is cyano; R3 is CH2CN; X and Y arc each oxygen; n is 0; and the values of R^maitch those'of the correspondingly numbered compounds of Table Al.
TABLE G6 Table G6 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is hydrogen; R3 is CH2CN; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Gl Table G7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fiuoro; R3 is CHjCN; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE G8 Table G8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2CN; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE G9
M Table G9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2CN; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G10 Table G10 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2CN; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Gil Table Gl 1 provides 352 compounds of formula (la) wherein R' is methyl; R2 is hydrogen; R3 is CH2CN; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G12
Table G12 provides 352 compounds of formula (la) wherein R' is methyl; R2 is
fiuoro; R3 is CH2CN; X is oxygen; Y is sulphur, n is 0; and the values of R* match those of
the correspondingly numbered compounds of Table Al.
.-.;} -f;:-:~ . • TABLE G13
,TableaG13 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2CN; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G14 Table Gl 4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2CN; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G15 Table G15 provides 352 compounds of formula (la) wherein Rl is methyl; R2 is cyano; R3 is CH2CN; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G16


Orth
Table Gl 6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2CN; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those e correspondingly numbered compounds of Table Al.
TABLE G17 Table Gl 7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2CN; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G18 Table Gl 8 provides 352 compounds of formula (la) wherein Rl is ethyl; R2 is chloro; R3 is CH2CN; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G19 Table Gl 9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CHjCN; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G20 Table G20 provides 352 compounds of formula (la) wherein R1 is ethyl; R3 is cyano; K3 is CH2CN;X is oxygen; Y is sulphur, nis 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G21 Table G21 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2CN; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G22 Table G22 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2CN; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE G23 Table G23 provides 352 compounds of formula (lb) wherein R' is methyl; R? is chloro; R3 is CH2CN; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE G24
Table G24 provides 352 compounds of formula (lb) wherein R! is methyl; R2 is b) wherein R1 is methyl; R2 is bromo; R3 is CH2CF3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE H35 Table H35 provides 352 compounds of fonnula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2CF3; X is oxygen; Y is sulphur, n is<0; andtjhe values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H36


Table H36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2CF3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those the correspondingly numbered compounds of Table Al.
TABLE H37 Table H37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2CF3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H38 Table H38 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2CF3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H39 Table H39 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CHjCF3; X is oxygen; Y is sulphur; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE H40 Table H40 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CHjCFj; X is oxygen; Y is sulphur, n is 0; and the values of R*match those of the correspondingly numbered compounds of Table A1.
TABLE H41 Table H41 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE H42 Table H42 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H43 Table H43 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cbJoro; R3 is CH3CF3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE H44
Table H44 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H45 Table H45 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is cyano; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE H46 Table H46 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is hydrogen; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H47 Table H47 provides 352 compounds of formula (lb) wherein R* is ethyl; R2 is fluoro; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the ^correspondingly numbered compounds of Table A1.
TABLE H48 Table H48 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H49 Table H49 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is bromo; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H50 Table H50 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H51


Table H51 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H52 Table H52 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H53 Table H53 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H54 Table H54 provides 352 compounds of formula (lb) wherein Rl is methyl; R2 is bromo; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H55 Table H55 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is cyano; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R* match those of me correspondingly numbered compounds of Table Al.
TABLE H56 Table H56 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H57 Table H57 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H58 Table H58 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE H59
Table H59 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; Rris CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H60 Table H60 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AI.
TABLE H61 Table H61 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H62 Table H62 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R* match those of the correspondinglynumbered compounds of Table Al. TABLE H63
Table H63 ovides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is GEjCFy. X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H64 Table H64,provides 352 compounds of formula (la) wherein R- is methyl; R2 is bromo; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; arid thelvalues("of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H65 Table H65 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE H66


Table H66 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is toirogen; R3 is CH2CF3; X is oxygen; Y is NR1; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H67 Table H67 provides 352 compounds of formula (la) wherein R! is ethyl; R2 is fluoro; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE H68 Table H68 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R' match those of the correspondingly numbered compounds of Table Al.
TABLE H69 Table H69 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2CF3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE H70 Table H70 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is cyano; R3 is GH2CF3; X is oxygen; Y is NR7; R7 is methyl; n isO; arid the values of RA match those of me correspondingly numbered compounds of Table Al.
TABLEH Table II provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al. "
TABLE 12 Table 12 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 13 Table 13 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE 14
Table 14 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; Bjus CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A \.
TABLE 15 Table 15 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 16 Table 16 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 17 Table 17 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is fluoro; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table ■ A1.
TABLE 18 Table 18 provides 352 compounds offbnmila (la) wherein R' is ethyl; R2 is chloro; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 19 Table 19 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE IIP Table II0 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is cyano; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 111


Table II1 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match flose of the correspondingly numbered compounds of Table Al.
TABLE 112 Table 112 provides 352 compounds of formula (la) wherein R' is methyl; R3 is fluoro; R3 is CH2C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 113 Table 113 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 114 Table 114 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 115 Table 115 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is CH2C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE 116 Table 116 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is hydrogen; R3 is CH2C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the corresponcungly numbered compounds of Table A1.
TABLE 117 Table 117 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE 118 Table 118 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R* match those of the correspondingly numbered compounds of Table A1.

TABLE 119
Table 119 provides 352 compounds of formula (la) wherein Rl is ethyl; R1 is bromo; R3 is CH2C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 120 Table 120 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 121 Table 121 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 122 Table 122 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2C03CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of TableAl.
TABLE123 Table 123 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is jchloro; R3 is CH2G02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 124 Table 124 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is bromo; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 125 Table 125 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 126


Table 126 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is hydrogen; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match t^se of the correspondingly numbered compound's of Table Al.
TABLE 127 Table 127 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 128 Table 128 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 129 Table 129 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 130 Table 130 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2C02CH3; X and Y are each oxygen;n isfl; andthe values of R4 match those of the correspondingly numbered compounds ofTable Al.
TABLE 131 Table 131 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds Of Table" Al.
TABLE 132 Table 132 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 133 Table 133 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE 134
Table 134 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is bromo; R3 is CH2C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 135 Table 135 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 136 Table 136 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 137 Table 137 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 138 Table 138 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is cbJoro; R3 is CH2C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 139 Table 139 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 140 Table 140 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is cyano; R3 is CH2C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE 143


Table 141 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is drogen; R3 is CH2C02CH3; X is oxygen; Y is NR1; R7 is hydrogen: n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE 142 Table 142 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 143 Table 143 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE 144 Table 144 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLEM5 Table 145 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CHiC02CH3; X is oxygen; Y is MR7; R7 is hydrogen; n is tyandthevalues^ofR'uiatch those of the correspondingly numbered compounds of Table Al.
TABLE 146 Table 146 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is hydrogen; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 147 Table 147 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE 148 Table 148 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.

TABLE 149
Table 149 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; OTs CH2C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE 150 Table 150 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 151 Table 151 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 152 Table 152 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is fluoro; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE 153 Table 153 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE 154 Table 154 provides 352 compounds of formula (lb) wherein Rl is methyl; R2 is bromo; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 155 Table 155 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE 156


Table 156 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is hydrogen; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of Rematch those of the correspondingly numbered compounds of Table A1.
TABLE 157 Table 157 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE 158 Table 158 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is chloro; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE 159 Table 159 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R' match those of the correspondingly numbered compounds of Table Al.
TABLE 160 Table 160 provides 352 jcompounds of formula (lb) wherein R1 is ethyl;*R? is cyano; R3 is CH2C02CH3; X is oxygen; Y isNR7;K7 is methyl; n is 0; and the values ofR- match those of the correspondmgJy numbered compounds of Table Al.
TABLE 161 Table 161 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al. ! '
TABLET62
Table 162 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n ist); and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 163 Table 163 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.

TABLE 164
Table 164 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 165 Table 165 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 166 Table 166 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 167 Table 167 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
VTABLE168 Table 168 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE 169 Table 169 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is bromo; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 170 Table 170 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Jl


Table Jl provides 352 compounds of formula (la) -wherein R1 is methyl; R: is hydrogen; R3 is CH2Ph; X and Y arc each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J2 Table J2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J3 Table J3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE J4 Table J4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CHjPh; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
/TABLE35 Table J5 provides 352 compounds offormula (la) wherein R' is methyl; R2 is cyano; R3 is CH2Ph; X and Y arc each oxygen; n is 0, and the values of R^ match "those of the correspondingly numbered compounds of Table Al.
TABLEJ6 Table J6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2Ph; X and Y are each oxygen; ivis 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J7 Table J7 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is fluoro; R3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE J8 Table J8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al;


TABLE J9
Table J9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; K3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J10 Table J10 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is cyano; R3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE Jll Table Jl 1 provides 352 compounds of formula (la) wherein R' is methyl; R2 is hydrogen; R3 is CH2Ph; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE J12
Table J12 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro;
R3 is CH2Ph; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the
conespondmgly ninnbered compounds of Table AL .
- TABLE 313
Table J13 provides 352 compounds of formula (la) wherein R' is methylvTR2 is chloro; R3 is CILPh; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Jl 4 Table J14 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2Ph;X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J15 Table J15 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R is CH2Ph; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE Jl 6


Table J] 6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2Ph; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Jl 7 Table Jl 7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CHjPh; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J18 Table Jl 8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2Ph; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Jl 9 Table J19 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is bromo; R3 is CH2Ph; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J20 Table J20 provides 352 compounds pf.fqnnula (la) wherein R1 is ethyl; R2 is cyano; R3 is CHjPh; X is oxygen; Y is sulphur, n is 0; and the values of R4match those of the correspondingly numbered compounds of Table Al.
TABLE J21 Table J21 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J22 Table J22 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J23 Table J23 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE J24
Table J24 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J25 Table J25 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J26 Table J26 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J27 Table J27 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CHjPh; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J28 Table J28 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J29 Table J29 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J30 Table J30 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2Ph; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J31


4
Table J31 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is ydrogen; R3 is CH2Ph; X is oxygen; Y is sulphur, n is 0; and the values of K match those of the correspondingly numbered compounds of Table Al.
TABLE J32 Table J32 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2Ph; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J33 Table J33 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2Ph; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J34 Table J34 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2Ph; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J35 Table J35 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is cyano; R3 is CH2Ph; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J36 Table J36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2Ph; X is oxygen; Y is sulphur; n is 0; and the values of RA match those of the correspondingly numbered compounds of Table Al.
TABLE J37 Table J37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2Ph; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J38 Table J38 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is chloro; R3 is CH2Ph; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE J39
Table J39 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2Ph; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J40 Table J40 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH,Ph; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J41 Table J41 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J42 Table J42 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2Ph; X is oxygen; Y isNR7; R7 is hydrogen;n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J43 Table J43 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J44 Table J44 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J45 Table J45 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J46


Table J46 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is .hydrogen; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J47 Table J47 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J48 Table J48 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE 349 Table J49 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is bromo; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE J50 Table J50 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 iscyano; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE J51 Table J51 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al'.
TABLE J52 Table J52 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J53 Table J53 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1,


TABLE J54
Table J54 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J55 Table J55 provides 352 compounds of formula (lb) wherein R! is methyl; R2 is cyano; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J56 Table J56 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J57 Table J57 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J58 Table J58 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 359 Table J59 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CHjPh; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J60 Table J60 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J61


Table J61 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J62 Table J62 provides 352 compounds-of formula (la) wherein R' is methyl; R2 is fluoro; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 363 Table J63 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J64 Table 364 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CrLPh; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLEJ65 Table J65 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2Pb; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J66 Table J66 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J67 Table J67 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J68 Table J68 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE J69
Table J69 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE J70 Table J70 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2Ph; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Kl Table Kl provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K2 Table K2 provides 352 compounds of formula (la) wherein R' is methyl; R2 is fluoro; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K3 Table K3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE K4 Table K4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE K5 Table K5 provides 352 compounds of formula (la) wherein R' is methyl; R2 is cyano; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K6


Table K6 provides 352 compounds of formula (la) wherein R1 is^ethyl; R2 is hydrogen; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K7 Table K7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K8 Table K8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K9 Table K9 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is bromo; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K10 Table K10 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Kll Table Kl 1 provides 352 compounds of formula (la) wherein Rl is methyl; R2 is hydrogen; R3 is CH2OCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K12 Table K12 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K13 Table K13 provides 352 compounds of formula (la) wherein R' is methyl; R2 is chloro; R3 is CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE K14
Table K14 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K15 Table K15 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K16 Table K16 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Kl 7 Table Kl 7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Kl 8 Table Kl 8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K19 Table Kl 9 provides 352 compounds of formula (la) wherein Rl is ethyl; R2 is bromo; R3 is CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K20 Table K20 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K21


Table K21 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is '
hydrogen; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R* match I those of the correspondingly numbered compounds of Table A1.
TABLE K22
Table K22 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K23 Table K23 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K24 Table K24 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K25 Table K25 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K26 Table K26 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K27 Table K27 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE K28 Table K28 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE K29
Table K29 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; RJ is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K30 Table K30 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K31 Table K31 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE K32 Table K32 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is fluoro; R3 is CH2OCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K33 Table K33 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K34 Table K34 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K35 Table K35 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K36


Table K36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K37 Table K37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R1 is CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K38 Table K38 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K39 Table K39 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is bromo; R3 is CH2OCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K40 Table K40 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is cyano; R3 is CH2OCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K41 Table K.41 provides 352 compounds of formula (lb) wherein R! is methyl; R2 is hydrogen; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K42 Table K42 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is fluoro; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K43 Table K43 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE K44
Table K44 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K45 Table K45 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K46 Table K46 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; h is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K47 Table K47 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K48 Table K48 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is chloro; R3 is CH2OCH3; X is oxygen; Y isNR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K49 Table K49 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K50 Table K50 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K51


Table K51 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE K52 Table K52 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is fluoro; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K53 Table K53 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K54 Table K54 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K55 Table K55 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K56 Table K56 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K57 Table K57 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K58 Table K58 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE K59
Table K59 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K60 Table K60 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K61 Table K61 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE K62 Table K62 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K63 Table K.63 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K64 Table K64 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K65 Table K65 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K66


Table K66 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K67 Table K67 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K68 Table K68 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is chloro; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K69 Table K69 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE K70 Table K70 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is cyano; R3 is CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE LI Table LI provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE L2 Table L2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE L3 Table L3 provides 352 compounds of formula (la) wherein R' is methyl; R2 is chloro; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE L4
Table L4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L5 Table L5 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L6 Table L6 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is hydrogen; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L7 Table L7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L8 Table L8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R- is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L9 Table L9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L10 Table L10 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE LI 1


Table LI 1 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L12 Table LI 2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L13 Table L13 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L14 Table LI 4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is brorno; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L15 Table L15 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE LI 6 Table LI 6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L17 Table LI 7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L18 Table LI 8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE LI 9
Table LI 9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L20 Table L20 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L21 Table L21 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L22 Table L22 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is
fluoro; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match
li'i those of the correspondingly numbered compounds of Table Al.
TABLE L23
Table L23 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L24 Table L24 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L25 Table L25 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L26


Table L26 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE L27 Table L27 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L28 Table L28 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE L29 Table L29 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE L30 Table L30 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE L31 Table L31 provides 352 compounds of formula (lb) wherein Rl is methyl; R2 is hydrogen; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L32 Table L32 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE L33 Table L33 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE L34
Table L34 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L35 Table L35 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L36 Table L36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L37 Table L37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L38 Table L38 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L39 Table L39 provides 352 compounds of formula (lb) wherein Rl is ethyl; R2 is bromo; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L40 Table L40 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L41


Table L41 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is .hydrogen; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values K of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L42 Table L42 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is fluoro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the coTrespondingty numbered compounds of Tabte A\.
TABLE L43 Table L43 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L44 Table L44 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
?TABLE L45 Table L45 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH2CHj; X is oxygen; Y is NR7; R7 is hydrogen; n is 0;~and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L46 Table L46 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L47 Table L47 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is CHjOCHjCH-,; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L48 Table L48 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE L49
Table L49 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo;
R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4
match those of the correspondingly numbered compounds of Table Al.
TABLE L50
Table L50 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano;
R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R"
match those of the correspondingly numbered compounds of Table Al.
TABLE L51
Table L51 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is
hydrogen; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of
R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L52
Table L52 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is
fluoro; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4
Hi match those of the correspondingly numbered compounds of Table Al.
TABLE L53
Table L53 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L54 Table L54 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L55 Table L55 provides 352 compounds of formula (lb) wherein Rl is methyl; R2 is cyano; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L56


Table L56 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L57 Table L57 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L58 Table L58 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L59 Table L59 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is bromo; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L6Q Table L60 provides 352 compounds of formula (lb) wherein Rl is ethyl; R2 is cyano; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L61 Table L61 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L62 Table L62 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L63 Table L63 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is i chloro; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE L64
Table L64 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L65 Table L65 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L66 Table L66 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numjbered compounds of Table A1.
TABLE L67 Table L67 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L68 Table L68 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L69 Table L69 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE L70 Table L70 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Ml
*

Table Ml provides 352 compounds of formula (la) wherein R' is methyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M2 Table M2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE M3 Table M3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M4 Table M4 provides 352 compounds of formula (la) wherein R' is methyl; R2 is bromo; R3 is CH2OCH2CH20CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M5
Table M5 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano
R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those
of the correspondingly numbered compounds of Table Al.
TABLE M6
Table M6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M7
Table M7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro;
R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M8 Table M8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match thos< of the correspondingly numbered compounds of Table Al.

TABLE M9
Table M9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M10 Table Ml 0 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Mil Table Ml 1 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M12 Table Ml 2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M13 Table M13 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M14 Table M14 provides 352 compounds of formula (la) wherein R' is methyl; R2 is bromo; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M15 Table Ml 5 provides 352 compounds of formula (la) wherein R' is methyl; R2 is cyano; R3 is CH2OCH2CH2OCR3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Ml6


Table Ml 6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M17 Table Ml 7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M18 Table M18 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 isCH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M19 Table Ml 9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M20 Table M20 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M21 Table M21 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M22 Table M22 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M23 Table M23 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE M24
Table M24 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M25 Table M25 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE M26 Table M26 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M27 Table M27 provides 352 compounds of formula (lb) wherein R1 is ethyl: R2 is fluoro; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M28 Table M28 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M29 Table M29 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE M30 Table M30 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH2CH2OCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M31

*

Table M31 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M32 Table M32 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE M33 Table M33 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M34 Table M34 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M35 Table M35 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Ah
TABLE M36 Table M36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M37 Table M37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M38 Table M38 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE M39
Table M39 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is bromo; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE M40 Table M40 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M41 Table M41 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M42 Table M42 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M43 Table M43 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M44 Table M44 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M45 Table M45 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M46


Table M46 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; RJ is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M47 Table M47 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M48 Table M48 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M49 Table M49 provides 352 compounds of formula (lb) wherein Rl is ethyl; R2 is bromo; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M50 Table M50 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M51 Table M51 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M52 Table M52 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M53 Table M53 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE M54
Table M54 provides 352 compounds of formula (lb) wheTein R' is methyl; R2 is bromo; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; RTis methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE M55 Table M55 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R5 is CH2OCH2CH2OCH3; X is oxygen; Y isNR1; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M56 Table M56 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M57 Table M57 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M58 Table M58 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 i match those of the correspondingly numbered compounds of Table Al.
TABLE M59
Table M59 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo;
R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4
match those of the correspondingly numbered compounds of Table Al.
i TABLE M60
Table M60 provides 352 compounds of formula (lb) wherein Rl is ethyl; R2 is cyano; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE M61

Table M61 provides 352 compounds of formula (la) wherein R' is methyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M62 Table M62 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE M63 Table M63 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M64 Table M64 provides 352 compounds of formula (la) wherein R1 is methyl; R3 is bromo; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M65 Table M65 provides 352 compounds of formula (lb) wherein R1 is methyl; R1 is cyano; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M66 Table M66 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M67 Table M67 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M68 Table M68 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE M69
Table M69 provides 352 compounds of formula (la) wherein R! is ethyl; R2 is bromo; R3 is CH2OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE M70 Table M70 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH3OCH2CH2OCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Nl Table Nl provides 352 compounds of formula (la) wherein R' is methyl; R2 is hydrogen; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE N2 Table N2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N3 Table N3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE N4 Table N4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N5 Table N5 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N6


