PYRAZOLYLAMINO SUBSTITUTED QUINAZOLES FOR THE TREATMENT OF CANCER
    13.
    发明申请
    PYRAZOLYLAMINO SUBSTITUTED QUINAZOLES FOR THE TREATMENT OF CANCER 审中-公开
    用于治疗癌症的吡唑啉胺取代的喹诺酮

    公开(公告)号:US20100022476A1

    公开(公告)日:2010-01-28

    申请号:US11722439

    申请日:2005-12-16

    摘要: The invention provided a compound of formula: (I) for use in the treatment of disease, in particular proliferative diseases such as cancer and for use in the preparation of medicaments for use in the treatment of proliferative diseases; the invention also processes for the preparation of such compounds, as well as pharmaceutical compositions containing them as active ingredient.

    摘要翻译: 本发明提供了一种式(I)化合物,其用于治疗疾病,特别是增殖性疾病如癌症和用于制备用于治疗增殖性疾病的药物; 本发明还用于制备这些化合物以及含有它们作为活性成分的药物组合物。

    PYRAZOLE DERIVATIVES AND THEIR USE AS PI3K INHIBITORS
    14.
    发明申请
    PYRAZOLE DERIVATIVES AND THEIR USE AS PI3K INHIBITORS 审中-公开
    吡唑衍生物及其作为PI3K抑制剂使用

    公开(公告)号:US20090118336A1

    公开(公告)日:2009-05-07

    申请号:US12299369

    申请日:2007-05-02

    CPC分类号: C07D401/04 C07D417/14

    摘要: The invention concerns pyrazole derivatives of Formula I or pharmaceutically-acceptable salts thereof, wherein each of R, Ring A, m, R1, R2 and R3 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.

    摘要翻译: 本发明涉及式I的吡唑衍生物或其药学上可接受的盐,其中R,环A,m,R 1,R 2和R 3中的每一个具有上文在描述中定义的任何含义; 其制备方法,含有它们的药物组合物及其在治疗中的用途,例如用于治疗由PI3K酶和/或mTOR激酶介导的疾病。

    Heterocyclic Sulfonamide Derivatives as Inhibitors of Factor Xa

    公开(公告)号:US20080214495A1

    公开(公告)日:2008-09-04

    申请号:US11994846

    申请日:2006-07-05

    摘要: The invention relates to compounds of formula (I), wherein R1 and R3 are independently selected from carbon and nitrogen; R2 is oxo or thioxo; n is 0, 1 or 2; each R10 is independently selected from hydrogen and C1-3alkyl; R4 and R5 are each selected from carbon and nitrogen, wherein at least one of R4 and R5 is nitrogen; R6 is hydrogen or oxo; R7 is an aliphatic, partially saturated or aromatic carbocyclic ring, said carbocyclic ring having 0, 1 or 2 hetero nitrogen; m is 0, 1 or 2; each R11 is independently selected from hydrogen, hydroxy, oxo, C1-5alkyl, carboxy, hydroxyC1-5alkyl, carboxyC1-5alkyl, C1-5alkoxy-oxoC1-5alkyl, carbamoyl, C1-5alkylcarbamoyl, di (C1-5 alkyl)carbamoyl, carbamoylC1-4alkyl,C1-5alkylcarbamoylC1-4alkyl, di(C1-5alkyl)carbamoylC1-4alkyl, hydroxyC1-5alkylcarbamoyl, C1-5 alkoxyC1-5alkylcarbamoyl, hydroxyC1-5alkylcarbamoylC1-4alkyl, C1-5alkoxyC1-5 alkylcarbamoylC1-4 alkyl, CONR80(CH2)xS(O)pR90, CONH(CH2)qNR100R100, —C1-5 alkyl-Y1, —COOCHR170R180 and —CON R170R180; R8 is a bond, C1-4alkylene or C2-6alkenylene; R9 is an aromatic ring system having 0, 1 or 2 hetero atoms; wherein R9 is substituted by 0 or 1 halogen; or a pharmaceutically acceptable salt thereof, said compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the compounds, to their use, to pharmaceutical compositions comprising them, to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, and to combinations comprising them.