Substituted Dihydropyrrolopyrazole Compound

Ube Industries Ltd.
Granted App No 201747016742 Patent 431692 Chemical

Patent information

IP India · live record
Application number
201747016742
Filing date
12 May 2017
Status
Granted
Legal status
Inforce
Publication number
20/2017
Publication type
INA
Invention field
Chemical
Patent number
431692
Grant date
12 May 2023
Next renewal due
30 October 2026Overdue

Abstract

11 6231231 445A compound represented by general formula (I) [in the formula L represents an optionally substituted C alkylene group or the like L represents a single bond or the like L represents a single bond or the like R R and R each independently represent an optionally substituted C alkyl group or the like R represents a hydrogen atom or the like and R represents a hydrogen atom or the like] or a pharmacologically acceptable salt thereof.

Applicants

1
Japan
UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633

Inventors

15
Japan
AGA Yasuhiroc/o UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633
Japan
USHIYAMA Shigeruc/o UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633
Japan
IWASE Noriakic/o UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633
Japan
KONO Shigeyukic/o UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633
Japan
SUNAMOTO Hidetoshic/o UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633
Japan
MATSUSHITA Takashic/o UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633
Japan
OGI Sayakac/o UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633
Japan
TANAKA Masayukic/o UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633
Japan
MATOYAMA Masaakic/o UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633
Japan
UMEZAKI Satoshic/o UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633
Japan
SHIRAISHI Yusukec/o UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633
Japan
ONUMA Kazuhiroc/o UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633
Japan
KOJIMA Masahiroc/o UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633
Japan
NISHIYAMA Hayatoc/o UBE INDUSTRIES LTD. 1978 96 Oaza Kogushi Ube shi Yamaguchi 7558633
Japan
KIMURA Tomio5 10 3209 Konan 3 chome Minato ku Tokyo 1080075

Specification

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CLAIMS 1. A compound represented by formula (I) or a pharmacologically acceptable salt thereof: [Chemical Formula 1 ] N-^-V P V-NH L3-0 wherein L1 is an optionally substituted linear or branched C,.6 alkylene group, an optionally substituted linear or branched C2-6 alkenylene group, an optionally substituted linear or branched C2-6 alkynylene group, an optionally substituted C3.6 cycloalkylene group, or an optionally substituted C3.6 cycloalkenylene group, L is a single bond, an oxygen atom, an optionally substituted nitrogen atom, an optionally substituted linear or branched C,.6 alkylene group, an optionally substituted linear or branched C2-6 alkenylene group, an optionally substituted linear or branched C2.6 alkynylene group, an optionally substituted C3.6 cycloalkylene group, or an optionally substituted C3.6 cycloalkenylene group, L" is a single bond, an optionally substituted linear or branched C|_6 alkylene group, an optionally substituted linear or branched C2-6 alkenylene group, an optionally substituted linear or branched Cq.(, alkynylene group, an optionally substituted C3.r, cycloalkylene group, or an optionally substituted C3.6 cycloalkenylene group,

R1, R% and R3 are each independently an optionally substituted linear or branched CM alkyl group, an optionally substituted linear or branched C2-4 alkenyl group, an optionally substituted linear or branched C2-4 alkynyl group, an optionally substituted C6-io aryl group, or an optionally substituted heterocyclic group, R is a hydrogen atom, an optionally substituted linear or branched C|_6 alkyl group, an optionally substituted linear or branched C2-6 alkenyl group, an optionally substituted linear or branched C2.6 alkynyl group, an optionally substituted C3.6 cycloalkyl group, an optionally substituted C3.6 cycloalkenyl group, an optionally substituted C6-m aryl group, or an optionally substituted heterocyclic group, and R is a hydrogen atom, an optionally substituted linear or branched C1.16 alkyl group, an optionally substituted linear or branched C2.!6 alkenyl group, an optionally substituted linear or branched C2.i6 alkynyl group, an optionally substituted C3.6 cycloalkyl group, an optionally substituted C3.6 cycloalkenyl group, an optionally substituted C6.10 aryl group, or an optionally substituted heterocyclic group. 2. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein L1 is an optionally substituted linear or branched C^ alkylene group or an optionally substituted C3.6 cycloalkylene group. 3. A compound represented by formula (II) or a pharmacologically acceptable salt thereof:

Chemical Formula 2

Y-NH L3-0 >CR' ^ (II) SI wherein L2 is a single bond, an oxygen atom, an optionally substituted nitrogen atom, an optionally substituted linear or branched Ci_6 alkylene group, an optionally substituted linear or branched C2.6 alkenylene group, an optionally substituted linear or branched C2-6 alkynylene group, an optionally substituted C^.b cycloalkylene group, or an optionally substituted C3.6 cycloalkenylene group, L3 is a single bond, an optionally substituted linear or branched C1.6 alkylene group, an optionally substituted linear or branched C2.6 alkenylene group, an optionally substituted linear or branched C2„6 alkynylene group, an optionally substituted C3_6 cycloalkylene group, or an optionally substituted C3.6 cycloalkenylene group, R', R , and RJ are each independently an optionally substituted linear or branched C[_4 alkyl group, an optionally substituted linear or branched C2.4 alkenyl group, an optionally substituted linear or branched C2_4 alkynyl group, an optionally substituted Q,.io aryl group, or an optionally substituted heterocyclic group, R4 is a hydrogen atom, an optionally substituted linear or branched Cj_6 alkyl group, an optionally substituted linear or branched C2_6 alkenyl group, an optionally substituted linear or branched C2_6 alkynyl group, an optionally substituted C3.6 cycloalkyl group, an

optionally substituted C3_6 cycloalkenyl group, an optionally substituted C6.10 aryl group, or an optionally substituted heterocyclic group, and R5 is a hydrogen atom, an optionally substituted linear or branched CM6 alkyl group, an optionally substituted linear or branched C2.l6 alkenyl group, an optionally substituted linear or branched C2-16 alkynyl group, an optionally substituted C3.6 cycloalkyl group, an optionally substituted C3_6 cycloalkenyl group, an optionally substituted C6-10 aryl group, or an optionally substituted heterocyclic group. 4. The compound or a pharmacologically acceptable salt thereof according to claim 3, wherein R1, R2, and R3 each independently represent an optionally substituted linear or branched C1.4 alkyl group. 5. A compound represented by formula (III) or a pharmacologically acceptable salt thereof:

