发明名称 SUBSTITUTED TETRAHYDROISOQUINOLINE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS
摘要 Compounds of formula (I), wherein R1 represents a substituent selected from a hydrogen or halogen atom; a hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, trifluoromethanesulfonyloxy, pentafluoroethyl, C1-4alkyl, C14alkoxy, arylC1-4alkoxy, C1-4alkylthio, C1-4alkoxyC1-4alkyl, C3-6cycloalkylC1-4alkoxy, C1-4alkanoyl, C1-4alkoxycarbonyl, C1-4alkylsulphonyl, C14alkylsulphonyloxy, C1-4alkylsulphonylC1-4alkyl, arylsulphonyl, arylsulphonyloxy, arylsulphonylC1-4alkyl, C1-4alkylsulphonamido, C14alkylamido, C1-4alkylsulphonamidoC1-4alkyl, C1-4alkylamidoC1-4alkyl, arylsulphonamido, arylcarboxamido, arylsulphonamidoC1-4alkyl, arylcarboxamidoC1-4alkyl, aroyl, aroylC1-4alkyl, or arylC1-4alkanoyl group; a group R3OCO(CH2)p, R3CON(R4)(CH2)p, R3R4NCO(CH2)p or R3R4NSO2(CH2)p where each of R3 and R4 independently represents a hydrogen atom or a C1-4alkyl group or R3R4 forms part of a C3-6 azacycloalkane or C3-6(2-oxo)azacycloalkane ring and p represents zero or an integer from 1 to 4; or a group Ar1Z, wherein Ar1 represents an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring and z represents a bond, O, S, or CH2; R2 represents a hydrogen atom or a C1-4alkyl group; q is 1 or 2; Ar represents an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring; or an optionally substituted bicyclic ring system; and salts thereof. Compounds of formula (I) and their salts have affinity for dopamine receptors, in particular the D3 receptor, and thus potential in the treatment of conditions wherein modulation of the D3 receptor is beneficial, e.g. as antipsychotic agents.
申请公布号 CA2288308(A1) 申请公布日期 1998.11.05
申请号 CA19982288308 申请日期 1998.04.27
申请人 SMITHKLINE BEECHAM P.L.C. 发明人 BRANCH, CLIVE LESLIE;STEMP, GEOFFREY
分类号 A61K31/4725;A61P25/18;A61P43/00;C07D217/04;C07D401/12;C07D409/12;(IPC1-7):C07D217/04;A61K31/47 主分类号 A61K31/4725
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