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US 8,772,297 B2Granted
TGF-β signal transduction inhibitor
AssigneeKyoto University
InventorsHideaki Kakeya, Akira Hattori, Yasuaki Takasu, Nobutaka Fujii, Shinya Oishi, Soichi Kojima, Mitsuko Hara
Life of this patent
Estimating the term…
Abstract
The present invention provides a compound represented by the following formula (I) or a physiologically acceptable salt thereof, and use thereof for the prophylaxis or treatment of TGF-β-related diseases: wherein Y is a hydrogen atom and the like; R2 is and the like; R3 is —NR8—R9— and the like; R4, R5, R6 and R7 are the same or different and each is a hydrogen atom and the like; and X is and the like.
Claims18
A compound represented by the following formula (I):
- wherein
- Y is a hydrogen atom, a carboxyl group or
- wherein
- L is an oxygen atom or a bond, and R1 is optionally substituted C1-6 alkyl;
- R2 is
- R3 is —NR8—R9— or a bond, wherein R8 is a hydrogen atom or C1-6 alkyl, and R9 is C1-6 alkylene;
- R4, R5, R6 and R7 are the same or different and each is a hydrogen atom or C1-6 alkyl;
- and
- X is
- wherein R10 is a hydrogen atom or C1-6 alkyl;
- and
- R11 is optionally substituted phenyl, optionally substituted C1-6 alkyl or a hydrogen atom, or
- R10 and R11 form, together with the nitrogen atom bonded thereto, an optionally substituted 5- to 7-membered cyclic amino group,
- or a physiologically acceptable salt thereof.
11 more elements
A compound which is
- 4-[3-(piperidine-1-sulfonyl)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(piperidine-1-sulfonyl)benzenesulfonylamino]-methyl}-piperidine-1-carboxylic acid benzyl ester,
- 4-({methyl-[3-(methyl-p-tolylsulfamoyl)benzenesulfonyl]amino}methyl)piperidine-1-carboxylic acid tert-butyl ester,
- 4-[({3-[(4-tort-butylphenyl)methylsulfamoyl]benzenesulfonyl}methylamino)-methyl]piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(4-tert-butylphenylsulfamoyl)-2,4,5,6-tetramethylbenzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(piperidine-1-sulfonyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-[(3-diethylsulfamoylbenzenesulfonylamino)methyl]piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(morpholine-4-sulfonyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-[(3-sulfamoylbenzenesulfonylamino)methyl]piperidine-1-carboxylic acid tert-butyl ester,
- 4-(benzenesulfonylaminomethyl)piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(cyclohexylmethylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-[(3-phenylsulfamoylbenzenesulfonylamino)methyl]piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(4-methoxyphenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(3-methoxyphenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(2-methoxyphenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(4-trifluoromethylphenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(2-acetylaminophenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-[(3-p-tolylsulfamoylbenzenesulfonylamino)methyl]piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(4-tert-butylphenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(4-piperidin-1-yl-phenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(4-diethylaminophenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(4-dimethylaminophenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(4-morpholin-4-yl-phenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(4-acetylphenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-({3-[4-(1-hydroxyethyl)phenylsulfamoyl]benzenesulfonylamino}methyl)piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(4-hydroxyphenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylicacid tert-butyl ester,
- 4-{[3-(4-oxanylmethoxyphenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(4-azidophenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-(4-{3-[(1-tert-butoxycarbonylpiperidin-4-ylmethyl)sulfamoyl]benzenesulfonylamino}phenyl)piperazine-1-carboxylic acid tert-butyl ester,
- 4-({3-[4-(4-benzoylpiperazin-1-yl)phenylsulfamoyl]benzenesulfonylamino}methyl)piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(4-dimethylamino-3-furan-2-yl-phenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(3-furan-2-yl-4-piperidin-1-yl-phenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(3-furan-2-yl-phenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- 4-{[3-(3-thiophen-2-yl-phenylsulfamoyl)benzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester,
- or a physiologically acceptable salt thereof.
32 more elements
Dependencies are inferred from the claim text.