发明名称 Indole and indoline derivatives as 5HT1D receptor antagonists
摘要 PCT No. PCT/EP94/02663 Sec. 371 Date Feb. 26, 1996 Sec. 102(e) Date Feb. 26, 1996 PCT Filed Aug. 9, 1994 PCT Pub. No. WO95/06637 PCT Pub. Date Mar. 9, 1995The present invention provides novel indole and indoline derivatives according to formula (I) below, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments. The present indole and indoline derivatives are compounds of formula (I) or a salt thereof: <IMAGE> (I) in which R is a group of formula (i): <IMAGE> (i) in which P1 is a phenyl or a 5 to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur; and R1 and R2 are independently hydrogen, halogen, C1-6alkyl, C1-6alkoxy, hydroxyC1-6alkyl, acyl, nitro, trifluoromethyl, cyano, SR5, SOR5, SO2R5, SO2NR5R6, CO2R5, CONR5R6, CONR5(CH2)xCO2R6, NR5R6, NR5CO2R6, CR5=NOR6, where R5 and R6 are independently hydrogen or C1-6alkyl and x is 1 to 3; or R is a group of formula (ii): <IMAGE> (ii) in which P2 is phenyl or biphenyl; P3 is phenyl or a 5 to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur; A is a bond or a group (CH2)p-R8-(CH2)q where R8 is oxygen, S(O)m where m is 0 to 2, carbonyl, CO2 or CH2 and p and q are independently 0 to 3; and R1 and R2 are as defined above in formula (i); R3 is hydrogen, halogen, hydroxy, C1-6alkyl or C1-6alkoxy; n is 1 or 2; R4 is hydrogen or C1-6alkyl; and B is -CHR9CHR10- or -CR9=CR10- where R9 and R10 are independently hydrogen or C1-6alkyl. C1-6alkyl groups, whether alone or as part of another group, may be straight chain or branched. The groups P1, P2, and P3 can be aromatic or saturated heterocyclic rings.
申请公布号 US5696122(A) 申请公布日期 1997.12.09
申请号 US19960605022 申请日期 1996.02.26
申请人 SMITHKLINE BEECHAM P.L.C. 发明人 GASTER, LARAMIE MARY;DUCKWORTH, DAVID MALCOLM;JENKINS, SARAH MARGARET;WYMAN, PAUL ADRIAN
分类号 A61K31/495;A61K31/496;A61P1/00;A61P9/08;A61P9/12;A61P25/00;A61P25/24;A61P25/26;A61P43/00;C07D209/08;C07D401/10;C07D409/06;C07D413/10;(IPC1-7):A61K31/495;C07D403/10;C07D403/14;C07D413/14 主分类号 A61K31/495
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