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    • 8. 发明授权
    • Indole and indoline derivatives as 5HT.sub.1D receptor antagonists
    • 吲哚和二氢吲哚衍生物作为5HT1D受体拮抗剂
    • US5696122A
    • 1997-12-09
    • US605022
    • 1996-02-26
    • Laramie Mary GasterDavid Malcolm DuckworthSarah Margaret JenkinsPaul Adrian Wyman
    • Laramie Mary GasterDavid Malcolm DuckworthSarah Margaret JenkinsPaul Adrian Wyman
    • A61K31/495A61K31/496A61P1/00A61P9/08A61P9/12A61P25/00A61P25/24A61P25/26A61P43/00C07D209/08C07D401/10C07D409/06C07D413/10C07D403/10C07D403/14C07D413/14
    • C07D401/10C07D209/08C07D409/06C07D413/10
    • The 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: ##STR1## in which R is a group of formula (i): ##STR2## in which P.sup.1 is a phenyl or a 5 to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur; and R.sup.1 and R.sup.2 are independently hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyC.sub.1-6 alkyl, acyl, nitro, trifluoromethyl, cyano, SR.sup.5, SOR.sup.5, SO.sub.2 R.sup.5, SO.sub.2 NR.sup.5 R.sup.6, CO.sub.2 R.sup.5, CONR.sup.5 R.sup.6, CONR.sup.5 (CH.sub.2).sub.x CO.sub.2 R.sup.6, NR.sup.5 R.sup.6, NR.sup.5 CO.sub.2 R.sup.6, CR.sup.5 =NOR.sup.6, where R.sup.5 and R.sup.6 are independently hydrogen or C.sub.1-6 alkyl and x is 1 to 3; or R is a group of formula (ii): ##STR3## in which P.sup.2 is phenyl or biphenyl; P.sub.3 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 (CH.sub.2).sub.p --R.sup.8 --(CH.sub.2).sub.q where R.sup.8 is oxygen, S(O).sub.m where m is 0 to 2, carbonyl, CO.sub.2 or CH.sub.2 and p and q are independently 0 to 3; and R.sup.1 and R.sup.2 are as defined above in formula (i); R.sup.3 is hydrogen, halogen, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;n is 1 or 2; R.sup.4 is hydrogen or C.sub.1-6 alkyl; and B is --CHR.sup.9 CHR.sup.10 -- or --CR.sup.9 .dbd.CR.sup.10 -- where R.sup.9 and R.sup.10 are independently hydrogen or C.sub.1-6 alkyl. C.sub.1-6 alkyl groups, whether alone or as part of another group, may be straight chain or branched. The groups P.sub.1, P.sub.2, and P.sub.3 can be aromatic or saturated heterocyclic rings.
    • PCT No.PCT / EP94 / 02663 371日期1996年2月26日 102(e)日期1996年2月26日PCT 1994年8月9日PCT公布。 公开号WO95 / 06637 日期1995年3月9日本发明提供了下述式(I)的新型吲哚和二氢吲哚衍生物,其制备方法,含有它们的药物组合物及其作为药物的用途。 本发明的吲哚和二氢吲哚衍生物是式(I)化合物或其盐:其中R是式(i)的基团:其中P1是苯基或 含有1至3个选自氧,氮或硫的杂原子的5至7元杂环; 酰基,硝基,三氟甲基,氰基,SR5,SOR5,SO2R5,SO2NR5R6,CO2R5,CONR5R6,CONR5(CH2)xCO2R6,NR5R6, NR5CO2R6,CR5 = NOR6,其中R5和R6独立地为氢或C1-6烷基,x为1至3; 或R为式(ⅱ)的基团:其中P2为苯基或联苯基;(ⅱ) P3是苯基或含有1至3个选自氧,氮或硫的杂原子的5至7元杂环; A是键或基团(CH 2)p -R 8 - (CH 2)q,其中R 8是氧,S(O)m,其中m是0至2,羰基,CO 2或CH 2,p和q独立地是0至3; 并且R 1和R 2如上述式(ⅰ)中所定义; R3是氢,卤素,羟基,C1-6烷基或C1-6烷氧基; n为1或2; R4是氢或C1-6烷基; 且B为-CHR 9 CHR 10 - 或-CR 9 = CR 10 - 其中R 9和R 10独立地为氢或C 1-6烷基。 不管是单独还是作为另一基团的一部分,C 1-6烷基可以是直链或支链的。 基团P1,P2和P3可以是芳族或饱和的杂环。