Claims
[Claim 1] A compound of the formula (I) or a salt thereof:
[Chem. 18]
(In the formula,
R1 is H, Ci-6 alkyl which may be substituted with OH, C3-8 cycloalkyl which may be substituted with R00, heterocycloalkyl which may be substituted with R00, phenyl which may be substituted with R00, heteroaryl which may be substituted with R00, -CO-C1-6 alkyl, or -CO-C3-8 cycloalkyl, in which R00 represents substituents selected from the group consisting of C1-6 alkyl, halogeno-Ci-6 alkyl, and halogen,
R2a is Ci-6 alkyl which may be substituted with R01, in which R01 represents substituents selected from the group consisting of C3-8 cycloalkyl, -0-(Ci-6 alkyl), -N(Ci-6 alkyl)2, -NH(Ci-6 alkyl), and -NH2,
R2b is H or Ci-6 alkyl,
R2a and R2b may be combined with the same carbon atom in the piperazine ring to form C3-8 cycloalkyl,
R3 is H or Ci-6 alkyl,
R4 is H or Ci-6 alkyl,
X is *-CR7=CR8-, *-CR7=N-, *-N=CR8-, or S, in which * represents a bond with a carbon atom substituted with R6,
R5, R6, and R7 are the same as or different from each other, and are H, Ci-6 alkyl, -0-(Ci-6 alkyl), halogen, or CN,
R5 and R6 may be combined with each other to form C5-7 cycloalkenyl,
R8 is H or F, and
the ring A is aryl which may be substituted with R02, C5-7 cycloalkenyl-fused phenyl which may be substituted with R02, heteroaryl which may be substituted with R02, or C6-8 cycloalkyl which may be substituted with R02, in which R02 represents substituents selected from the group consisting of C1-6 alkyl, halogeno-O-6 alkyl, C3-8 cycloalkyl, -O-(C1-6 alkyl), -0-(halogeno-Ci-6 alkyl), halogen, and -CN.)

[Claim 2] The compound or a salt thereof according to claim 1, wherein
RMs
i. tert-butyl which may be substituted with OH, ii. C3-5 cycloalkyl which may be substituted with C1-6 alkyl, iii. 4-tetrahydropyranyl which may be substituted with C1-6 alkyl, iv. phenyl which may be substituted with halogen,
v. heteroaryl which may be substituted with substituents selected from the group consisting of C1-6 alkyl and halogeno-Ci-6 alkyl, vi. -CO-C1-6 alkyl, or vii. -CO-C3-5 cycloalkyl, R2a is C1-6 alkyl which may be substituted with R03, in which R03 represents substituents selected from the group consisting of C3-5 cycloalkyl, -0-(Ci-6 alkyl), and -N(Ci-6 alkyl)2,
R2b is H or C1-6 alkyl,
R5, R6, and R7 are the same as or different from each other, and are H, C1-6 alkyl, or halogen, and
the ring A is
i. aryl which may be substituted with substituents selected from the group consisting of C1-6 alkyl, halogeno-Ci-6 alkyl, C3-5 cycloalkyl, -0-(Ci-6 alkyl), -0-(halogeno-C1-6 alkyl), halogen, and -CN,
ii. C5-7 cycloalkenyl-fused phenyl which may be substituted with substituents selected from the group consisting of C1-6 alkyl and halogen, iii. heteroaryl which may be substituted with halogen, or iv. C6-8 cycloalkyl which may be substituted with C1-6 alkyl.
[Claim 3] The compound or a salt thereof according to claim 2, wherein
RMs
i. tert-butyl,
ii. 4-tetrahydropyranyl,
iii. pyridyl which may be substituted with halogeno-Ci-6 alkyl, or
iv. 1,6-dihydro-6-oxopyridazinyl which may be substituted with C1-6 alkyl, R2a is C1-6 alkyl, R2b is H,
R3 is H or methyl, R4 is H or methyl, X is *-CR7=CR8-, or *-N=CR8-, R5 is H or halogen, R6 is halogen,
1 /IT

