Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline
    9.
    发明授权
    Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline 有权
    六氢茚基吡啶和八氢苯并喹啉的芳基和杂芳基羰基衍生物

    公开(公告)号:US08686149B2

    公开(公告)日:2014-04-01

    申请号:US13289418

    申请日:2011-11-04

    IPC分类号: C07D221/16

    CPC分类号: C07D401/06

    摘要: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.

    摘要翻译: 本发明涉及由式I定义的化合物,其中变量R1,R2,R3,R4和m如权利要求1所定义,具有有价值的药理学活性。 特别地,化合物是11β-羟基类固醇脱氢酶(HSD)1的抑制剂,因此适用于治疗和预防可受该酶抑制影响的疾病,例如代谢疾病,特别是2型糖尿病,肥胖症和 血脂异常

    Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
    10.
    发明授权
    Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 有权
    11β-羟基类固醇脱氢酶的循环抑制剂1

    公开(公告)号:US08680093B2

    公开(公告)日:2014-03-25

    申请号:US13318271

    申请日:2010-04-30

    IPC分类号: C07D413/14 A61K31/535

    CPC分类号: C07D413/10

    摘要: This invention relates to novel compounds of the Formula Ik, Im1, Im2, Im5, In1, In2, In5, lo1, lo2, lo5, Ip1, Ip3, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.

    摘要翻译: 本发明涉及可用于治疗性治疗的式Ik,Im1,Im2,Im5,In1,In2,In5,lo1,lo2,lo5,Ip1,Ip3,其药学上可接受的盐及其药物组合物的新型化合物 与哺乳动物调节或抑制11& -HSD1相关的疾病。 本发明进一步涉及新化合物的药物组合物及其用于减少或控制细胞中皮质醇的产生或抑制细胞中可的松转化为皮质醇的方法。