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    Azolopyridin-2-one derivatives as lipase and phospholipase inhibitors
    29.
    发明授权
    Azolopyridin-2-one derivatives as lipase and phospholipase inhibitors 有权
    偶氮吡啶-2-酮衍生物作为脂肪酶和磷脂酶抑制剂

    公开(公告)号：US07846943B2

    公开(公告)日：2010-12-07

    申请号：US11950932

    申请日：2007-12-05

    申请人： Gerhard Zoller ,  Stefan Petry ,  Gunter Müller ,  Hubert Heuer ,  Norbert Tennagels

    发明人： Gerhard Zoller ,  Stefan Petry ,  Gunter Müller ,  Hubert Heuer ,  Norbert Tennagels

    IPC分类号： A61K31/4355 ,  C07D498/04 ,  A61P3/00 ,  A61P9/00

    CPC分类号： C07D498/04

    摘要： The present invention provides compounds which have an inhibitory effect on hormone-sensitive lipase or endothelial lipase. The compounds of the invention are azolopyridin-2-one derivatives of the general formula I wherein the substituents are as defined herein. The compounds of formula I wherein R2 is hydrogen are distinguished by favorable effects on disorders of lipid metabolism. They beneficially influence the HDL to LDL ratio and increase in particular the HDL level and are suitable for the prevention and treatment of dyslipidemias and metabolic syndrome and their diverse sequelae such as atherosclerosis, coronary heart disease, heart failure, obesity and diabetes. The compounds of formula I wherein R1 and R2 together form a ring system are distinguished by favorable effects on metabolic disorders. They beneficially influence lipid and sugar metabolism; in particular they lower the triglyceride level and are suitable for the prevention and treatment of type II diabetes and arteriosclerosis and the diverse sequelae thereof.

    摘要翻译： 本发明提供对激素敏感性脂肪酶或内皮脂肪酶具有抑制作用的化合物。 本发明的化合物是通式I的偶氮吡啶-2-酮衍生物，其中取代基如本文所定义。 其中R2是氢的式I化合物的特征在于对脂质代谢紊乱的有利影响。 它们有利地影响HDL与LDL的比例，特别是HDL水平的升高，适用于预防和治疗血脂异常和代谢综合征及其各种后遗症如动脉粥样硬化，冠心病，心力衰竭，肥胖和糖尿病。 其中R1和R2一起形成环系的式I化合物的特征在于对代谢紊乱的有利影响。 它们有利地影响脂质和糖代谢; 特别是它们降低甘油三酯水平，并且适合于预防和治疗II型糖尿病和动脉硬化及其各种后遗症。