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Indole derivatives, process for their preparation, pharmaceutical compositions containing indole derivatives and their pharmaceutical applications

机译:吲哚衍生物,其制备方法,含有吲哚衍生物的药物组合物及其药物用途

摘要

A chemical compound of formula (I) wherein: R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4, R6 and R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsufoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; R5 is selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; A is a 5- or 6-membered partially unsaturated or aromatic heterocyclic ring or a 5- or 6-membered partially unsaturated carbocyclic ring, wherein if A is a 6-membered partially unsaturated carbocyclic ring then at least one of R4 to R7 is other than hydrogen, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof, and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinial disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.
机译:式(I)的化合物,其中:R 1和R 2独立地选自氢和烷基;和R3是烷基; R4,R6和R7独立地选自氢,卤素,羟基,烷基,芳基,氨基,烷基氨基,二烷基氨基,烷氧基,芳氧基,烷硫基,烷基亚磺酰基,烷基磺酰基,硝基,腈,碳烷氧基,碳芳芳氧基和羧基; R5选自氢,卤素,羟基,烷基,芳基,氨基,烷基氨基,二烷基氨基,烷氧基,芳氧基,烷硫基,烷基亚磺酰基,烷基磺酰基,硝基,甲腈,碳烷氧基,碳芳芳氧基和羧基; A是5或6元部分不饱和或芳族杂环或5或6元部分不饱和碳环,其中如果A是6元部分不饱和碳环,则R 4至R <7中的至少一个不同于氢及其药学上可接受的盐,加成化合物和前药,及其在治疗中的用途,特别是作为5HT受体,特别是5HT2C受体的激动剂或拮抗剂,例如在治疗中枢神经系统疾病中神经系统;损害中枢神经系统;心血管疾病;胃肠道疾病;尿崩症和睡眠呼吸暂停,特别是用于治疗肥胖症。

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