Benzamide compounds useful as histone deacetylase inhibitors
    5.
    发明授权
    Benzamide compounds useful as histone deacetylase inhibitors 有权
    可用作组蛋白脱乙酰酶抑制剂的苯甲酰胺化合物

    公开(公告)号:US08207202B2

    公开(公告)日:2012-06-26

    申请号:US12090611

    申请日:2006-10-17

    IPC分类号: A61K31/454 C07D401/06

    CPC分类号: C07D401/06

    摘要: The invention concerns benzamide compounds of formula (I), wherein R1 is a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from C1-4alkyl, C3-4cycloalkyl, C1-4alkoxy and C3-4cycloalkoxy; or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumors or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC).

    摘要翻译: 本发明涉及式(I)的苯甲酰胺化合物,其中R 1是C连接的吡唑环,其任选被一个或多个选自C 1-4烷基,C 3-4环烷基,C 1-4烷氧基和C 3-4环烷氧基的基团取代; 或其药学上可接受的盐或前药形式。 本发明还涉及制备此类化合物的方法,含有它们的药物组合物及其在制备用于预防或治疗肿瘤或其它增殖性病症中的药物中的用途,所述肿瘤或其它增殖性病症对抑制 组蛋白脱乙酰酶(HDAC)。

    Benzamide Compounds Useful as Histone Deacetylase Inhibitors
    6.
    发明申请
    Benzamide Compounds Useful as Histone Deacetylase Inhibitors 有权
    用作组蛋白脱乙酰酶抑制剂的苯甲酰胺化合物

    公开(公告)号:US20080269294A1

    公开(公告)日:2008-10-30

    申请号:US12090611

    申请日:2005-10-17

    CPC分类号: C07D401/06

    摘要: The invention concerns benzamide compounds of formula (I), wherein R1 is a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from C1-4alkyl, C3-4cycloalkyl, C1-4alkoxy and C3-4cycloalkoxy; or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC).

    摘要翻译: 本发明涉及式(I)的苯甲酰胺化合物,其中R 1是C连接的吡唑环,其任选被一个或多个选自C 1-4的基团取代 烷基,C 3-4环烷基,C 1-4烷氧基和C 3-4环烷氧基; 或其药学上可接受的盐或前药形式。 本发明还涉及制备此类化合物的方法,含有它们的药物组合物及其在制备用于预防或治疗肿瘤或其它增殖性病症中的药物中的用途,所述肿瘤或其它增殖性病症对抑制 组蛋白脱乙酰酶(HDAC)。

    Benzamide compounds useful as histone deacetylase inhibitors
    7.
    发明授权
    Benzamide compounds useful as histone deacetylase inhibitors 有权
    可用作组蛋白脱乙酰酶抑制剂的苯甲酰胺化合物

    公开(公告)号:US08735429B2

    公开(公告)日:2014-05-27

    申请号:US13472095

    申请日:2012-05-15

    IPC分类号: A61K31/445

    CPC分类号: C07D401/06

    摘要: The invention concerns benzamide compounds of formula (I): compound of formula (I): wherein R1 is a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from C1-4alkyl, C3-4cycloalkyl, C1-4alkoxy and C3-4cycloalkoxy; or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumors or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC).

    摘要翻译: 本发明涉及式(I)的苯甲酰胺化合物:式(I)化合物:其中R 1是C连接的吡唑环,其任选被一个或多个选自C 1-4烷基,C 3-4环烷基,C 1-4烷氧基 和C3-4环烷氧基; 或其药学上可接受的盐或前药形式。 本发明还涉及制备此类化合物的方法,含有它们的药物组合物及其在制备用于预防或治疗肿瘤或其它增殖性病症中的药物中的用途,所述肿瘤或其它增殖性病症对抑制 组蛋白脱乙酰酶(HDAC)。

    BENZAMIDE COMPOUNDS USEFUL AS HISTONE DEACETYLASE INHIBITORS
    8.
    发明申请
    BENZAMIDE COMPOUNDS USEFUL AS HISTONE DEACETYLASE INHIBITORS 有权
    苯甲酸化合物有效用作脱乙酰壳多糖酶抑制剂

    公开(公告)号:US20120225907A1

    公开(公告)日:2012-09-06

    申请号:US13472095

    申请日:2012-05-15

    CPC分类号: C07D401/06

    摘要: The invention concerns benzamide compounds of formula (I): compound of formula (I): wherein R1 is a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from C1-4alkyl, C3-4cycloalkyl, C1-4alkoxy and C3-4cycloalkoxy; or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC).

    摘要翻译: 本发明涉及式(I)的苯甲酰胺化合物:式(I)化合物:其中R 1是C连接的吡唑环,其任选被一个或多个选自C 1-4烷基,C 3-4环烷基,C 1-4烷氧基 和C3-4环烷氧基; 或其药学上可接受的盐或前药形式。 本发明还涉及制备此类化合物的方法,含有它们的药物组合物及其在制备用于预防或治疗肿瘤或其它增殖性病症中的药物中的用途,所述肿瘤或其它增殖性病症对抑制 组蛋白脱乙酰酶(HDAC)。

    2-ANILINOPURIN-8-ONES AS INHIBITORS OF TTK/MPS1 FOR THE TREATMENT OF PROLIFERATIVE DISORDERS
    9.
    发明申请
    2-ANILINOPURIN-8-ONES AS INHIBITORS OF TTK/MPS1 FOR THE TREATMENT OF PROLIFERATIVE DISORDERS 审中-公开
    作为TTK / MPS1抑制剂的2-ANILINOPURIN-8-ONES用于治疗增殖性疾病

    公开(公告)号:US20110118238A1

    公开(公告)日:2011-05-19

    申请号:US12674749

    申请日:2008-08-20

    CPC分类号: C07D487/04

    摘要: This invention relates to chemical compounds of the formula (I), or a pharmaceutically acceptable salt thereof, which possess inhibitory activity against the spindle checkpoint kinase: Tyrosine Threonine Kinase (TTK)/monopolar spindle 1 (Mps1) and are accordingly useful for their anti-cancer effect in a warm-blooded animal such as man. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them, and to their use in the manufacture of a medicament for the treatment of conditions mediated by TTK/Mps1, for use either alone or in combination with other anti-pro liferative agents.

    摘要翻译: 本发明涉及对主轴检查点激酶:酪氨酸苏氨酸激酶(TTK)/单极纺锤体1(Mps1)具有抑制活性的式(I)化合物或其药学上可接受的盐,因此可用于其抗 - 在温血动物如男人中的癌症效应。 本发明还涉及制备所述化合物的方法,含有它们的药物组合物及其在制备用于治疗由TTK / Mps1介导的病症的药物中的用途,用于单独使用或与其它组合使用 抗衰老剂。