Table N6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N7
Table N7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE N8 Table N8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N9 Table N9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is brorno; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N10 Table N10 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE Nil Table Nl 1 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH(CH3)2; X is oxygen; Y is sulphur, n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE N12 Table N12 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH(CH3)2; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N13 Table N13 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE N14
Table N14 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is Horomo; R3 is CH(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE N15 Table Nl 5 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is CH(CH3)2; X is oxygeir, Y is sulphur, n is 0; 2cnd the values of R" match those of the correspondingly numbered compounds of Table A1.
TABLE N16 Table Nl 6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH(CHj)j; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TA§LEN17 Table Nl 7 provides 352 compounds of formula (la) wherein R1 is ethyl; RJ is fiuoro; R3 is CH(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table
TABLE Nl 8 Table Nl 8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH(CH3)2; X is oxygen; V* is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N19 Table N19 provides 352 compounds of formula (la) wherein Rl is ethyl; R2 is bromo; R3 is CH(CH3)2; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N20 Table N20 provides 352 compounds of formula (la) wherein Rl is ethyl; R2 is cyano; R3 is CH(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N21

Table N21 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those , of the correspondingly numbered compounds of Table Al.
TABLE N22 Table N22 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is fluoro; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE N23 Table N23 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N24 Table N24 provides 352 compounds' of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N25 Table N25 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N26 Table N26 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N27 Table N27 provides 352 compounds of formula (lb) wherein R1 is ethyl;.R2 is fluoro; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N28 Table N28 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE N29
Table N29 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; W is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N30 Table N30 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N31 Table N31 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N32 Table N32 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N33 Table N33 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N34 Table N34 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N35 Table N35 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH(CH3)2; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N36


Table N36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N37 Table N37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N38 Table N38 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N39 Table N39 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N40 Table N40 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N41 Table N41 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N42 Table N42 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N43 Table N43 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE N44 Table N44 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE N45 Table N45 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE N46 Table N46 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of KA match those of the correspondingly numbered compounds of Table Al.
TA'BLEN47 Table N47 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N48 Table N48 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N49 Table N49 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE N50 Table N50 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N51

Table N5I provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al'.
TABLE N52 Table N52 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N53 Table N53 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N54 Table N54 provides 352 compounds'of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N55 Table N55 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH(CH3)j; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N56 Table N56 provides 352 compounds of formula (lb) wherein R' is ethyl; R? is hydrogen; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N57 Table N57 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N58 Table N58 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE N59
Table N59 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N60 Table N60 provides 352 compounds of formula (lb) wherein R1 is ethyl; RJ is cyano; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE N61 Table N61 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N62 Table N62 provides 352 compounds of formula (la) wherein R} is methyl; R2 is fluoro; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N63 Table N63 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CJ(CH3)2 X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE N64 Table N64 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N65 Table N65 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N66


Table N66 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N67 Table N67 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH(CH3)i; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N68 Table N68 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N69 Table N69 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE N70 Table N70 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 01 Table 01 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 02 Table 02 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q3 Table 03 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


Table 011 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those ^1 of the correspondingly numbered compounds of Table Al.
TABLE 012 Table 012 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE 013 Table 013 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 014 Table 014 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 015 Table 015 provides 352 compounds of formula (la) wherein Rl is methyl; R2 is cyano; R3 is C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 016 Table 016 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 017 Table 017 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q18 Table 018 provides 352 compounds of formula (la) wherein Rl is ethyl; R1 is chloro; 1 R3 is C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE 019
Table 019 provides 352 compounds of formula (la) wherein R1 is ethyl; R" is bromo; R3 is C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 020 Table 020 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 021 Table 021 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 022 Table 022 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is fluoro; R3 is C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q23 Table 023 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q24 Table 024 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q25 Table 025 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is cyano; R3 is C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q26


Table 026 provides 352 compounds of formula (lb) wherein R1 is ethyl: R2 is hydrogen; R3 is C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those Wthe correspondingly numbered compounds of Table Al.
TABLE 027 Table 027 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 028 Table 028 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is chloro; R3 is C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 029 Table 029 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE O30 Table 030 provides 352 compounds of formula (lb) wherein R! is ethyl; R2 is cyano; R3 is C02CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 031 Table 031 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 032 Table 032 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q33 Table 033 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE Q34
Table 034 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE 035 Table 035 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of KA match those of the correspondingly numbered compounds of Table Al.
TABLE Q36 Table 036 provides 352 compounds of formula (lb) wherein R1 is ethyl; R3 is hydrogen; R3 is C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 037 Table 037 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of K4 match those of the correspondingly numbered compounds' of Table A1.
TABLE Q38 Table 038 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q39 Table 039 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is C02CH3; X is oxygen; Y is sulphur; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE 040 Table 040 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is C02CH3; X is oxygen; Y is sulphur, n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE Q41

Table 041 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE 042 Table 042 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fjuoro; R3 is C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 043 Table 043 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CO:CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE Q44 Table 044 provides 352 compounds of formula (lb) wherein R is methyl; R2 is bromo; R3 is C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 045 Table 045 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 046 Table 046 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 047 Table 047 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 048 Table 048 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE Q49
Table 049 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE O50 Table O50 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is C02CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table A1.
TABLE Q51 Table 051 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q52 Table 052 provides 352 compounds of formula (lb) wherein Rl is methyl; R2 is fluoro; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE 053 Table 053 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q54 Table 054 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q55 Table 055 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q56

Table 056 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 057
Table 057 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 058
Table 058 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 059
Table 059 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
STABLE 06O
Table 060 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE 061
Table 061 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE 062
Table 062 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 063
Table 063 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE 064
Table 064 provides 352 compounds of formula (la) wherein R1 is methyl; R: is
romo; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4
match those of the correspondingly numbered compounds of Table Al.
TABLE 065
Table 065 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is
cyano; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match
those of the correspondingly numbered compounds of Table Al.
TABLE 066
Table 066 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is
hydrogen; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4
match those of the correspondingly numbered compounds of Table Al.
TABLE 067
Table 067 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro;
R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those
of the correspondingly numbered compounds of Table Al.
TABLE 068
Table 068 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 069 Table 069 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 070 Table 070 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is C02CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE PI


Table PI provides 352 compounds of formula (la) wherein R' is methyl; R1 is hydrogen; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P2 Table P2 provides 352 compounds of formula (la) wherein R1 is methyl; R" is fluoro; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P3
Table P3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; i R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1,
TABLE P4
Table P4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P5
Table P5 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P6
Table P6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P7 Table P7 provides 352 compounds of formula (la) wherein R1 is ethyl; R? is fluoro; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE P8
Table P8 provides 352 compounds of formula (la) wherein R' is ethyl; R3 is chloro; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE P9
Table P9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE F10 Table PI 0 provides 352 compounds of formula (la) wherein R' is ethyl; R7 is cyano; R^ is C02CB2CH3; X and Y are each oxygen; n is 0; and the values of 1C match those of the correspondingly numbered compounds of Table Al.
TABLE PI 1 Table PI 1 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P12
Table PI 2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is
fluoro; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those
y
of the correspondingly numbered compounds of Table Al.
TABLE P13 Table PI 3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Ah
TABLE P14 Table PI 4 provides 352 compounds of formula (la) wherein R' is methyl; R2 is bromo; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al,
TABLE PI 5 Table P15 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is C02CH3CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE PI6

Table PI 6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE PI 7 Table PI 7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P18 Table PI 8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is C03CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P19 Table PI 9 provides 352 compounds of formula (la) wherein R is ethyl; R2 is bromo; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P20 Table P20 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is C02CH2CH3; X is oxygen; Y is sulphur, n is 0; and the values of K* match those of the correspondingly numbered compounds of Table Al.
TABLE P21 Table P21 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P22 Table P22 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is fluoro; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P23 Table P23 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is chloro; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE P24
Table P24 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P25 Table P25 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is cyano; R1 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P26 Table P26 provides 352 compounds of formula (lb) wherein R1 is ethyl; R: is hydrogen; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P27 Table P27 provides 352 compounds of formula (lb) wherein Rl is ethyl; R2 is fluoro; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P28 Table P28 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chldro; R3 is C02CHjCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P29 Table P29 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is bromo; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P30 Table P30 provides 352 compounds of formula (lb) wherein R1 is ethyl; R3 is cyano; R3 is C02CH2CH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE P31

Table P31 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is
hydrogen; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match
those of the correspondingly numbered compounds of Table Al.
TABLE P32
Table P32 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is fluoro; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P33 Table P33 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE P34 Table P34 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is bromo; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P35 Table P35 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P36 Table P36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P37 Table P37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P38 Table P38 provides 352 compounds of formula (lb) wherein R! is ethyl; R2 is chloro; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE P39
Table P39 provides 352 compounds of formula (lb) wherein R1 is ethyl; R3 is bromo; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P40 Table P40 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is C02CH2CH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P41 Table P41 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P42
Table P42 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is
fluoro; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4
J i-fT- '"" ■: ' .'r'r
match those of-the correspondingly numbered compounds of Table Al.
TABLE P43 Table P43 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P44 Table P44 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P45 Table P45 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P46

Table P46 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of 1 R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P47 Table P47 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P48 Table P48 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P49 Table P49 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P50 Table P50 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P51 Table P51 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE P52 Table P52 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P53 Table P53 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE P54
Table P54 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P55 Table P55 provides 352 compounds of formula (lb) wherein R' is methyl; R3 is cyano; R3 is C02CH2CH3; X is oxygen; Y is NR1; R7 is methyl; n is 0; and the values of R' match those of the correspondingly numbered compounds of Table Al.
TABLE P56 Table P56 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is hydrogen; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P57 Table P57 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P58 Table P58 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and ihevalues of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P59 Table P59 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P60 Table P60 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P61

Table P61 provides 352. compounds of fonnula (la) wherein R1 is methyl; R2 is hydrogen; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P62 Table P62 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P63 Table P63 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P64 Table P64 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P65 Table P65 provides 352 compounds of fonnula (lb) wherein R1 is methyl; R2 is cyano; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P66 Table P66 provides 352 compounds of fonnula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P67 Table P67 provides 352 compounds of fonnula (la) wherein R1 is ethyl; R2 is fluoro; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE P68 Table P68 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE P69
Table P69 provides 352 compounds of formula (fa) wherein R' is ethyl; R2 is bromo; is C02CH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AJ.
TABLE P70 Table P70 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is COjCH2CH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE 01 Table Ql provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TAflt'E Q2 Table Q2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 03
Table Q3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 04
Table Q4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 05
Table Q5 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is CON(CHj),; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 06


Table Q6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE 07 Table Q7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the concspondm^lv numbered compounds of Table AL
TABLE 08 Table Q8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 09 Table Q9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE O10 Table Q10 provides 352 compounds of formula (la) wherein Rl is ethyl; R2 is cyano; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE Oil Table Ql 1 provides 352 compounds of formula (la) wherein R' is methyl; R2 is hydrogen; R3 is CON(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 012 Table Q12 provides 352 compounds of formula (la) wherein R1 is methyl; R3 is fluoro; R3 is CON(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 013 Table Q13 provides 352 compounds of formula (la) wherein H'1 is methyl; R* is chloro; R3 is CON(CH3)3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE Q14
Table Q14 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CON(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q15 Table Q15 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is CON(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE 016 Table Q16 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CON(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q17 Table Ql 7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CON(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q18 Table Q18 provides 352 compounds of formula (la) wherein Rl is ethyl; R2 is chloro; R3 is CON(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q19 Table Q19 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is bromo; R3 is CON(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE O20 Table Q20 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CON(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q21

,e Q21 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is , R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R* match the correspondingly numbered compounds of Table Al.
TABLE 022 Table Q22 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is joro; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 023 Table Q23 provides 352 compounds of formula (lb) wherein R1 is methyl; R1 is chJoro; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 024 Table Q24 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is bromo; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 025 Table Q25 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 026 Table Q26 provides 352 compounds of formula (lb) wherein R1 is ethyl; R1 is hydrogen; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 027 Table Q27 provides 352 compounds of formula (lb) wherein R" is ethyl; R2 is fiuoro; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q28 Table Q2B provides 352 compounds of formula (lb) wherein ft1, is ethyl; R1 is chloro; R3 is CON(CH3)2; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

Table Q36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CON(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R* match ' those of the correspondingly numbered compounds of Table Al.
TABLE 037 Table Q37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R3 is fluoro; R3 is CON(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 038 Table Q38 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CON(CH3)2; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 039 Table Q39 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is bromo; R3 is CON(CH3)2; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE O40 Table Q40 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CON(CH3)2; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 041 Table Q41 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 042 Table Q42 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 043 Table Q43 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is chloro; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE 044
Table Q44 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is Tromo; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q45 Table Q45 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 046 Table Q46 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE O47 Table Q47 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compdjmds of Table Al.
TABLE 048 Table Q48 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CON(CH3)j; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 049 Table Q49 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE 05Q Table Q50 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is cyano; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q51


Table Q51 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 r match those of the correspondingly numbered compounds of Table Al.
TABLE 052
' Table Q52 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is
fiuoro; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 053 Table Q53 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is chloro; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 054 Table Q54 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is bromo; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 055 Table Q55 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is cyano; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 056 Table Q56 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q57 Table Q57 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Q58 Table Q58 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE Q59
Table Q59 provides 352 compounds of formula (lb) wherein R5 is ethyl; R2 is bromo; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE O60 Table Q60 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 061 Table Q61 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 062 Table Q62 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is
fluoro; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4
match those of the correspondingly numbered compounds of Table Al.
TABLE 063
Table Q63 provides 352 compounds of formula (la) wherein R! is methyl; R2 is chloro; R3 is C0N(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 064 Table Q64 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CON(CH3)j; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 065 Table Q65 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 066

Table Q66 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE 067 Table Q67 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 068 Table Q68 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE 069 Table Q69 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE O70 Table Q70 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CON(CH3)2; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Rl Table Rl provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R2 Table R2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R3 Table R3 provides 352 compounds of formula (la) wherein R' is methyl; R2 is chloro; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE R4
Table R4 provides 352 compounds of formula (la) wherein R"1 is methyl; R^ is bromo; te3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R5 Table R5 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is CONtfCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R6 Table R6 provides 352 compounds of formula (la) wherein Rl is ethyl; R2 is hydrogen; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TSBLE R7 Table R7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of,Table A1.
TABLE R8 Table R8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CONHCH3; X and Y are each oxygen;.n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R9 Table R9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R10 Table R10 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CONHCH}; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R11

Table Rl 1 provides 352 compounds of formula (la) wherein Rl is methyl; R2 is hydrogen; R3 is CONHCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R12 Table R12 provides 352 compounds of formula (la) wherein R' is methyl; R2 is fluoro; R3 is CONHCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE R13 Table R13 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CONHCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R14 Table R14 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CONHCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R15 Table R15 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is CONHCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Rl 6 Table Rl 6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CONHCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R17 Table R17 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CONHCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE Rl 8 Table R18 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is chloro; R3 is CONHCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE R19
Table R19 provides 352 compounds of formula (la) wherein R1 is ethyl; R- is bromo; R3 is CONHCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R20 Table R20 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CONHCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE R21 Table R21 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R22 Table R22 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is
fluoro; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those
of the correspondingly numbered compounds of Table Al.
TABLE R23
Table R23 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R24 Table R24 provides 352 compounds of formula (lb) wherein Rl is methyl; R2 is bromo; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R25 Table R25 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R26

Table R26 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R27 Table R27 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R28 Table R28 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R29 Table R29 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R30 Table R30 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CONHCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R31 Table R31 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is CONHCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R32 Table R32 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is fluoro; R3 is CONHCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R33 Table R33 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CONHCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE R34
Table R34 provides 352 compounds of formula (lb) wherein R^ is methyl; R1 is bromo; R3 is CONHCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R35 Table R35 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CONHCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R36 Table R36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CONHCH3; X is oxygen; Y is sulphur; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE R37 Table R37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CONHCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R38 Table R38 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CONHCH3; X is oxygen; Y is sulphur, n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE R39 Table R39 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CONHCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R40 Table R40 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CONHCH3; X is oxygen; Y is sulphur; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE R41

TABLE R49
Table R49 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CONHCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE R50 Table R50 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CONHCH3; X is oxygen; Y is NR1; R7 is hydrogen; n is 0; and the values of R' match those of the correspondingly numbered compounds of Table Al.
TABLE R51 Table R51 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
" TA'BLE R52 Table R52 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CONHCH3; X is oxygen; Y isNR7; R7 is methyl; n is 0; and the values of R4
(;
match those of the correspondingly numbered compounds of Table Al.
TABLE R53 Table R53 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE RS4 Table R54 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R55 Table R55 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CONHCH3; X is oxygen; Y isNR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R56

Table R56 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen;;R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of RJ match those of the correspondingly numbered compounds of Table Al.
TABLE R57
Table R57 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is CONHCHj; X is oxygen; Y is NR1; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R58
Table R58 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R59
.> *^, Table R59 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo;
R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match
those of the correspondingly numbered compounds of Table Al.
TABLE R60
Table R60 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano;
R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match
those of the correspondingly numbered compounds of Table Al.
TABLE R61
Table R61 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is
hydrogen; R3 is CONHCH/, X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4
match those of the correspondingly numbered compounds of Table Al.
TABLE R62
Table R62 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is
fluoro; R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4
match those of the correspondingly numbered compounds of Table Al.
TABLE R63
Table R63 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is
chloro; R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4
match those of the correspondingly numbered compounds of Table Al.

TABLE R64
Table R64 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is
bromo; R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4
match those of the correspondingly "numbered compounds of Table Al.
TABLE R65
Table R65 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is
cyano; R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4
match those of the correspondingly numbered compounds of Table Al.
TABLE R66
Table R66 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is
hydrogen; R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4
match those of the correspondingly numbered compounds of Table Al.
TABLE R67
Table R67 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro;
R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match
■% those of the correspondingly numbered compounds of Table Al.
TABLE R68
Table R68 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R69 Table R69 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE R70 Table R70 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is cyano; R3 is CONHCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE SI


Table SI provides 352 compounds of formula (la) wherein R' is methyl; R2 is hydrogen; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S2 Table S2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S3 Table S3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S4 Table S4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
* TABLE S5 Table S5 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S6 Table S6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S7 Table S7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S8 Table S8 provides 352 compounds of formula (la) wherein R' is ethyl; R7 is chloro; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE S9
Table S9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE SI 0 Table S10 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLESH Table SI 1 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is CH2SCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S12 Table S12 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2SCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S13 Table SI 3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S14 Table S14 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE SI 5 Table S15 provides 352 compounds of formula (la) wherein R' is methyl; R2 is cyano; R3 is CH2SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S3 6


Table SI 6 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is hydrogen; R3 is CH2SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE SI7 Table S17 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE SI 8 Table SI 8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2SCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S19 Table S19 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S20 Table S20 provides 352 compounds of formula (la) wherein Rl is ethyl; R2 is cyano; R3 is CH2SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLES2I Table S21 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S22 Table S22 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S23 Table S23 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE S24
Table S24 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S25 Table S25 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S26 Table S26 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S27 Table S27 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro;
R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the
Hi correspondingly numbered compounds of Table A1.
TABLE S28
Table S28 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S29 Table S29 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S30 Table S30 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S31


Table S31 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S32 Table S32 provides 352 compounds of formula (lb) wherein R1 is methyl; R3 is fluoro, R3 is CH2SCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S33 Table S33 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is CH2SCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S34 Table S34 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is CH2SCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
■ TABLES35 Table S35 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2SCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S36 Table S36 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is hydrogen; R3 is CH2SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S37 Table S37 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is CH2SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S38 Table S38 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.

