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    Inhibitors of cyclin dependent kinases and their use
    8.
    发明授权
    Inhibitors of cyclin dependent kinases and their use 有权
    细胞周期蛋白依赖性激酶抑制剂及其用途

    公开(公告)号：US07915301B2

    公开(公告)日：2011-03-29

    申请号：US11779577

    申请日：2007-07-18

    申请人： Bansi Lal ,  Kalpana Joshi ,  Sanjeev Kulkarni ,  Malcolm Mascarenhas ,  Shrikant Kamble ,  Maggie Joyce Rathos ,  Rajendrakumar Joshi

    发明人： Bansi Lal ,  Kalpana Joshi ,  Sanjeev Kulkarni ,  Malcolm Mascarenhas ,  Shrikant Kamble ,  Maggie Joyce Rathos ,  Rajendrakumar Joshi

    IPC分类号： A61K31/4025 ,  A61K31/353 ,  C07D405/04 ,  C07D311/32

    CPC分类号： A61K31/4025 ,  C07D405/04 ,  C07D405/14

    摘要： The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ia), wherein R1, R2, R3, R4, R5, R6, R7 and A have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (Ia), to methods of inhibiting cyclin-dependent kinases and of inhibiting cell proliferation, to the use of the compounds of formula (Ia) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of cyclin-dependent kinases such as cancer, to the use of the compounds of formula (Ia) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (Ia) either alone or in combination with another active agent, in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (Ia) either alone or in combination with another active agent, together with pharmaceutically acceptable carrier substances and auxiliary substances.

    摘要翻译： 本发明涉及用于抑制细胞周期蛋白依赖性激酶的新化合物，更具体地，涉及式（Ia）的色烯酮衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和A具有如 索赔。 本发明还涉及制备式（Ia）化合物的方法，抑制细胞周期蛋白依赖性激酶和抑制细胞增殖的方法，以使用式（Ia）化合物在治疗和预防疾病中的用途 ，其可以通过抑制细胞周期蛋白依赖性激酶（例如癌症）来治疗或预防使用式（Ia）化合物在制备用于这些疾病的药物中的用途。 本发明还涉及含有式（Ia）化合物的组合物，其单独或与另一种活性剂组合，与惰性载体混合或以其它方式结合，特别是含有式（Ia）化合物的药物组合物，其单独或 与另一种活性剂，药学上可接受的载体物质和辅助物质一起使用。

    Tricyclic guanidine derivatives as sodium-proton exchange inhibitors
    9.
    发明授权
    Tricyclic guanidine derivatives as sodium-proton exchange inhibitors 失效
    三环胍衍生物作为钠 - 质子交换抑制剂

    公开(公告)号：US07834001B2

    公开(公告)日：2010-11-16

    申请号：US11667583

    申请日：2005-11-08

    申请人： Bansi Lal ,  Swati Bal-Tembe ,  Usha Ghosh ,  Arun Kumar Jain ,  Tulsidas More

    发明人： Bansi Lal ,  Swati Bal-Tembe ,  Usha Ghosh ,  Arun Kumar Jain ,  Tulsidas More

    IPC分类号： C07D327/08 ,  A61K31/382

    CPC分类号： C07D327/08

    摘要： Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.

    摘要翻译： 公开了具有式1的稠合三环的胍衍生物，其中U是C（O），CR a R b，O，NR a或S（O）m; V是CRaRb或NRa; W为S（O）m; 其中R a是H，烷基，环烷基，烯基或芳烷基; Rb是H，烷基，OH，ORa或OCORa，m是整数0,1或2; R1，R2，R3，R4，R5，R6，R7和R8如本文所定义，条件是R 1，R 2，R 3，R 4，R 5，R 6，R 7或R 8中的至少一个是胍基或胍基羰基。 这些衍生物是钠 - 质子交换抑制剂，并且可用作治疗例如与缺血和再灌注相关的器官疾病，心律失常，心脏肥大，高血压，细胞增殖性疾病和糖尿病的药物。