Chemical Formula 3

H^r^\ P °V-NH L3-0 f^V R5 ( I I 1 ) R3 R wherein L2 is a single bond, an oxygen atom, an optionally substituted nitrogen atom, an optionally substituted linear or branched Cu, alkylene group, an optionally substituted linear or branched C2-6 alkenylene group, an optionally substituted linear or branched C2-6 alkynylene group, an optionally substituted C3.6 cycloalkylene group, or an optionally substituted C3.6 cycloalkenylene group,

L3 is a single bond, an optionally substituted linear or branched Cj_6 alkylene group, an optionally substituted linear or branched C2-6 alkenylene group, an optionally substituted linear or branched C2.6 alkynylene group, an optionally substituted C3.<-, cycloalkylene group, or an optionally substituted C3.6 cycloalkenylene group, R', Rz, and RJ are each independently an optionally substituted linear or branched Ci„4 alkyi group, an optionally substituted linear or branched C2.4 alkenyl group, an optionally substituted linear or branched C2-4 alkynyl group, an optionally substituted Q.io aryl group, or an optionally substituted heterocyclic group, R is a hydrogen atom, an optionally substituted linear or branched C,.6 alkyl group, an optionally substituted linear or branched C2-6 alkenyl group, an optionally substituted linear or branched C2-e alkynyl group, an optionally substituted C3.6 cycloalkyl group, an optionally substituted C3.6 cycloalkenyl group, an optionally substituted Ce-jo aryl group, or an optionally substituted heterocyclic group, and R5 is a hydrogen atom, an optionally substituted linear or branched CM6 alkyl group, an optionally substituted linear or branched C2-16 alkenyl group, an optionally substituted linear or branched C2.i6 alkynyl group, an optionally substituted C3.6 cycloalkyl group, an optionally substituted C3.6 cycloalkenyl group, an optionally substituted C6-10 aryl group, or an optionally substituted heterocyclic group. 6. The compound or a pharmacologically acceptable salt thereof according to claim 5, wherein R1, R2, and R3 are each independently an optionally substituted linear or branched C1.4 alkyl group. 7. A compound represented by formula (IV) or a

pharmacologically acceptable salt thereof: [Chemical Formula 4] M' N-f R" V-NH L3-0 wherein L* is a single bond, an oxygen atom, an optionally substituted nitrogen atom, an optionally substituted linear or branched C|.f, alkylene group, an optionally substituted linear or branched C2.f, alkenylene group, an optionally substituted linear or branched C2-6 alkynylene group, an optionally substituted C3.6 cycloalkylene group, or an optionally substituted C3.6 cycloalkenylene group, L3 is a single bond, an optionally substituted linear or branched C)_6 alkylene group, an optionally substituted linear or branched C2-6 alkenylene group, an optionally substituted linear or branched C2-6 alkynylene group, an optionally substituted C3.6 cycloalkylene group, or an optionally substituted C3.6 cycloalkenylene group, R', R2, and R3 are each independently an optionally substituted linear or branched Ci_4 alkyl group, an optionally substituted linear or branched C2_4 alkenyl group, an optionally substituted linear or branched C2-4 alkynyl group, an optionally substituted Cf,_ i () aryl group, or an optionally substituted heterocyclic group, R is a hydrogen atom, an optionally substituted linear or branched Cj.6 alkyl group, an optionally substituted linear or branched

C2.6 alkenyl group, an optionally substituted linear or branched C2_6 alkynyl group, an optionally substituted C3.6 cycloalkyl group, an optionally substituted C3.<5 cycloalkenyl group, an optionally substituted C6.io aryl group, or an optionally substituted heterocyclic group, and R5 is a hydrogen atom, an optionally substituted linear or branched CM6 alky) group, an optionally substituted linear or branched C2-16 alkenyl group, an optionally substituted linear or branched C2-16 alkynyl group, an optionally substituted C3.6 cycloalkyl group, an optionally substituted C3.6 cycloalkenyl group, an optionally substituted C6-10 aryl group, or an optionally substituted heterocyclic group, 8. The compound or a pharmacologically acceptable salt thereof according to claim 7, wherein R1, R2, and R3 are each independently an optionally substituted linear or branched ClA alkyl group. 9. A compound represented by formula (V) or (VI) or a pharmacologically acceptable salt thereof:

Chemical Formula 5

N->-~A P N-~~r^\ P N I) N-f R" Nx I N^f R" V"^7 I 7—( \^^J ,2 / O/ \ 0/ ^ , -y-NH L3-0 y-NH L3-0 I \ / \ K R3 R2 (V) R3 R2 (v , ) wherein L is an optionally substituted linear or branched Cu, alkylene group, an optionally substituted linear or branched C2-6 alkenylene group, an optionally substituted linear or branched C2-6 alkynylene group, an optionally substituted Cv6 cycloalkylene group, or an

optionally substituted C3.6 cycloalkenylene group, L2 is a single bond, an oxygen atom, an optionally substituted nitrogen atom, an optionally substituted linear or branched Ci_6 alkylene group, an optionally substituted linear or branched C2-6 alkenylene group, an optionally substituted linear or branched C2.(, alkynylene group, an optionally substituted C3.6 cycloalkylene group, or an optionally substituted C3.6 cycloalkenylene group, L3 is a single bond, an optionally substituted linear or branched Ci-6 alkylene group, an optionally substituted linear or branched C2,6 alkenylene group, an optionally substituted linear or branched C2-6 alkynylene group, an optionally substituted C3.6 cycloalkylene group, or an optionally substituted C3.6 cycloalkenylene group, R1, R2, and R3 are each independently an optionally substituted linear or branched C|.4 alkyl group, an optionally substituted linear or branched C2-4 alkenyl group, an optionally substituted linear or branched C2-4 alkynyl group, an optionally substituted C6-10 aiyl group, or an optionally substituted heterocyclic group, R is a hydrogen atom, an optionally substituted linear or branched Ci.6 alkyl group, an optionally substituted linear or branched C2_6 alkenyl group, an optionally substituted linear or branched C2-6 alkynyl group, an optionally substituted C3.6 cycloalkyl group, an optionally substituted C3.6 cycloalkenyl group, an optionally substituted Cfi-io aryl group, or an optionally substituted heterocyclic group, R6 is a hydrogen atom, an optionally substituted linear or branched Ci_i6 alkyl group, an optionally substituted linear or branched C2.i6 alkenyl group, an optionally substituted linear or branched C2-16

