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    Biphenyl(thio)amide and bipennylethan(thi) one derivatives, their preparation and their use as 5-HT.sub.1D receptor antagonists
    3.
    发明授权
    Biphenyl(thio)amide and bipennylethan(thi) one derivatives, their preparation and their use as 5-HT.sub.1D receptor antagonists 失效

    公开(公告)号：US5972935A

    公开(公告)日：1999-10-26

    申请号：US11338

    申请日：1998-04-24

    申请人： Laramie Mary Gaster

    发明人： Laramie Mary Gaster

    IPC分类号： C07D491/048 ,  A61K31/00 ,  A61K31/47 ,  A61K31/4738 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5383 ,  A61P1/00 ,  A61P3/00 ,  A61P3/04 ,  A61P9/00 ,  A61P9/12 ,  A61P15/00 ,  A61P15/10 ,  A61P25/14 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D491/04 ,  C07D491/052 ,  C07D498/04 ,  A61K31/44 ,  C07D413/00 ,  C07D491/00

    CPC分类号： C07D491/04

    摘要： The invention relates to novel heterocyclic compounds of formula (I) or a salt or N-oxide thereof, in which R is a group of formulae (i), (ii) or (iii), where R.sup.1 is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, COC.sub.1-6 akyl, C.sub.1-6 alkoxy, hydroxy, hydroxyC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkoxy, C.sub.1-6 alkoxyC.sub.1-6 alkoxy, acyle, nitro, trifluoromethyl, cyano, SR.sup.9, SOR.sup.9, SO.sub.2 R.sup.9, NR.sup.9 CONR.sup.10 R.sup.11, NR.sup.10 SO.sub.2 R.sup.11, SO.sub.2 NR.sup.11 r.sup.11, SO.sub.2 NR.sup.10 R.sup.11, CO.sub.2 R.sup.10, CONR.sup.10 R.sup.11, CO.sub.2 NR.sup.10 R.sup.11, CONR.sup.10 (CH.sub.2).sub.a CO.sub.2 R.sup.11, (CH.sub.2).sub.a NR.sup.10 R.sup.11, ##STR1## (CH.sub.2).sub.a CONR.sup.10 R.sup.11, (CH.sub.2).sub.a COR.sup.11, (CH.sub.2).sub.a CO.sub.2 C.sub.1-6 alkyl, CO.sub.2 (CH.sub.2).sub.a OR.sup.10, NR.sup.10 R.sup.11, N.dbd.CNR.sup.9 NR.sup.10 R.sup.11, NR.sup.10 CO(CH.sub.2).sub.a NR.sup.10 R.sup.11, NR.sup.10 CO.sub.2 R.sup.11, CONHNR.sup.10 R.sup.11, CR.sup.10 .dbd.NOR.sup.11, CNR.sup.10 .dbd.NOR.sup.11, where R.sup.9, R.sup.10 and R.sup.11 are independently hydrogen or C.sub.1-6 alkyl and a is 1 to 4; or R.sup.1 is a group --X--R.sup.12 where R.sup.12 is an optionally substituted 5- to 7-membered heterocyclic ring containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulphur and X is a bond, O, S, CH.sub.2, C.dbd.O, NR.sup.13 CO or NR.sup.13 where R.sup.13 is hydrogen or C.sub.1-6 alkyl; R.sup.4 and R.sup.5 are independently hydrogen, halogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkenyl, C.sub.1-6 alkoxy, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkylOC.sub.1-6 alkyl, acyl, aryl, acyloxy, hydroxy, nitro, trifluoromethyl, cyano, CO.sub.2 R.sup.10, CONR.sup.10 R.sup.11, NR.sup.10 R.sup.11 where R.sup.10 and R.sup.11 are independently hydrogen or C.sub.1-6 alkyl, or R.sup.4 and R.sup.5 together form a group --CH.sub.2).sub.r --R.sup.14 --(CH.sub.2).sub.s -- where R.sup.14 is O, S, CH.sub.2 or NR.sup.15 where R.sup.15 is hydrogen or C.sub.1-6 alkyl and r and s are independently 0, 1 or 2; R.sup.2 is hydrogen, C.sub.1-6 alkyl, optionally substituted aryl or optionally substituted heteroaryl; R.sup.3 is hydrogen or C.sub.1-6 alkyl or together with R.sup.8 forms a group (CH.sub.2).sub.q where q is 2, 3 or 4; Z is oxygen or sulphur, p is 1 or 2; P is an optionally substituted bicyclic ring optionally containing one to four heteroatoms; or P is an optionally substituted 5- to 7-membered saturated or partially saturated ring optionally containing one to three heteroatoms; and B is oxygen or sulphur, D is nitrogen, carbon or a CH group; R.sup.6 is hydrogen or C.sub.1-6 alkyl and R.sup.7 is C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen, or R.sup.6 together with R.sup.7 forms a group --A-- where A is (CR.sup.16 R.sup.17).sub.t where t is 1, 2 or 3 and R.sup.16 and R.sup.17 are independently hydrogen or C.sub.1-6 alkyl or A is (CR.sup.16 R.sup.17).sub.u --J where u is 0, 1, or 2 and J is oxygen, sulphur, CR.sup.16 .dbd.C.sup.17, CR.sup.16 .dbd.N, CR.sup.16 NR.sup.17 or N.dbd.N; R.sup.18 and R.sup.19 are independently hydrogen or C.sub.1-6 alkyl; R.sup.20 and R.sup.21 are independently hydrogen, C.sub.1-6 alkyl, 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 Q is an optionally substituted 5- to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur, processes for their preparation, and their use as 5-HT.sub.1D receptor antagonists.