TABLE S54 Table S54 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is bromo; R3 is CH2SCH3; X is oxygen; Y is NR1; R7 is methyl; n is 0; and the values of R' match those of the correspondingly numbered compounds of Table Al.
TABLE S55 Table S55 provides 352 compounds of formula (lb) wherein R1 is methyl; R: is cyano; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE S56 Table S56 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
J£&BLE_S57 Table S57 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S58 Table S58 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is chloro; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S59 Table S59 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE S60 Table S60 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE S61


Table S46 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S47 Table S47 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is CH2SCH3; X is oxygen; Y is NR1; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S48 Table S48 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S49 Table S49 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
' TABLE S50 Table S50 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is cyano; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE SSI Table S51 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S52 Table S52 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S53 Table S53 provides 352 compounds of formula (lb) wherein R! is methyl; R2 is chloro; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


Table S61 provides 352 compounds of formula (la) wherein R' is methyl; R2 is hydrogen; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S62 Table S62 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S63 Table S63 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S64 Table S64 provides 352 compotin&S'of formula (la) wherein R1 is methyl; R2 is bromo; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
'TABLE S65 Table S65 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S66 Table S66 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is hydrogen; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S67

Table S67 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S68
Table S68 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE S69
Table S69 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE S70 Table S70 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is CH2SCH3; X is oxygen; Y is NR7; R7 is methyl; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE Tl Table Tl provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
- f ABLE T2 Table T2 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compoundsfbf Table Al.
TABLE T3 Table T3 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is SCH3; X and Y are eachtoxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE T4 Table T4 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T5 Table T5 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T6


Table T6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T7 Table T7 provides 352 compounds of formula (la) wherein R1 is ethyl; R3 is fluoro; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T8 Table T8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T9 Table T9 provides 352 compoundS?OFformula (la) wherein R1 is ethyl; R2 is bromo; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
STABLE TIP Table T10 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Til Table Tl 1 provides 352 compounds of formula 0a) wherein R1 is methyl; R2 is hydrogen; R3 is SCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T12 Table T12 provides 352 compounds of formula (la) wherein R' is methyl; R2 is fluoro; R3 is SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE T13 Table T13 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLETl4
Table T14 provides 352 compounds of formula (la) wherein R' is methyl; R2 is bromo; R3 is SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Tl 5 Table Tl 5 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Tl 6 Table Tl 6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TKBLET17 Table T17 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compoundsfcf Table Al.
TABLE Tl 8 Table Tl 8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is SCH3; X is oxygen; Y is^sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE Tl 9 Table T19 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table AL
TABLE T20 Table T20 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T21


Table T21 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T22 Table T22 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T23 Table T23 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T24 Table T24 provides 352 compouutisNjf formula (lb) wherein R1 is methyl; R2 is bromo; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
STABLE T25 Table T25 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T26 Table T26 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T27 Table T27 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is fluoro; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R" match those of the correspondingly numbered compounds of Table Al.
TABLE T28 Table T28 provides 352 compounds of formula (lb) wherein R" is ethyl; R2 is chloro; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE T29
Table T29 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T30 Table T30 provides 352 compounds of formula (lb) wherein R' is ethyl; R2 is cyano; R3 is SCH3; X and Y are each oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T31 Table T31 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is hydrogen; R3 is SCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
fXBLE T32 Table T32 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds/of Table Al.
TABLE T33 Table T33 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is SCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T34 Table T34 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is SCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T35 Table T35 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is SCH3; X is oxygen; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T36

Table T36 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T37 Table T37 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T38 Table T38 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T39 Table T39 provides 352 compound of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
•1 TABLE T40 Table T40 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is SCH3; X is oxygen; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T41 Table T41 provides 352 compounds of formula (lb) wherein R' is methyl; R2 is hydrogen; R3 is SCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE T42 Table T42 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is fluoro; R3 is SCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T43 Table T43 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is chloro; R3 is SCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.


TABLE T44
Table T44 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is bromo; R3 is SCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T45 Table T45 provides 352 compounds of formula (lb) wherein R1 is methyl; R2 is cyano; R3 is SCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T46 Table T46 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is hydrogen; R3 is SCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TWBLE T47 Table T47 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is fluoro; R3 is SCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T48 Table T48 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is chloro; R3 is SCH3; X is oxygen; Y isNR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T49 Table T49 provides 352 compounds of formula (lb) wherein R1 is ethyl; R2 is bromo; R3 is SCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE T50 Table T50 provides 352 compound's of formula (lb) wherein R1 is ethyl; R2 is cyano; R3 is SCH3; X is oxygen; Y is NR7; R7 is hydrogen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE TS1
3LuifdVof formula (la) wherein R' is methyl; R2 is bromo; R3 is hydrogen; X is sulphur; Y is oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE V5 Table V5 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is cyano; R3 is hydrogen; X is sulphur; Y is oxygen; ri is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE V6 Table V6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is hydrogen; X is sulphur; Y is oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE V7 Table V7 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is fluoro; R3 is hydrogen; X is sulphur; Y is oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE V8 Table V8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is hydrogen; X is sulphur; Y is oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

TABLE V9
Table V9 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is bromo; R3 is hydrogen; X is sulphur; Y is oxygen; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE VI0 Table VI0 provides 352 compounds of formula (la) wherein R' is ethyl; R2 is cyano; R3 is hydrogen; X is sulphur; Y is oxygen; n is 0; and the values of R* match those of the correspondingly numbered compounds of Table Al.
TABLE VI1 Table VI1 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is hydrogen; R3 is hydrogen; X is sulphur; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE V12 Table V12 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is fluoro; R3 is hydrogen; X is sulphur; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE V13 Table V13 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is chloro; R3 is hydrogen; X is sulphur; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE VI4 Table V14 provides 352 compounds of formula (la) wherein R1 is methyl; R2 is bromo; R3 is hydrogen; X is sulphur, Y is sulphur; n is 0; and the values of R4 match those oi the correspondingly numbered compounds of Table Al.
TABLE V15 Table V15 provides 352 compounds of formula (la) wherein R' is methyl; R2 is cyano; R3 is hydrogen; X is sulphur, Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE VI6

Table VI6 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is hydrogen; R3 is hydrogen; X is sulphur; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE VI7 Table V] 7 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is fluoro; R3 is hydrogen; X is sulphur; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table A1.
TABLE VI8 Table VI8 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is chloro; R3 is hydrogen; X is sulphur; Y is sulphur, n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
TABLE VI9 Table VI9 provides 352 compounds of formula (la) wherein R is ethyl; R is bromo; R3 is hydrogen; X is sulphur; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.
%ABLEV20 Table V20 provides 352 compounds of formula (la) wherein R1 is ethyl; R2 is cyano; R3 is hydrogen; X is sulphur; Y is sulphur; n is 0; and the values of R4 match those of the correspondingly numbered compounds of Table Al.

The following abbreviations are used throughout this description:
mp = melting point ppm = parts per million
s = singlet b = broad
d= doublet dd = doublet of doublets
t = triplet
m = multiplet T _
q = quartet
AH = coupling constant between atom A and atom B

Table W shows selected melting point and selected NMR data all with CDCI,as the solvent (unless otherwise sated; if a mixture of solvents is present, this is indicated as for example, (CDO, / dt-DMSO)), (no anentp, is made to lis. al, characterising data in allcases)

for compounds of Tables Al, A3, A4, A5, A8, A13, A23, A43, B3, C3, D3, E3, F35 H3, K3, L3,M3,N3andV3. '
Table W



^^_\%-»


-a\^

—V^o -—


A compound of formula (I) may be prepared by acylating a compound of formula (II) with a compound of formula (III), preferably in the presence of a known coupling agent such as 13-dicyclohexylcarbodiimide, 1,3-diisopropylcarbodiirnide or l-(3-dimethy]aminopropyl)-3-ethy]carbodiimide. Alternatively a compound of formula (III) may first be converted to an acid chloride, anhydride OT chloroformate suitable for reaction with an amine to form an amide; such procedures are well known and are described, for example, in J. March, Advanced Organic Chemistry, Third Edition, John Wiley and Sons, New York, 1985, pages 370-376 and references therein.
Compounds of formula (II) are either known compounds or may be prepared from commercially available starting materials by methods described in the literature (see, for example, C. Oliver Kappe, Robert Flammang, and Curt Wentrup, Heterocycles, Vol. 37, No. 3,1615, (1994); A. Adams and R. Slack, J. Chem. Soc, 3061, (1959); and Ronald E Hackler.


Kenneth W. Burow, Jr., Sylvester V. Kaster and David I. Wickiser, J. Heterocyclic Chem, 26,1575,(1989)).
A compound of formula (III) may be prepared by hydrolysis of the corresponding compound of formula (IV) (whereinR is preferably C1-6 alkyl) by a method known in the art. A compound of formula (IV) may be hydrolysed under neutral, basic or acidic conditions, the reaction conditions are chosen such that substituent R4 is unchanged during the hydrolysis reaction. Compounds of formula (IV) capable of ready hydrolysis under different conditions are known in the literature and suitable compounds of formula (IV) may be selected, for example, by reference to Theodora W. Greene, Protective Groups in Organic Synthesis, Chapter 5, John Wiley and Sons, New York, 1981.
A "compound of formula (IV) may be prepared from a compound of formula (V) under conditions described in the literature (see, for example, David W. Dunwell, Delme Evans, Terence A. Hicks, J. Med. Chem'.,*1075, Vol. 18, No. 1, 53; Abdou 0. Abdelhamid, Cyril Parkanyi, S.M. Khaledur Rashid and Winston D. Lloyd, J. Heterocyclic Chem., 25, 403, (1988); Teruyuki Kondo, Sungbong Yang, Keun-Tae Huh, Masanobu Kobayasbi, Shinju Kotachi and Yoshihisa Watanabl, Chemistry Letters, 1275-1278, 1991; Dale L. Boger, J. Org. Chem., 43, No 11,2296,1978 ). The substituent R4 may be an atom or group which itself may be converted into other functional groups; procedures are known in the literature for such transformations involving benzoxazoles and benzothiazoles (for example, Lazer, Edward S., Adams, Julian; Miao, Clara K.; Farina, Peter, Eur. Pat. Appl. EP0535521). Alternatively R4 may contain atoms or groups which may be replaced by other moieties under known conditions.
A compound of formula (V) may be prepared by reduction of a compound of formula (VI) and such procedures are known in the art (see, for example, J. March, Advanced Organic Chemistry, Third Edition, John Wiley and Sons, New York, 1985, and references therein). A compound of formula (VI), wherein Y is oxygen, may be prepared by the nitration of a compound of formula (VII) under known conditions. A compound of formula (VI), wherein Y is sulfur, may be prepared from a compound of formula (VI), wherein Y is oxygen, using conditions similar to those described by J. Scheigetz, R. Zamboni and B. Roy, Synth. Commun., 25 (1995) (18), pages 2791-2806. A compound of formula (VI), wherein Y

is nitrogen, may be prepared from a compound of formula (VII) by a sequence of acylation, nitration and deacylation; using conditions known in the art.
Compounds of formula (VII) are either commercially available compounds or may be made from commercially available materials by known methods.
Alternatively, a compound of formula (I) may be prepared by treating a compound of formula (VIII) with, for example, an acid in the presence of a coupling reagent, an orthoester, acid chloride, hydroxyimoyl chloride or an alcohol in the presence of a ruthenium catalyst as described previously for the preparation of a compound of formula (IV).
A compound of formula (VIII) may be obtained by reduction of a compound of fonnula (IX), itself obtained from a compound of formula (X) using the procedures described above for the transformation of a compound of formula (VII) to a compound of formula (V).
A compound of formula (X) may be prepared by reacting a compound of formula (VII) with a compound of formula (IT) in a manner analogous to that described above for the transformation of a compound of formula (III) to a compound of formula (I).
Alternatively, a compound of formula (X), wherein Y is oxygen, may be obtained by reacting a compound of fonnula (XT), wnerein Y is oxygen, with a suitable reagent such as boron tribromide, hydriodic acid or another suitable reagent, as described by Theodora W. Greene, Protective Groups in Organic Synthesis, Chapter 1, John Wiley and Sons, New York, 1981.
A compound of formula (XI), wherein Y is oxygen, may be prepared by coupling a compound of formula (II) with a compound of formula (XII), wherein Y is oxygen, in a manner analogous to that described above for the transformation of a compound of formula (III) to a compound of formula (I).
Compounds of fonnula (XII), wherein Y is oxygen, are known compounds.
An alternative method for preparing a compound of formula (TV), wherein Y is sulfur, involves the cyclisation of a a compound of formula (XIII) wherein Z is a halogen (such as fluorine, chlorine or bromine) as described, for example, in Comprehensive Heterocyclic Chemistry, Volume 6, Ed. Katritzky and Rees, Pergamon Press, 1984. A compound of formula (XIII) may be prepared by reacting a compound of fonnula (XIV) with 2,4-bis(4~methoxyphenyl)-1,3-dithia-2,4-diphosphetane-2,4-disulfide (Lawesson's reagent) or phophorus pentasulfide in a solvent such as toluene. A compound of formula (XIV) may

be derived from a compound of formula (XIV) by nitration followed by reduction of the resultant nitrohalobenzene compound and subsequent acylation of the resultant aminohalobenzene compound, using procedures well known to those skilled in the art.
Compounds of formula (XV) are commercially available or may be made from commercially available materials using known methods.
A compound of formula (III), wherein n is zero, may also be prepared by halogenation of a compound of formula (XVI) followed by displacement of the resultant compound of formula (XVII) (where Hal is chloro or bromo) with cyanide. Hydrolysis of the resultant compound of formula (XVIII) gives a compound of formula (III).
Treatment of a compound of formula (I), wherein R3 is hydrogen, with an alkylating
or acylating agent, optionally in the presence of a base and a phase transfer catalyst, provides
a compound of formula (I), wherein R3 is an alkyl or acyl group. Examples of suitable
alkylating agents include, but are not restricted to, alkyl haudes (such as methyl iodide) and
alkyl sulfates (such as dimethylsulfate). Suitable acylating agents include anhydrides (such
as acetic anhydride), acid chlorides (such as acetyl chloride or benzoyl chloride) and
chlorofonnates (such as ethyl chloroformate). Suitable bases include organic bases (such as
triethylamine or pyridine), alkali metal alkoxides (such as potassium /er/-butoxide) and
inorganic bases (such as sodium hydride or sodium hydroxide). Suitable phase transfer
catalysts may be selected by reference to the literature (see, for example, J. March, Advanced
Organic Chemistry, Third Edition, John Wiley and Sons, New York, 1985, pages 320-322
and references therein).
A compound of formula (I), wherein X is sulphur, may be prepared by reacting a compound of formula (I), wherein X is oxygen, with 2,4-bis(4-methoxyphenyl)-l,3-dithia-2,4-diphosphetane-2,4-disulfide (Lawesson's reagent) or phophorus pentasulfide in a solvent such as toluene.
The compounds of formula (I) can be used to combat and control infestations of insect pests such as Lepidoptera, Diptera, Hemiptera, Thysanoptera, Orthoptera, Dictyoptera, Coleoptera, Siphonaptera, Hymenoptera and Isoptera and also other invertebrate pests, for example, acarine, nematode and mollusc pests. Insects, acarines, nematodes and molluscs are hereinafter collectively referred to as pests. The pests which may be combated and controlled by the use of the invention compounds include those pests associated with

agriculture (which term includes the growing of crops for food and fibre products), horticulture and animal husbandry, companion animals, forestry and the storage of products of vegetable origin (such as fruit, grain and timber); those pests associated with the damage of man-made structures and the transmission of diseases of man and animals; and also nuisance pests (such as flies).
Examples of pest species which may be controlled by the compounds of formula (I) include: Myzuspersicae (aphid), Aphis gossypii (aphid), Aphisfabae (aphid), Lygus spp. (capsids), Dysdercus spp. (capsids), Nilaparvata lugens (planthopper), Nephotettixc inciiceps (leafhopper), Nezara spp. (stinkbugs), Euschistus spp. (stinkbugs), Leptocorisa spp. (stinkbugs), Franldiniella occidentalis (thrip), Thrips spp. (thrips), Leptinotarsa decemlineata (Colorado potato beetle), Anthonomus grandis (boll weevil), Aonidiella spp. (scale insects), Trialeurodes spp. (white flies), Bemisia tabaci (white fly), Ostrinia nubilalis (European com borer), Spodoptera littoralis (cotton leafworm), Heliothis virescens (tobacco budworm), Helicoverpa armigera (cotton bollworm), Helicoverpa zea (cotton bollworm), Sylepta derogata (cotton leaf roller), Pieris brassicae (white butterfly), Plutella xylostella (diamond back moth), Agrotis spp. (cutworms), Chilo suppressalis (rice stem borer), Locusta migratoria (locust), Chortiocetes termini/era (locust), Diabrotica spp. (rootworms), Panonychus ulmi (European red mite), Panonychus citri (citrus red mite), Tetranychus urticae (two-spotted spider mite), Tetranychus cinnabarinus (carmine spider mite), Phyllocoptrma oleivora (citrus rust mite), Polyphagotarsonemus latus (broad mite), Brevipalpus spp. (flat mites), Boophilus microplus (cattle tick), Dermacentor variabilis (American dog tick), Ctenocephalides felis (cat flea), Liriomyza spp. (leafminer), Musca domestica (housefly), Aedes aegypti (mosquito), Anopheles spp. (mosquitoes), Culex spp. (mosquitoes), Lucillia spp. (blowflies), Blattella germanica (cockroach), Periplaneta americana (cockroach), Blatta orientalis (cockroach), termites of the Mastotermilidae (for example Mastotermes spp.), the Kalotermitidae (for example Neotermes spp.), the RHnotermitidae (for example Coptotermesformosanus, Reticulitermes flavipes, R speratu, R. virginicus, R. hesperus, and R santonensis) and the Termitidae (for example Ghbiiermes sulphweiis), Soknopsis geminate (fire ant), Monomorium pharooms (pharaoh'sam), Damalinia spp. and Linognathus spp. (biting and sucking lice), Meloidogyne spp. (root knot nematodes), Globodera spp. and Heterodera spp. (cyst nematodes), Pratylenchus spp.


(lesion nematodes), Rhodopholus spp. (banana burrowing nematodes), Tylenchulus spp.(citrus nematodes), Haemonchus contortus (barber pole worm), Caenorhabditis elegans (vinegar eelworm), Trichostrongylus spp. (gastro intestinal nematodes) and Deroceras reticulatum (slug).
The compounds of formula (1) are also active fungicides and may be used to control one or more of the following pathogens: Pyriculaha oryzae {Magnaporthe grisea) on rice and wheat and other Pyricularia spp. on other hosts; Puccinia recondita, Puccinia striiformis and other rusts on wheat, Puccinia hordei, Puccinia striiformis and other rusts on barley, and rusts on other hosts (for example turf, rye, coffee, pears, apples, peanuts, sugar beet, vegetables and ornamental plants); Erysiphe cichoracearum on cucurbits (for example melon); Erysiphe graminis (powdery mildew) on barley, wheat, rye and turf and other powdery mildews on various hosts, such dxSphaerotheca macularis on hops, Sphaerotheca juliginea on cucurbits (for example cucumber), Leveillula taurica on tomatoes, aubergine and green pepper, Podosphaera leucotricha on apples and Uncinula necator on vines; Cochliobolus spp., Helminthosporium spp., Drechslera spp. (Pyrenophora spp.), Rhynchosporium spp., Mycosphaerellagrammicola (Septoria tritici) and Phaeosphaeria nodorum (Stagonospora nodorum or Septoria nodosum), Pseudocercosporella herpotrichoides and Gaeumannomyces graminis on cereals (for example wheat, barley, rye), turf and other hosts; Cercospora arachidicola and Cercosporidium personatum on peanuts and other Cercospora spp. on other hosts, for example sugar beet, bananas, soya beans and rice; Botrytis cinerea (grey mould) on tomatoes, strawberries, vegetables, vines and other hosts and other Botrytis spp. on other hosts; Alternaria spp. on vegetables (for example carrots), oil-seed rape, apples, tomatoes, cereals (for example wheat) and other hosts; Venturia spp. (including Venturia inaequalis (scab)) on apples, pears, stone fruit, tree nuts and other hosts; Cladosporium spp. on a range of hosts including cereals (for example wheat) and tomatoes; Monilinia spp. on stone fruit, tree nuts and other hosts; Didymella spp. on tomatoes, turf, wheat and other hosts; Phoma spp. on oil-seed rape, turf, rice, potatoes, wheat and other hosts; Aspergillus spp. and Aureobasidium spp. on wheat, lumber and other hosts; Ascochyta spp. on peas, wheat, barley and other hosts; Stemphylium spp. (Pleospora spp.) on apples, pears, onions and other hosts; summer diseases (for example bitter rot {Glomerella cingulata), black rot or frogeye leaf spot (Botryosphaeria obtusa). Brooks fruit spot


(Mycosphaerella pomf), Cedar apple rust {Gymnosporangiumjunipeh-virginianae), sooty blotch (Gloeodes potnigena), flyspeck {Schizothyrium pomi) and white rot {Botryosphaeria dothidea)) on apples and pears; Plasmopara viticola on vines; other downy mildews, such as Bremia lactucae on lettuce, Peronospora spp. on soybeans, tobacco, onions and other hosts, Pseudoperonospora humuli on hops and Pseudoperonospora cubensis on cucurbits; Pythium spp. (including Pythium ultimum) on turf and other hosts; Phytophthora infesians on potatoes and tomatoes and other Phytophthora spp. on vegetables, strawberries, avocado, pepper, ornamentals, tobacco, cocoa and other hosts; Thanatephorus cucumeris on rice and turf and other Rhizoctonia spp. on various hosts such as wheat and barley, peanuts, vegetables, cotton and turf; Sclerotinia spp. on turf, peanuts, oil-seed rape and other hosts; Sclerotium spp. on turf, peanuts and other hosts; Gibberella Jujikuroi on rice; Colletotrichum spp. on a range of hosts including turf, coffee and vegetables; Laetisaria fuciformis on turf; Mycosphaerella spp. on bananas, peanuts, citrus, pecans, papaya and other hosts; Diaporthe spp. on citrus, soybean, melon, pears, lupin and other hosts; Elsinoe spp. on citrus, vines, olives, pecans, roses and other hosts; Verticillium spp. on a range of hosts including hops, potatoes and tomatoes; Pyrenopeziza spp. on oil-seed rape and other hosts; Oncobasldium theobromae on cocoa causing vascular streak dieback; Fusarium spp., Typhula spp., Microdochium nivale, Ustilago spp., Urocystis spp., Tilletia spp. and Claviceps purpurea on a variety of hosts but particularly wheat, barley, turf and maize; Ramularia spp. on sugar beet and other hosts; post-harvest diseases particularly of fruit (for example Penicillium digitatum, Penicillium italicum and Trichoderma viride on oranges, Colletotrichum musae and Gloeosporium musarum on bananas and Botrytis cinerea on grapes); other pathogens on vines, notably Eutypa lata, Guignardia bidwellii, Phellinus igniarus, Phomopsis viticola, Pseudopeziza tracheiphila and Stereum hirsutum; other pathogens on trees (for example Lophodermium seditiosum) or lumber, notably Cephaloascus fragrans, Ceratocystis spp., Ophiostoma piceae, Penicillium spp., Trichoderma pseudokoningii, Trichoderma viride, Trichoderma harzianum, Aspergillus niger, Leptographium lindbergi and Aureobasidiumpullulans; and fungal vectors of viral diseases (for example Polymyxa graminis on cereals as the vector of barley yellow mosaic virus (BYMV) and Polymyxa betae on sugar beet as the vector of rhizomania).