alkynyl group, an optionally substituted C3_6 cycloalkyl group, an optionally substituted C3.6 cycloalkenyl group, an optionally substituted linear or branched C{.6 alkoxy group, an optionally substituted C6.io aryl group, or an optionally substituted heterocyclic group, R7 is an optionally substituted linear or branched C].l6 alkyl group, an optionally substituted linear or branched C2-16 alkenyl group, an optionally substituted linear or branched C2-16 alkynyl group, an optionally substituted C3.6 cycloalkyl group, an optionally substituted C3.<5 cycloalkenyl group, an optionally substituted C6-io aryl group, or an optionally substituted heterocyclic group, and R8 and R9 are each independently a hydrogen atom or a CM alkyl group. 10. The compound or a pharmacologically acceptable salt thereof according to claim 9, wherein L1 is an optionally substituted linear or branched C|.6 alkylene group or an optionally substituted C3.6 1 0 1 cycloalkylene group, and R , R , and R are each independently an optionally substituted linear or branched CM alkyl group. 11. A compound selected from a compound group consisting of (S)-N-(2-hydroxy-l-phenylethyl)-6,6-dimethyl-3-[l-(trimethylsilyl)cycl obutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carbox amide, (S)-N-(2-hydroxy-l-phenylethyl)-6,6-dimethyl-3~[l-(trimethylsilyl)cycl opropanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carbo xamide, (S)-N-(2-hydroxy-l-phenylethyl)-6,6-dimethyl-3-[2-methyl-2-(trimethy lsilyl)propaneamido]-4,6-dihydropyn-olo[3,4-c]pyrazole-5(lH)-carboxa

mide, (S)-3-[l-(ethyldimethylsilyl)cyclobutanecarboxamido]-N-(2-hydroxy-l-phenylethyl)-6,6-dimethyI-4,6-dihydropyiToIo[3,4-c]pyrazole-5(lH)-car boxamide, (S)-3-[2-(ethyldimethylsilyl)-2-methy]propaneamido]-N-(2-hydroxy-l-phenylethyl)-6,6-dimethyl-4,6-dihydropyiTolo[3,4-c]pyrazole-5(lH)-car boxamide, (S)-N-(2-hydroxy-l-phenylethyl)-N,6,6-trimethyl-3-[l-(trimethylsilyl)c yclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carb oxamide, (S)-2-[(2-methoxypropan-2-yl)oxy]-l-phenylethyl 6,6-dimethyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydro pyrrolo[3,4-c]pyrazole-5(lH)-carboxylate, (S)-2-hydroxy-1 -phenylethyl 6,6-dimethyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydro pyrrolo[3,4-c]pyrazole-5(lH)-carboxylate, 2-Methoxy-1 -phenylethyl 6,6-dimethyl-3-[l-(trimethylsily])cyclopropanecarboxamido]-4,6-dihydr opyrrolo[3,4-c]pyrazole-5( 1 H)-carboxylate, N-[5-(4-hydroxy-3-phenylbutanoyl)-6,6-dimethyl-l,4,5,6-tetrahydropyr rolo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide, N-[5-(3-hydroxy-3-phenylpropanoyl)-6,6-dimethyl-l,4>5,6-tetrahydropy rrolo[3,4-c]pyrazol-3-yl]-l-(tiimethylsilyl)eyclobutanecarboxamide, (R)-N-(3-hydroxy-l-phenylpropyl)-6,6-dimethyl-3-[l-(trimethylsilyl)cy clobutanecarboxamido]-4,6-dihydropyrrolo[3)4-c]pyrazole-5(lH)-carbo xamide,

(R)-N-(3-hydroxy-l-pheny]propyl)-6,6-dimethy]-3-[l-(trimethylsilyl)cy clopropanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-cai"b oxamide, (R)-N-(4-hydroxy-l-phenylbutyl)-6,6-dimethyl-3-[l-(trimethylsilyl)cycl obutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carbox amide, (R)-N-(5-hydroxy-l-phenylpentyl)-6,6-dimethyl-3-[l-(trimethylsilyl)cy clobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carbo xamide, (S)-N-(2-hydroxy-2-methy]-l-phenylpropyl)-6,6-dimethyl-3-[l-(trimeth y]silyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(l H)-carboxamide, (S)-N-(2-hydroxy-2-methyl-l-phenylpropyl)-6,6-diniethyl-3-[l-(trimeth ylsilyl)cyclopropanecarboxamido]-4,6-dihydropyiTolo[3,4-c]pyrazole-5( lH)-carboxamide, N-(3-hydroxy-2,2-dimethyl-l-phenylpropyl)-6,6-dimethyl-3-[l-(trimeth ylsilyl)cyclobutanecarboxamido]-4,6-dihydropyn-olo[3,4-c]pyrazole-5(l H)-carboxamide, (R)-N-(3-hydroxy-3-methyl-l-phenylbutyl)-6,6-dimethyl-3-[l-(trimethy lsilyl)cyclobutanecarboxamido]-4,6-dihydropyn-olo[3,4-c]pyrazole-5(l H)-carboxamide, (S)-N-(2-methoxy-l-phenylethyl)-6,6-dimethyl-3-[l-(trimethylsi]yl)cycl obutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carbox amide, (S)-N-[2-(difluoromethoxy)-l-phenylethyI]-6,6-dimethyl-3-[l-(trimethy lsi]yl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazo]e-5(l

