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1.发明公开TRICYCLIC ALKYLHYDROXAMATES, THEIR PREPARATION AND THEIR USE AS CELL PROLIFERATION INHIBITORS 有权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
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.
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公开(公告)号：EP2274278A1
公开(公告)日：2011-01-19
申请号：EP09728035.8
申请日：2009-03-26
发明人： HARNETT, Gerard, John , HOFFMANN, Ursula , JANSEN, Michael , REENTS, Reinhard , SATTELKAU, Tim , SMITH, Dennis, A. , STAHR, Helmut
IPC分类号： C07C253/30 , C07C255/46 , C07C231/06 , C07C233/58 , C07C51/06 , C07C61/08 , C07C323/42 , C07C329/10
CPC分类号： C07C233/58 , C07C51/06 , C07C253/30 , C07C2601/14 , C07C61/08 , C07C255/46
摘要： A process for the preparation of a compound of formula (Ia): which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.
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3.发明授权TETRAHYDROPYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS CELL PROLIFERATION INHIBITORS 有权四氢吡啶，制备方法及其用途作为细胞增殖抑制剂
公开(公告)号：EP1353921B1
公开(公告)日：2006-04-19
申请号：EP01995721.6
申请日：2001-12-21
IPC分类号： C07D471/04 , C07D217/04 , A61K31/472 , A61P35/00
CPC分类号： C07D471/04 , C07D217/04
摘要： A compound of the formula (I) wherein A, R1, R2 and X have the meanings defined in the specification, process of manufacturing such as compound and a pharmaceutical composition with HDAC inhibitor activity and anti-cell proliferation activity containing such a compound.
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4.发明授权TRICYCLIC ALKYLHYDROXAMATES, THEIR PREPARATION AND THEIR USE AS CELL PROLIFERATION INHIBITORS 有权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
IPC分类号： C07D313/12 , A61K31/335 , C07C259/06 , C07D209/88 , A61P35/00
CPC分类号： C07C259/06 , C07D209/88 , C07D313/12
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5.发明授权TRICYCLIC LACTAM AND SULTAM DERIVATIVES AND THEIR USE AS HISTONE DEACETYLASE INHIBITORS 有权三环内酰胺磺内酰胺及其衍生物及其作为抑制剂组蛋白去乙酰使用
公开(公告)号：EP1358168B1
公开(公告)日：2005-08-10
申请号：EP02714107.6
申请日：2002-01-24
IPC分类号： C07D275/06 , C07D209/92 , A61K31/403 , A61K31/428 , A61P35/00
CPC分类号： C07D275/06 , C07D209/92
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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
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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7.发明授权NEW PROCESS FOR THE PREPARATIION OF CYCLOHEXANECARBOXYLIC ACID DERICATIVES 有权VERFAHREN ZUR HERSTELLUNG VONCYCLOHEXANCARBOXYLSÄURE-DERIVATEN
公开(公告)号：EP2274278B1
公开(公告)日：2016-08-17
申请号：EP09728035.8
申请日：2009-03-26
发明人： HARNETT, Gerard, John , HOFFMANN, Ursula , JANSEN, Michael , REENTS, Reinhard , SATTELKAU, Tim , SMITH, Dennis, A. , STAHR, Helmut
IPC分类号： C07C253/30 , C07C255/46 , C07C231/06 , C07C233/58 , C07C51/06 , C07C61/08 , C07C323/42 , C07C329/10
CPC分类号： C07C233/58 , C07C51/06 , C07C253/30 , C07C2601/14 , C07C61/08 , C07C255/46
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8.发明公开TRICYCLIC LACTAM AND SULTAM DERIVATIVES AND THEIR USE AS HISTONE DEACETYLASE INHIBITORS 有权三环内酰胺磺内酰胺及其衍生物及其作为抑制剂组蛋白去乙酰使用
公开(公告)号：EP1358168A1
公开(公告)日：2003-11-05
申请号：EP02714107.6
申请日：2002-01-24
IPC分类号： C07D275/06 , C07D209/92 , A61K31/403 , A61K31/428 , A61P35/00
CPC分类号： C07D275/06 , C07D209/92
摘要： A compound of formula (I) wherein A and B are optionally substituted cyclohexenyl or phenyl groups, X is carbonyl or sulfonyl, and Y is 5-7 atoms-linker, is useful as histone deacetylase inhibitors, particularly for inhibiting cell proliferation.
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9.发明公开TETRAHYDROPYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS CELL PROLIFERATION INHIBITORS 有权四氢吡啶，制备方法及其用途作为细胞增殖抑制剂
公开(公告)号：EP1353921A1
公开(公告)日：2003-10-22
申请号：EP01995721.6
申请日：2001-12-21
IPC分类号： C07D471/04 , C07D217/04 , A61K31/472 , A61P35/00
CPC分类号： C07D471/04 , C07D217/04
摘要： A compound of the formula (I) wherein A, R1, R2 and X have the meanings defined in the specification, process of manufacturing such as compound and a pharmaceutical composition with HDAC inhibitor activity and anti-cell proliferation activity containing such a compound.
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