A compound of formula (I) may move acropetally, basipetally or locally in plant . tissue to be active against one or more fungi. Moreover, a compound of formula (!) may be volatile enough to be active in the vapour phase against one or more fungi on the plant.
The invention therefore provides a method of combating and controlling insects, acarines, nematodes or molluscs which comprises applying an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula (I), or a composition containing a compound of formula (I), to a pest, a locus of pest, or to a plant susceptible to attack by a pest, and a method of combating and controlling fungi which comprises applying a fungicidally effective amount of a compound of formula (I), or a composition containing a compound of formula (I), to a plant, to a seed of a plant, to the locus of the plant or seed or to soil. The compounds of formula (I) are preferably used against insects, acarines, nematodes or fungi.
The term "plant" as used herein includes seedlings, bushes and trees. Furthermore, the fungicidal method of the invention includes protectant, curative, systemic, eradicant and antisporulant treatments.
As fungicides, the compounds of formula (I) are preferably used for agricultural, horticultural and turfgrass purposes in the form of a composition.
In order to apply a compound of formula (I) as an insecticide, acaricide, nematicide or molluscicide to a pest, a locus of pest, or to a plant susceptible to attack by a pest, or, as a fungicide to a plant, to a seed of a plant, to the locus of the plant or seed or to soil, a compound of formula (I) is usually formulated into a composition which includes, in addition to the compound of formula (I), a suitable inert diluent or carrier and, optionally, a surface active agent (SFA). SFAs are chemicals which are able to modify the properties of an interface (for example, liquid/solid, liquid/air or liquid/liquid interfaces) by lowering the interfacial tension and thereby leading to changes in other properties (for example dispersion, emulsification and wetting). It is preferred that all compositions (both solid and liquid formulations) comprise, by weight, 0.0001 to 95%, more preferably 1 to 85%, for example 5 to 60%, of a compound of formula (I). The composition is generally used for the control of pests or fungi such that a compound of formula (I) is applied at a rate of from O.lg tolOkg per hectare, preferably from lg to 6kg per hectare, more preferably from lg to 1kg per hectare.

When used in a seed dressing, a compound of formula (I) is used at a rate of 0.000 lg to lOg (for example 0.001 g or 0.05g), preferably 0.005g to lOg, more preferably 0.005g to 4g, per kilogram of seed.
In another aspect the present invention provides an insecticidal, acaricidal, nematicidal, molluscicidal or fungicidal composition comprising an'insecticidally, acaricidally, nematicidally, molluscicidally or fungicidally effective amount of a compound of formula (I) and a suitable carrier or diluent therefor. The composition is preferably an insecticidal, acaricidal, nematicidal or fungicidal composition.
In a still further aspect the invention provides a method of combating and controlling pests or fungi at a locus which comprises treating the pests or fungi or the locus of the pests or fungi with an insecticidally, acaricidally, nematicidally, molluscicidally or fungicidally effective amount of a composition comprising a compound of formula (I). The compounds of formula (I) are preferably used against insects, acannes, nematodes or fungi.
The compositions can be chosen from a number of formulation types, including dustable powders (DP), soluble powders (SP), water soluble granules (SG), water dispersible granules (WG), wettable powders (WP), granules (GR) (slow or fast release), soluble concentrates (SL), oil miscible liquids (OL), ultra low volume liquids (UL), emulsifiable concentrates (EC), dispersible concentrates (DC), emulsions (both oil in water (EW) and water in oil (EO)), micro-emulsions (ME),, suspension concentrates (SC), aerosols, fogging/smoke formulations, capsule suspensions (CS) and seed treatment formulations. The formulation type chosen in any instance will depend upon the particular purpose envisaged and the physical, chemical and biological properties of the compound of formula
(I)-
Dustable powders (DP) may be prepared by mixing a compound of formula (I) with one or more solid diluents (for example natural clays, kaolin, pyrophyllite, bentonite, alumina, montmorillonite, kieselguhr, chalk, diatomaceous earths, calcium phosphates, calcium and magnesium carbonates, sulphur, lime, flours, talc and other organic and inorganic solid carriers) and mechanically grinding the mixture to a fine powder.
Soluble powders (SP) can be prepared by mixing a compound of formula (I) with one or more water-soluble inorganic salts (such as sodium bicarbonate, sodium carbonate or magnesium sulphate) or one or more water-soluble organic solids (such as a polysaccharide)

and, optionally, one or more wetting agents, one or more dispersing agents or a mixture of said agents to improve water dispersibility/solubility. The mixture is then ground to a fine powder. Similar compositions may also be granulated to form water soluble granules (SG).
Wettable powders (WP) can be prepared by mixing a compound of formula (I) with one or more solid diluents or carriers, one or more wetting agents and, preferably, one or more dispersing agents and, optionally, one or more suspending agents to facilitate the dispersion in liquids. The mixture is then ground to a fine powder. Similar compositions may also be granulated to form water dispersible granules (WG).
Granules (GR) may be formed either by granulating a mixture of a compound of formula (I) and one or more powdered solid diluents or carriers, or from pre-formed blank granules by absorbing a compound of formula (I) (or a solution thereof, in a suitable agent) in a porous granular material (such as pumice, attapulgite clays, fuller's earth, kieselguhi, diatomaceous earths or ground com cobs) or by adsorbing a compound of formula (I) (or a solution thereof, in a suitable agent) on to a hard core material (such as sands, silicates, mineral carbonates, sulphates or phosphates) and drying if necessary. Agents which are commonly used to aid absorption or adsorption include solvents (such as aliphatic and aromatic petroleum solvents, alcohols, ethers, ketones and esters) and sticking agents (such as polyvinyl acetates, polyvinyl alcohols, dextrins, sugars and vegetable oils). One or more other additives may also be included in granules (for example an emulsifying agent, wetting agent or dispersing agent).
Dispersible Concentrates (DC) can be prepared by dissolving a compound of formula (I) in water or an organic solvent, such as a ketone, alcohol or glycol ether. These solutions may contain a surface active agent (for example to improve water dilution or prevent crystallisation in a spray tank).
Emulsifiable concentrates (EC) or oil-in-water emulsions (EW) may be prepared by dissolving a compound of formula (I) in an organic solvent (optionally containing one or more wetting agents, one or more emulsifying agents or a mixture of said agents). Suitable organic solvents for use in ECs include aromatic hydrocarbons (such as alkylbenzenes or alkylnaphthalenes, exemplified by SOLVESSO 100, SOLVESSO 150 and SOLVESSO 200; SOLVESSO is a Registered Trade Mark), ketones (such as cyclohexanone or methylcyclohexanone) and alcohols (such as benzyl alcohol, furfuryl alcohol or butanol),


N-alkylpyrrolJdones (such as N-methylpyrrolidone or N-octylpyrrolidone), dimethyl amides of fatty acids (such as CrC,0 fatty acid dimethylamide) and chlorinated hydrocarbons. An EC product may spontaneously emulsify on addition to water, to produce an emulsion with sufficient stability to allow spray application through appropriate equipment. Preparation of an EW involves obtaining a compound of formula (1) either as a liquid (if it is not a liquid at room temperature, it may be melted at a reasonable temperature, typically below 70°C) or in solution (by dissolving it in an appropriate solvent) and then emulsifiying the resultant liquid or solution into water containing one or more SFAs, under high shear, to produce an emulsion. Suitable solvents for use in EWs include vegetable oils, chlorinated hydrocarbons (such as chlorobenzenes), aromatic solvents (such as alkylbenzenes or alkylnaphthalenes) and other appropriate organic solvents which have a low solubility in water.
Microemulsions (ME) may be prepared by mixing water with a blend of one or more solvents with one or more SFAs, to produce spontaneously a thermodynamically stable isotropic liquid formulation. A compound of formula (I) is present initially in either the water or the solvent/SFA blend. Suitable solvents for use in MEs include those hereinbefore described for use in in ECs or in EWs. An ME may be either an oil-in-water or a water-in-oil system (which system is present may be determined by conductivity measurements) and may be suitable for mixing water-soluble and oil-soluble pesticides in the same formulation. An ME is suitable for dilution into water, either remaining as a microemulsion or forming a conventional oil-in-water emulsion.
Suspension concentrates (SC) may comprise aqueous or non-aqueous suspensions of finely divided insoluble solid particles of a compound of formula (I). SCs may be prepared by ball or bead milling the solid compound of formula (I) in a suitable medium, optionally with one or more dispersing agents, to produce a fine particle suspension of the compound. One or more wetting agents may be included in the composition and a suspending agent may be included to reduce the rate at which the particles settle. Alternatively, a compound of formula (I) may be dry milled and added to water, containing agents hereinbefore described, to produce the desired end product.
Aerosol formulations comprise a compound of formula (I) and a suitable propellant (for example H-butane). A compound of formula (I) may also be dissolved or dispersed in a

suitable medium (for example water or a water miscible liquid^ such as n-propanol) to provide compositions for use in non-pressurised, hand-actuated spray pumps.
A compound of formula (I) can be mixed in the dry state with a pyrotechnic mixture to form a composition suitable for generating, in an enclosed space, a smoke containing the compound.
Capsule suspensions (CS) can be prepared in a manner similar to the preparation of EW formulations but with an additional polymerisation stage such that an aqueous dispersion of oil droplets is obtained, in which each oil droplet is encapsulated by a polymeric shell and contains a compound of formula (I) and, optionally, a carrier or diluent therefor. The polymeric shell may be produced by either an interfacial polycondensation reaction or by a coacervation procedure. The compositions may provide for controlled release of the compound of formula (I) and they can be used for seed treatment. A compound of formula (I) may also be formulated in a biodegradable polymeric matrix to provide a slow, controlled release of the compound.
A composition may include one or more additives to improve the biological performance of the composition (for example by improving wetting, retention or distribution on surfaces; resistance to rain on treated surfaces; or uptake or mobility of a compound of formula (I)). Such additives include surface active agents, spray additives based on oils, for example certain mineral oils or natural plant oils (such as soy bean and rape seed oil), and blends of these with other bio-enhancing adjuvants (ingredients which may aid or modify the action of a compound of formula (I)).
A compound of formula (I) may also be formulated for use as a seed treatment, for example as a powder composition, including a powder for dry seed treatment (DS), a water soluble powder (SS) or a water dispersible powder for slurry treatment (WS), or as a liquid composition, including a flowable concentrate (FS), a solution (LS) or a capsule suspension (CS). The preparations of DS, SS, WS, FS and LS compositions are very similar to those of, respectively, DP, SP, WP, SC and DC compositions described above. Compositions for treating seed may include an agent for assisting the adhesion of the composition to the seed (for example a mineral oil or a film-forming barrier).
Wetting agents, dispersing agents and emulsifying agents may be surface SFAs of the cationic, anionic, amphoteric or non-ionic type.

Suitable SFAs of the cationic type include quaternary ammonium compounds (for example cetyltrimethyl ammonium bromide), imidazolines and amine salts.
Suitable anionic SFAs include alkali metals salts of fatty acids, salts of aliphatic monoesters of sulphuric acid (for example sodium lauryl sulphate), salts of sulphonated aromatic compounds (for example sodium dodecylbenzenesulphonate, calcium dodecylbenzenesulphonate, butylnaphthalene sulphonate and mixtures of sodium di-/sopropyl- and trwsopropyl-naphthalene sulphonates), ether sulphates, alcohol ether sulphates (for example sodium laureth-3-sulphate), ether carboxylates (for example sodium laureth-3-carboxylate), phosphate esters (products from the reaction between one or more fatty alcohols and phosphoric acid (predominately mono-esters) or phosphorus pentoxide (predominately di-esters), for example the reaction between lauryl alcohol and tetraphosphoric acid; additionally these products may be ethoxylated), sulphosuccinamates, paraffin or define sulphonates, taurates and lignosulphonates.
Suitable SFAs of the amphoteric type include betaines, propionates and glycinates.
Suitable SFAs of the non-ionic type include condensation products of alkylene oxides, such as ethylene oxide, propylene oxide, butylene oxide or mixtures thereof, with fatty alcohols (such as oleyl alcohol or cetyl alcohol) or with alkylphenols (such as octylphenol, nonylphenol or octylcresol); partial esters derived from long chain fatty acids or hexitol anhydrides; condensation products of said partial esters with ethylene oxide; block polymers (comprising ethylene oxide and propylene oxide); alkanolamides; simple esters (for example fatty acid polyethylene glycol esters); amine oxides (for example lauryl dimethyl amine oxide); and lecithins.
Suitable suspending agents include hydrophilic colloids (such as polysaccharides, polyvinylpyrrolidone or sodium carboxymethylcellulose) and swelling clays (such as bentonite or attapulgite).
A compound of formula (I) can be applied by any of the known means of applying pesticidal or fungicidal compounds. For example, it can be applied, formulated or unformulated, to the pests or to a locus of the pests (such as a habitat of the pests, or a growing plant liable to infestation by the pests) or to any part of the plant, including the foliage, stems, branches or roots, to the seed before it is planted or to other media in which plants are growing or are to be planted (such as soil surrounding the roots, the soil generally,

paddy water or hydroponic culture systems), directly or it can be sprayed on, dusted on, applied by dipping, applied as a cream or paste formulation, applied as a vapour or applied through distribution or incorporation of a composition (such as a granular composition or a composition packed in a water-soluble bag) in soil or an aqueous environment.
A compound of formula (I) may also be injected into plants or sprayed onto vegetation using electrodynamic spraying techniques or other low volume methods, or applied by land or aerial irrigation systems.
Compositions for use as aqueous preparations (aqueous solutions or dispersions) are generally supplied in the form of a concentrate containing a high proportion of the active ingredient, the concentrate being added to water before use. These concentrates, which may include DCs, SCs, ECs, EWs, MEs SQs, SPs, WPs, WGs and CSs, are often required to withstand storage for prolonged periods and, after such storage, to be capable of addition to water to form aqueous preparations which remain homogeneous for a sufficient time to enable them to be applied by conventional spray equipment. Such aqueous preparations may contain varying amounts of a compound of formula (I) (for example 0.0001 to 10%, by weight) depending upon the purpose for which they are to be used.
A compound of formula (I) can be used in mixtures with fertilisers (for example nitrogen-, potassium- or phosphorus-containing fertilisers). Suitable formulation types include granules of fertiliser. The mixtures suitably contain up to 25% by weight of the compound of formula (I).
The invention therefore also provides a fertiliser composition comprising a fertiliser and a compound of formula (I).
The compositions of this invention may contain other compounds having biological activity, for example micronutrients or compounds having similar or complementary fungicidal activity or which possess plant growth regulating, herbicidal, insecticidal, nematicidal or acaricidal activity.
By including another fungicide, the resulting composition can have a broader spectrum of activity or a greater level of intrinsic activity than the compound of formula (I) alone. Further the other fungicide can have a synergistic effect on the fungicidal activity of the compound of formula (I).

The compound of formula (I) may be the sole active ingredient of the composition or it may be admixed with one or more additional active ingredients such as a pesticide, fungicide, synergist, herbicide or plant growth regulator where appropriate. An additional active ingredient may: provide a composition having a broader spectrum of activity or increased persistence at a locus; synergise the activity or complement the activity (for example by increasing the speed of effect or overcoming repellency) of the compound of formula (I); or help to overcome or prevent the development of resistance to individual components. The particular additional active ingredient will depend upon the intended utility of the composition. Examples of suitable pesticides include the following:
a) Pyrethroids, such as permethrm, cypermethrin, fenvalerate, esfenvalerate, deltamethrin, cyhalothrin (in particular lambda-cyhalothrin), bifenthrin,'fenpropathrin, cyfluthrin, tefluthrin, fish safe pyrethroids (for example ethofenprox), natural pyrethrin, tetramethrin, s-bioallethrin, fenfluthrin, prallethrin or 5-ben2yl-3-fuiylmethyl-(T^(lR3S>2,2-dimethyl-3-(2-oxothiolan-3-ylidenemethyl)cyclopropane carboxylate;
b) Organophosphates, such as, profenofos, sulprofos, acephate, methyl parathion, azinphos-methyl, demeton-s-methyl, heptenophos, thiometon, fenamiphos, monocrotophos, profenofos, triazophos, methamidophos, dimethoate, phosphamidon, malathion, chlorpyrifos, phosalone, terbufos, fensulfothion, fonofos, pnorate, phoxim, pirimiphos-methyl, pirimiphos-ethyl, fenitrothion, fosthiazate or diazinon;
c) Carbamates (including aryl carbamates), such as pirimicarb, triazamate, cloethocarb, carbofuran, furathiocarb, ethiofencarb, aldicarb, thiofurox, carbosulfan, bendiocarb, fenobucarb, propoxur, methomyl or oxamyl;
d) Benzoyl ureas, such as diflubenzuron, triflumuron, hexaflumuron, flufenoxuron or chlorfluazuron;
e) Organic tin compounds, such as cyhexatin, fenbutatin oxide or azocyclotin;
f) Pyrazoles, such as tebufenpyrad and fenpyroximate;
g) Macrolides, such as avermectins or milbemycins, for example abamectin, emamectin benzoate, ivermectin, milbemycin, spinosad or azadirachtin;
h) Hormones or pheromones;
i) Organochlorine compounds such as endosulfan, benzene hexachloride, DDT, chlordane or
dieldrin;

j) Amidines, such as chlordimeform or amitraz;
k) Fumigant agents, such as chloropicrin, dichloropropane, methyl bromide or metam;
1) Chloronicotinyl compounds such as imidacloprid, thiaclopnd, acetamiprid, nitenpyram or
thiamethoxam;
m) Diacylhydrazines, such as tebufenozide, chromafenozide or methoxyfenozide;
n) Diphenyl ethers, such as diofenolan or pyriproxifen;
o) Indoxacarb;
p) Chlorfenapyr; or
q) Pymetrozine.
In addition to the major chemical classes of pesticide listed above, other pesticides
having particular targets may be employed in the composition, if appropriate for the intended
utility of the composition. For instance, selective insecticides for particular crops, for