H)-carboxamide, (S)-N-(2-ethoxy-1 -phenylethyl)-6,6-dimethyl-3-[ 1 -(trimethylsilyl)cyclo butanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carboxa mide, (R)-N-(3-methoxy-1 -phenylpropyl)~6,6-dimethy l-3-[ 1 -(trimethylsilyl)cy clobutanecarboxamido]-4,6-dihydropyiTolo[3,4-c]pyrazole-5(lH)-carbo xamide, Sodium (S)-2-{6,6-dimethyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-l,4. 5.6-tetrahydropyrrolo[3,4-c]pyrazole-5-carboxamide}-2-phenylacetate, (R)-N-(2-hydroxy-1 -phenylethyl)-6,6-dimethyl-3-[ 1 -(trimethylsilyl)cycl obutanecarboxamido]-4,6-dihydropyiTolo[3,4-c]pyrazole-5(lH)-carbox amide, N-[l-(2-fluorophenyl)-2-hydroxyetliyl]-6,6-dimethyl-3-[l-(trimethylsily l)cyclobutanecarboxamido]-4,6-dihydropyiTolo[3,4-c]pyrazole-5(lH)-c arboxamide, (S)-N-[ 1 -(3-fluorophenyl)-2-hydroxyethyl]-6,6-dimethyl-3-[ 1 -(trimethy lsilyl)cyclobutanecarboxamido]-4,6-dihydropyn-olo[3,4-c]pyrazole-5(l H)-carboxamide, (S)-N-[ 1 -(4-fluorophenyl)-2-hydroxyethyl]-6,6-dimethyl-3-[ 1 -(trimethy lsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(l H)-carboxamide, N-[2-hydroxy-l-(pyridin-2-yl)ethyl]-6,6-dimethyl-3-[l-(trimethylsilyl)c yclobutanecarboxamido]-4,6-dihydropyn-olo[3,4-c]pyrazole-5(lH)-carb oxamide, N-[2-hydroxy-l-(pyridin-3-yl)ethyl]-6,6-dimethyl-3-[l-(trimethylsilyl)c

yclobutanecarboxamido]-4,6-dihydropyiTolo[3,4-c]pyrazole-5(lH)-carb oxamide, N-[l-(benzo[d][l,3]dioxol-4-yl)-2-hydroxyethyl]-6,6-dimethyl-3-[l-(tri methylsilyl)cyclobutanecarboxamido]-4,6-dibydropyiTolo[3,4-c]pyrazol e-5(lH)-carboxamide, (S)-N-(l-cyclohexyl~2-hydroxyethyl)-6,6-dimetbyl-3-[l-(trimethylsilyl) cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-car boxamide, (S)-N-( 1 -hydroxy-3-methylbutan-2-yl)-6,6-dimethyl-3-[ 1 -(trimethylsily l)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyi-azole-5(lH)-c arboxamide, (S)-N-(l-hydroxypropan-2-yl)-6,6-dimethyl-3-[l-(trimethylsilyl)cyclob utanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazoIe-5(lH)-carboxam ide, N-(2-hydroxyethyl)-6,6-dimethyl-3-[l-(trimethylsilyl)cyclobutanecarbo xamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carboxamide, N-(2-hydroxy-2-phenylethyl)-6,6-dimethyl-3-[l-(trimethylsilyl)cyclobu tanecarboxamido]-4,6-dihydropyiTolo[3,4-c]pyrazole-5(lH)-carboxami de, N-(2-hydroxypropyl)-6,6-dimethyl-3-[]-(trimethylsilyl)cyclobutanecarb oxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carboxaraide, N-[(2S)-1 -hydroxy-3-methyl-1 -phenylbutan-2-yl]-6,6-dimethyl-3-[ 1 -(tri methylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazol e-5(lH)-carboxamide, N-(4-hydroxy-1 -phenyl-2-butyn-1 -yl)-6,6-dimethyl-3-[ 1 -(trimethylsilyl) cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(rH)-car

boxamide, (S)-2-{6,6-dimethyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-l,4, 5,6-tetrahydropyrro]o[3,4-c]pyrazole-5-carboxamido}-2-phenylethyl acetate, (S)-2-{6,6-diraethyl-3-[l-(trimethylsilyl)cyclobutanecarboxaniido]-l,4, 5,6-tetrahydropyrrolo[3,4-c]pyrazole-5-carboxamido}-2-phenylethyl propionate, (S)-2-{6,6-dimethyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-l,4. 5,6-tetrahydropyiTolo[3,4-c]pyrazole-5-carboxamido}-2-phenylethyl butanoate, (S)-2-{6,6-dimethyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-l,4, 5,6-tetrahydropyrrolo[3,4-c]pyrazole-5-carboxamido}-2-phenylethyl pentanoate, (S)-2-{6,6-dimethyl-3-[l-(trimethylsilyl)cyclobutanecarboxaraido]-l,4, 5,6-tetrahydropyrrolo[3,4-c]pyrazole-5-carboxamido}-2-phenylethyl octanoate, (S)-2-{6,6-dimethyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-l,4. 5,6-tetrahydropyrro]o[3,4-c]pyrazole-5-carboxamido}-2-phenylethyl dodecanoate, (S)-2-{6,6-dimethyl-3-[l-(trimethylsilyl)cyc]obutanecarboxamido]-l,4; 5,6-tetrahydropyn-olo[3,4-c]pyrazoJe-5-carboxamido}-2-phenylethyl palmitate, (S)-2-{6,6-diraethyl-3-[l-(trimetbylsilyl)cyclobutanecarboxamido]-l,4, 5,6-tetrahydropyrrolo[3,4-c]pyrazole-5-carboxamido}-2-phenylethyJ isobutanoatc, (S)-2-{6,6-dimethyl-3-[l-(trimethylsi]yl)cyclobutanecarboxamido]-l,4,

