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31 条记录 (耗时 0.035 秒)

    Morpholine derivatives and their use as therapeutic agents
    1.
    发明授权
    Morpholine derivatives and their use as therapeutic agents 失效
    吗啉衍生物及其作为治疗剂的用途

    公开(公告)号：US5719149A

    公开(公告)日：1998-02-17

    申请号：US793573

    申请日：1997-02-27

    申请人： Paul Finke ,  Timothy Harrison ,  Richard Thomas Lewis ,  Angus Murray MacLeod ,  Andrew Pate Owens

    发明人： Paul Finke ,  Timothy Harrison ,  Richard Thomas Lewis ,  Angus Murray MacLeod ,  Andrew Pate Owens

    IPC分类号： A61K31/535 ,  A61K31/5375 ,  A61P1/08 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D265/32 ,  C07D413/06

    CPC分类号： C07D413/06 ,  C07D265/32

    摘要： The present invention relates to compounds of formula (I) wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are selected from a variety of suitable aromatic substituents; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, or C.sub.2 -alkyl substituted by C.sub.1-4 alkoxy or hydroxy; R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, C.sub.2-4 alkyl substituted by C.sub.1-4 alkoxy or hydroxy, or the group C(.dbd.NR.sup.c)NR.sup.a R.sup.b ; or R.sup.6 and R.sup.7, together with the nitrogen atom to which they are attached, form an optionally substituted saturated heterocyclic ring of 4 to 7 ring atoms which may optionally contain in the ring one oxygen or sulphur atom or a group selected from NR.sup.8, S(O) or S(O).sub.2 ; or R.sup.6 and R.sup.7, together with the nitrogen atom to which they are attached, form a piperidino ring substituted by a spiro-fused indene or indoline group, each of which may be unsubstituted or substituted; R.sup.8 is hydrogen, C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl or C.sub.1-4 alkoxyC.sub.1-4 alkyl; R.sup.9a and R.sup.9b are each independently hydrogen or C.sub.1-4 alkyl, or R.sup.9a and R.sup.9b are joined so, together with the carbon atoms to which they are attached, there is formed a C.sub.5-7 ring; X is selected from --CH.sub.2 CH.sub.2 --, --COCH.sub.2 -- or --CH.sub.2 CO--; and Y is hydrogen, or C.sub.1-4 alkyl optionally substituted by a hydroxyl group; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia. ##STR1##

    摘要翻译： PCT No.PCT / GB95 / 02039 Sec。 371日期1997年2月27日 102（e）1997年2月27日PCT PCT 1995年8月30日PCT公布。 公开号WO96 / 07649 日期：1996年3月14日本发明涉及式（I）化合物，其中：R 1，R 2，R 3，R 4和R 5选自多种合适的芳族取代基; R 6是氢，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基或被C 1-4烷氧基或羟基取代的C 2-烷基; R 7是氢，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基，被C 1-4烷氧基或羟基取代的C 2-4烷基或基团C（= NR c）NR a R b; 或R6和R7与它们所连接的氮原子一起形成任选取代的4至7个环原子的饱和杂环，其可以任选地在环中含有一个氧或硫原子或选自NR8，S（ O）或S（O）2; 或R6和R7与它们所连接的氮原子一起形成被螺稠合的茚或二氢吲哚基团取代的哌啶子基环，它们各自可以是未取代的或取代的; R 8是氢，C 1-4烷基，羟基C 1-4烷基或C 1-4烷氧基C 1-4烷基; R9a和R9b各自独立地为氢或C1-4烷基，或者R9a和R9b与它们所连接的碳原子一起连接形成C5-7环; X选自-CH 2 CH 2 - ， - COCH 2 - 或-CH 2 CO-; Y为氢或任选被羟基取代的C 1-4烷基; 或其药学上可接受的盐。 该化合物特别用于治疗或预防疼痛，炎症，偏头痛，呕吐和带状疱疹后神经痛。 （一）

    Ethane-1-2-diamine derivatives and tachykinin antagonists
    6.
    发明授权
    Ethane-1-2-diamine derivatives and tachykinin antagonists 失效
    乙烷-1,2-二胺衍生物和速激肽拮抗剂

    公开(公告)号：US5922744A

    公开(公告)日：1999-07-13

    申请号：US6028

    申请日：1998-01-12

    申请人： Timothy Harrison ,  Andrew Pate Owens

    发明人： Timothy Harrison ,  Andrew Pate Owens

    IPC分类号： C07D257/04 ,  A01N43/78

    CPC分类号： C07D257/04

    摘要： The present invention provides a compound of formula: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6a and R.sup.6b are defined herein or a pharmaceutically acceptable salt thereof, a process for its preparation, intermediates and its use as a tachykinin antagonist.

