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    Novel compounds as histone deacetylase inhibitors
    1.
    发明申请
    Novel compounds as histone deacetylase inhibitors 审中-公开
    新型化合物作为组蛋白脱乙酰酶抑制剂

    公开(公告)号：US20050176686A1

    公开(公告)日：2005-08-11

    申请号：US10624571

    申请日：2003-07-23

    申请人： Alexander Maurer ,  Sascha Hoevelmann ,  Elke Martin ,  Bernd Hentsch ,  Michael Gassen ,  Juergen Kraus ,  Rolf Krauss ,  Adam-Spencer Vincek

    发明人： Alexander Maurer ,  Sascha Hoevelmann ,  Elke Martin ,  Bernd Hentsch ,  Michael Gassen ,  Juergen Kraus ,  Rolf Krauss ,  Adam-Spencer Vincek

    IPC分类号： A61K31/19 ,  A61K31/66 ,  C07C259/04

    CPC分类号： C07C259/04 ,  C07C2601/08 ,  C07C2601/14

    摘要： The present invention is directed to compounds of the general formula (I) or pharmaceutical acceptable salts or physiologically functional derivatives thereof wherein: n is a non-aromatic ring system containing two to seven carbon atoms, wherein the ring system can contain one ore two double bonds; X is C, CH or CH2; Y is selected from C, CH, CH2, S, NR, CH2-CH2, H2C—CH, HC—CH2, C—CH2, H2C—C, or C—C; one or more of the hydrogen atoms can optionally be substituted by one or more substituents R′; each of the dotted lines means a single, a double or triple bond with the exclusion of a combination of a triple with triple bond and a double with a triple bond; R′ is independently H, —CN, alkyl, cycloalkyl, aminoalkyl, alkylamino, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, hydroxyalkylamino, halogene, haloalkyl, haloalkyloxy; R is H, an alkyl or cycloalkyl group; Z is CH, C, or P; p is 0 or 1.

    摘要翻译： 本发明涉及通式（I）的化合物或其药学上可接受的盐或生理功能衍生物，其中：n是含有2至7个碳原子的非芳族环系统，其中所述环体系可以包含一个二价双 债券 X是C，CH或CH 2; Y选自C，CH，CH 2，S，NR，CH 2 -CH 2，H 2， C-CH，HC-CH 2，C-CH 2，H 2 CC或CC; 一个或多个氢原子可以任选被一个或多个取代基R'取代; 每个虚线意味着单，双或三键，排除三元组与三键的组合和具有三键的双键; R'独立地是H，-CN，烷基，环烷基，氨基烷基，烷基氨基，烷氧基，-OH，-SH，烷硫基，羟基烷基，羟烷基氨基，卤素基，卤代烷基，卤代烷氧基。 R是H，烷基或环烷基; Z是CH，C或P; p为0或1。

    Compounds as histone deacetylase inhibitors
    2.
    发明授权
    Compounds as histone deacetylase inhibitors 失效
    化合物作为组蛋白脱乙酰酶抑制剂

    公开(公告)号：US08227516B2

    公开(公告)日：2012-07-24

    申请号：US11778297

    申请日：2007-07-16

    申请人： Alexander B. Maurer ,  Sascha Hoevelmann ,  Elke Martin ,  Bernd Hentsch ,  Michael Gassen ,  Juergen Kraus ,  Rolf Krauss ,  Adam-Spencer Vincek

    发明人： Alexander B. Maurer ,  Sascha Hoevelmann ,  Elke Martin ,  Bernd Hentsch ,  Michael Gassen ,  Juergen Kraus ,  Rolf Krauss ,  Adam-Spencer Vincek

    IPC分类号： A61K31/16

    CPC分类号： C07C259/04 ,  C07C2601/08 ,  C07C2601/14

    摘要： The present invention relates to compounds as inhibitors of enzymes having histone deacetylase activity, to the processes for the preparation of those compounds, and to their use for the treatment of diseases which are associated with hypoacetylation of histones and/or other molecules, or in which induction of hyperacetylation has a beneficial effect for example by inhibition of proliferation and/or induction of differentiation and/or induction of apoptosis in transformed cells, such as cancer. Furthermore, the compounds are useful for the treatment of other proliferative diseases, for therapy or prophylaxis of conditions associated with abnormal gene expression.

    摘要翻译： 本发明涉及作为具有组蛋白脱乙酰酶活性的酶的抑制剂的化合物，这些化合物的制备方法及其用于治疗与组蛋白和/或其他分子的低乙酰化相关的疾病的用途，或其中 超乙酰化的诱导例如通过抑制转化细胞（例如癌症）的增殖和/或诱导分化和/或诱导细胞凋亡具有有益的作用。 此外，该化合物可用于治疗其他增殖性疾病，用于治疗或预防与异常基因表达相关的病症。