5,6-tetrahydi-opyrrolo[3,4-c]pyrazole-5-carboxamido}-2-phenylethy] pivalate, (S)-2- (6,6-dimethyl-3-[ 1 -(trimethylsilyl)cyclobutanecarboxamido]-l ,4, 5,6-tetrahydropyrrolo[3,4-c]pyrazole-5-carboxamido}-2-phenylethyl 3-methylbutanoate, (S)-2-{6,6-dimethyl-3-[l-(tnmethylsilyl)cyclobutanecarboxamido]-l,4, 5,6-tetrahydropyrrolo[3,4-c]pyrazole-5-carboxamido}-2-phenylethyl benzoate, (S)-2-{6,6-dimethyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-l,4, 5,6-tetrahydropyrrolo[3,4-c]pyrazole-5-carboxamido}-2-phenylethyl ethyl carbonate, Sodium (S)-4-(2-{6,6-dimethyl-3-[l-(ti-imethylsilyl)cyclobutanecarboxamido]-l, 4,5,6-tetrahydi-opyrrolo[3,4-c]pyrazole-5-carboxamido}-2-phenylethoxy )-4-oxobutanoate, (S)-(2-{6,6-dimethyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-l,4, 5,6-tetrahydropyrrolo[3,4-c]pyrazole-5-carboxamido}-2-phenylethoxy) methyl pivalate, (S)-2-acetoxy-1 -phenylethyl 6,6-dimethyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydro pyrrolo[3,4-c]pyrazole-5(lH)-carboxylate, (S)-benzyl 2- {6,6-dimethyl-3-[ 1 -(trimethylsilyl)cyclobutanecarboxamido]-1,4,5,6-t etrahydropyrrolo[3,4-c]pyrazole-5-carboxamido}-2-phenylacetate, (S)-methyl 2-{6,6-dimethyl-3-[l-(trimethylsilyl)cyelobutanecarboxamido]-l,4,5,6-t

etrahydropyrrolo[3,4-c]pyrazole-5-carboxamido}-2-phenyiacetate, N-(2,2-difluoi"0-3-hydroxy-l-phenylpropyl)-6,6-dimethyl-3-[l-(trimeth ylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(l H)-carboxamide, N-(2-isopropoxy-1 -phenylethyl)-6,6-dimethyl-3-[ 1 -(trimethylsilyl)cyclo butanecarboxamido]-4,6-dihydropyn-olo[3,4-c]pyrazole-5(lH)-carboxa mide, 6,6-Dimethyl-N-(2-phenoxy-1 -phenylethyl)-3-[ 1 -(trimethylsilyl)cyclob utanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carboxam ide, (S)-N-[l-(2-chlorophenyl)-2-hydroxyethyl]-6,6-dimethy]-3-[l-(trimethy lsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyi-azole-5(] H)-carboxamide, (S)-N-[2-hydroxy-l-(o-tolyl)ethyl]-6,6-dimethyl-3-[l-(trimethyIsilyl)cy clobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carbo xamide, (S)-N-( 1 -hydroxy-3-phenylpropan-2-yl)-6,6-dimethyl-3-[ 1 -(trimethylsil yl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carboxamide, N-(2-hydroxy-3-methylbutyl)-6,6-dimethyl-3-[l-(trimethylsilyl)cyclobu tanecarboxamido]-4,6-dihydropyiTolo[3,4~c]pyrazole-5(lH)-carboxami de, (R)-N-( 1 -hydroxy-3-phenylpropan-2-yl)-6,6-dimethyl-3-[ 1 -(trimethylsil yl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carboxamide, (R)-N-(2-hydroxy-2-phenylethyl)-6,6-dimethyl-3-[l-(trimethylsilyl)cycl

obutanecarboxamido]-4,6-dihydropyiTolo[3,4-c]pyrazole-5(lH)-carbox amide, (S)-N-(2-hydroxy-2-phenylethyl)-6,6-dimethyl-3-[l-(trimethylsilyl)cycl obutanecai-boxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carbox amide, 2-Hydroxy-2-phenylethyl 6,6-dimethyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydro pyrrolo[3,4-c]pyrazole-5(lH)-carboxylate, (R)-N-[6,6-dimethyl-5-(2-phenoxypropanoyl)-l,4,5,6-tetrahydropyrrolo [3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide, (S)-N-[6,6-dimethyl-5-(2-phenoxypropanoyl)-l,4,5,6-tetrahydropyrrolo [3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide, N-[6,6-dimethyl-5-(2-phenoxyacetyl)-l,4,5,6-tetrahydropyrrolo[3,4-c]p yrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide, (R)-N-[6,6-dimethyl-5-(2-phenoxypropanoyl)-l,4,5,6-tetrahydropyiTolo [3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclopropanecarboxamide, N-{5-[3-(benzyloxy)-2-phenoxypropanoyl]-6,6-dimethyl-l,4,5,6-tetrahy dropyrrolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutanecarboxami de, N-[5-(3-hydroxy-2-phenoxypropanoyl)-6,6-dimethyl-l,4,5,6-tetrahydro pyrrolo[3,4-c]pyrazol-3-y]]-l-(trimethylsilyl)cyclobutanecarboxamide, N-{5-[2-(4-chlorophenoxy)propanoyl]-6,6-dimethyl-l,4,5,6-tetrahydrop yrrolo[3,4-c]pyrazol-3-yl}-l-(trimethy.lsilyl)cyclobutanecarboxamide, N-{5-[2-(2-chlorophenoxy)propanoyl]-6,6-dimethyl-l,4,5,6-tetrahydrop yiTolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutanecarboxamide, N-{5-[2-(cyclohexyloxy)propanoyl]-6,6-dimethyl-l,4,5,6-tetrahydropyr

rolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutanecarboxamide, N-{5-[2-(3-chlorophenoxy)propanoyl]-6,6-dimethyl-l,4,5,6-tetrahydrop yrrolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutanecarboxamide, N-[5-(2-methoxypropanoyl)-6,6-dimethyl-l,4,5,6-tetraliydropyrrolo[3,4 -c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide, N-[5-(3-methoxy-2-phenoxypropanoyl)-6,6-dimethyl-l,4,5,6-tetrahydro pyrroIo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide, N-{6,6-dimethyl-5-[2-(pyridin-3-yloxy)propanoyl]-l,4,5,6-tetrahydropy rrolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutanecarboxamide, N-{5-[3-(dimethylamino)-2-phenoxypropanoyl]-6,6-dimethyl-l,4,5,6-te trahydropyrrolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutanecarbo xamide, N-[6,6-dimethyl-5-(2-phenoxy-2-phenylacetyl)-l,4,5,6-tetrahydropyrro] o[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide, N-{5-[3-(3,3~difluoropyrrolidin-l-yl)-2-phenoxypropanoyl]-6,6-dimeth yl-l,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclo butanecarboxamide, N-[5-(3-hydroxy-2-phenylpropanoyl)-6,6-dimethyl-l,4,5,6-tetrahydropy rrolo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide, (S)-N-[5-(3-hydroxy-2-pheny]propanoyl)-6,6-dimethyl-l,4,5,6-tetrahyd ropyrrolo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide (R)-N-{5-[3-(benzyloxy)-2-phenylpropanoyl]-6,6-dimethyl-l,4,5,6-tetra hydropyrrolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutanecarboxa midc, (R)-N-[5-(3-hydroxy-2-phenylpropanoyl)-6,6-dimethyl-l,4,5,6-tetrahyd

