申请人:Hodge L. Kirvin
公开号:US20080015254A1
公开(公告)日:2008-01-17
Agents 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, 4, or 5; q is 0 or 1; t is 0 or 1; R
2
is alkyl having from 1 to 3 carbon atoms; R
3
is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; 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; and
R
1
is hydrogen or alkyl having 1 or 2 carbon atoms. Alternatively, when R
1
is hydrogen, the biologically active agent can be a pharmaceutically acceptable salt of the compound of Formula I.
本发明揭示了用于治疗各种代谢性疾病的药物,例如胰岛素抵抗综合征、糖尿病、高脂血症、脂肪肝病、消瘦、肥胖症、动脉硬化和动脉粥样硬化等。其中n为1或2;m为0、1、2、4或5;q为0或1;t为0或1;R2为具有1至3个碳原子的烷基;R3为氢、卤素、具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基;A为苯基,未取代或取代为1或2个选自:卤素、具有1或2个碳原子的烷基、全氟甲基、具有1或2个碳原子的烷氧基和全氟甲氧基的基团;或具有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;或具有1或2个选自N、S和O的环杂芳基,且所述杂芳环通过一个环碳原子与化合物的其余部分共价结合;以及R1为氢或具有1或2个碳原子的烷基。或者,当R1为氢时,化合物I的药物活性剂可以是其药学上可接受的盐。