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    • 32. 发明申请
    • ANTI-ATHEROSCLEROTIC ARYL COMPOUNDS
    • 抗甲状腺素ARYL化合物
    • WO1992006075A1
    • 1992-04-16
    • PCT/GB1991001646
    • 1991-09-25
    • THE WELLCOME FOUNDATION LIMITEDFRANZMANN, Karl, Witold
    • THE WELLCOME FOUNDATION LIMITED
    • C07C275/34
    • C07D333/28C07C45/71C07C47/575C07C217/58C07C275/30C07C275/34C07D317/22Y10S514/824
    • The present invention is concerned with compounds of formula (I) wherein Ar is a mono- or bicyclic aromatic group optionally containing one or two heteroatoms independently selected from nitrogen, oxygen and sulphur, said group being optionally substituted by one or more atoms or groups independently selected from halogen, nitro, amino, -NRR where R and R are independently selected from hydrogen, C1-8 alkyl and C1-8 alkanoyl, cyano, carboxyalkoxy, alkoxycarbonylalkoxy, C1-8 alkyl (including cycloalkyl and cycloalkylalkyl), C1-8 alkoxy (including cycloalkoxy and cycloalkylalkoxy), C1-8 thioalkyl, said alkyl, alkoxy and/or thioalkyl group(s) being optionally substituted by one or more halogen atoms, aryl, aryloxy, aralkyl and aralkyloxy, said aryl, aryloxy, aralkyl and/or aralkyloxy group(s) being optionally substituted by one or more atoms or groups independently selected from halogen, alkyl, alkoxy, alkanoyl, hydroxyalkyl, perfluoroalkyl, perfluoroalkoxy, carboxyalkoxy, alkoxycarbonylalkoxy, and C3-8 polyether groups containing from one to three oxygen atoms; D is -CH2-, -NH-, or -O-; E is ( alpha ) or ( beta ); F is -O- or ( psi ); G is C3-12 straight, branched, or cyclic alkyl, or aralkyl, said aralkyl group being optionally substituted by one or more atoms or groups independently selected from halogen, amino, N-(C1-6 alkyl)amino, N,N-di(C1-6 alkyl)amino, C1-6 alkyl and C1-6 alkoxy, or a C3-8 polyether group containing one to three oxygen atoms; J is a bond or C1-6 straight or branched alkylene; X is a C2-8 straight, branched, or cyclic alkylene group optionally substituted by one or more halogen atoms or C1-4 alkoxy groups, wherein one or two of the linear carbon atom(s) is/are replaced by oxygen; and Z is hydrogen, hydroxy, C1-4 alkyl, C2-5 alkanoyl, or carboxyl, said alkyl group being optionally substituted by one or more halogen atoms; and their physiologically functional derivatives, with processes for their preparation, with medicaments containing them and with their use as therapeutic agents, particularly in the prophylaxis and treatment of atherosclerosis.
    • 本发明涉及式(I)化合物,其中Ar是任选含有一个或两个独立地选自氮,氧和硫的杂原子的单环或双环芳基,所述基团任选被一个或多个独立地被一个或多个原子或基团取代 选自卤素,硝基,氨基,-NRR 1,其中R和R 1独立地选自氢,C 1-8烷基和C 1-8烷酰基,氰基,羧基烷氧基,烷氧基羰基烷氧基,C 1-8烷基(包括环烷基和 环烷基烷基),C 1-8烷氧基(包括环烷氧基和环烷基烷氧基),C1-8硫代烷基,所述烷基,烷氧基和/或硫代烷基任选被一个或多个卤素原子,芳基,芳氧基,芳烷基和芳烷氧基取代,所述 芳基,芳氧基,芳烷基和/或芳烷氧基任选被一个或多个独立地选自卤素,烷基,烷氧基,烷酰基,羟烷基,全氟烷基,全氟烷氧基,羧烷氧基,烷氧基 芳基烷氧基和含1-3个氧原子的C3-8聚醚基团; D是-CH 2 - , - NH-或-O-; E为(α)或(β); F为-O-或(psi); G为C3-12直链,支链或环状烷基或芳烷基,所述芳烷基任选被一个或多个独立选自卤素,氨基,N-(C 1-6烷基)氨基,N, 二(C 1-6烷基)氨基,C 1-6烷基和C 1-6烷氧基,或含有1-3个氧原子的C 3-8聚醚基团; J是键或C1-6直链或支链亚烷基; X是任选被一个或多个卤素原子或C 1-4烷氧基取代的C 2-8直链,支链或环状亚烷基,其中一个或两个直链碳原子被氧代替; Z为氢,羟基,C 1-4烷基,C 2-5烷酰基或羧基,所述烷基任选被一个或多个卤素原子取代; 及其生理功能衍生物,其制备方法,含有它们的药物和用作治疗剂,特别是用于预防和治疗动脉粥样硬化。