ropyiTolo[3?4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide (R)-N-[5-(2-methoxy-2-phenylacetyl)-6,6-dimethyl-l,4,5,6-tetrahydrop yiTolo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide. (S)-N-[5-(2-methoxy-2-phenylacetyl)-6,6-dimethyl-l,4,5,6-tetrahydrop yrrolo[3?4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide, N-[5-(3-methoxy-2-phenylpropanoyl)-6,6-dimethyl-l,4,5,6-tetrahydrop yn-olo[3,4-c]pyrazol-3-yl]-l-(trimethylsily])cyclobutanecarboxamide, N-[5-(4-methoxy-2-phenylbutanoyl)-6,6-dimethyl-l,4,5,6-teti-ahydi-opyr rolo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide, (S)-N-[5-(3-hydroxy-2-phenylpropanoyl)-6,6-diraethyl-l,4,5,6-tetrahyd ropyn-olo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclopropanecarboxami de, (R)-N-[5-(2-methoxy-2-phenylacetyl)-6,6-dimethyl-l,4,5,6-tetrahydrop yrrolo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclopropanecarboxaraide, (R)-N-{5-[2-(difluoromethoxy)-2-phenylacetyl]-6,6-dimethyl-l,4,5,6-te trahydropyiTolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutanecarbo xamide, (R)-N-[5-(2-ethoxy-2-phenylacetyl)-6,6-dimethyl-l,4,5,6-tetrahydropyrr olo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide, (R)-l-(ethyldimethylsilyl)-N-[5-(2-methoxy-2-phenylacetyl)-6,6-dimeth ybl,4,5,6-tetrahydropyn"olo[3,4-c]pyrazol-3-yl]cyclobutanecarboxaraid e, (R)-N-[5-(2-cyclopropoxy-2-phenylacetyl)-6:,6-dimediyl-l?4:,5,6-tetrahy dropyrrolo[3,4-c]pyrazol-3-y]]~l-(trimethylsilyl)cyclobutanecarboxamid

(R)-N-[5-(2-isopropoxy-2-phenylacety l)-6,6-dimethyl-1,4,5,6-tetrahydr opyrrolo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide, (R)-N-{6,6-dimethyl-5-[2-phenyl-2~(trifluoromethoxy)acetyl]-l,4,5,6-te trahydi-opyn-olo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutanecarbo x amide, (R)-N-[6,6-dimethyl-5-(2-phenyl-2-propoxyacetyl)-l,4,5,6-tetrahydropy rrolo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxamide, N-{5-[2-(4-fluorophenyl)-2-methoxyacetyl]-6,6-dimethyl-l,4,5,6-tetrah ydi'opyrrolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutanecarboxam ide, N- {5-[2-(3-fluorophenyl)-2-metIioxyacetyl]-6,6-dimethyI-1,4,5,6-tetrah ydropyn-olo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutanecarboxam ide, (R)-N-{5-[2-(2-fluorophenyl)-2-methoxyacetyl]-6,6-dimethyl-l,4,5,6-te trahydropyrrolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutanecarbo xamide, N-{5-[2-methoxy-2-(thiophen-2-yl)acetyl]-6,6-dimethyl-l,4,5,6-tetrahy dropyrrolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutanecarboxami de, (-)-N- {5-[2-methoxy-2-(thiophen-2-yl)acetyl]-6,6-dimethyl-1,4,5,6-tetra hydropyrrolo[3,4-c]pyrazol-3~yl}-l-(trimethylsilyl)cyclobutanecarboxa mide, (+)-N-{5-[2-methoxy-2-(thiopben-2-yl)acetyl]-6,6-dimethyl-l,4,5,6-tetr ahydropyrrolo[3,4-c]pyrazo]-3-yl}-l-(trimethylsilyl)cyciobutanecarbox amide, N-{[l-(hydi-oxymethyl)cyclobutyl](phenyl)methyl}-6,6-dimethyl-3-[l-(

trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyraz ole-5(lH)-carboxamide, (R)-N-[2-( 1 -hydro xycyclopropyl)-1 -phenylethyl]-6,6-dimethyl-3-[ 1 -(tri methylsilyl)cyclobutanecarboxamido]-4,6-dihydropyiTolo[3,4-c]pyrazol e-5(lH)-carboxamide, (R)-N-(3-ethyl-3-hydroxy-1 -phenylpentyl)-6,6-dimethyl-3-[ 1 -(trimethyl silyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH )-carboxamide, (R)-N-[l-(4-fluorophenyl)-3-hydroxy-3-methylbutyl]-6,6-dimethyl-3-[l -(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyiTolo[3,4-c]pyr azole-5 (1 H)-carboxamide, (R)-N-[ 1 -(3-fluorophenyl)-3-hydroxy-3-methylbutyl]-6,6-dimethyl-3-[ 1 -(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyiTolo[3,4-c]pyr azole-5(lH)-carboxamide, (R)-N-[l-(2-fluorophenyI)-3-hydroxy-3-methylbutyI]-6,6-dimethyl-3-[l -(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyr azole-5(lH)-carboxamide, (R)-N-(5-hydroxy-2,5-dimethylhexan-3-yl)-6,6-dimethyl~3-[l-(trimethy lsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(l H)-carboxaraide, N-[l-(4-fluorophenyl)-3-hydroxy2,2-diraethylpropyl]-6,6-dimethyl-3-[l -(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyr azole-5(lH)-carboxamide, N-[l-(3-fluorophenyl)-3-hydroxy-2,2-dimethylpropyl]-6,6-dimethyl-3-[ l-(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]py razole-5( 1 H)-carboxamide,

