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US 7,407,958 B2Granted
2-pyridyl substituted imidazoles as ALK5 and/or ALK4 inhibitors
AssigneesSK Chemicals Co., Ltd., Ewha University-Industry Collaboration Foundation
InventorsDae-Kee Kim, Yung-Jue Bang, Hun-Taek Kim, Il-Sang Cho, Myoung-Soon Park, Young Jae An, Joon Hun Choi
Life of this patent
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Abstract
Compounds of the formula: wherein R1, R2, R3, A1 and A2 are as defined herein, which are used advantageously in inhibiting the TGF-β and/or activin signaling pathway in mammals.
Claims10
A compound of formula (I):
- wherein:
- R1 is
- wherein X1 is N;
- R2 is H, OH, —O—C1-6 alkyl, —S—C1-6 alkyl, C1-6 alkyl, phenyl, C1-6 haloalkyl, NH2, NH(CH2)n-Ph, NH—C 1-6 alkyl, halo, CN, NO2, CONHR or SO2NHR, wherein R is H or C1-6 alkyl, and n is 0, 1, 2, or 3;
- R3 is H, C1-6 alkyl, C3-7 cycloalkyl, —(CH2)p-NO2, —(CH2)p-NR4R5, —(CH2)p-CHO, —(CH2)p-CONHOH, —(CH2)p-CN, —(CH2)p-CO2H, —(CH2)p-CO2R4, —(CH2)p-CONR4R5, —(CH2)p-tetrazole, —(CH2)p-COR4, —(CH2)q-(COR6)2, —(CH2)p-OR4, (CH2)p-CH═CH—CN, —(CH2)p-CH═CH—CO2H, —(CH2)p-CH═CHCO2R4, —(CH2)pCH═CH—CONR4R5, —(CH2)p-NHCOR4, —(CH2)p-NHCO2R4, —(CH2)p-CONHSO2R4, (CH2)p-NHSO2R4 or —(CH2)p-CH═CH-tetrazole;
- R4 and R5 are independently H or C1-6 alkyl;
- R6 is C1-6 alkyl;
- p is 0, 1, 2, 3, or 4;
- q is 1, 2, 3, or 4;
- X is C1-10 alkylene, C2-10 alkenylene or C2-10 alkynylene;
- one of A1 and A2 is N and the other is NR7;
- and
- R7 is H, OH, C1-6 alkyl, or C3-7 cycloalkyl;
- or a pharmaceutically-acceptable salt or hydrate thereof.
11 more elements
Dependencies are inferred from the claim text.