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    Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
    4.
    发明授权
    Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 失效
    环烷基内酰胺衍生物作为11-β-羟基类固醇脱氢酶1的抑制剂

    公开(公告)号：US07834194B2

    公开(公告)日：2010-11-16

    申请号：US11722101

    申请日：2005-12-16

    申请人： Thomas Daniel Aicher ,  Mark Joseph Chicarelli ,  Ronald Jay Hinklin ,  Hongqi Tian ,  Owen Brendan Wallace

    发明人： Thomas Daniel Aicher ,  Mark Joseph Chicarelli ,  Ronald Jay Hinklin ,  Hongqi Tian ,  Owen Brendan Wallace

    IPC分类号： C07D411/06 ,  A61K31/4025

    CPC分类号： C07D207/26 ,  C07D405/06 ,  C07D409/06 ,  C07D409/14 ,  C07D495/04

    摘要： The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, R0 is (II), or (III) G1 is methylene or ethylene; L is a divalent linking group selected from —(C1-C4) alkylene-, —S—, —CH(OH)—, or —O—; A is methylene, —S—, —O—, or —NH—; and the other substituents are as defined in the claims.

    摘要翻译： 本发明提供了可用作11-β羟基类固醇脱氢酶1的有效和选择性抑制剂的式I化合物。本发明还提供一种药物组合物，其包含式I化合物或其药学上可接受的盐 载体，稀释剂或赋形剂。 此外，本发明提供包含式I化合物用于治疗代谢综合征，糖尿病，高血糖症，肥胖，高血压，高脂血症，与高血糖症相关的其它症状以及相关疾病的组合物。 式（I）其中R 0为（II）或（III），G 1为亚甲基或亚乙基; L是选自 - （C 1 -C 4）亚烷基 - ， - S - ， - CH（OH） - 或-O-的二价连接基团; A是亚甲基，-S-，-O-或-NH-; 而其它取代基如权利要求中所定义。

    Cycloalkyl Lactam Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1
    5.
    发明申请
    Cycloalkyl Lactam Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1 失效
    环烷基内酰胺衍生物作为11-β-羟基类固醇脱氢酶抑制剂1

    公开(公告)号：US20080207691A1

    公开(公告)日：2008-08-28

    申请号：US11722101

    申请日：2005-12-16

    申请人： Thomas Daniel Aicher ,  Mark Joseph Chicarelli ,  Ronald Jay Hinklin ,  Hongqi Tian ,  Owen Brendan Wallace

    发明人： Thomas Daniel Aicher ,  Mark Joseph Chicarelli ,  Ronald Jay Hinklin ,  Hongqi Tian ,  Owen Brendan Wallace

    IPC分类号： A61K31/4535 ,  C07D409/06 ,  A61K31/4436 ,  A61K31/4025 ,  A61P3/08

    CPC分类号： C07D207/26 ,  C07D405/06 ,  C07D409/06 ,  C07D409/14 ,  C07D495/04

    摘要： The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, Ru0 is (II), or (III) G1 is methylene or ethylene; L is a divalent linking group selected from —(C1-C4) alkylene-, —S—, —CH(OH)—, or —O—; A is methylene, —S—, —O—, or —NH—; and the other substituents are as defined in the claims.

    摘要翻译： 本发明提供了可用作11-β羟基类固醇脱氢酶1的有效和选择性抑制剂的式I化合物。本发明还提供一种药物组合物，其包含式I化合物或其药学上可接受的盐 载体，稀释剂或赋形剂。 此外，本发明提供包含式I化合物用于治疗代谢综合征，糖尿病，高血糖症，肥胖，高血压，高脂血症，与高血糖症相关的其它症状以及相关疾病的组合物。 式（I）其中，R 0为（II）或（III）G 1为亚甲基或亚乙基; L是选自 - （C 1 -C 4 -C 4）亚烷基 - ， - S - ， - CH（OH） - 或-O-的二价连接基团。 A是亚甲基，-S-，-O-或-NH-; 而其它取代基如权利要求中所定义。