申请人:Wellstat Therapeutics Corporation
公开号:US08022249B2
公开(公告)日:2011-09-20
Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. wherein n is 1 or 2; m is 0, 1, 2, 3, 4 or 5; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; R3 is hydrogen or —(CH2)gOH wherein g is 0, 1 or 2; R4 is hydrogen, methyl or ethyl; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula I by a ring carbon; or a pharmaceutically acceptable salt of the compound.
本发明揭示了用于治疗各种代谢性疾病的化合物,例如胰岛素抵抗综合征、糖尿病、高脂血症、脂肪肝病、消瘦症、肥胖症、动脉粥样硬化和动脉硬化。其中n为1或2;m为0、1、2、3、4或5;q为0或1;t为0或1;R1为1至3个碳原子的烷基;R2为氢、卤素、1至3个碳原子的烷基或1至3个碳原子的烷氧基;R3为氢或—(CH2)gOH,其中g为0、1或2;R4为氢、甲基或乙基;A为苯基,未取代或取代为1或2个选自卤素、1或2个碳原子的烷基、全氟甲基、1或2个碳原子的烷氧基和全氟甲氧基的基团;或有3至6个环碳原子的环烷基,其中环烷基未取代或一个或两个环碳原子独立地被甲基或乙基单取代;或有1或2个选自N、S和O的环杂芳基,且该杂芳环通过一个环碳原子与公式I的余部共价结合;或该化合物的药学上可接受的盐。