    摘要翻译： 本发明提供下式的化合物：其中R，R 1，R 2，R 3，R 4，R 5，R 6a和R 6b在本文中定义或其药学上可接受的盐，其制备方法，中间体及其作为速激肽拮抗剂的用途。

    Morpholine derivatives and their use as therapeutic agents
    7.
    发明授权
    Morpholine derivatives and their use as therapeutic agents 失效
    吗啉衍生物及其作为治疗剂的用途

    公开(公告)号：US5824678A

    公开(公告)日：1998-10-20

    申请号：US793186

    申请日：1997-02-13

    申请人： Timothy Harrison ,  Andrew Pate Owens ,  Christopher John Swain

    发明人： Timothy Harrison ,  Andrew Pate Owens ,  Christopher John Swain

    IPC分类号： A61K31/5375 ,  A61K31/5377 ,  A61P1/08 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P43/00 ,  C07D265/32 ,  C07D413/06 ,  C07D487/08 ,  C07F7/18 ,  A61K31/535

    CPC分类号： C07D413/06 ,  C07D265/32 ,  C07D487/08 ,  C07F7/1856

    摘要： The present invention relates to compounds of formula (I) ##STR1## wherein X is --NR.sup.6 R.sup.7 or C-- or N-linked imidazolyl; Y is hydrogen or C.sub.1-4 alkyl optionally substituted by hydroxy; R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are selected from a variety of suitable aromatic substituents; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, or C.sub.2-4 alkyl substituted by C.sub.1-4 alkoxy or hydroxy; R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, phenyl, or C.sub.2-4 alkyl substituted by one or two of C.sub.1-4 alkoxy, hydroxy or a 4, 5 or 6 membered heteroaliphatic ring containing one or two heteroatoms selected from N, O and S; or NR.sup.6 R.sup.7 is a saturated or partially saturated heterocyclic ring of 4 to 7 ring atoms, optionally containing one of O, S, NR.sup.8, S(O) or S(O).sub.2 and optionally substituted by one or two of hydroxy.sub.1-4 alkyl, C.sub.1-4 alkoxy C.sub.1-4 alkyl, oxo, COR.sup.a or CO.sub.2 R.sup.a ; or NR.sup.6 R.sup.7 forms a non-aromatic azabicyclic ring system of 6 to 12 ring atoms; and R.sup.9a and R.sup.9b are each independently hydrogen or C.sub.1-4 alkyl, or R.sup.9a and R.sup.9b are joined so, together with the carbon atoms to which they are attached, there is formed a C.sub.5-7 ring; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.

    摘要翻译： PCT No.PCT / GB95 / 01868 Sec。 371日期1997年2月13日 102（e）日期1997年2月13日PCT提交1995年8月7日PCT公布。 公开号WO96 / 05181 日期：1996年2月22日本发明涉及式（I）化合物：其中X为-NR6R7或C-或N-连接的咪唑基; Y是氢或任选被羟基取代的C 1-4烷基; R1，R2，R3，R4和R5选自多种合适的芳族取代基; R 6是氢，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基或被C 1-4烷氧基或羟基取代的C 2-4烷基; R 7是氢，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基或被一个或两个C 1-4烷氧基，羟基或含有一个或两个的4或5元或6元杂脂肪族环取代的C 2-4烷基 选自N，O和S的杂原子; 或NR6R7是4至7个环原子的饱和或部分饱和的杂环，任选地含有O，S，NR 8，S（O）或S（O）2之一并且任选地被一个或两个羟基-4-烷基，C 1 -4-烷氧基C 1-4烷基，氧代，CORa或CO 2 R a; 或NR 6 R 7形成6-12个环原子的非芳族氮杂双环系统; 并且R9a和R9b各自独立地为氢或C1-4烷基，或者R9a和R9b与它们所连接的碳原子一起连接形成C5-7环; 或其药学上可接受的盐。 该化合物特别用于治疗或预防疼痛，炎症，偏头痛，呕吐和带状疱疹后神经痛。