KAWAMOTO RICHARD MASARU,WARSHAKOON NAMAL CHITHRANGA,GREIS KENNETH DONALD,BOYER ANGELIQUE SUN,WU SHENGDE,EDOKIMOV ARTEM G.
申请号：
NZ60173007
公开号：
NZ601730A
申请日:
2007.06.26
申请国别(地区):
NZ
年份:
2014
代理人:
摘要：
601730 Disclosed are { [5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino} -acetic acid derivatives as represented by the general formula, as inhibitors of human protein prolyl hydroxylase for stimulating an angiogenic response for increasing blood flow, oxygen delivery and energy utilization in ischemic tissues； wherein R and R1 are each independently: i) hydrogen； ii) substituted or unsubstituted phenyl； or iii) substituted or unsubstituted heteroaryl； provided that R and R1 are not both hydrogen； R2 is OR6 or NR7aR7b； R6 is hydrogen or linear, branched, or cyclic alkyl； R7a and R7b are each independently: hydrogen, linear, branched, or cyclic alkyl； or R7a and R7b can be taken together to form a ring having from 3 to 7 atoms； R3 is hydrogen, methyl, or ethyl； L is an C1-C3 optionally substituted alkylene moiety； R9 is hydrogen or methyl； or a pharmaceutically acceptable salt thereof； and wherein the remaining substituents are as defined herein. Representative compounds include { [5-(4-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino} acetic acid methyl ester, [(3-hydroxy-5-(4-methylphenyl)pyridine-2-carbonyl)amino]acetic acid methyl ester, { [3-hydroxy-5-(3-trifluoromethylphenyl)-pyridine-2-carbonyl]amino} acetic acid methyl ester, [(3-hydroxy-5-isoquinolin-4-yl-pyridine-2-carbonyl)amino]acetic acid methyl ester, ({ 5-[3-(cyclopropanecarbonylamino)phenyl]-3-hydroxypyridine-2-carbonyl} amino)acetic acid methyl ester, 5-(3-chlorophenyl)-N-(2-dimethylamino-2-oxoethyl)-3-hydroxypyridin-2-yl amide, 5-(3-chlorophenyl)-N-(2-isopropylamino-2-oxoethyl)-3-hydroxypyridin-2-yl amide, 2-{ [5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino} -2-methyl-propionic acid methyl ester and 5-(3-chlorophenyl)-N-(2-methylamino-2-oxo-1,1-dimethylethyl)-3-hydroxylpyridin-2-yl amide. Further disclosed is a composition comprising one or more compounds as defined above, or a pharmaceutically acceptable salt thereof； and one or more excipients or carriers； for treating a disease selec
