Indole derivatives process for their preparation, pharmaceutical compositions containing them and their medicinal application
申请人:Vernalis Research Limited
公开号:US06706750B1
公开(公告)日:2004-03-16
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.
一种化学化合物的化学式(I),其中:R1和R2独立选择自氢和烷基;R3是烷基;R4、R6和R7独立选择自氢、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、烷基硫基、烷基亚砜基、烷基磺基、硝基、碳氰基、羰基烷氧基、羰基芳氧基和羧基;R5选择自氢、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、烷基硫基、烷基亚砜基、烷基磺基、硝基、碳氰基、羰基烷氧基、羰基芳氧基和羧基;A是一个5-或6-成员部分不饱和或芳香杂环环或一个5-或6-成员部分不饱和脂环环,如果A是一个6-成员部分不饱和脂环环,则R4至R7中至少一个不是氢,以及其在治疗中的使用,特别是作为5HT受体的激动剂或拮抗剂,特别是5HT2C受体,例如在治疗中枢神经系统疾病;中枢神经系统损伤;心血管疾病;胃肠疾病;尿崩症和睡眠呼吸暂停症,特别是用于肥胖症的治疗。