(-)-N-[l-(3-fluorophenyl)-3-hydroxy-2,2-dimethylpropyl]-6,6-dimethyl- 3-[l-(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyn-olo[3,4-c ]pyrazole-5( 1 H)-carboxamide, (+)-N-[l-(3-fluorophenyl)-3-hydroxy-2,2-dimethylpropyl]-6,6-dimethyl -3-[l-(tiimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrroIo[3,4-c]pyrazole-5(lH)-carboxamide, N-[l-(2-fluorophenyl)-3-hydroxy-2,2-dimethylpropyl]-6,6-dimethyl-3-[ l-(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]py razole-5(lH)-carboxamide, N-( 1 -hydroxy-2,2,4-trimethylpentan-3-yl)-6,6-dimethyl-3-[l -(trimethyls ilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH) -carboxamide, (R)-N-(3-hydroxy-3-methyl-l-phenylbutyl)-6,6-dimethyl-3-[l-(trimethy lsilyl)cyclopropanecarboxamido]-4;,6-dihydropyiTolo[3,4-c]pyrazole-5(] H)-carboxamide, N-(3-hydi-oxy-2,2-dimethyl-l-pheny]propyl)-6,6-dimethyl-3-[l-(trimeth ylsilyl)cycJopropanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5( lH)-carboxamide, (-)-N-(3-hydroxy-2,2-dimethyl-1 -phenylpropyl)-6,6-dimetiiyl-3-[ 1 -(trim ethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole- 5(1 H)-carboxamide, (+)-N-(3-hydroxy-2,2-dimethyl-l-pber)ylpropyl)-6,6-dimethyl-3-[l-(tri methylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazol e-5(.l H)-carboxamide, (R)-N-[5-(2-butoxy-2-phenylacetyl)-6,6-dimethyl-l,4,5,6-tetrahydropyr rolo[3,4-c]pyrazol-3-yl]-1 -(trimethylsiJyJ)cyclobutanecarboxamide, and

N-(3-methoxy-2,2-dimethyl-1 -phenylpropyl)-6,6-dimethyl-3-[ 1 -(trimet hylsilyl)cyclobutanecai"boxamido]-4,6-dihydropyn-olo[3,4-c]pyrazole-5( 1 H)-carboxamide or a pharmacologically acceptable salt thereof. 12. (R)-N-[l-(4-fluorophenyl)-3-hydroxy-3-methylbutyl]-6,6-dimet hyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3 ,4-c]pyrazole-5(lH)-carboxamide or a pharmacologically acceptable salt thereof. 13. (-)-N-(3-hydroxy-2,2-dimethyl-1-phenylpropyl)-6,6-dimethyl-3-[l-(trimethylsilyl)cyclopropane-l-carboxamido]-4,6-dihydropyrrolo[3,4 -c]pyrazole-5(lH)-carboxamide or a pharmacologically acceptable salt thereof 14. (R)-N-[5-(2-methoxy-2-phenylacetyl)-6,6-dimethyl-l,4,5,6-tetra hydropyiTolo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxa mide or a pharmacologically acceptable salt thereof. 15. (R)-N-[6,6-dimethyl-5-(2-phenyl-2-propoxyacetyl)-l,4,5,6-tetra hydropyn-olo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarboxa mide or a pharmacologically acceptable salt thereof. 16. (R)-N- {5-[2-(2-fluorophenyl)-2-methoxyacetyl]-6,6-dimethyl-1, 4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobuta necarboxamide or a pharmacologically acceptable salt thereof

17. (R)-N-[5-(2-ethoxy-2-phenylacetyl)-6,6-dimethyl-l,4,5,6-teti-ah ydropyrrolo[3,4-c]pyrazol-3-y]]-l-(trimethylsilyl)cyclobutanecarboxami de or a pharmacologically acceptable salt thereof. 18. (R)-N-[5-(2-cyclopropoxy-2-phenylacetyl)-6,6-dimethyl-1,4,5,6 -tetrahydropyrrolo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecar boxamide or a pharmacologically acceptable salt thereof. 19. (R)-N-[5-(2-isopropoxy-2-phenylacetyl)-6,6-dimethyl-l,4,5,6-te trahydropyrrolo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclobutanecarbo xamide or a pharmacologically acceptable salt thereof. 20. (+)-N-{5-[2-methoxy-2-(thiophen-2-yl)acetyl]-6,6-dimethyl-l,4, 5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutane carboxamide or a pharmacologically acceptable salt thereof. 21. (-)-N-[l-(3-fluorophenyl)-3-hydroxy-2,2-dimethylpropyl]-6,6-di methyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrol o[3,4-c]pyrazole-5(lH)-carboxamide or a pharmacologically acceptable salt thereof. 22. N-{5-[2-(3-fluorophenyl)-2-methoxyacetyl]-6,6-dimethyl-l ,4,5, 6-tetrahydropyiTolo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobutaneca rboxamide or a pharmacologically acceptable salt thereof. 23.

N-[l-(4-fluorophenyl)-3-hydroxy-2f2-dimethylpropyl]-6,6-dime thyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[ 3,4-c]pyrazole-5(lH)-carboxamide or a pharmacologically acceptable salt thereof. 24. (R)-N-[ 1 -(3-fluorophenyl)-3-hydroxy-3-methylbutyl]-6,6-dimet hyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3 ,4-c]pyrazole-5(lH)-carboxamide or a pharmacologically acceptable salt thereof. 25. (R)-N- {6,6-dimethyl-5-[2-phenyl-2-(trifluoromethoxy)acetyl]-1, 4,5,6-tetrahy dropyrrolo [3,4-c]pyrazol-3-yl} -1 -(trimethylsilyl)cyclobuta necarboxamide or a pharmacologically acceptable salt thereof 26. (R)-N-[2-(l-hydroxycyclopropyl)-l-phenylethyl]-6,6-dimethyl-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyn-olo[3,4-c ]pyrazole-5(lH)-carboxamide or a pharmacologically acceptable salt thereof. 27. (R)-N-(3-hydroxy-3-methyl-l-phenylbutyl)-6,6-dimethyl-3-[l-(t rimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyraz ole-5(lH)-carboxamide or a pharmacologically acceptable salt thereof. 28. (R)-N-[5-(2-methoxy-2-phenylacetyl)-6,6-dimethyl-l,4,5,6-tetra hydropyiTolo[3,4-c]pyrazol-3-yl]-l-(trimethylsilyl)cyclopropanecarboxa mide or a pharmacologically acceptable salt thereof.