example stemborer specific insecticides (such as cartap) or hopper specific insecticides (such as buprofezin) for use in rice can be employed. Alternatively insecticides or acaricides specific for particular insect species/stages may also be included in the compositions (for example acaricidal ovo-larvicides, such as clofentezine, fiubenzimine, hexythiazox or tetradifon; acaricidal motilicides, such as dicofol or propargite; acaricides, such as bromopropylate or chlorobenzilate; or growth regulators, such as hydramethylnon, cyromazine, methoprene, chlorfluazuron or diflubenzuron).
Examples of fungicidal compounds which may be included in the composition of the mventionare(£)-A'-methyl-2-[2-(2,5-dimethylphenoxymethyl)phenyI]-2-methoxy-iminoacetamide (SSF-129), 4-bromo-2-cyano-MA'Ldimethyl-6-trifluoromethyl-benzimidazole-1 -sulphonamide, a-[7^-(3-chloro-2,6-xylyl)-2-methoxy-acetamido]-y-butyrolactone, 4-chloro-2-cyano-^^/-dimethyl-5-/>tolylimidazo]e-1 -sulfonamide (IKF-916, cyamidazosulfamid),
3-5-dichloro-//-(3H;Uoro-l^myl-l-memyl-2-oxopropyl)^inethylbenzamide(RH-7281, zoxamide), ^allyM,5,-dimemyl-2-trimemylsilylthiophene-3-carboxamide(MON65500), A^-(l-cyanc-l^-dimethylpropyl)-2-(2,4-dichlorophenoxy)propionamide(AC382042), A^-(2-methoxy-5-pyridyl)-cyclopropane carboxamide, acibenzolar (CGA245704), alanycarb, aldimorph, anilazine, azaconazole, azoxystrobin, benalaxyl, benomyl, biloxazol, bitertanol, blasticidin S, bromuconazole, bupirimate, captafol, captan, carbendazim, carbendazim


chlorhydrate, carboxin, carpropamid, carvone, CGA41396, CGA41397, chinomethionate, chlorothalonil, chlorozolinate, clozylacon, copper containing compounds such as copper oxychloride, copper oxyquinolate, copper sulphate, copper tallate and Bordeaux mixture, cymoxanil, cyproconazole, cyprodinil, debacarb, di-2-pyridyl disulphide 1,1'-dioxide, dichjofluanid, diclomezine, dicloran, diethofencarb, difenoconazole, difenzoquat, diflumetorim, O.Odi-wo-propyl-S-benzyl thiophosphate, dimefluazole, dimetconazole, dimethomorph, dimethirimol, diniconazole, dinocap, dithianon, dodecyl dimethyl ammonium chloride, dodemorph, dodine, doguadine, edifenphos, epoxiconazole, ethirimol, emyl(Z)-N-benzyl-N([methyl(methyl-thioethylideneammooxycarbonyl)aniino]thio)--p-alaninate, etridiazole, famoxadone, fenamidone (RPA407213), fenarimol, fenbuconazole, fenfuram, fenhexamid (KBR2738), fenpiclonil, fenpropidin, fenpropimorph, fentin acetate, fentin hydroxide, ferbam, ferimzone, fluazinam, fludioxonil, flumetover, fluoroimide, fluquinconazole, flusilazole, flutolanil, flutriafol, folpet, fuberidazole, fiiralaxyl, furametpyr, guazatine, hexaconazole, hydroxyisoxazole, hymexazole, imazalil, imibenconazole, irninoctadine, iminoctadine triacetate, ipconazole, iprobenfos, iprodione, iprovalicarb (SZX0722), isopropanyl butyl carbamate, isoprothiolane, kasugamycin, kresoxim-methyl, LYl 86054, LY211795, LY248908, mancozeb, maneb, mefenoxam, mepanipyrim, mepronil, metalaxyl, metconazole, metiram, metiram-zinc, metominostrobin, myclobutanil, neoasozin, nickel dimethyldithiocarbamate, nitrothal-j'jopropyl, nuarimol, ofurace, organomercury compounds, oxadixyl, oxasulfuron, oxolinic acid, oxpoconazole, oxycaiboxin, pefurazoate, penconazole, pencycuron, phenazin oxide, phosetyl-Al, phosphorus acids, phthalide, picoxystrobin (ZA1963), polyoxinD, polyram, probenazole, prochloraz, procymidone, propamocarb, propiconazole, propineb, propionic acid, pyrazophos, pyrifenox, pyrimethanii, pyroquilon, pyroxyfur, pyrrolnitrin, quaternary ammonium compounds, quinomethionate, quinoxyfen, quintozene, sipconazole (F-155), sodium pentachlordphenate, spiroxamine, streptomycin, sulphur, tebuconazole, tecloflalam, tecnazene, tetraconazole, thiabendazole, thifluzamid, 2-(thiocyanomethylthio)benzothiazole, thiophanate-methyl, thiram, timibenconazole, tolclofos-methyl, tolylfluanid, triadimefon, triadimenol, triazbutil, triazoxide, tricyclazole, tridemorph, trifloxystrobin (CGA279202), triforine, triflumizole, triticonazole, validamycin A, vapam, vinclozolin, zineb and ziram.

In a further aspect, the present invention provides a method of combating and controlling fungi comprising applying to a plant, to a seed of a plant, to the locus of the plant or seed or to the soil a fungicidally effective amount of either a first active ingredient, which is a compound of formula (I) or a composition, containing a first active ingredient which is a compound of formula (1); and a second active ingredient which is azoxystrobin, picoxystobin, kresoxim-methyl, trifloxystrobin, metominostrobin or SSF129; wherein the weight ratio of the first active ingredient to the second active ingredient is in the range from 5000:1 to 1:10, preferably in the range from 3000:1 to 1:1, the relative amounts of the first and second active ingredients being such as to produce a synergistic effect.
It is preferred that the first active ingredient is a compound as hereinbefore defined (such as a compound of Table A3).
It is preferred that the second active ingredient is azoxystrobin.
It is preferred that the fungi are fungal infections of plants caused by Plasmopara spp. (especially Plasmopara viticola), Septoria spp. (especially Septoria nodorum), or Rhizoctonia spp. (especially Rhizoctonia solani).
In a further aspect, the present invention provides a method of combating and controlling fungal infections of plants caused by Plasmopara spp. or Rhizoctonia spp., the method comprising applying to a plant, to a seed of a plant, to the locus of the plant or seed or to the soil a fungicidally effective amount of either a first active ingredient, which is a compound of formula (I) or a composition, containing a first active ingredient which is a compound of formula (I); and a second active ingredient which is fluazinam; wherein the weight ratio of the first active ingredient to the second active ingredient is in the range from 500:1 to 1:10, preferably in the range from 100:1 to 1:5, the relative amounts of the first and second active ingredients being such as to produce a synergistic effect.
It is preferred that the first active ingredient is a compound as hereinbefore defined (such as a compound of Table A3).
It is preferred that the fungal infections are those caused by Plasmopara viticola or Rhizoctonia solani.
In a further aspect, the present invention provides a method of combating and controlling fungal infections of plants caused by Plasmopara spp., the method comprising applying to a plant, to a seed of a plant, to the locus of the plant or seed or to the soil a


ungicidally effective amount of either a first active ingredient, which is a compound of tbrmula (I) or a composition, containing a first active ingredient which is a compound of formula (I); and a second active ingredient which is fenamidone or famoxadone; wherein the weight ratio of the first active ingredient to the second active ingredient is in the range from 10:1 to 1:10, preferably in the ratio 1:1, the relative amounts of the first and second active ingredients being such as to produce a synergistic effect.
It is preferred that the first active ingredient is a compound as hereinbefore defined (such as a compound of Table A3).
It is preferred that the second active ingredient is fenamidone. It is preferred that the fungal infections are those caused by Plasmopara viticola.. The compounds of formula (I) can be mixed with soil, peat or other rooting media for the protection of plants against seed-bome, soil-bome or foliar fungal diseases
Examples of suitable synergists for use in the compositions include piperonyl butoxide, sesamex, safroxan and dodecyl imidazole.
Suitable herbicides and plant-growth regulators for inclusion in the compositions will depend upon the intended target and the effect required.
An example of a rice selective herbicide which can be included is propanil. An example of a plant growth regulator for use in cotton is PK™.
as a
Some mixtures may comprise active ingredients which have significantly different physical, chemical or biological properties such that they do not easily lend themselves to the same conventional formulation type. In these circumstances other formulation types may be prepared. For example, where one active ingredient is a water insoluble solid and the other a water insoluble liquid, it may nevertheless be possible to disperse each active ingredient in the same continuous aqueous phase by dispersing the solid active ingredient as a suspension (using a preparation analogous to that of an SC) but dispersing the liquid active ingredient an emulsion (using a preparation analogous to that of an EW). The resultant composition is suspoemulsion (SE) formulation.
The invention is illustrated by the following Examples, in which the ingredients below are referred to by their Registered Trade Marks and have the following compositions.


Registered Trade Mark Composition
SYNPERONIC NP8 } SYNPERONICNP13} Nonylphenol-ethylene oxide condensate
SYNPERONIC A7 Synthetic primary alcohol-ethylene oxide condensate
AROMASOL H AUcylbenzene solvent
SOLVESSQ 200 ' Inert organic diluent
KELTROL Polysaccharide
PROXEL Bactericide
EXAMPLE 1 This Example illustrates the preparation of Compound 4 (Table A3).
Stepl
Methyl 4-hydroxyphenylacetate (49.8g, OJmol) was dissolved in glacial acetic acid (500ml) and the resultant solution was cooled to below 15°C. Concentrated nitric acid (40ml) was added slowly and the reaction mixture was stirred until completion and then poured onto a mixture of ice and water. The precipitated solid was filtered, washed with ice cold water and dried to give methyl 4-hydroxy-3-nitrophenylacetate (51.2g) as a yellow solid.
'H NMR (CDClj) 8: 3.65(s,2H); 3.75(s,3H); 7.15(d,lH); 7.5(dd,lH); 8.0(d,lH); 10.5(s,lH)ppm. Step 2
Methyl 4-hydroxy-3-nitrophenylacetate (52.2g, 0.247mol) was dissolved in methanol (400ml) and the resultant solution was then hydrogenated at 5bar over a 5% w/w palladium on carbon catalyst. The catalyst was removed by filtration and the filtrate was evaporated in vacuo. Trituration with hexane gave methyl 3-amino-4-hydroxyphenylacetate (43.4g),
'HNMR (CDC13) 5: 3.45(s,2H); 3.65(s,3H); 6.5(dd,lH); 6.6(d,lH); 6.7(d,lH)ppm. Step 3
The product from Step 2 (5.43g, 0.03mol), triethylamine (3.27g , 0.033mol) and pyridimum;?tfrtf-toluenesulfonate (2.01 g, 0.008mol) were stirred together in xylene (250ml). n-Butyryl chloride (3.96g , 0.033mol) was added dropwise at room temperature and once the


addition was complete stirring was continued for 30minutes. The mixture was heated to reflux for 17hours, then cooled to room temperature, diluted with ethyl acetate and washed with water and brine sequentially. The organic solution was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 2:1 mixture of hexane : ethyl acetate, to give methyl (2-propyl-5-benzoxazolyl)acetate (4.2g) as a pale orange liquid.
'HNMRCCDC],) 5: 1.05(t,3H); 1.9(m,2H); 2.9(t,2H); 3.7(s,3H); 3.75(s,2H); 7.2(m,lH); 7.4(d,lH); 7.65(d,lH)ppm. Step 4
The product from Step 3 (4.0g, 0.0172mol) was dissolved in methanol (30ml) and potassium hydroxide flakes (1.06g, 0.0188mol) were added. The mixture was heated at reflux for 2hours, then cooled and the solvent was evaporated in vacuo. The residue was taken up in water and extracted with diethyl ether. The aqueous phase was collected, acidified to pHl with dilute aqueous hydrochloric acid and extracted with ethyl acetate. The organic extract was washed with brine, dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo to afford (2-propyl-5-benzoxazolyl)acetic acid (2.9g) as an off-white solid, m.p. 67-68°C.
'HNMR (CDC13) 5: 1.0(t,3H); 1.9(m,2H); 2.9(UH); 3.75(s,2H); 7.2(dd,lH); 7.4(d,lH); 7.6(d,lH)ppm. Step 5
The acid prepared in Step 4 (0.876g, 0.004mol) was suspended in dichloromethane (10ml) and one drop of A^-dimethylformamide and oxalyl chloride (0.559g, 0.0044mol) were added sequentially. The mixture was stirred for 2hours and then the solvent was removed in vacuo. The residue was taken up in xylene (10ml), 5-amino-4-chloro-3-methylisothiazole was added and the mixture was heated under reflux for 2hours. The mixture was cooled to room temperature, diluted with ethyl acetate and washed with brine. The organic solution was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on siVica gel, eluting with a 2:1 mixture of hexane : ethyl acetate, to give Compound 4 (Table A3) as a yellow-orange solid.
EXAMPLE 2


This Example illustrates the preparation of Compound 3 (Table A3).
Stepl
4-Methoxyphenylacetic acid (33.2g, 0.2mol) and A^N-dimethylformamide (1ml) were dissolved in dichloromethane (300ml) and the mixture was cooled in an ice-bath. Oxalyl chloride (27.9g, 0.22mol) was added dropwise and once the addition was complete the cooling bath was removed and the mixture was stined for 3hours. The solvent was removed in vacuo, the residue taken up in xylene (300ml) and 5-amino-4-cWoro-3-methylisothiazole added. The mixture was heated under reflux for 2hours and was then cooled to room temperature before the solvent was evaporated in vacuo. The residue was taken up in ethyl acetate and washed with aqueous sodium hydroxide solution. On standing, 7/-(4-chloro-3-methyl-5-isothiazolyl)-4-rnethoxvphenylacetamide (27.3g) precipitated from the aqueous
solution.
HNMR (CDC13) 6: 2.4(s,3H); 3.8(s,2H); 3.85(s,3H); 6.95(m,2H); 7.25(m,2H); 8.1(b,lH)ppm. Step 2
7/^4-Ghloro-3-memyl-5-isothiazblyl>4-methoxyphenylacetamide (32.8g, 0.1 lmol) was dissolved in dichloromethane (300 ml) and the solution was then cooled to below -70°C. A solution of boron tribromide in dichloromethane (1M, 332ml, 0.332mol) was added dropwise, maintaining the internal temperature below -65°C. When the addition was complete, the mixture was allowed to warm to room temperature and stirring was continued for 3hours. With ice-bath cooling, methanol (100ml) was cautiously added and the mixture was stirred for several minutes. The solvent was removed in vacuo, methanol was added, the mixture was stirred and then the solvent was evaporated once more. The residue was partitioned between ethyl acetate and saturated aqueous sodium bicarbonate solution. The organic extract was washed with brine, dried over magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was triturated with hexane to afford //-(4-chloro-3-methyl-5-isothiazolyl)-4-hydroxyphenylacetamide (28g) as a solid.
*H NMR (oVDMSO / CDC13) 5: 2.35(s,3H); 3.8(s,2H); 6.85(m,2H); 7.15(m,2H); 8.65(b,lH);9.1(b,lH)ppm. Step 3

The phenol (28g, 0.099mol) obtained in Step 2 was suspended in ethanol (200ml) and ferric nitrate nonahydrate (40.0g, 0.99mol) was added. The mixture was stirred at 50°C for 90minutes and was then cooled to room temperature before the solvent was removed in vacuo. The residue was partitioned between 2M aqueous hydrochloric acid and ethyl acetate. The organic extract was washed sequentially with 2M aqueous hydrochloric acid and brine, dried over magnesium sulfate, filtered and the filtrate was evaporated in vacuo. Trituration with hexane afforded A^-(4-chloro-3-methyl-5-isothiazolyl)-4-hydroxy-3-nitrophenylacetarnide (3 0.1 g) as a solid.
'H NMR (oVDMSO / CDC13) 5: 2.4(s,3H); 3.9(s,2H); 7.1(d,lH); 7.65(dd,lH); 8.15(d,lH);11.0(s,lH)ppm. Step 4
/*/-(4-Chloro-3-methyl-5-isothiazolyI)-4-hydroxy-3-nitrophenylacetamide(37.4g, 0.114mol) was hydrogenated at 15bar over a 3% w/w platinum on carbon catalyst (I5g) in A^^-dimethylformamide (180ml). Once the reduction was complete, the catalyst was removed by filtration and the filtrate was evaporated in vacuo to give Ar-(4-chloro-3-methyl-5-isothiazolyl)-3-amino-4-hydroxyphehylacetamide (26.8g) as a pale brown solid, which used without further purification in the next step.
'H NMR (bVDMSO) 5:2.25(s,3H); 3.6(s,2H); 6.3(dd,lH); 6.5(m,2H); 8.9(b,lH); 11.5(s,lH)ppm. Step 5
The product from Step 4 (0.58g, 0.002mol) was suspended in toluene (5ml) and propionyl chloride (0.204g, 0.0022mol) and^-toluenesulfonic acid (0.125g, 0.0007mol) were added. The mixture was heated to reflux for 2hours, a further quantity ofp-toluenesulfonic acid (0.125g, 0.0007mol) was added and heating was continued until cyclisation was complete. The mixture was cooled to room temperature, diluted with ethyl acetate and washed with brine. The organic solution was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 1:1 mixture of hexane : ethyl acetate, to give Compound 3 (Table A3) (0.188g) as a colourless solid.
EXAMPLE 3
This Example illustrates the preparation of Compound 10 (Table A3).

Step!
Methyl 4-hydroxy-3-nitrophenylacetate (21.1 g, 0.1 mol) was suspended in a mixture of water (55ml) and methanol (105ml). The suspension was stirred at room temperature while a solution of sodium hydroxide (8.8g, 0.22mol) in water (50ml) was added dropwise over 20minutes, maintaining the reaction temperature between 20 and 25°C by water bath cooling. The resultant dark red solution was stirred at room temperature for 15minutes, diluted with water and acidified to pHl-2 by addition of 2M hydrochloric acid and extracted with ethyl acetate. The organic extract was washed with brine (200ml), dried over magnesium sulphate, filtered and concentrated under reduced pressure to give 4-hydroxy-3-nitrophenylacetic acid (19.6g) as a yellow solid.
*H NMR (CDC13) 5: 3.55(s,2H); 7.1(d,lH); 7.5(dd,lH); 8.0(d,lH) ppm. Step 2
4-Hydroxy-3-nitrophenylacetic acid (lOg, O.OSmoI) was suspended in dichloroethane (50ml) and stirred at room temperature under a nitrogen atmosphere. A^V-Dimethyl-formamide (0.1ml) was added followed by dropwise addition of oxalyl chloride (6.77g, 0.05mol) over 20minutes. The mixture was stirred at room temperature for 25minutes and then at 40°C for 20minutes. The reaction mixture was then heated under reflux while a solution of 5-aniino-4-chloro-3-methylisothia2ole (7.54g, 0.05mol) in dichloroethane (30ml) was added over 30minutes. The resultant pale orange suspension was stirred at reflux for 2hours and then cooled to room temperature, to give a precipitate, which was collected by filtration and washed with dichloromethane. The solid was suspended in water (150ml), treated with 10% (w/v) sodium hydroxide (50ml) and the resulting red solution was washed with dichloromethane (2x50ml). The combined washings were extracted with water (50ml) and the combined aqueous layers were acidified to pH4-5 by addition of concentrated hydrochloric acid (approximately 10ml). The resultant yellow suspension was filtered and the solid was washed with water and dried under suction to give iV-(4-chloro-3-methyl-5-isothiazolyl)-4-hydroxy-3-nitrophenylacetamide (14.6g) as a yellow solid.
*H NMR (drDMSO: 8: 2.3(s,3H); 3.9(s,2H); 7.05(d,lH); 7.4(dd,lH); 7.8(d,lH); 10.85(s,lH);11.7(s,lH)ppm. Step 3_

A^-(4-Chloro-3-methyl-5-isothiazolyl>4-hydroxy-3-nitrophenylacetamide(50g, 0.15mol), 1% w/w platinum on carbon (15g) and yV^-dimethylformamide (400ml) were charged to a 600ml stainless steel hydrogenation vessel. Once purged the vessel was pressurised to 35bar with hydrogen, stirring was started and the reaction was heated to 35°C. After 6hours the uptake of hydrogen had stopped; the stirring and heating were turned off and the mixture was allowed to cool to ambient temperature. The vessel was vented, purged with nitrogen and was heated to 50°C to ensure complete solution. The reaction mixture was filtered to remove the catalyst and the liquors concentrated under high vacuum to remove the JV^dimethylformamide. The resultant residue was slurried in dichloromethane (300ml), filtered, washed with dichloromethane (200ml) and dried to give give JV-(4-chloro-3-methyl-5-isothiazolyl)-3-amino-4-hydroxy-phenylacetamide (43.9g) as a buff solid, m.p. 239-243°C.
>H NMR (d6-DMSO) 8:2.25(s,3H); 3.6(s,2H); 4.6(b,2H); 6.3(dd,lH); 6.5(2d,2H); 8.8(b,lH);ll-6(s,lH)ppm. Step 4
^-(4-chloro-3-methyl-5-isothiazolyl)-3-amino-4-hydroxy-phenylacetamide(0.42g, O.OOlmol), 2-methylbutyryl chloride (037g, 0.003mol) and/wa-toluenesulfonic acid (0.05g) were stirred together in 2-methoxyethyl ether (5ml) at 110PC for 6hours. The mixture was cooled to room temperature and partitioned between ethyl acetate and saturated aqueous sodium bicarbonate solution. The organic extract was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 1:1 mixture of hexane : ethyl acetate. Fractions containing the desired product were combined arid the solvent was evaporated in vacuo to afford a yellow residue. Trituration with hexane gave Compound 10 (Table A3) as a colorless solid.
EXAMPLE 4
This Example illustrates the preparation of Compound 113 (Table A3). Stepl
.A^-Diisopropylcarbodiimide (0.630g, 0.005mol) was added dropwise to a solution of both cyanoacetic acid (0.425g, O.OOSmol) andW-(4-chloro-3-methyl-5-isothiazolyl)-3-amino-4-hydroxy-phenylacetamide (1.49g, 0.005mol) in A^-dimethylacetamide (20ml). The

Tesultant mixture was stirred at room temperature for lhour and was then poured into water. The resultant precipitate (1.34g) was collected by filtration, washed with water and dried. Step 2
The product from Step 1 (0.365g, O.OOlmol) was suspended in 1,1,2,2-tetrachloroethane (4ml), />ara-toluenesulfonic acid (0.095g) was added and the mixture was healed at 140°C for 2hours. The mixture was cooled to room temperature and partitioned between ethyl acetate and saturated aqueous sodium bicarbonate solution. The organic extract was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 2:1 mixture of hexane : ethyl acetate to give Compound 113 (Table A3) as a pale yellow solid.
EXAMPLE 5
This Example illustrates the preparation of Compound 221 (Table A3).
Stepl
Methyl 3-amino-4-hydroxyphenylacetate (5.43g, 0.03mol) was suspended in toluene (60ml) and l,l'-triiocarbonyldiimidazofe (5.34g, 0.03mol) was added. The resultant mixture was stirred for 30minutes, then acetic acid (10 ml) was added and the mixture was heated under reflux for 3hours. The mixture was cooled to room temperature and the solvent was removed in vacuo. The residue was partitioned between water and ethyl acetate. The organic extract was dried over magnesium sulfate, filtered and the filtrate was evaporated to give methyl (23-dihydro-2-thioxo-5-benzoxazolyl)acetate (6.2g) as a light brown solid, m.p. 120-122°C.
'HNMR(CDC13) 5: 3.7(s,2H); 3.75(s,3H); 7.15(m,2H); 7.3(m,lH)ppm. Step 2
The compound prepared in Step 1 (1.12g, 0.005mol) and potassium carbonate (0.69g, 0.005mol) were stirred together in acetone (20ml). Ethyl iodide |0.78g, 0.005mol) was added and the mixture was heated under reflux for lhour. The mixture was cooled to room temperature and partitioned between water and ethyl acetate. The organic extract was dried over magnesium sulfate, filtered and the filtrate was evaporated in vacuo to give methyl (2-ethylthio-5-benzoxazolyl)acetate (1.22g) as a brown liquid used without further purification in the next step.

