发明名称 SUBSTITUTED PYRROLIDINE-2-CARBOXAMIDES
摘要 Disclosed herein are subsitituted pyrrolidine-2-carboxamides of formula I and II, wherein the substituents are as defined within the specification, processes for their preparation, compositions comprising said compounds and uses thereof. Said compounds are useful in the treatment or control of cell proliferative disorders, in particular oncological disorders. The compounds and formulations containing said compounds may be particularly useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors. Particularly preferred compounds include: (2R,3R,4R,5S)-3-(3-chloro-phenyl)-4-(4-chloro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carboxylic acid (2-morpholin-5 4-yl-ethyl)-amide; (S)-2-{ [(2R,3R,4R,5S)-3-(3-chloro-phenyl)-4-(4-chloro-phenyl)-4-cyano-5-(2,2-dimethylpropyl)-pyrrolidine-2-carbonyl]-amino} -3-methyl-butyric acid methyl ester; (2S,3S,4S,5R)-3-(3-chloro-phenyl)-4-(4-chloro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carboxylic acid ((R)-1-hydroxymethyl-3-methyl-butyl)-amide; rac-(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-phenyl)-4-cyano-5-cyclopentylmethyl-pyrrolidine-2-carboxylic acid ((S)-3,4-dihydroxy-butyl)-amide; rac-(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-phenyl)-4-cyano-5-(2,2-dimethylpropyl)-pyrrolidine-2-carboxylic acid ((S)-3,4-dihydroxy-butyl)-amide; (2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2 -fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carboxylic acid [4-(1H-tetrazol-5-yl)-phenyl]-amide.
申请公布号 NZ591024(A) 申请公布日期 2013.01.25
申请号 NZ20090591024 申请日期 2009.09.08
申请人 F. HOFFMANN-LA ROCHE AG 发明人 DING, QINGJIE;JIANG, NAN;LIU, JIN-JUN;ROSS, TINA MORGAN;ZHANG, JING;ZHANG, ZHUMING
分类号 C07D401/06;A61K31/40;A61K31/4025;A61P35/00;C07D207/16;C07D401/12;C07D401/14;C07D403/06;C07D403/12;C07D405/06;C07D405/12;C07D409/04;C07D409/12;C07D413/12;C07D417/12 主分类号 C07D401/06
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