29. (R)-N- {5-[2-(difluoromethoxy)-2-pheny]acetyl]-6,6-dimethyl-1, 4,5,6-tetrahydropyn-olo[3,4-c]pyrazol-3-yl}-l-(trimethylsilyl)cyclobuta necarboxamide or a phannacologically acceptable salt thereof. 30. (R)-l-(ethyldimethylsilyl)-N-[5-(2-methoxy-2-phenylacetyl)-6,6 -dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl]cyclobutanecarb oxamide or a phannacologically acceptable salt thereof. 31. N- {[ 1 -(hydroxymethyl)cyclobutyl](phenyl)methyl} -6,6-dimethy l-3-[l-(trimethylsilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(lH)-carboxamide or a phannacologically acceptable salt thereof. 32. A pharmaceutical composition comprising the compound or a phannacologically acceptable salt thereof according to any one of claims 1 to 31. 33. The pharmaceutical composition according to claim 32, wherein the phannaceutical composition is a CDK7 inhibitor. 34. The pharmaceutical composition according to claim 32 or 33, wherein the pharmaceutical composition is for treating or preventing a cancer or an inflammatory disease. 35. The phannaceutical composition according to claim 34, wherein the inflammatory disease is an autoimmune disease. 36. The phannaceutical composition according to claim 35, wherein the autoimmune disease is rheumatoid arthritis. 37. The phannaceutical composition according to claim 35, wherein

the autoimmune disease is psoriasis.

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1 Translated Copy of Priority Document [12-05-2017(online)].pdf 12 May 2017
2 PROOF OF RIGHT [12-05-2017(online)].pdf 12 May 2017
3 Priority Document [12-05-2017(online)].pdf 12 May 2017
4 Power of Attorney [12-05-2017(online)].pdf 12 May 2017
5 Form 5 [12-05-2017(online)].pdf 12 May 2017
6 Form 3 [12-05-2017(online)].pdf 12 May 2017
7 Form 1 [12-05-2017(online)].pdf 12 May 2017
8 Description(Complete) [12-05-2017(online)].pdf_197.pdf 12 May 2017
9 Description(Complete) [12-05-2017(online)].pdf 12 May 2017
10 201747016742.pdf 16 May 2017
11 Correspondence by Agent_Form-1_19-05-2017.pdf 19 May 2017
12 Verified English Translation [19-06-2017(online)].pdf_40.pdf 19 Jun 2017
13 Verified English Translation [19-06-2017(online)].pdf_39.pdf 19 Jun 2017
14 Verified English Translation [19-06-2017(online)].pdf 19 Jun 2017
15 201747016742-FORM 3 [20-10-2017(online)].pdf 20 Oct 2017
16 201747016742-FORM 18 [14-06-2018(online)].pdf 14 Jun 2018
17 201747016742-FER.pdf 20 Nov 2019
18 201747016742-FORM 4(ii) [05-05-2020(online)].pdf 05 May 2020
19 201747016742-PETITION UNDER RULE 137 [03-07-2020(online)].pdf 03 Jul 2020
20 201747016742-OTHERS [03-07-2020(online)].pdf 03 Jul 2020
21 201747016742-FORM 3 [03-07-2020(online)].pdf 03 Jul 2020
22 201747016742-FER_SER_REPLY [03-07-2020(online)].pdf 03 Jul 2020
23 201747016742-CLAIMS [03-07-2020(online)].pdf 03 Jul 2020
24 201747016742-FORM 3 [12-11-2021(online)].pdf 12 Nov 2021
25 201747016742-PatentCertificate12-05-2023.pdf 12 May 2023
26 201747016742-IntimationOfGrant12-05-2023.pdf 12 May 2023
27 201747016742-PROOF OF ALTERATION [10-08-2023(online)].pdf 10 Aug 2023
28 201747016742-PROOF OF ALTERATION [10-08-2023(online)]-1.pdf 10 Aug 2023
Search strategy
1searchstrategy25_18-11-2019.pdf

ERegister / renewals

Inforce
3rd Renewed 27 Jul 2023 Period 30 Oct 2017 – 30 Oct 2018 · CBR 33622 · Certificate 63166 ₹4,000
4th Renewed 27 Jul 2023 Period 30 Oct 2018 – 30 Oct 2019 · CBR 33622 · Certificate 63167 ₹4,000
5th Renewed 27 Jul 2023 Period 30 Oct 2019 – 30 Oct 2020 · CBR 33622 · Certificate 63168 ₹4,000
6th Renewed 27 Jul 2023 Period 30 Oct 2020 – 30 Oct 2021 · CBR 33622 · Certificate 63169 ₹4,000
7th Renewed 27 Jul 2023 Period 30 Oct 2021 – 30 Oct 2022 · CBR 33622 · Certificate 63170 ₹12,000
8th Renewed 27 Jul 2023 Period 30 Oct 2022 – 30 Oct 2023 · CBR 33622 · Certificate 63171 ₹12,000
9th Renewed 27 Jul 2023 Period 30 Oct 2023 – 30 Oct 2024 · CBR 33622 · Certificate 63172 ₹12,000
10th Renewed 13 Sep 2024 Period 30 Oct 2024 – 30 Oct 2025 · CBR 56673 · Certificate 147863 ₹12,000
11th Renewed 11 Sep 2025 Period 30 Oct 2025 – 30 Oct 2026 · CBR 53538 · Certificate 64723 ₹24,000