Step 3
The product from Step 2 (122g, 0.0049mol) was dissolved in a mixture of methanol (15ml) and water (5ml) and the mixture was cooled in an ice-bath. Potassium hydroxide flakes (0.302g, 0.0054mol) were added, and the mixture was stirred for 2hours, wanning slowly to room temperature. The solvent was evaporated in vacuo. The residue was taken up in water and extracted with diethyl ether and the aqueous fraction was acidified with 2M aqueous hydrochloric acid, with ice-bath cooling, to afford (2-ethylthio-5-benzoxazolyl)acetic acid (0.98g).
'HNMR (CDC13) 6: 1.5(t,3H); 3.3(q,2H); 3.75(s,2H); 7.15(dd,lH); 7.4(d,lH); 7.5(d,lH)ppm. Step 4
The compound prepared in Step 3 (0.474g, 0.002mol) was suspended in dichloromethane (10ml) and one drop of AVV-dimethylformamide and oxalyl chloride (0.254g, 0.0022moi) were added sequentially. The mixture was stirred for 2hours and then the solvent was removed in vacuo. The residue was taken up in xylene (10ml), 5-amino-4-chloro-3-methylisothiazole (0.32g, 0.002lmol) was added and the mixture was heated under reflux for 2hours. The mixture was cooled to room temperature, diluted with ethyl acetate and washed sequentially with water and 2M aqueous hydrochloric acid. The organic solution was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 1:1 mixture of hexane : ethyl acetate, to give Compound 221 (Table A3) as a pale yellow solid. ~
EXAMPLE 6
This Example illustrates the preparation of Compound 224 (Table A3). Step!
Methyl 3-amino-4-hydroxyphenylacetate (16.29g, 0.09mol) was suspended in toluene (180ml) and l,r-thiocarbonyldiimidazole (15.96g, 0.09mol) was added and the mixture was stirred until the exothermic reaction had subsided. Acetic acid (3ml) was added and the mixture was heated at reflux for 4hours, then cooled to room temperature and the solvent was removed in vacuo. The residue was partitioned between ethyl acetate and brine and the organic extract was dried over anhydrous magnesium sulfate, filtered and the filtrate was


evaporated in vacuo. The residue was taken up in chloroform (200ml) and the solution was saturated with chlorine. The mixture was stirred for lhour at room temperature, then, diluted with chloroform and washed sequentially with a 10% (w/v) solution of aqueous sodium bicarbonate and water. The organic solution was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 3:1 mixture of hexane : ethyl acetate, to give methyl (2-cnloro-5-benzoxazolyl)acetate (8.4g) as a pale yellow liquid which solidified on standing.
•H NMR (CDC13) 5:3.7(s,3H); 3.75(s,2H); 7.3(dd,lH); 7.45(d,lH); 7.6(d,lH)ppm.
Step 2
Sodium /er/-butylthiolate (0.496g, 0.0044mol) was dissolved in NJJ-dimethylformamide (5ml) and the solution was cooled in an ice bath. A solution of methyl (2-cWoTO-5-benzoxazoty\)acrta\e {\ .00g, 0.0044moY) in N^-dvc&tthytfoTmarmde (5TnY) v?as added dropwise and once the addition was complete the reaction mixture was stirred for lhour, being allowed to warm slowly to room temperature. The reaction mixture was poured onto ice-water and extracted with ethyl acetate. The organic extract was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 3:1 mixture of hexane : ethyl acetate, to give methyl (2-/er/-butylthio-5-benzoxazol-yl)acetate (0.5 lg) as a pale yellow liquid.
, 'H NMR (CDC13) 5:1.65(s,9H); 3.7(s,3H); 3.73(s,2H); 7.2(dd,lH); 7.4(d,lH); 7.55(d,lH)ppm. Step 3
The product from Step 2 (0,44g, 0.0016mol) was dissolved in a mixture of methanol (10ml) and water (5ml) and the mixture was cooled in an ice-bath. Potassium hydroxide flakes (0.1 lg, 0.016mol) were added and the mixture was stirred for 4hours, being allowed to warm slowly to room temperature. The solvent was evaporated in vacuo. The residue was taken up in water and extracted with diethyl ether and the aqueous fraction was acidified with 2M aqueous hydrochloric acid, with ice-bath cooling, to afford (2-/er/-butylthio-5-benzoxazolyl)acetic acid (0.4lg).
»HNMR (CDC13) 5:1.6(s,9H); 3.75(s,2H); 7.2(dd,lH); 7.4(d,lH); 7.55(d,lH)ppm.

Step 4
The acid prepared in Step 3 (0.39g, 0.0015mol) was suspended in dichloromethane (10ml) and one drop of A^-dimethylformamide and oxalyl chloride (0.205g, 0.0016mol) were added sequentially. The mixture was stirred for 2hours and then the solvent was removed in vacuo. The residue was taken up in xylene (10ml), 5-amino-4-chloro-3-methylisothiazole (0.33g, 0.0022mol) added and the mixture heated together under reflux for 2hours. The mixture was cooled to room temperature and partitioned between ethyl acetate and brine. The organic solution was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 2:1 mixture of hexane : ethyl acetate, to give Compound 224 (Table A3) as a sandy-brown solid.
EXAMPLE 7
This Example illustrates the preparation of Compound 183 (Table A3).
Stepl
A solution of methyl (2-chloro-5-benzoxazolyl)acetate (l.OOg, 0.004mol) in dichloromethane (5ml) was added drppwise to a chilled (ice-bath) solution of /er/-butylamine (0.648g, 0.009mol) in dichloromethane (10ml) and once the addition was complete the mixture was stored for 2hours, allowing it to warm to room temperature. 1,2-Dichloroethane (15ml) was added and the mixture was heated to reflux for 17hours. The mixture was cooled to room temperature, diluted with dichloromethane and washed with water. The organic extract was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo to give methyl (2-/er/-bUtylamino-5-benzoxazolyl)acetate as a yellow gum (1.09g). The product was used without further purification in the next step. Step 2
Potassium hydroxide flakes (0.236g, 0.004mol) were added to a chilled (ice-bath) solution of methyl (2-/er/-butylamino-5-benzoxazolyl)acetate (l.OOg, 0.004mol) in methanol (10ml) and water (5ml) and the mixture was stirred for 2hours, being allowed to warm slowly to room temperature. The solvent was removed in vacuo, the residue taken up in water and extracted with diethyl ether. The aqueous extract was cooled in an ice-bath and dilute aqueous hydrochloric acid was added until the solution reached pH3. The precipitate


was collected by filtration and dried to give (2-/er/-butylamino-5-benzoxazolyl)acetic acid (0.685g) as a colourless solid, m.p. 175-176°C.
'HNMR (CDCI3) 8: 1.6(s,9H); 3.6(s,2H); 6.4(b,lH); 6.95(dd,lH); 7.2(d,lH); 7.3(d,lH)ppm. Step 3
The acid prepared in Step 2 (0.67g, 0.003mol) was suspended in dichloromethane (10ml) and one drop of A^-dimethylformamide and oxalyl chloride (0.38g, 0.003mol) were added sequentially. The mixture was stirred for 2hours and then the solvent was removed in vacuo. The residue was taken up in 1,2-dichloroethane (20ml) and the mixture was heated to reflux. 5-Ainino-4-chloro-3-methylisothia2ole (0.33g, 0.0022mol) was added and the mixture was heated under reflux for 2hours. The mixture was cooled to room temperature, diluted with 1,2-dichloroethane and washed sequentially with saturated aqueous sodium bicarbonate solution and brine. The organic extract was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 2:1 mixture of hexane : ethyl acetate to give an orange-yellow residue^ The product was taken up in a small volume of ether and allowed to stand. Compound 183 (Table A3) precipitated as a cream coloured solid.
EXAMPLE 8
This Example illustrates the preparation of Compound 248 (Table A43). Stepl
Methyl 3,4-diaminophenylacetate (0.38g, 0.0021mol) and triethyl orthobenzoate (0.8ml, 0.003 5mol) were stirred together in refluxing ethanol (10ml) for 8hours. The mixture was cooled and partitioned between ethyl acetate and water. The organic solution was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, gradient eluting with a mixture of hexane : ethyl acetate, to give methyl (2-phenyl-5-benzimidazolyl)acetate (0.34g) as a brown oil.
'HNMR(CDC13) 5: 3.5(s,3H), 3.52(s,2H), 7.15(m,lH), 7.5(m,5H), 8.0(m,2H)ppm. Step 2

The ester (0.34g, 0.0013mol) prepared in Step 1 was dissolved in methanol (1 Oml) and potassium hydroxide flakes (0.08g, 0.0014mol) were added. The mixture was heated at reflux for 2hours, then cooled and the solvent was evaporated in vacuo. The residue was taken up in water and extracted with diethyl ether. The aqueous phase was collected, acidified to pH 1 with dilute aqueous hydrochloric acid and the resultant precipitate (0.18g) was collected and dried to give (2-phenyl-5-berizimidazolyl)acetic acid hydrochloride, which was used without further purification in the next step.
'H NMR (CDC13) 5: 3.7(s,2H), 7.3(m,lH), 7.55(m,3H), 7.65(m,2H), 8.25(m,2H)ppm. Step 3
The benzimidazole prepared in Step 2 (0.18g, 0.0007mol) was suspended in chloroform (20ml) and 7*/JV-dimethylformamide (0.5ml) and triethylarnine (0.2ml, 0.0014mol) were added. To the resultant solution was added oxalyl chloride (0.07ml, 0.00079mol) and the mixture was stirred* Tdr 2hours at room temperature. 5-Amino-4-chloro-3-methyl-isothiazole (0.107g, 0.00072mol) was added and the mixture was heated at room temperature for 15hours and then under reflux for 48hours. The mixture was cooled and partitioned between ethyl acetate and water. The organic solution was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 2 :1 mixture of hexane : ethyl acetate, to give Compound 248 (Table A43) (0.012g) as a yellow oil.
EXAMPLE 9 This illustrates the preparation of Compound 2 (Table A13). Stepl
Methyl 4-hydroxy-3-nitrophenylacetate (21.1g, 0.1 mol), dimethylthiocarbamoyl chloride (13.0g, 0.1 mol) and potassium carbonate (14.0g, O.lmol) were suspended in 4-methylpentan-2-one (150ml) and the mixture was heated at reflux with stirring for lhour. The mixture was cooled and kept overnight at room temperature. The reaction mixture was diluted with water and was extracted with ethyl acetate. The organic extract was washed sequentially with dilute aqueous sodium hydroxide solution and brine and then dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo to give a buff solid, which was triturated with diethyl ether to provide methyl 3-nitro-4-(C>-dimethylthiocarbamoyl)phenylacetate (24.5g).


'H NMR (CDCI3) 6: 3.40(s,2H); 3.45(s,3H); 3.75(s,6H); 7.25(d,lH); 7.6(dd,lH); 8.5(d,lH)ppm. Step 2
The product from Step 1 (24.5g, 0.083mol), was dissolved in xylene (100ml) and heated at reflux with stirring for 17hours. The reaction was cooled and the xylene was evaporated in vacuo to afford an oil which crystallised on standing. Trituration with diethyl ether gave methyl 3-nitro-4-(5-dknethylthiocarbamoyl)phenylacetate (21.5g) m.p. 56-57°C.
'H NMR (CDCI3) S: 3.1(bd,6H); 3.7(s,5H); 7.5(dd,lH); 7.7(d,lH); 7.95(d,lH)ppm. Step 3
The product from Step 2 (6.0g, 0.02mol) was dissolved in methanol (250ml) and a solution of sodium hydroxide pellets (2.0g , 0.05mol) in water (15ml) was added. The mixture was stirred at room temperature for 17hours, then acidified with concentrated hydrochloric acid, diluted with water and extracted with ethyl acetate. The organic extract was washed with brine, dried over anhydrous magnesium sulphate, filtered and the filtrate was evaporated in vacuo. Trituration with hexane gave a brown solid (4.5g), comprising a mixture of 4-mercapto-3-nitrophenyla6etic acid and bis(4-carboxymethyl-2-nitrophenyl) disulfide. Step 4
The products of Step 3 (4.5g, 0.015mol) were dissolved in methanol (50ml), and a few drops of concentrated hydrochloric acid were added. The mixture was refluxed for 2hours and was then cooled and allowed to stand overnight at room temperature. The precipitate was collected and washed with diethyl ether and dried to give bis(4-carbomethoxymethyl-2-nitrophenyl) disulfide as a yellow solid (1.2g).
'H NMR (CDC13) 5: 3.7(s,2H); 3.725(s,3H); 7.5(dd,lH); 7.8(d,lH); 8.3(d,lH)ppm.
The ethereal and methanol solution was evaporated in vacuo to afford a yellow solid (2.2g) after trituration with diethyl ether. 'H NMR (CDC13) showed this to be a mixture of methyl 4-mercapto-3-nitrophenylacetate and bis(4-<;arbomethoxymethyl-2-nitrophenyl) disulfide. StepS
The product obtained in Step 4 (3.0g, O.013mo3) was dissolved in glacial acetic acid (30ml). Iron power (5.2g) was added to the solution and the mixture was heated and stirred

at reflux for 3hours. The mixture was cooled to room temperature, diluted with water and extracted with diethyl ethei (200ml). The ethereal extract was washed sequentially with water and aqueous sodium hydrogen carbonate solution, dried over anhydrous magnesium sulphate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 1:1 mixture of hexane : diethyl ether, to give methyl (2-methyl-5-benzothiazolyl)-acetate (0.95g) as a yellow liquid.
'HNMR (CDCI3) 5: 2.85(s,3H); 3.7(s,2H); 3.8(s;3H); 7.3(dd,lH); 7.8(d,lH); 7.85(d,lH)ppm. Step 6
The product from Step 5 (0.85g, 0.0385mol) was dissolved in methanol (10ml) and a solution of potassium hydroxide pellets (0.35g) in water (2ml) was added. The mixture was then stirred at room temperature for 17hours. The mixture was acidified with concentrated hydrochloric acid to pH4 and the solution^as then diluted with water and extracted with ethyl acetate. The organic extract was washed with brine, dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. Trituation with hexane afforded (2-methyl-5-benzothioazolyl)acetic acid (0.62g) as a buff solid, m.p. 194-196°C.
'H NMR (CDCI3) 5: 2.85(s,3H); 3.5(s,2H); 7.1(dd,lH); 7.55(d,lH); 7.65(d,lH)ppm. Step 7
The acid prepared in Step 6 (0.2g, 0.00lmol) was suspended in dichloromethane (10ml) and one drop of//^/-dimethylformamide and oxalyl chloride (0.559g, 0.0044mol) were added sequentially. The mixture was stirred for 2hours and then the solvent was removed in vacuo. The residue was taken up in xylene (10ml), 5-amino-4-chloro-3-methylisothiazole was added and the mixture was heated under reflux for 2hours. The mixture was cooled to room temperature, diluted with ethyl acetate and washed with brine. The organic solution was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 2:1 mixture of hexane : ethyl acetate, to give Compound 2 (Table A13) (0.125g) as a buff solid.
EXAMPLE 10
This Example illustrates the preparation of Compound 15 (Table 13). Stepl

[2-(2,2-DimemylpropyI)-5-benzoxazolyl]acetic acid (0.800g, 0.003mol) was suspended in dichloromethane (10ml) and one drop of A^-dimethylformamide and oxalyl chloride (0.45lg, 0.004mol) were added sequentially. The mixture was stirred for 2hours and then the solvent was removed in vacuo. The residue was taken up in xylene (10ml), 5-amino-4-chloro-3-methylisothiazole (0.829g, 0.006mol) was added and the mixture was heated under reflux for 2hours. The mixture was cooled to room temperature, diluted with ethyl acetate and washed with brine. The organic solution was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 2:1 mixture of hexane : ethyl acetate, to give Compound 15 (Table A3) (0.325g) as a pale orange solid. Step 2
Compound 15 (Table A3) (1.7g, 0.0045mol) was dissolved in tetrahydrofuran (30ml) and a 1M solution of lithium bis(trimethylsflyl)amide in tetrahydrofuran (4.95ml) was added. The reaction mixture was stirred for 30minutes at room temperature and then chloromethylethyl ether (0.85lg, 0.009mdl) was added. The reaction mixture was stirred for 2hours at room temperature and then petered into water. The mixture was extracted with ethyl acetate, the organic extract washed with brine, dried over anhydrous magnesium sulfate filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 2:1 mixture of hexane : ethyl acetate, to give Compound 15 (Table L3) (0.55g) as a viscous gum.
EXAMPLE 11
This Example illustrates the preparation of Compound 15 (Table C3).
[2-(2,2-Dimethylpropyl)-5-benzoxazolyl]acetic acid (0.729g, 0.003mol) was suspended in dichloromethane (10ml) and a few drops of A^-dimemylformamide and oxalyl chloride (0.419g, 0.003mol) were added sequentially. The mixture was stirred for 2hours, and then the solvent removed in vacuo. The residue was taken up in 1,2-dichloroethane (2ml) and xylene (10ml), 4-chloro-5-emylamino-3-methylisothiazole (0.590g , 0.003mol) were added and the mixture was then heated under reflux for 3hours. The mixture was cooled to room temperature, the solvent evaporated in vacuo and the residue taken up in ethyl acetate and washed with brine. The organic solution was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further

