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