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    • 71. 发明授权
    • Aryl-oxo-acetic acids useful in the treatment of insulin resistance and
hyperglycemia
    • 可用于治疗胰岛素抵抗和高血糖症的芳基 - 氧代 - 乙酸
    • US6110963A
    • 2000-08-29
    • US307918
    • 1999-05-10
    • Michael S. Malamas
    • Michael S. Malamas
    • C07C59/90C07D257/04C07D307/80C07D333/56C07D405/12C07D413/06C07D417/12A61K31/38A61K31/35A61K31/415C07D417/00
    • C07D257/04C07C59/90C07D307/80C07D333/56C07D405/12C07D413/06C07D417/12
    • This invention provides compounds of Formula I having the structure ##STR1## wherein A is C or N;B is O, S, N, or CH.dbd.CH;E is ##STR2## or --X--D; D is ##STR3## or alkyl of 1-12 carbon atoms; X is CO, CH(OH), CH.sub.2, or --CH--S-2-benzothiazole;Y is hydrogen, alkyl of 1-6 carbon atoms, or halogen;Z is O, S, or N;R is hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, or trifluoromethyl;R.sup.1 is alkyl of 1-12 carbon atoms, aryl of 6-10 carbon atoms, aralkyl of 7-15 carbon atoms, halogen, Het-alkyl wherein the alkyl moiety contains 1-6 carbon atoms, or aryl mono-, di- or tri-substituted with a substituent selected from the group consisting of halogen, alkyl of 1-6 carbon atoms, trifluoromethyl, and alkoxy of 1-6 carbon atoms;Het is ##STR4## G is O, S, or N; and the remaining variables are as defined in claim 1, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin or hyperglycemia.
    • 本发明提供具有其中A为C或N的结构的式I化合物; B是O,S,N或CH = CH; E为或-X-D; D是1-12个碳原子的烷基; X是CO,CH(OH),CH 2或-CH-S-2-苯并噻唑; Y为氢,1-6个碳原子的烷基或卤素; Z是O,S或N; R为氢,1-6个碳原子的烷基,1-6个碳原子的烷氧基,卤素或三氟甲基; R1为1-12个碳原子的烷基,6-10个碳原子的芳基,7-15个碳原子的芳烷基,卤素,其中烷基部分含有1-6个碳原子的Het-烷基,或芳基一,二或二 被选自卤素,1-6个碳原子的烷基,三氟甲基和1-6个碳原子的烷氧基的取代基取代三取代; Het是G是O,S或N; 并且其余变量如权利要求1所定义,或其药学上可接受的盐,其可用于治疗与胰岛素或高血糖相关的代谢紊乱。