.purified by flash column chromatography on silica gel, eluting with a 2:1 mixture of hexane : ethyl acetate, to give Compound 15 (Table C3) (0.62g) as a yellowish gum.
EXAMPLE 12
This Example illustrates the preparation of Compound 15 (Table V3).
Compound 15 (Table A3) (1.88g , O.OOSmol) and [2,4-bis(4-methoxyphenyl)-l,3-dithia-2-2,4-diphosphetane-2,4-disulfide] (3.03g, 0.0075mol) were heated in refluxing toluene for 6hours. The mixture was cooled to room temperature, the solvent was removed in vacuo and the residue partitioned between ethyi acetate and water. The organic extract was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 2:1 mixture of hexane : ethyl acetate, to give Compound 15 (Table C3)
(0.195g).
EXAMPLE 13
This Example illustrates the preparation of Compound 204 (Table A3).
Compound 220 (Table A3) (0.400g, 0.00 lmol) was dissolved in ethanol (10ml) and potassium hydroxide flaked (0.126g, 0.002mol) were added. The mixture was stirred at room temperature for lhour, was then warmed to 50°C for a further lhour and finally was heated at reflux for 30minutes. The mixture was cooled to room temperature and the solvent was evaporated in vacuo. The residue was taken up in water, the solution was neutralised with dilute aqueous hydrochloric acid and extracted with ethyl acetate. The organic extract was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 2:1 mixture of hexane : ethyl acetate, to give Compound 204 (Table A3) (0.120g) as a colourless solid.
EXAMPLE 14
This Example illustrates the preparation of Compound 9 (Table Al 3). Stepl
Methyl 4-fluoro-3-nitrophenylacetate (5.0g, 0.023mol) and iron powder (3g, 0.053mol) were suspended in a mixture of propan-2-ol (50ml) and water (5ml). Concentrated hydrochloric acid (5 drops) was added at room temperature and the mixture was heated at reflux with stirring for 2hours. The reaction mixture was cooled, diluted with

diethyl ether, filtered through diatomaceous earth and the resulting filtrate was evaporated in vacuo. The residue was further purified by chromatography on silica gel, eluting with diethyl ether to yield methyl 3~amino-4-fluorophenylacetate (3.5g) as a yellow oil.
'HNMR (CDCI3) 6: 3.50(s,2H); 3.8(s,3H); 3.5-3.9(bs,2H); 6.6(rn,lH); 6.85(dd,lH);7.9(dd,lH)ppm. Step 2
The product from Step 1 (2.0g, 0.0] lmol), was dissolved in pyridine (] 0ml) and was then cooled to 0°C. 2,2-Dimethylpropanoyl chloride (1.5g, 0.012mol) was added dropwise over 5minutes. The reaction was stirred at 0°C for 30minutes and left to stand overnight at ambient temperature. The mixture was poured onto ice and extracted with diethyl ether. The ethereal extract was washed sequentially with water and brine, dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo to afford methyl 3-N-(2,2-dimethylpropanoyl)amino-4-fluorophenylacetate (2.9g), which was used without further purification in the next step.
'HNMR(CDCI3) 5: 1.4(s,9H); 3.6(s,2H); 3.7(s,3H); 6.95(m,lH); 7.05(m,lH); 7.6(bs,lH);8.3(dd,lH)ppm. Step 3
The product from Step 2 (2.8g, 0.0105mol) and [2,4-bis(4-methoxyphenyl)-l,3-dithia-2-2,4-diphosphetane-2,4-disulfide] (8.5g 0.021mol) were dissolved in dry toluene (100ml) and the mixture was heated under reflux for 17hours. The reaction was cooled to room temperature and the solvent was evaporated in vacuo. The residue was triturated with a 1:1 mixture of hexane : diethyl ether (100ml), the solution was decanted and solvent was evaporated in vacuo to yield an oil, which was further purified by flash column chromatography on silica gel, eluting sequentially with dichloromethane and diethyl ether, to yield methyl 3-jV-(2,2-dimethylthiopropionyl)amino-4-fluorophenylacetate (1.4g) as a yellow oil.
'HNMR (CDC13) 6: 1.5(s,9H); 3.65(s,2H); 3.75(s,3H); 7.1(m,2H); 8.4(d,lH); 8.7-8.9(bs,lH)ppm. Step 4
The product from Step 3 (1.3g, 0.046mol) and potassium carbonate (0.7g, 0.046mol) were dissolved in dry 7/^V-dimethylacetamide (10ml) with stirring and the mixture was

brought to reflux for 15minutes. The reaction mixture was cooled to room temperature, diluted with brine and extracted with diethyl ether. The ethereal extract was washed sequentially with water and brine, dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting sequentially with dichloromethane and diethyl ether, to yield methyl (2-/er/-butyl-5-benzothiazolyl)acetate (l.Og) as a yellow oil.
'HNMR (CDCI3) 5: 1.5(s,9H); 3.65(s,2H); 3.75(s,3H); 7.3(d,lH); 7.8(d,lH); 7.9(dd,lH)ppm. Step 5
The product from Step 4 (1 .Og, 0.039mol) was dissolved in methanol (8ml) and a solution of potassium hydroxide pellets (0.35g) in water (2ml) was added. The mixture was stirred at room temperature for 17hours. The mixture was acidified with concentrated hydrochloric acid to pH4 and the resultant Solution was diluted with water and extracted with ethyl acetate. The organic extract was washed with brine, dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo to afford 2-/er/-butyl-5-benzothioazolyl)acetic acid (0.62g) as a viscous oil.
'HNMR (CDCI3) 5:1.5(s,9H); 3.8(s,2H); 7.3(d,lH); 7.8(d,lH); 8.1(s,lH)ppm. Step 6
The acid prepared in Step 5 (0.2g, 0.001 mol) was suspended in dichloromethane (10ml) and one drop of A^^-dimethylformamide and oxalyl chloride (0.559g, 0 0044mol) were added sequentially. The mixture was stirred for 2hours and then the solvent was removed in vacuo. The residue was taken up in xylene (10ml), 5-amino-4-chloro-3-methylisothiazole was added and the mixture was heated under reflux for 2hours. The mixture was cooled to room temperature, diluted with ethyl acetate and washed with brine. The organic solution was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flash column chromatography on silica gel, eluting with a 1:1 mixture of hexane: diethyl ether, to give Compound 9 (Table A13)(0.04g).
EXAMPLE 15 This Example illustrates an alternative preparation of 2-/er/-butyl-5-benzothiazolylacetic acid (XX) (used in Example 14).


Step]
2-Fluoro-4-methylaniline (12.5g, O.lmol), was dissolved in pyridine (50ml) and cooled to 5°C. 2,2-Dimethylpropanoyl chloride (12.5g 0. Imol) was added dropwise over 1 Sminutes. The reaction was stirred at 5°C for 30minutes and then at ambient temperature for lhour. The reaction mixture was poured onto ice and the precipitate was collected by filtration, washed with water and dried to afford 3-fluoro-4-(#-2,2-dimethylethanoyl)aminotoluene 9.5g (46%) as a white solid, m.p. 88-89°C.
'H NMR (CDC13) 6: 1.3(s,9H); 2J(s,3H); 6.8(m,lH); 6.95(dd,lH); 7.6(blH); 8.2(dd,lH)ppm. Step 2
The product from Step 1 (8.0g, 0.039mol) and [2,4-bis(4-methoxyphenyl)-l,3-dithia-2-2,4-diphosphetane-2,4-disulfide] (15.5g, 0.039mol) were dissolved in dry toluene (200ml) with stirring and the mixture was heated at reflux for 6hours. The reaction mixture was cooled to room temperature and the solvent was evaporated in vacuo. The residue was further purified by passing through a plug of silica gel, eluting with a 9:1 mixture of hexane : diethyl ether (1000ml) to afford 3-fluoro-4-(iV-2,2-dimethylthioethanoyl)aniinotoluene 8.0g (91%) as a solid, m.p. 55-56°C.
'H NMR (CDCI3) 8: 1.5(s,9H); 2.3(s,3H); 7.0(dd,2H); 8.2(dd,lH); 8.8(bs,lH)ppm. Step 3
The product from Step 2 (8.0g, 0.036mol) and potassium carbonate (6.0g, 0.046 mol) were dissolved in dry A^A'-dimethylacetamide (30ml) with stirring and the mixture was heated at reflux for 60minutes. The reaction mixture was cooled to room temperature, diluted with brine and extracted with diethyl ether. The ethereal layer was washed sequentially with water and brine, dried over anhydrous magnesium sulfate and evaporated in vacuo to afford 2-/e/7-butyl-5-methylbenzothiazole as a colourless solid (5.4g), m.p. 55-57°C
'H NMR (CDC13) 6: 1.5(s,9H); 2.5(s,3H); 7.15(d,lH); 7.7(d,lH); 7.8(s,lH)ppm. Step 4

The product from Step 3 (5.1g, 0.025mol), //-bromosuccimide (4.8g, 0.030mol) and a catalytic quantity of 2,2'-azo-i»/j-isobutyronitrile were dissolved in carbon tetrachloride, with stirring and refluxed for about 3 Ominutes whilst being exposed to light generated from a 500W spotlight. The reaction mixture was cooled to room temperature, the precipitate removed by filtration and the filtrate was evaporated to an orange liquid (6.1g), which was used directly in the next step. StepS
A solution of potassium cyanide (2.0g, 0.03 lmol) in dimethyl sulphoxide (DMSO) (10ml) was added, dropwise, to a solution of the product from Step 4 (2.0g, 0.007mol) in dry DMSO (5ml). The mixture was stirred at room temperature for 1 Ominutes, then poured into water, diluted with brine and extracted with diethyl ether. The ethereal layer was washed sequentially with water and brine, dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by flashed column chromatography on silica gel, eluting with a 1:1 mixture of hexane : diethylether, to give 2-/er/-butyl-5-benzothiazolylacetonitrile as a yellow solid (0.90g), m.p. 50-52°C
'HNMR (CDC13) 8: 1.5(s,9H); 3.9(s,2H); 7.3(d,lH); 7.85(d,lH); 8.0(s,lH)ppm. Step 6
The product from Step5 (0.90g, 0.004mol) was dissolved in methanol (8ml) and a solution of potassium hydroxide pellets (0.3 5g, 0.006mol) in water (2ml) was added. The mixture was refluxed fori 7 hours and was then cooled to room temperature. The mixture was acidified with concentrated hydrochloric acid to pH4 and the resultant solution was diluted with water~and extracted with ethyl acetate. The organic extract was washed with brine, dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo to afford 2-terf-butyl-5-benzothiazolylacetic acid (0.5g) as a viscous oil.
'HNMR (CDCI3) 5: 1.5(s,9H); 3.8(s,2H); 7.3(d,lH); 7.8(d,lH); 8.1(s,lH)ppm.
EXAMPLE 16
This Example illustrates the preparation of Compound 4 (Table A43). Stepl
4-Aminophenylacetic acid (15g, O.lmol) was stirred in n-butyric anhydride (70ml) at room temperature for 1 hour. The mixture was poured into iced water and the resultant

precipitate was collected by filtration and washed with ethyl acetate to afford 4-N-(«-propionyl)amino-phenylacetic acid (11.4g) as a pink solid.
lH NMR (CDCI3) 5:1.0(t,3H); 1.8(m,2H); 2.3(t,2H); 3.6(s,2H); 7.2(dr2H); 7.5(d2H); 8.0(b,lH)ppm. Step 2
Concentrated nitric acid (8ml) was added dropwise to a chilled (ice-bath) solution of 4-A^-(n-propionyl)aminophenylacetic acid (11.4g, 0.05 lmol) in acetic anhydride (30ml) and the mixture was stirred until the reaction was complete. The mixture was poured onto ice and the resultant precipitate was collected by filtration and dried to give 2~mUoA-N-(n-propionyl)aminophenylacetic acid (7.6g) as a yellow solid.
'H NMR (CDCI3) 8:1.0(t,3H); 1.8(naH); 2.5(t,2H); 3.6(s,2H); 7.6(dd,lH); 8.2(d,lH); 8.7(d,lH)ppm. Step 3
The acid prepared in Step 2 (5.4g, 0.02mol) was suspended in dichloromethane (30ml) and one drop of #^-dimemylfonaamide and oxalyl chloride (2.8g, 0.022mol) were added sequentially. The mixture was stirred for 2hours and then the solvent was removed in vacuo. The residue was taken upip^ 1^2-dichloroethane (10ml), S-ammtf^^hldro^--methylisothiazole (3.3g, 0.02mol) was added arid the mixture was heated under reflux for . 2hours. The mixture was cooled to room temperature, diluted with ethyl acetate and washed with saturated aqueous sodium bicarbonate solution. The organic solution was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. Trituration with dichloromethane and gave A^(4-chlorc>-3-meftyl-5-isothiazolyl)-[3-nitro-4-^-(n-propionyl)amino]phenylacetamide (0.42g) as a cream solid.
'H NMR (CDCI3) 6:1.0(t,3H); 1.8(m,2H); 2.4(s,3H); 2.5(t,2H); 4.0(s,2H); 7.7(dd,lH); 8.3(d,lH); 8.4(d,lH); 10.2(s,lH); 10.6(s,lH)ppm.
The dichlormethane washings were evaporated in vacuo and triturated with a 1:1 mixture of ethyl acetate and hexane to give a further quantity (3.80g) of desired product Step 4
A mixture of the product obtained in Step 3 (0.4g, 0.001 mol) and iron powder (0.54g) in a mixture of isopropanol (10ml) and water (1ml) were heated at reflux until thin layer chromotography showed the reaction to be complete. The mixture was cooled to room


L temperature, filtered through diatomaceous earth and the filtrate was evaporated in vacuo. Ethyl acetate was added and insoluble material was collected by filtration to give A44-
chloro-3-methyl-5-isothiazolyl)-[3-amino-4-A'-(/j-propionyl)amino]phenylacetamide (0.085g) as a grey solid.
•H NMR (CDC13) 6: 1.0(t,3H); 1.8(m,2H); 2.3-2.5(m,5H); 3.8(s,2H); 6.7(dd,lH); 6.8(d,lH)ppm. Step 5
The product obtained in Step 4 (0.085g, 0.0002mol) was suspended in 2-methoxyethyl ether (5ml) and/vtoluenesulfonic acid (0.045g, 0.0002mol) was added. The mixture was heated to reflux for 6hours. The mixture was cooled to room temperature, diluted with ethyl acetate and washed with saturated aqueous sodium bicarbonate solution. The organic solution was dried over anhydrous magnesium sulfate, filtered and the filtrate was evaporated in vacuo. The residue was further purified by chromatgraphy to afford Compound 4 (Table A43).
EXAMPLE 17 This Example illustrates an emiu'sifiable concentrate composition which is readily convertible, by addition to water, into a preparation suitable for spraying purposes. The emulsifiable concentrate has the following composition:
% by weight
Compound No. 4 (Table A23) 25.0
SYNPERONICNP13 2.5
Calcium dodecylbenzenesuiphonate 2.5
AROMASOLH 70.0
EXAMPLE 18 This Example illustrates a wettable powder composition which is readily convertible, by addition to water, into a preparation suitable for spraying purposes. The wettable powder has the following composition:
% by weight
Compound No. 272 (Table A3) 25.0
Silica 25.0

Sodium lignosulphonate 5.0
Sodium lauryl sulphate 2.0
Kaolin 43.0
EXAMPLE 19 This Example illustrates a dustable powder which may be applied directly to plants or other surfaces. The dustable powder has the following composition:
% by weight
Compound No. 4 (Table K3) 1.0
Talc 99.0
EXAMPLE 20 This Example illustrates an oil miscible liquid formulation suitable for application by ultra low volume techniques after mixing with an organic diluent. The formulation has the following composition:
% by weight
Compound No. 2 (Table D3) 10.0
SOLVESSO 200 90.0
EXAMPLE 21 This Example illustrates a capsule suspension concentrate which is readily convertible, by addition to water, into'a. preparation suitable for application as an aqueous spray. The capsule suspension concentrate has the following composition:
% by weight
Compound No. 15 (Table H3) 10.0
AROMASOLH 10.0
Toluene di-isocyanate 3.0
SYNPERON1CA7 1.0
Polyvinyl alcohol 2.0
Bentonite 1.5
KELTROL 0.1
Water 72.4


EXAMPLE 22 This Example illustrates a ready for use granular formulation which is prepared from a preformed granular carrier. The granular formulation has the following composition:
% by weight
Compound No. 251 (Table A43) 0.5
SOLVESSO 200 0.2
SYNPERON1CA7 0.1
Calcium carbonate granules (diameter 0_3-0.7mm) 992
EXAMPLE 23 This Example illustrates a ready for use granular formulation which is prepared by granulation of the powdered components. The granular formulation has the following composition:
% by weight
Compound No. 4 fTaDleE3) 0.5
Sodium lignosulphpnate 5.0
Kaolin ; 94.5
EXAMPLE 24 This Example illustrates an aqueous suspension concentrate composition wnich is readily convertible, by addition to water, into a preparation suitable for spraying purposes. The suspension concentrate has the following composition:
% by weight
Compound No. 331 (Table A3) 25.0
Sodium lignosulphonate 3.0
Propylene glycol 10.0
Bentonite 2.0
KELTROL 0.1
PROXEL 0.1
Water 59.8


EXAMPLE 25 This Example illustrates a water dispersible granule formulation which is readily convertible, by addition to water, into a preparation suitable for spraying purposes. The water dispersible granule has the following composition:
% by weight
Compound No. 343 (Table A3) 25.0
Silica 5.0
Sodium lignosulphonate 10.0
Sodium lauryl sulphate 5.0
Sodium acetate 10.0
Montmorillonite powder 45.0
.■ -v.-,
EXAMPLE 26
This Example illustrates the pesticidal / insecticidal properties of compounds of formula (I). The activities of individual ^compounds of formula (I) were determined using a variety of pests. With the exception of nematodes, the pests were treated with a liquid composition containing 500 parts per million (ppm) by weight of a compound unless otherwise stated. Each composition was made, by dissolving the compound in an acetone and ethanol (50:50 by volume) mixture and diluting the solution with water containing 0.05% by volume of a wetting agent, SYNPERONIC NP8, until the liquid composition contained the required concentration of the compound.
The test procedure adopted with regard to each pest, except nematodes, was essentially the same and comprised supporting a number of the pests on a medium which was usually a substrate, a host plant or a foodstuff on which the pests feed, and treating either or both the medium and the pests with a composition. Pest mortality was assessed usually between three and five days after treatment. Knockdown of housefly(Musca domestica) was assessed 15 minutes after treatment.
The test procedure for nematodes involved dissolving the compound in an acetone and ethanol (50:50 by volume) mixture and diluting the solution with water to obtain a final concentration of the compound of 12.5ppm. J2 infective juveniles ofMeloidogyne incognita

were suspended in the solution in a glass vial and mortality assessed after a period of three days.
The results of the tests are presented in Tables XI and X2. The results indicate a grading of mortality (score) designated as 9, 5 or 0 wherein 9 indicates BO-100% mortality, 5 indicates 40-79% mortality and 0 indicates less than 40% mortality.


