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bentsimidatsolonijohdannaisia 5 - ht1a and greater 5 ht2 than d2 activity antagonisteina

机译:Bentsimidatsolonijohdannaisia 5-ht1a和5 ht2比d2活动拮抗剂

摘要

Pharmacologically active benzimidazolone derivatives as 5-HT1A and 5-HT2 receptors, useful in the treatment of CNS disorders of formula: CHEM wherein R1 and R2 may be at the same time or not a hydrogen atom, halogen, trifluoromethyl, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 acyl, carboxyl, C1-6 alkoxy- carbonyl, hydroxy, nitro, amino optionally C1-4 alkyl N-mono or di-substituted, C1-6 acylamino, C1-6 alkoxycarbonylamino, carbamoyl optionally C1-4 alkyl N-mono or di-substituted, cyano, C1-6 alkylsulphinyl, C1-6 alkylsulphonyl, amino sulphonyl optionally C1-4 alkyl N-mono or di-substituted, C1-4 alkyl N-mono or di-substituted aminosulphonylamino, aminosulphonylamino; R3 is hydrogen, C1-6 alkyl, C2-6 alkenyl or C2-C6 alkynyl; A is -CO- or -CONH- or it is absent; B is a straight or branched, saturated or unsaturated C2-6 alkyl; m and n are both independently an integer from 1 to 3; R4 is an aryl, aralkyl, a heteroaryl or heteroaralkyl group, each group being optionally substituted by one or more substituents selected from halogen, trifluoromethyl, cyano, C1-3 alkoxy, C1-4 alkyland acid addition salts thereof. The process for the preparation of the compounds of formula I as well as pharmaceutical compositions containing them are also described.
机译:具有药理活性的苯并咪唑酮衍生物作为5-HT1A和5-HT2受体,可用于治疗下式的化学式:其中R1和R2可以同时或不同时为氢原子,卤素,三氟甲基,C1-6烷基,C 1-6烷氧基,C 1-6烷硫基,C 1-6酰基,羧基,C 1-6烷氧基-羰基,羟基,硝基,氨基(可选)C 1-4烷基N-单或双取代,C 1-6酰基氨基,C 1 -6烷氧基羰基氨基,氨基甲酰基任选地为C1-4烷基N-单或双取代的,氰基,C1-6烷基亚磺酰基,C1-6烷基磺酰基,氨基磺酰基,任选地为C1-4烷基N-单或双取代的,C1-4烷基N -单或二取代的氨基磺酰基氨基,氨基磺酰基氨基; R3是氢,C1-6烷基,C2-6链烯基或C2-C6炔基; A是-CO-或-CONH-或不存在; B是直链或支链的,饱和或不饱和的C2-6烷基; m和n均独立地为1至3的整数; R 4是芳基,芳烷基,杂芳基或杂芳烷基,每个基团任选地被一个或多个选自卤素,三氟甲基,氰基,C 1-3烷氧基,C 1-4烷基及其酸加成盐的取代基取代。还描述了制备式I化合物的方法以及包含它们的药物组合物。

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