    Piperidine derivatives as 5-HT.sub.4 receptor antagonists
    4.
    发明授权
    Piperidine derivatives as 5-HT.sub.4 receptor antagonists 失效
    哌啶衍生物作为5-HT 4受体拮抗剂

    公开(公告)号：US5705498A

    公开(公告)日：1998-01-06

    申请号：US433369

    申请日：1995-05-04

    申请人： Laramie Mary Gaster ,  Paul Adrian Wyman

    发明人： Laramie Mary Gaster ,  Paul Adrian Wyman

    IPC分类号： A61K31/443 ,  A61K31/445 ,  A61K31/535 ,  A61P43/00 ,  C07D405/12 ,  C07D405/14 ,  C07D498/04 ,  C07D513/04 ,  C07D213/80 ,  A61K31/395 ,  C07D401/12

    CPC分类号： C07D405/12 ,  C07D405/14

    摘要： Compounds of formula (I): ##STR1## wherein X.sup.g is O, S, SO, SO.sub.2, CH.sub.2, CH, N or NR wherein R is hydrogen or C.sub.1-6 alkyl; A is a saturated or unsaturated polymethylene chain of 2-4 carbon atoms; R.sub.1.sup.g and R.sub.2.sup.g are hydrogen or C.sub.1-6 alkyl; R.sub.3.sup.g is hydrogen, halo, C.sub.1-6 alkyl, amino, nitro or C.sub.1-6 alkoxy; R.sub.4.sup.g is hydrogen, halo, C.sub.1-6 alkyl or C.sub.1-6 alkoxy, Y is O or NH, or CO--Y together are a heterocyclic bioisostere; Z is of sub-formula: ##STR2## wherein --(CH.sub.2).sub.n.sup.1 is attached at carbon; and n.sup.1 is 0, 1, 2, 3 or 4; q is 0, 1, 2 or 3; R.sub.a is a straight or branched chain alkylene of chain length 1-6 carbon atoms terminally substituted by R.sub.7 wherein R.sub.7 is 3 to 8 membered heterocyclyl, 5 or 6 membered monocyclic heteroaryl or 9 or 10 membered fused bicyclic heteroaryl linked through carbon, or R.sub.7 is C.sub.2-7 alkoxycarbonyl or secondary or tertiary hydroxy substituted C.sub.1-6 alkyl; and R.sub.6 is hydrogen or C.sub.1-6 alkyl; are useful as 5HT.sub.4 receptor antagonists.

    摘要翻译： PCT No.PCT / EP93 / 03054 Sec。 371日期：1995年5月4日 102（e）日期1995年5月4日PCT提交1993年11月2日PCT公布。 公开号WO94 / 10174 （I）化合物：其中Xg为O，S，SO，SO 2，CH 2，CH，N或NR，其中R为氢或C 1-6烷基; A是2-4个碳原子的饱和或不饱和多亚甲基链; R1g和R2g是氢或C1-6烷基; R3g是氢，卤素，C1-6烷基，氨基，硝基或C1-6烷氧基; R4g是氢，卤素，C1-6烷基或C1-6烷氧基，Y是O或NH，或CO-Y一起是杂环生物电子等排体; Z为子式：其中 - （CH 2）n1连接在碳上; n1为0,1,2,3或4; q为0,1,2或3; R a是被R 7末端取代的链长1-6个碳原子的直链或支链亚烷基，其中R 7是3-8元杂环基，5或6元单环杂芳基或通过碳连接的9或10元稠合双环杂芳基，或者R 7是 C 2-7烷氧基羰基或仲或叔羟基取代的C 1-6烷基; R6为氢或C1-6烷基; 可用作5HT4受体拮抗剂。

    Indole and indoline derivatives as 5HT.sub.1D receptor antagonists
    5.
    发明授权
    Indole and indoline derivatives as 5HT.sub.1D receptor antagonists 失效
    吲哚和二氢吲哚衍生物作为5HT1D受体拮抗剂

    公开(公告)号：US5696122A

    公开(公告)日：1997-12-09

    申请号：US605022

    申请日：1996-02-26

    申请人： Laramie Mary Gaster ,  David Malcolm Duckworth ,  Sarah Margaret Jenkins ,  Paul Adrian Wyman

    发明人： Laramie Mary Gaster ,  David Malcolm Duckworth ,  Sarah Margaret Jenkins ,  Paul Adrian Wyman

    IPC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 ,  C07D403/10 ,  C07D403/14 ,  C07D413/14

    CPC分类号： C07D401/10 ,  C07D209/08 ,  C07D409/06 ,  C07D413/10

    摘要： 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.

    摘要翻译： 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。