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    • 1. 发明申请
    • COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
    • 用于治疗代谢性疾病的化合物
    • WO2004073611A2
    • 2004-09-02
    • PCT/US2004/003718
    • 2004-02-09
    • WELLSTAT THERAPEUTICS CORPORATIONHODGE, Kirvin, L.LEE, AlbertSHARMA, ShaliniVON BORSTEL, Reid, W.
    • HODGE, Kirvin, L.LEE, AlbertSHARMA, ShaliniVON BORSTEL, Reid, W.
    • A61K
    • C07C69/734A61K31/192A61K31/24C07C59/68C07C65/24C07C69/76C07C69/92
    • Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, artherosclerosis and arteriosclerosis are disclosed. Formula (I) 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 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 or 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 cycloaldyl having from 3 to 6 ring carbon atoms wherein the cycloaldyl is unsubstitited 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 compounds 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).
    • 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剂。 式(I)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; R 2是1至3个碳原子的烷基; R 3是氢,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个环碳原子的环戊烯基,其中所述环烯基未被取代或一个或两个环碳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元杂芳环,杂芳环通过环碳与其余的式(I)化合物共价结合; 和R 1是氢或具有1或2个碳原子的烷基。 或者,当R 1是氢时,生物活性剂可以是式(I)化合物的药学上可接受的盐。
    • 2. 发明申请
    • COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
    • 用于治疗代谢性疾病的化合物
    • WO2004093806A2
    • 2004-11-04
    • PCT/US2004/012142
    • 2004-04-20
    • WELLSTAT THERAPEUTICS CORPORATIONHODGE, Kirvin, L.KAUFMAN, Robert, J.LEE, AlbertSHARMA, ShaliniVON BORSTEL, Reid, W.
    • HODGE, Kirvin, L.KAUFMAN, Robert, J.LEE, AlbertSHARMA, ShaliniVON BORSTEL, Reid, W.
    • A61K
    • C07C69/734A61K31/235
    • 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 2 or 3; 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).
    • 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剂。 式(I)其中n为1或2; m为2或3; q为0或1; t为0或1; R 2是具有1至3个碳原子的烷基; R 3是氢,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: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取代的苯基; 或具有3至6个环碳原子的环烷基,其中环烷基是未取代的或一个或两个环碳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元杂芳环,杂芳环通过环碳与式I化合物的其余部分共价结合; 和R 1是氢或具有1或2个碳原子的烷基。 或者,当R 1是氢时,生物活性剂可以是式(I)化合物的药学上可接受的盐。