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1. 发明公开

EP1385837A1 TRICYCLIC ALKYLHYDROXAMATES, THEIR PREPARATION AND THEIR USE AS CELL PROLIFERATION INHIBITORS 有权
标题翻译： TRIZYCLISCHE ALKYLHYDROXAMATE，生产及其作为细胞增殖抑制剂
公开(公告)号：EP1385837A1
公开(公告)日：2004-02-04
申请号：EP02724292.4
申请日：2002-04-19
申请人： F. HOFFMANN-LA ROCHE AG
发明人： GROSSMANN, Adelbert , VON DER SAAL, Wolfgang , SATTELKAU, Tim , TIBES, Ulrich
IPC分类号： C07D313/12 , A61K31/335 , C07C259/06 , C07D209/88 , A61P35/00
CPC分类号： C07C259/06 , C07D209/88 , C07D313/12
摘要： Compounds of formula (I), wherein R1, R2, A, X, Y and Z have the meanings defined in the specification, process of manufacturing these compounds and pharmaceuticals with HDAC inhibitor activity containing such a compound.

2. 发明授权

EP1385837B1 TRICYCLIC ALKYLHYDROXAMATES, THEIR PREPARATION AND THEIR USE AS CELL PROLIFERATION INHIBITORS 有权
标题翻译： TRIZYCLISCHE ALKYLHYDROXAMATE，生产及其作为细胞增殖抑制剂
公开(公告)号：EP1385837B1
公开(公告)日：2005-10-12
申请号：EP02724292.4
申请日：2002-04-19
申请人： F. HOFFMANN-LA ROCHE AG
发明人： GROSSMANN, Adelbert , VON DER SAAL, Wolfgang , SATTELKAU, Tim , TIBES, Ulrich
IPC分类号： C07D313/12 , A61K31/335 , C07C259/06 , C07D209/88 , A61P35/00
CPC分类号： C07C259/06 , C07D209/88 , C07D313/12

3. 发明公开

EP1575933A1 ENANTIOMERS OF THIOPHENE HYDROXAMIC ACID DERIVATIVES AND THEIR USE AS HDAC INHIBITORS 审中-公开
标题翻译： THIOPHENHYDROXAMSÄUREDERIVATE对映异构体及其作为HDAC抑制剂
公开(公告)号：EP1575933A1
公开(公告)日：2005-09-21
申请号：EP03789278.3
申请日：2003-12-15
申请人： F. HOFFMANN-LA ROCHE AG
发明人： GROSSMANN, Adelbert , HERTING, Frank , KOERNER, Matthias , KUENKELE, Klaus-Peter , LIMBERG, Anja , MUNDIGL, Olaf , TIBES, Ulrich
IPC分类号： C07D333/38 , C07D409/12 , C07D413/12 , A61K31/381 , A61K31/4025 , A61K31/422 , A61K31/4436 , A61P35/00
CPC分类号： C07D409/12 , C07D333/38 , C07D413/12
摘要： Compounds of Formula (I) wherein Ar, R1 and R2 have the meanings defined in the specification, process of manufacturing these compounds and medicaments with HDAC inhibitor activity containing such a compound.

4. 发明公开

EP1349830A1 TETRALONE DERIVATIVES AS ANTITUMOR AGENTS 审中-公开
标题翻译： TETRALONDERIVATE ALS ANTITUMORMITTEL
公开(公告)号：EP1349830A1
公开(公告)日：2003-10-08
申请号：EP01999552.1
申请日：2001-12-06
申请人： F. HOFFMANN-LA ROCHE AG
发明人： GEORGES, Guy , GROSSMANN, Adelbert , SATTELKAU, Tim , SCHAEFER, Wolfgang , TIBES, Ulrich
IPC分类号： C07C259/06 , A61K31/165
CPC分类号： C07D295/116 , C07C259/06 , C07C2601/02 , C07C2602/10 , C07D213/50 , Y02P20/55
摘要： Compounds of formula (I) wherein R1, R2, R3, R4, R5, X and Y have the meanings defined below, process of manufacturing these compounds and pharmaceuticals containing such a compound have HDAC inhibitor activity. R1 is selected from hydrogen, (1-4C)alkyl, COOH, COO(1-4C)alkyl, R2, R3, R4, R5 are independently selected from hydrogen, a halogen atom, an (1-4C)alkyl-, trifluoromethyl-, hydroxy-, (1-4C)alkoxy-, aryloxy-, arylalkyloxy-, nitro-, amino-, (1-4C)alkylamino-, di[1-4C)alkyl]-amino, piperidino, morpholino, pyrrolidino, (1-4C)alkanoylamino-, or an aryl group, or a heteroaryl group, or R2 and R3 together or R3 and R4 together or R4 and R5 together, respectively, can form an (1-3C)alkylenedioxy ring, or R2 and R3 together or R3 and R4 together or R4 and R5 together, respectively, can form an (3-5C)alkylene chain. Y is CH2-CH2-. X is an alkylene-chain of 4 to 10 carbon atoms which can be saturated or unsaturated with one or two double bonds or one or two triple bonds or a one double and one triple bond, and which can be branched or unbranched or interrupted by a (3-7C) cycloalkylring.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐，其中R1，R2，R3，R4，R5，X和Y具有本说明书中定义的含义。该化合物具有可用于癌症治疗的组蛋白脱乙酰酶（HDAC）抑制活性。还提供了通过使式III化合物与式IV化合物反应制备式I化合物的方法，其中A是可置换基团，PG是保护基团。

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