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    • 7. 发明公开
    • COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
    • 用于治疗代谢性疾病的化合物
    • EP1656127A1
    • 2006-05-17
    • EP04781277.1
    • 2004-08-16
    • Wellstat Therapeutics Corporation
    • SHARMA, ShaliniVON BORSTEL, Reid, W.HODGE, Kirvin, L.
    • A61K31/19A61K31/235C07C323/00
    • C07C323/62
    • 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. Formula (I), wherein n is 1 or 2; m is 0 or 1; q is 0 or 1; t is 0 or 1; R5 is alkyl having from 1 to 3 carbon atoms; R9 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 mono­substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and 0 and the heteroaromatic ring is covalently bound to the remainder of the compound of formula I by a ring carbon; and X is -CH2-, Q is -OR1and R1 is methyl or ethyl; or X is -CH2CR12R13- or - CH2CH(NHAc)-wherein each of R12 and R13 is independently hydrogen or methyl, Q is OR1 and R1 is hydrogen or alkyl having from 1 to 7 carbon atoms; or X is -CH2CH2- and Q is NR10R1' wherein one of R10 and R11 is hydrogen, alkyl having from 1 to 3 carbon atoms or hydroxy, and the other is hydrogen. Alternatively, when R1 is hydrogen, the biologically active agent can be a pharmaceutically acceptable salt of the compound of Formula (I).
    • 公开了用于治疗各种代谢疾病如胰岛素抵抗综合征,糖尿病,高脂血症,脂肪肝疾病,恶病质,肥胖症,动脉粥样硬化和动脉硬化的药物。 式(I),其中n是1或2; m是0或1; q是0或1; t是0或1; R5是具有1至3个碳原子的烷基; R9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是未取代的或被1或2个选自以下的基团取代的苯基: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; 或具有3至6个环碳原子的环烷基,其中所述环烷基未被取代或者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的环杂原子的5或6元杂芳族环,并且所述杂芳族环通过环碳与式I化合物的其余部分共价结合; 且X是-CH 2 - ,Q是-OR 1且R 1是甲基或乙基; 或X为-CH 2 CR 12 R 13 - 或-CH 2 CH(NHAc) - 其中R 12和R 13各自独立地为氢或甲基,Q为OR 1且R 1为氢或具有1至7个碳原子的烷基; 或X是-CH 2 CH 2 - ,并且Q是NR 10 R 1',其中R 10和R 11之一是氢,具有1至3个碳原子的烷基或羟基,另一个是氢。 或者,当R 1为氢时,生物活性剂可以是式(I)化合物的药学上可接受的盐。