Key to Tables XI and X2:
TETRUR - Tetranychus urticae MYZUPE = Myzuspersicae
MUSCDO AKL = Musca domesiica (kill) MUSCDO AC == Musca domestica (knockdown)
HELIVI = Heliolhis virescem LAPHEG = Spodoptera exigua
MELGIN = Meloidogyne incognita N/T = Not tested

EXAMPLE 27
This Example illustrates the fungicidal properties of compounds of formula (I). The compounds were tested against a variety of foliar fungal diseases of plants. The technique employed was as follows.
Plants were grown in John Innes Potting Compost (No.l or 2) in 4cm diameter, 3.5cm depth minipots. The test compounds were individually formulated as a solution either in acetone or acetone/ethanol (1:1 by volume) which was diluted in deionised water to a concentration of lOOppm (that is, lmg of compound in a final volume of 10ml) immediately before use. When foliar sprays were applied to monocotyledonous crops, TWEEN 20 (0.1% by volume) was added. TWEEN is a registered trade mark.
Individual compounds of formula (I) were applied as a foliar (Folr) application (where the chemical solution was applied \6 the foliage of the test plants by spraying the plant to maximum droplet retention); as a systemic (Syst) application (where the chemical solution, 10ml, was applied as a root drench treatment) or as a stem (Stem) application (where the chemical solution was applied to the stems of the test plants by spraying the plants to run off).
These tests were carried out against Plasmopara viticola (PLASVI) and Uncinula necator (UNCINE), on vinesfPhytophthora infestans lycopersici (PHYTTN) and Botrytis cinerea (BOTRCI), on tomatoes; Venturia inaequalis (VENTIN), on apples; Erysiphe graminis fsp. tritici (ERYSGT), Septoria nodorum (LEPTNO) and Puccinia recondita (PUCCRT), on wheat; and Pyricularia oryzae (PYRIOR) and Rhizoctonia solani (RHIZSO), on rice. Each treatment was applied to two or more replicate plants for Plasmopara viticola, Phytophthora infestans lycopersici, Botrytis cinerea, Uncinula necator and Venturia inaequalis. In tests on Erysiphe graminis f.sp. tritici, Septoria nodorum, Puccinia recondita, Rhizoctonia solani and Pyricularia oryzae two replicate pots each containing 6 tolO plants were used for each treatment. The plants were inoculated with a calibrated fungal spore suspension one or two days before (Erad) or 6hours, one day or two days after (Prot) chemical application.
After chemical application and inoculation, the plants were incubated under high humidity conditions and then put into an appropriate environment to allow infection to

1 proceed, untiJ the disease was ready for assessment. The Erysiphe graminis f.sp. tritici plants were inoculated using a 'shake' inoculation technique. The Uncinula necator plants were inoculated using a 'blowing' inoculation technique. For Plasmopara viticola, the plants were reincubated under high humidity conditions for 24hours prior to assessment. The time period between chemical application and assessment varied from five to fourteen days according to the disease and environment. However, each individual disease was assessed after the same time period for all compounds.
Assessments were performed on a single leaf of each of the two replicate plants for Plasmopara viticola and Venturia inaequalis and on each of two leaves on each of the replicate plants for Phytophthora infestans lycopersici andBotrytis cinerea. Assessments were performed on a single leaf of each of the three replicate plants for Uncinula necator. Vox Erysiphe graminis f.sp. tritici, Septoria nodorum, Puccinia recondita and Pyricularia recondita assessments were earned out collectively on the plants in each replicate pot. For Rhizoctonia solani, the number of infected plants in each of two replicate pots were assessed.
The disease level present (that is, the percentage leaf area covered by actively sporulating disease) or percentage of infected plants per pot was assessed visually. For each treatment, the assessed values for all its replicates were meaned to provide mean disease values. Untreated control plants were assessed in the same manner. The data were then processed by either of two alternative methods, described hereinafter, each providing its own PRCO (Percentage Reduction from Control) value.
METHOD 1
This method uses banded assessment values.
The mean disease values are banded in the manner shown below. If the disease level value falls exactly mid-way between two of the points, the result will be the lower of the two points.
0 = 0% disease present 10 = 5.1-10% disease present
1 = 0.1 -1 % disease present 20 - 10.1 -20% disease present 3= 1.1-3% disease present 30= 20.1-30% disease present 5= 3.1-5% disease present 60= 30.1-60% disease present
90 = 60.1-100% disease present


An example of a typical banded calculation is as follows:
Mean disease level for treatment A = 25% Therefore handed mean disease level SOT txeaimeni A =30 Mean disease level on untreated controls = 85% Therefore banded mean disease level on untreated controls = 90
PRCO = 100 - { Banded mean disease level for treatment A } x 100 {Banded mean disease level on untreated controls}
= 100- (30x100) = 66.7 90
The PRCO is then rounded to the nearest whole number; therefore, in this particular example, the PRCO *esult is 67.
METHOD 2
This method tjses unhanded assessment values (that is, the mean disease values are used in the PRCO cakulation.without a banding step).
An example Qf a typical unhanded calculation is as follows:
Mean disease level for treatment A = 25% Mean disease level on untreated controls = 85%
PRCO - 100 - { Mean disease level for treatment A } x 100 {Mean disease level on untreated controls}
= 100- (25 xlOO) = 70.6 85
The PRCO is then roijnded to the nearest whole number; therefore, in this particular example, the PRCO result is 71.


It is possible for negative PRCO values to be obtained. PRCO results are shown below.

TABLE Yl



TABLE Y2




PYRJOR = Pyricularia oryzae RHIZO = Rhizoctonia solani
VENTIN = Venturia inaegualis ' BOTRCI = Botryiis cinerea

EXAMPLE 28
This Example illustrates the synergistic fungicidal properties of compounds of formula (1) when used in mixture with other compounds. The compounds were tested against a variety of foliar fungal diseases of plants. The technique employed was as follows.
Plants were grown in John Innes Potting Compost (No.l or 2) in 4cm diameter, 3.5cm depth minipots or 8cm diameter, 7cm depth pots. Compounds were tested individually or in two-compound mixtures. The test compounds were individually formulated as a solution either in acetone or acetone/ethanol (1:1 by volume) which was then diluted in deionised water to give a compound concentration such as lOOppm (that is, lmg of a compound in a final volume of 10ml) immediately before use. Solutions of two-compound mixtures were prepared by mixing two appropriate solutions of individual compounds. Sprays were applied as foliar applications (where the chemical solution was applied to the foliage of the test plants by spraying the plant to maximum droplet retention). When applied to monocotyledonous crops, TWEEN 20 (0. ] % by volume) was added. TWEEN is a registered trade mark. For each two-compound mixture tested, each of the two compounds was also tested individually, the concentration of an individual compound in an individual test being the same as the concentration of that same compound when present in the corresponding two-compound mixture test.
These tests were carried out against Plasmopara viticola (PLASVI), on vines; Septoria nodorum (LEPTNO), on wheat; and Rhizoctonia solani (RHIZSO), on turf. Each treatment was applied to four replicate plants for Plasmopara viticola. In tests on Septoria nodorum four replicate pots each containing 6 to 10 plants were used for each treatment In tests on Rhizoctonia solani four replicate pots each containing a covering of turf were used for each treatment. The plants were inoculated with a calibrated fungal spore suspension one day after chemical application.
After chemical application and inoculation, the plants were incubated under high humidity conditions and then put into an appropriate environment to allow infection to proceed, until the disease was ready for assessment. For Plasmopara viticola, the plants were reincubated under high humidity conditions for 24hours prior to assessment. The time period between chemical application and assessment varied from four to fourteen days according to the disease and environment However, each individual disease was assessed after the same time period for all compounds and mixtures.


Key to Tables Yl and Y2
* = METHOD 1 (otherwise METHOD 2) 6h = l hour ld= lday
ER YSGT = Erysiphe graminis tritici PHYTIN = Phytophthora infestans lycopersici
PLASVI = Plasmopara viticola PUCCRT = Puccinia recondita
LEPTNO = Septoria nodorum UNCINE = Unc'mula necator

Assessments were performed on a single leaf of each of the replicate plants for Plasmopara viticola. For Septoria nodorum and Rhizoctonia solani assessments were carried out collectively on the plants in each replicate pot.
Step 1. Determination of fungicidal control.
For each replicate of a treatment the disease level present (that is, the percentage leaf area covered by actively sporulating disease for Plasmopara viticola, lesion area caused by Septoria nodorum and percentage area of turf infected for Rhizoctonia solani) was assessed visually. The data obtained were then processed according to METHOD 2 of Example 27 in order to obtain PRCO (Percentage Reduction from Control) values.
Step 2. Synergy assessment.
Limpel's formula (Pesticide Science (1987)19 309-315 at 312) is used to determine the PRCO which a two-compound mixture is expected to provide, assuming that in mixture the compounds provide fungicide control jn an additive manner. The expected control of the mixture is based on the PRCO data for the two individual compounds, when each is applied individually at the same rate as that used in mixture. If in tests the observed PRCO of the mixture is greater than the expected PRCO, then according to Limpel the two compounds are displaying synergistic behaviour when applied in mixture.
Limpel's formula is:
E = X+Y-XY 100
where:
X is the PRCO of substance A applied at a rate of p mg/1;
Y is the PRCO of substance B applied at a rate of q mg/1; and
E is the expected PRCO of two-compound mixture [A+B] (A and B applied
respectively at p and q mg/1).


The table below provides example data for two compounds tested individually and in mixure together.

In this example the PRCO observed for the mixture is greater than the value E calculated according to Limpel, therefore this mixture of A and B is synergistic.
The following tables contain observed and expected disease control data for a number compound mixtures, each of which contains Compound 15 of Table A3.

TABLE ZI: SEPTORIA NODORUM ~ Compound 15 (A3) and azoxvstrobin.

Conclusion: The mixtures show synergy.

TABLE Z2: PLASMOPARA VITICOLA - Compound 15 (A3) and azoxystrobin.

Conclusion: The mixture shows synergy.



TABLE Z3-.PLASM0PARA VITICOLA - Compound 15 f A3) and nuazinam.
Conclusion: The mixture shows synergy.

TABLE Z4: PLASMOPARA VITICOLA - Compound 15 (A3) and fenamidohe.

Conclusion: The mixture shows synergy.

TABLE Z5: RHIZOCTONIA SOLANI - Compound 15 fA3) and nzoxvstrobln.

Conclusion: The mixtures show synergy.

TABLE Z6: RHIZOCTONIA SOLANI - Compound 15 f A3^ and fluaanam.

Conclusion: The mixtures show synergy.

Chemical Formulae in the Description


WE CLAIM:-
1. A isothiazole compound of formula (I)

wherein X is O or S; n is 0 or 1; Y is O, S or NR7; R1 is hydrogen,
halogen, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6
alkylthio, C1-6 haloalkylthio, C3-6 cycloalkyl, C1-6 alkoxy(C1-6) alkyl or
SF5; R2 is hydrogen, halogen, Ci-6 alkyl, Ci-6 alkoxy, Ci-e haloalkoxy,
C1-6 alkylthio, C1-6 haloalkylthio, C1-6 alkylsulfinyl, C1-6
haloalkylsulfinyl, C1-6 alkylsulfonyl, C1-6 haloalkylsulfonyl, C1-6
haloalkyl, cyano, nitro, CHO, CH=NOR5, C1-6 alkylcarbonyl, C1-6
alkoxycarbonyl or SF5; or together R1 and R2 form a five or six
membered saturated or unsaturated carbocyclic ring, optionally
substituted by one or two C1-6 alkyl groups; R3 is hydrogen, C1-6
alkyl, CH2(C1-4 haloalkyl), C1-6 cyanoalkyl, C1-6 alkenyl, C1-6 alkynyl,
C1-6 alkoxy(C1-6)alkyl, C1-6 alkylthio(C1-6)alkyl, C1-6 alkoxy(Ci-
6)alkoxy(C1-6)alkyl, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, formyl,
C1-6 alkylcarbonyl(C1-6)alkyl, C1-6 alkoxycarbonyl(C1-6)alkyl, C1-6
alkylaminocarbonyl, di(C1-6)alkylaminocarbonyl, optionally
substituted phenoxycarbonyl, optionally substituted phenyl(Ci-4)alkyl or S(0)qR6; R4 is hydrogen, halogen, cyano, C1-6 alkyl, C1-6 haloalkyl, C1-6 cyanoalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C3-7 halocycloalkyl, C3-7 cyanocycloalkyl, C1-3 alkyl(C3-7)cycloalkyl, C1-3 alkyl(C3-7)lhalocyclQalkyU C3-6 cycloalkyl(C1-6jalkyl, C5-6 cycloalkenyl, C5-6 cycloalkenyl(C1-6)alkyl, C2-6 haloalkenyl, C1-6 cyanoalkenyl, C1-6 alkoxy(C1-6)alkyl, formyl, C1-6 carboxyalkyl, C1-6 alkylcarbonyl(C1-6)alkyl, C1-6 alkoxycarbonyl(C1-6)alkyl, C1-6

alkylthio(Ci-e)alkyl, Ci-6 alkylsulfinyl(Ci-6)alkyl, Ci-6 alkylsulfonyl(Ci-6)alkyl, aminocarbonyl(Ci-6)alkyl, Ci-6 alkylaminocarbonyl(Ci-6)alkyl, di(Ci-6)alkylaminocarbonyl(Ci-6)alkyl, Ci-6 alkoxycarbonyl, Ci-e alkyl carbonyl, aminocarbonyl, Ci-6 alkylaminocarbonyl, di(Ci-6)alkylaminocarbonyl, optionally substituted phenyl, optionally substituted phenyl(Ci-4)alkyl, optionally substituted phenyl(C2-4)alkenyl, optionally substituted heteroaryl, optionally substituted heteroaryl(Ci-4)alkyl, optionally substituted heterocyclyl, optionally substituted heterocyclyl(C1-4)alkyl, a group OR8, a group SH, a group S(0)PR9, a group NR">R" or a group C(Ri2)=NOR13; R5 is hydrogen, C1-6 alkyl, optionally substituted phenyl or optionally substituted phenyl(C1-4)alkyl; R6 is C1-6 alkyl, C1-6 haloalkyl or optionally substituted phenyl; R7 is hydrogen, cyano, C1-8 alkyl, C1-6 haloalkyl, C1-6 cyanoalkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 cycloalkyl, C2-6 haloalkenyl, C3-6 cycloalkyl (C1-6)alkyl, C1-6 alkoxy(Ci-6)alkyl, Ci-6 alkoxycarbonyl, C1-6 alkylcarbonyl, Ci-6 alkyl amino carbonyl, di(C1-6)alkylaminocarbonyl, optionally substituted phenyl or optionally substituted heteroaryl; R8 is hydrogen, C1-6 alkyl, C1-6 haloalkyl, C3-6 alkenyl, C1-4 cyanoalkyl, C1-6 alkoxycarbonyl(C1-6)alkyl, optionally substituted phenyl, optionally substituted phenyl(C1-4)alkyl, optionally substituted heteroaryl, N=C(CH3J2; R9 is C1-6 alkyl, C1-6 haloalkyl, C3-6 alkenyl, cyano, C1-4 cyanoalkyl, C1-6 alkoxycarbonyl(Ci-6)alkyl, optionally substituted phenyl, optionally substituted phenyl(C1-4)alkyl or optionally substituted heteroaryl; R10 and R11 are, independently, hydrogen, C1-8 alkyl, C3-7 cycloalkyl, C1-6 alkenyl, C1-6 alkynyl, C1-6 haloalkyl, C1-6 alkoxy(C1-6)alkyl, C1-6 alkoxycarbonyl, optionally substituted phenoxycarbonyl, formyl, C1-6 alkylcarbonyl, C1-6 alkylS02 optionally substituted phenylS02 or optionally substituted phenyl(C1-4)alkyl; R12 is C1-3 alkyl; R13 is C1-6 alkyl, optionally substituted phenyl(C1-6)alkyl; and p and q are, independently, 0, 1 or 2.


2. A compound of formula (la) or a compound of formula (lb):

wherein R1, R2, R3, R4, X, Y and n are as claimed in claim 1.
3. A compound of formula (I) as claimed in claim 1 or 2 wherein n is zero.
4. A compound of formula (la) or a compound of formula (lb) as claimed in claim 3 wherein R1 is C1-2 alkyl.

5. A compound of formula (la) or a compound of formula (lb) as claimed in claim 3 or 4 wherein R2 is hydrogen, cyano or halogen.
6. A compound of formula (la) or a compound of formula (lb) as claimed in claim 3, 4 or 5 wherein R3 is hydrogen, C1-6 alkyl or C1-6 alkoxy(C 1-6)alkyl.
7. A compound of formula (la) or a compound of formula (lb) as claimed in claim 3, 4, 5 or 6 wherein R4 is hydrogen, SH, C1-6 alkyl, C3-6 cycloalkyl, C2-6 alkenyl, C2-5 alkynyl, C1-4 haloalkyl, C1-4 cyanoalkyl, C2-6haloalkenyl, optionally substituted heterocyclyl(Ci-4)alkyl), C2-6 cyanoalkenyl, phenyl (optionally substituted with fluoro, chloro, bromo, nitro, cyano, C1-6 alkyl, Ci-2alkoxy, C1-4


haloalkyl, C1-4 haloalkoxy, methanesulfonyl, methylenedioxy or di(C1-4 alkyl)amino), phenyl(C1-3)alkyl (phenyl optionally substituted with halogen, nitro, cyano, C1-6 alkyl, C1-2 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, methanesulfonyl, or methylenedioxy); formyl, optionally substituted heterocyclyl, optionally substituted heteroaryl, optionally substituted heteroaryl(C1-4) alkyl, C1-2 alkylcarbonyl, C1-4 alkoxycarbonyl, C1-5 alkoxycarbonyl(C1-4)alkyl, a group NR10Rn, a group OR8, C1-4 alkoxymethyl, chlorine, a group SR9, or a group C(R12)=NOR13; R8 is hydrogen, C1-5 alkyl, C1-4 haloalkyl, C2-4 alkenyl, phenyl (optionally substituted with fiuoro, chloro, bromo, nitro, cyano, C1-6 alkyl, C1-2 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, methanesulfonyl, or methylenedioxy), phenyl(CHa) (phenyl optionally substituted with fiuoro, chloro, bromo, nitro, cyano, C1-2 alkyl, C1-2 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, methanesulfonyl, or methylenedioxy), N=C(CH3)2: R9 is C1-5 alkyl, phenyl (optionally substituted with fiuoro, chloro, bromo, nitro, cyano, C1-6 alkyl, C1-2 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, methanesulfonyl, methylenedioxy or di(C1-4 alkyl) amino), C1-2 haloalkyl, cyano, cyanomethyl or C1-2 alkoxycarbonylmethyl; R10 and R11 are, independently, hydrogen, C1-4 alkyl, C5-6 cycloalkyl, formyl, C1-3 alkylcarbonyl, phenoxycarbonyl, C1-2 alkylS02 or phenylSCh; R12 is C1-2 alkyl; and R13 is C1-2 alkyl or benzyl.
8. A compound of formula (I) as claimed in any one of the preceding
claims wherein
logioKo/w (calculated using the CLOGP3 program, available from BioByte Corp.) of the compound is in the range zero to 8.
9. A compound of formula (I) as claimed in any one of the preceding
claims wherein in the side chain portion of formula (XIX):



no atom having an atomic weight greater than 10 Dal tons is more than four bond lengths away from at least one atom present in the longest bond path or, where there is a set of longest bond paths, no atom having an atomic weight greater than 10 Dal tons is more than four bond lengths away from at least one atom present in each of the longest bond paths.
10.A fungicidal, insecticidal, acaricidal, molluscicidal or nematicidal composition comprising a fungicidally, insecticidally, acaricidally, molluscicidally or nematicidally effective compound of formula (I) as claimed in claim 1 and a carrier or diluent therefore, wherein said compound is present in the range of 0.0001 to 95%.
Dated this 19th day of May, 2005
[DEEPA KACHROO TIKU]
Of REMFRY & SAGAR
ATTORNEY FOR THE APPLICANTS

Documents

Application Documents

# Name Date
1 471-mumnp-2005-power of authority(7-4-2008).pdf 2018-08-09
2 471-mumnp-2005-power of authority(6-10-2008).pdf 2018-08-09
3 471-mumnp-2005-petition under rule 137(7-4-2006).pdf 2018-08-09
4 471-mumnp-2005-form-pct-ipea-409(7-4-2006).pdf 2018-08-09
5 471-mumnp-2005-form 5(19-5-2008).pdf 2018-08-09
6 471-mumnp-2005-form 3(7-4-2006).pdf 2018-08-09
7 471-mumnp-2005-form 3(19-5-2008).pdf 2018-08-09
8 471-mumnp-2005-form 2(granted)-(7-4-2006).pdf 2018-08-09
9 471-mumnp-2005-form 18(8-11-2005).pdf 2018-08-09
10 471-mumnp-2005-form 13(13-8-2007).pdf 2018-08-09
11 471-mumnp-2005-form 1(20-5-2008).pdf 2018-08-09
12 471-mumnp-2005-form 1(13-8-2007).pdf 2018-08-09
13 471-mumnp-2005-correpondence(ipo)-(21-1-2008).pdf 2018-08-09
14 471-mumnp-2005-correpondence(10-8-2007).pdf 2018-08-09
15 471-mumnp-2005-claims(granted)-(7-4-2006).pdf 2018-08-09
16 471-mumnp-2005-cancelled pages(7-4-2006).pdf 2018-08-09

ERegister / Renewals

3rd: 29 Apr 2008

From 21/07/2001 - To 21/07/2002

4th: 29 Apr 2008

From 21/07/2002 - To 21/07/2003

5th: 29 Apr 2008

From 21/07/2003 - To 21/07/2004

6th: 29 Apr 2008

From 21/07/2004 - To 21/07/2005

7th: 29 Apr 2008

From 21/07/2005 - To 21/07/2006

8th: 29 Apr 2008

From 21/07/2006 - To 21/07/2007

9th: 29 Apr 2008

From 21/07/2007 - To 21/07/2008

10th: 29 Apr 2008

From 21/07/2008 - To 21/07/2009

11th: 29 Jun 2009

From 21/07/2009 - To 21/07/2010

12th: 18 Jun 2010

From 21/07/2010 - To 21/07/2011

13th: 20 Jun 2011

From 21/07/2011 - To 21/07/2012

14th: 22 Jun 2012

From 21/07/2012 - To 21/07/2013

15th: 11 Jul 2013

From 21/07/2013 - To 21/07/2014