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1. 发明授权

US5807855A 1-piperazino-1,2-dihydroindene derivatives 失效
标题翻译： 1-哌嗪基-1,2-二氢茚衍生物
公开(公告)号：US5807855A
公开(公告)日：1998-09-15
申请号：US331213
申请日：1994-10-28
申请人： Klaus B.o slashed.ges.o slashed. , Peter Bregnedal
发明人： Klaus B.o slashed.ges.o slashed. , Peter Bregnedal
IPC分类号： C07D241/04 , A61K31/495 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , C07D241/38 , C07D295/02 , C07D295/033 , C07D295/073 , C07D333/20 , C07D471/04 , C07D487/04 , C07D409/08
CPC分类号： C07D241/38 , C07D295/033 , C07D295/073 , C07D333/20 , C07D471/04
摘要： Trans isomers of 1-piperazino-1,2-dihydroindene compounds having formula (I), ##STR1## wherein X and Y are hydrogen, halogen, trifluoromethyl, alkyl, alkylthio, trifluoromethylthio, alkoxy, hydroxy, alkylsulfonyl, amino, alkylamino, nitro or cyano; Ar is a phenyl, thienyl or furyl group, each optionally substituted; R.sub.1 is hydrogen, or optionally hydroxy substituted alkyl, alkenyl, cycloalkyl or cycloalkylalkyl; R.sub.2 is alkyl, alkenyl, cycloalkyl, or cycloalkylalkyl; or R.sub.1 and R.sub.2 together form a 5 to 7-membered heterocyclic ring fused with the piperazine ring, which ring may be substituted with hydroxy; R.sub.3 is hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkylalkyl; or R.sub.2 and R.sub.3 together form a 3 to 7-membered carbocyclic ring which is spiro-fused to the piperazine ring; and R.sub.4 is hydrogen or alkyl. The compounds of the invention have potent antagonist action on dopamine D.sub.1 receptors and are useful in the treatment of diseases of the central nervous system, such as psychoses, schizophrenia (positive as well as negative symptoms), anxiety, depression, sleep disturbances, migraine, Parkinson's disease or cocaine abuse.
摘要翻译：具有式（I）的1-哌嗪基-1,2-二氢茚化合物的反式异构体，其中X和Y是氢，卤素，三氟甲基，烷基，烷硫基，三氟甲硫基，烷氧基，羟基，烷基磺酰基，氨基，烷基氨基，硝基或氰基; Ar是苯基，噻吩基或呋喃基，各自任选被取代; R 1是氢或任选的羟基取代的烷基，烯基，环烷基或环烷基烷基; R2是烷基，烯基，环烷基或环烷基烷基; 或者R 1和R 2一起形成与哌嗪稠合的5至7元杂环，该环可以被羟基取代; R3是氢，烷基，烯基，环烷基或环烷基烷基; 或者R 2和R 3一起形成与哌嗪环螺稠合的3至7元碳环; 和R4是氢或烷基。本发明的化合物对多巴胺D1受体具有有效的拮抗剂作用，可用于治疗中枢神经系统疾病，如精神病，精神分裂症（阳性和阴性症状），焦虑症，抑郁症，睡眠障碍，偏头痛，帕金森病或可卡因滥用。

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