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公开(公告)号:US06790834B1
公开(公告)日:2004-09-14
申请号:US09514083
申请日:2000-02-28
IPC分类号: C07K506
CPC分类号: C07D333/34 , A61K31/216 , A61K31/223 , A61K31/341 , A61K31/381 , A61K31/4406 , A61K31/445 , C07C259/06 , C07C2601/08 , C07D211/46 , C07D213/55 , C07D307/20
摘要: Compounds of formula I are disclosed wherein R4 is an ester or thioester group, and R, R1, R2, and R3 are as defined in the specification are inhibitors of rapidly dividing tumor cells.
摘要翻译: 公开了式I化合物,其中R 4是酯或硫酯基,R 1,R 2,R 2和R 3如本说明书中所定义,是快速分裂肿瘤细胞的抑制剂。
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公开(公告)号:US06462023B1
公开(公告)日:2002-10-08
申请号:US09100539
申请日:1998-06-19
IPC分类号: C07K506
CPC分类号: A61K31/216 , A61K31/223 , A61K31/341 , A61K31/381 , A61K31/4406 , A61K31/445 , C07C259/06 , C07C2601/08 , C07D211/46 , C07D213/55 , C07D307/20 , C07D333/34
摘要: The present invention provide compounds exemplified by 2(R or S)-[2R-(S-Hydroxy-hydroxycarbamoyl-methyl)-4-methyl-pentanoylamine]-2-phenyl-ethanoic acid cyclopentyl ester; 2(R or S)-(3S-Hydroxycarbamoyl-2R-isobutyl-hex-5-enoylamino)-2-phenylethanoic acid isopropyl ester; 2(R or S)-[2R-(S-Hydroxycarbamoyi-methoxy-methyl)-4-methyl-pentanoylamino]-3-phenylethanoic acid cyclopentyl ester; 2(R or S)-(3S-Hydroxycarbamoyl-2R-isobutyl-hex-5-enoylamino)-2-(4-methoxyphenyl)ethanoic acid cyclopentyl ester; 2(R or S)-(3S-Hydroxycarbamoyl-2R-isobutyl-hex-5-enoylamino)-2-(thien-2-yl)ethanoic acid cyclopentyl ester; and 2(R or S)-(3S-Hydroxycarbamoyl-2R-isobutyl-hex-5-enoylamino)-2-(thien-3-yl)ethanoic acid cyclopentyl ester are cytostatic agents. Methods of treating proliferative cell growth disorders as well a methods of inhibiting hyper-proliferative cells are also disclosed.
摘要翻译: 本发明提供了2(R或S) - [2R-(S-羟基 - 羟基氨基甲酰基 - 甲基)-4-甲基 - 戊酰胺] -2-苯基 - 乙酸环戊酯的实例化合物; 2(R或S) - (3S-羟基氨基甲酰基 - 2R-异丁基 - 己-5-烯酰基氨基)-2-苯基乙酸异丙酯; 2(R或S) - [2R-(S-羟基氨基甲酰基 - 甲氧基 - 甲基)-4-甲基 - 戊酰基氨基] -3-苯基乙酸环戊酯; 2(R或S) - (3S-羟基氨基甲酰基-2R-异丁基 - 己-5-烯酰基氨基)-2-(4-甲氧基苯基)乙酸环戊酯; 2(R或S) - (3S-羟基氨基甲酰基-R 2R-异丁基 - 己-5-烯酰基氨基)-2-(噻吩-2-基)乙酸环戊酯; 和2(R或S) - (3S-羟基氨基甲酰基-R 2R-异丁基 - 己-5-烯酰基氨基)-2-(噻吩-3-基)乙酸环戊酯是细胞抑制剂。 还公开了治疗增殖性细胞生长障碍的方法以及抑制高增殖细胞的方法。
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公开(公告)号:US06169075A
公开(公告)日:2001-01-02
申请号:US08925584
申请日:1997-09-08
IPC分类号: C07K506
CPC分类号: C07D333/34 , A61K31/216 , A61K31/223 , A61K31/341 , A61K31/381 , A61K31/4406 , A61K31/445 , C07C259/06 , C07C2601/08 , C07D211/46 , C07D213/55 , C07D307/20
摘要: Compounds of formula 1 wherein R4 is an ester or thioester group, and R, R1, R2 and R3 are as defined in the specification are inhibitors of rapidly dividing tumour cells.
摘要翻译: R 1的化合物是R 4是酯或硫酯基,R 1,R 2,R 2和R 3如本说明书中所定义的是快速分裂肿瘤细胞的抑制剂。
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