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    Compounds as histone deacetylase inhibitors
    1.
    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。

    Using inhibitors of histone deacetylases for the suppression therapy of inherited disease predisposing conditions
    2.
    发明授权
    Using inhibitors of histone deacetylases for the suppression therapy of inherited disease predisposing conditions 失效
    使用组蛋白脱乙酰酶抑制剂进行遗传性疾病易感条件的抑制治疗

    公开(公告)号：US07892833B2

    公开(公告)日：2011-02-22

    申请号：US11275263

    申请日：2005-12-21

    申请人： Bernd Hentsch ,  Alexander B. Maurer ,  Sascha Hövelmann ,  Monika Raab ,  Elke Martin

    发明人： Bernd Hentsch ,  Alexander B. Maurer ,  Sascha Hövelmann ,  Monika Raab ,  Elke Martin

    IPC分类号： C12N15/01 ,  G01N33/53

    CPC分类号： A61K31/20 ,  A61K31/19 ,  A61K31/4436 ,  A61K31/505 ,  A61K2300/00

    摘要： Compounds can be used to act as inhibitors of enzymes having histone deacetylase activity for the medical therapy of conditions which predispose a person for the development of a disease, such as but not limited to cancer, inflammatory or metabolic diseases. Such conditions are linked to genetically inherited mutations of crucial genes which predispose a person with this condition to develop the disease phenotype. Thus, such compounds can be used for a suppressive therapeutic approach—the SUPPRESSION THERAPY—in order to inhibit or delay the onset or progression of the genetically predisposed disorder. Furthermore, a clinically used medicament can be manufactured for the SUPPRESSION THERAPY of such inherited predisposing conditions.

    摘要翻译： 化合物可用作具有组蛋白脱乙酰酶活性的酶的抑制剂，用于药物治疗易于使人发展疾病（例如但不限于癌症，炎性或代谢性疾病）的病症。 这种情况与关键基因的遗传遗传突变有关，这种突变使患有这种病症的人发展为疾病表型。 因此，这些化合物可以用于抑制性治疗方法 - 抑制疗法 - 以抑制或延缓遗传易感疾病的发作或进展。 此外，可以制造临床使用的药物用于这种遗传易感条件的抑制治疗。

    Using Inhibitors of Histone Deacetylases for the Suppression Therapy of Inherited Disease Predisposing Conditions
    3.
    发明申请
    Using Inhibitors of Histone Deacetylases for the Suppression Therapy of Inherited Disease Predisposing Conditions 失效
    使用组蛋白脱乙酰酶抑制剂抑制继发性疾病预防条件

    公开(公告)号：US20070037738A1

    公开(公告)日：2007-02-15

    申请号：US11275263

    申请日：2005-12-21

    申请人： Bernd Hentsch ,  Alexander Maurer ,  Sascha Hovelmann ,  Monika Raab ,  Elke Martin

    发明人： Bernd Hentsch ,  Alexander Maurer ,  Sascha Hovelmann ,  Monika Raab ,  Elke Martin

    IPC分类号： A61K38/12 ,  A61K31/19 ,  A61K31/20

    CPC分类号： A61K31/20 ,  A61K31/19 ,  A61K31/4436 ,  A61K31/505 ,  A61K2300/00

    摘要： Compounds can be used to act as inhibitors of enzymes having histone deacetylase activity for the medical therapy of conditions which predispose a person for the development of a disease, such as but not limited to cancer, inflammatory or metabolic diseases. Such conditions are linked to genetically inherited mutations of crucial genes which predispose a person with this condition to develop the disease phenotype. Thus, such compounds can be used for a suppressive therapeutic approach—the SUPPRESSION THERAPY—in order to inhibit or delay the onset or progression of the genetically predisposed disorder. Furthermore, a clinically used medicament can be manufactured for the SUPPRESSION THERAPY of such inherited predisposing conditions.

    摘要翻译： 化合物可用作具有组蛋白脱乙酰酶活性的酶的抑制剂，用于药物治疗易于使人发展疾病（例如但不限于癌症，炎性或代谢性疾病）的病症。 这种情况与关键基因的遗传遗传突变有关，这种突变使患有这种病症的人发展为疾病表型。 因此，这些化合物可以用于抑制性治疗方法 - 抑制疗法 - 以抑制或延缓遗传易感疾病的发作或进展。 此外，可以制造临床使用的药物用于这种遗传易感条件的抑制治疗。

    Novel compounds as histone deacetylase inhibitors
    5.
    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。

    Use of Inhibitors of Histone Deacteylases in Combination With Compounds Acting as Nsaid for the Therapy of Human Diseases
    7.
    发明申请
    Use of Inhibitors of Histone Deacteylases in Combination With Compounds Acting as Nsaid for the Therapy of Human Diseases 审中-公开
    使用组蛋白酶抑制剂与化合物作为人类疾病治疗的化合物

    公开(公告)号：US20080207724A1

    公开(公告)日：2008-08-28

    申请号：US11995711

    申请日：2006-06-14

    申请人： Sigrun Mink ,  Elke Martin ,  Bernd Hentsch

    发明人： Sigrun Mink ,  Elke Martin ,  Bernd Hentsch

    IPC分类号： A61K31/415 ,  A61K31/19 ,  A61P35/00 ,  A61P3/10

    CPC分类号： A61K45/06 ,  A61K31/19 ,  A61K2300/00

    摘要： The present invention relates to the medical use of compounds acting as inhibitors of enzymes having histone deacetylase activity in conditions where their combination with compounds known as NSAID's, Non Steroidal Anti Inflammatory Drugs, causes an enhanced beneficial therapeutic effect. These conditions comprise cancer, cancer predisposing conditions, inflammatory and metabolic diseases. Furthermore, the invention includes the manufacture of clinically used medicaments for the therapy of the diseases mentioned herein, administering the compounds separately in the form of two individual drugs or in an administrative form which contains both drugs in a single application unit.

    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的医疗用途，其与被称为NSAID's非甾体抗炎药物的化合物的组合引起增强的有益治疗效果。 这些病症包括癌症，癌症易感条件，炎症和代谢疾病。 此外，本发明包括制备用于治疗本文所述疾病的临床使用的药物，以两种单独药物的形式分开施用化合物，或以单一施用单位包含两种药物的管理形式。