发明名称 Amide derivatives having 5HT1D-antagonist activity
摘要 PCT No. PCT/EP95/01890 Sec. 371 Date Nov. 21, 1996 Sec. 102(e) Date Nov. 21, 1996 PCT Filed May 16, 1995 PCT Pub. No. WO95/32967 PCT Pub. Date Dec. 7, 1995Compound of formula (1), processes for their preparation and their use as CNS agents are disclosed, in which A is CONR where R is hydrogen or C1-6alkyl; Q is an optionally substituted 5 to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur, R1 is hydrogen, halogen, C1-6alkyl, C3-6cycloalkyl, COC1-6-alkyl, C1-6alkoxy, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, acyl, nitro, trifluoromethyl, cyano, SR9, SOR9, SO2R9, SO2NR10R11, CO2R10, CONR10R11, CO2NR10R11, CONR10(CH2)aCO2R11, (CH2)aNR10R11, (CH2)aCONR10R11, (CH2)aNR10COR11, (CH2)aCO2C1-6alkyl, CO2(CH2)aOR10, NR10R11, NR10CO2l R11, NR10CONR10R11, CR10=NOR11, CNR10=NOR11, where R10 and R11 are independently hydrogen or C1-6alkyl and a is 1 to 4 or R1 is an optionally substituted 5 to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur, R2 and R3 are independently hydrogen, halogen, C1-6alkyl, C3-6cycloaallyl, C3-6cycloalkenyl, C1-6alkoxy, acyl, aryl, acyloxy, hydroxy, nitro, trifluoromethyl, cyano, CO2R10, CONR10R11, NR10R11 where R10 and R11 are as defined for R1; R4 and R5 are independently hydrogen or C1-6alkyl; R6 is halogen, hydroxy, C1-6alkyl or C1-6alkoxy; R7 and R8 are independently hydrogen, C1-6alkyl, aralkyl, or together with the nitrogen atom to which they are attached form an optionally substituted 5 to 7-membered heterocyclic ring containing one or two heteroatoms selected from oxygen, nitrogen or sulphur, m is 0 to 4; and n is 0, 1 or 2.
申请公布号 US5756496(A) 申请公布日期 1998.05.26
申请号 US19960737660 申请日期 1996.11.21
申请人 SMITHKLINE BEECHAM P.L.C. 发明人 HAM, PETER;GASTER, LARAMIE MARY;KING, DAVID FRANCIS;DUCKWORTH, DAVID MALCOLM
分类号 A61K31/40;A61K31/41;A61K31/535;A61K31/55;A61P25/00;A61P25/20;A61P25/26;A61P25/28;A61P43/00;C07D249/12;C07D413/12;(IPC1-7):C07D413/12 主分类号 A61K31/40
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