R7 is H or halogen, R8 is F, and the ring A is
i. phenyl which may be substituted with substituents selected from the group consisting of C1-6 alkyl, C3-5 cycloalkyl and halogen,
ii. naphthyl,
iii. 2,3-dihydro-lH-inden-5-yl which may be substituted with substituents selected from the group consisting of C1-6 alkyl and halogen,
iv. cyclohexyl which may be substituted with C1-6 alkyl, or
v. cycloheptyl which may be substituted with C1-6 alkyl.
[Claim 4] The compound or a salt thereof according to claim 3, wherein
the formula (I) is the following formula (la): [Chem. 19]
R!is
i. tert-butyl,
ii. 4-tetrahydropyranyl,
iii. pyridyl which may be substituted with difluoromethyl, or
iv. 1,6-dihydro-6-oxopyridazinyl which may be substituted with methyl, R2a is methyl, ethyl, or n-propyl, Xis*-CR7=CR8-, R5 is H, R6 is F or CI, R7 is H, and the ring A is
i. phenyl which may be substituted with substituents selected from the group consisting of Ci-6 alkyl, C3-5 cycloalkyl, and halogen,
ii. naphthyl,
iii. 2,3-dihydro-lH-inden-5-yl which may be substituted with substituents
selected from the group consisting of C1-6 alkyl and halogen, or
143

iv. cyclohexyl which may be substituted with Ci-6 alkyl.
[Claim 5] The compound or a salt thereof according to claim 4, wherein
the formula (la) is the following formula (lb): [Chem. 20]
RMs
i. tert-butyl or
ii. 4-tetrahydropyranyl, R3 is H, R4 is H, and the ring A is
i. phenyl which may be substituted with substituents selected from the group consisting of Ci-6 alkyl and halogen,
ii. naphthyl, or
iii. 2,3-dihydro-lH-inden-5-yl.
[Claim 6]
The compound or a salt thereof according to claim 1, wherein the compound is a compound selected from the group consisting of:
(2S)-2-[(3S)-4-{[(3S,4R)-4-(4-chloro-2-fluorophenyl)-l-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3 -yl] carbonyl} -3 -methylpiperazin-1 -yl] -3 -(2-fluoro-4-methylphenyl)propanoic acid,
(2S)-2-[(3S)-4-{[(3S,4R)-4-(4-chloro-2-fluorophenyl)-l-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3 -yl] carbonyl} -3 -methylpiperazin-1 -yl] -3 -(2-fluoro-4,6-dimethylphenyl)propanoic acid,
(2S)-2-[(3S)-4-{[(3S,4R)-l-tert-butyl-4-(4-chloro-2-fluorophenyl)pyrrolidin-3-yl]carbonyl} -3 -methylpiperazin-1 -yl]-3-mesitylpropanoic acid,
(2S)-2-[(3S)-4-{[(3S,4R)-l-tert-butyl-4-(4-chloro-2-fluorophenyl)pyrrolidin-3-yl]carbonyl}-3-methylpiperazin-1 -yl]-3-(2-fluoro-4-methylphenyl)propanoic acid,

(2S)-2-[(3S)-4-{[(3S,4R)-l-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl}-3-methylpiperazin-l-yl]-3-(2,3-dihydro-lH-inden-5-yl)propanoic acid,
(2S)-2-[(3S)-4-{[(3S,4R)-l-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl} -3 -propylpiperazin-1 -yl] -3 -(2-naphthyl)propanoic acid, and
(2S)-2-[(3S)-4-{[(3S,4R)-l-tert-butyl-4-(4-chloro-2-fluorophenyl)pyrrolidin-3-yl]carbonyl}-3-methylpiperazin-1-yl]-3-(4-methylphenyl)propanoic acid.
[Claim 7] A pharmaceutical composition comprising the compound or a salt thereof
according to claim 1, and a pharmaceutically acceptable excipient.
[Claim 8] The pharmaceutical composition according to claim 7, for preventing or
treating bladder and/or urinary tract diseases.
[Claim 9] Use of the compound or a salt thereof according to claim 1 for the
manufacture of a pharmaceutical composition for preventing or treating bladder and/or urinary tract diseases.
[Claim 10] Use of the compound or a salt thereof according to claim 1 for preventing
or treating bladder and/or urinary tract diseases.
[Claim 11] The compound or a salt thereof according to claim 1 for preventing or
treating bladder and/or urinary tract diseases.
[Claim 12] A method for preventing or treating bladder and/or urinary tract diseases,
comprising administering an effective amount of the compound or a salt thereof according to claim 1 to a subject.