发明名称 Substituerte tetracykliske azepinderivater som har affinitet for 5-HT2-reseptorer
摘要 This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. <IMAGE> (I) wherein: R1 and R2 each independently are hydrogen; C1-6alkyl; C1-6alkylcarbonyl; trihalomethylcarbonyl; C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3, R4, R5, R6, R9, R10, R11 or R12 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)-amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)-aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxy-carbonyl; R7 and R8 are each independently hydrogen, hydroxy, C1-6alkyl, C1-6alkyloxy or R7 and R8 taken together may form mono- or di(cyano)methylene, or together with the carbon atom to which they are attached form a carbonyl or a spiro substituent; or R7 and R8 taken together may form methylene; R13 is hydrogen, C1-6alkyl, or trifluoromethyl; R14 is hydrogen, C1-6alkyl, cyano, or trifluoromethyl; n is zero to 6. These compounds were tested as mCPP-antagonists in rats. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.
申请公布号 NO308035(B1) 申请公布日期 2000.07.10
申请号 NO19970002017 申请日期 1997.04.30
申请人 JANSSEN PHARMACEUTICA NV 发明人 SIPIDO, VICTOR KAREL;FERNSNDEZ-GADEA, FRANCISCO JAVIER;ANDRES-GIL, JOSE IGNACIO;MEERT, THEO FRANS;GIL-LOPETEGUI, PILAR
分类号 A61K31/535;A61K31/55;A61P9/00;A61P25/00;A61P25/18;A61P25/24;A61P25/26;C07D223/20;C07D223/30;C07D261/00;C07D498/04 主分类号 A61K31/535
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