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Substituted pyrrolidine-2-carboxamides
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
BARTKOVITZ DAVID JOSEPH,CHU XIN-JIE,DING QINGJIE,JIANG NAN,LIU JIN-JUN,ROSS TINA MORGAN,ZHANG JING,ZHANG ZHUMING
申请号:
NZ60142211
公开号:
NZ601422A
申请日:
2011.02.04
申请国别(地区):
NZ
年份:
2014
代理人:
摘要:
Disclosed are compounds having a common { [(2R,3 S,4R,5S)-4-(4-chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino} structure, wherein the nitrogen of the amino group is substituted by a further subsituent. Specific examples of the compounds are 4-{ [(2R,3S,4R,5S)-4-(4-chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino} -2-ethoxy-benzoic acid, 5-{ [(2R,3S,4R,5S)-4-(4-chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino} -pyrazine-2-carboxylic acid and 4-{ [(2R,3S,4R,5S)-4-(4-chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino} -3-methoxy-benzoic acid. Also disclosed are methods of synthesising these compounds and their use as a medicament in the treatment of cancers, particularly solid tumours of the breast, colon, lung and prostate.
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