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    • 8. 发明授权
    • Phthalazine-containing antidiabetic compounds
    • 含有酞嗪的抗糖尿病化合物
    • US08575166B2
    • 2013-11-05
    • US13146457
    • 2010-02-04
    • Jason L. DavisMichael John MayerHubert B. Josien
    • Jason L. DavisMichael John MayerHubert B. Josien
    • A61K31/50A61K31/501C07D237/30
    • C07D417/12C07D417/14C07D487/04
    • This invention provides for certain phthalazine-containing compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein G is an optionally substituted N—N containing heteroaryl group and the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
    • 本发明提供了式(I)的某些含酞嗪化合物或其药学上可接受的盐,酯或溶剂化物,其中G是任选取代的含N-N杂芳基并且变量在本文中定义; 本发明化合物是G蛋白偶联受体40(GPR40,也称为游离脂肪酸受体FFAR)的激动剂。 本发明还涉及含有这些化合物的药物组合物,以及这些化合物在哺乳动物体内调节胰岛素水平的用途。 该化合物可用于例如预防和治疗2型糖尿病以及预防和治疗与2型糖尿病相关的病症,例如胰岛素抵抗,肥胖症和脂质疾病。