发明名称 1-piperazino-1,2-dihydroindene derivatives
摘要 Trans isomers of 1-piperazino-1,2-dihydroindene compounds having formula (I), <IMAGE> I 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; R1 is hydrogen, or optionally hydroxy substituted alkyl, alkenyl, cycloalkyl or cycloalkylalkyl; R2 is alkyl, alkenyl, cycloalkyl, or cycloalkylalkyl; or R1 and R2 together form a 5 to 7-membered heterocyclic ring fused with the piperazine ring, which ring may be substituted with hydroxy; R3 is hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkylalkyl; or R2 and R3 together form a 3 to 7-membered carbocyclic ring which is spiro-fused to the piperazine ring; and R4 is hydrogen or alkyl. The compounds of the invention have potent antagonist action on dopamine D1 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.
申请公布号 US5807855(A) 申请公布日期 1998.09.15
申请号 US19940331213 申请日期 1994.10.28
申请人 H. LUNDBECK A/S 发明人 BOGESO, KLAUS;BREGNEDAL, PETER
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;(IPC1-7):A61K31/495;C07D409/08 主分类号 C07D241/04
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