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29 条记录 (耗时 0.028 秒)

    Spiro-substituted azacyclic derivatives and their use as therapeutic agents
    1.
    发明授权
    Spiro-substituted azacyclic derivatives and their use as therapeutic agents 失效

    公开(公告)号：US5811431A

    公开(公告)日：1998-09-22

    申请号：US765360

    申请日：1997-01-07

    申请人： Tamara Ladduwahetty ,  Richard Thomas Lewis ,  Angus Murray MacLeod ,  Kevin John Merchant

    发明人： Tamara Ladduwahetty ,  Richard Thomas Lewis ,  Angus Murray MacLeod ,  Kevin John Merchant

    IPC分类号： A61K31/435 ,  A61P1/04 ,  A61P1/08 ,  A61P11/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/28 ,  A61P29/00 ,  A61P37/00 ,  A61P43/00 ,  C07D471/10 ,  A61K31/445 ,  C07D401/04

    CPC分类号： C07D471/10

    摘要： The present invention relates to compounds of formula (I), wherein n is zero, 1, 2 or 3; R represents C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halogen, cyano, trifluoromethyl SO.sub.2 C.sub.1-6 alkyl, NR.sup.a R.sup.b, NR.sup.a COR.sup.b or CONR.sup.a R.sup.b, where R.sup.a and R.sup.b are each H, C.sub.1-4 alkyl, phenyl or trifluoromethyl; R.sup.1 represents phenyl optionally substituted by 1, 2 or 3 of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, --O(CH.sub.2).sub.p O-- (where p is 1 or 2), halogen, cyano, nitro, trifluoromethyl, trimethylsilyl, OR.sup.a, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, NR.sup.a R.sup.b, NR.sup.a COR.sup.b, NR.sup.a CO.sub.2 R.sup.b, COR.sup.a, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b ; naphthyl; benzhydryl; or benyl, where the naphthyl group or each phenyl moiety of benzyl and benzhydryl may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or trifluoromethyl; R.sup.2 represents hydogen, a substituent as defined for R.sup.1 or heteroaryl selected from indazolyl, thienyl, furanyl, pyridyl, thiazolyl, tetrazolyl and quinolinyl; wherein each heteroaryl may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or trifluoromethyl; R.sup.3 and R.sup.4 are each H or C.sub.1-6 alkyl or R.sup.3 and R.sup.4 together are linked so as to form a C.sub.1-3 alkylene chain; R.sup.5 represents H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenylC.sub.1-4 alkyl, CO.sub.2 R.sup.a, CONR.sup.a R.sup.b, SOR.sup.a or SO.sub.2 R.sup.a, wherein the phenyl moiety may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or trifluoromethyl; X and Y are each H, or together represents .dbd.O; and Z represents a bond, O, S, SO, SO.sub.2, NR.sup.6, or --(CR.sup.6 R.sup.6)-- where R.sup.6 is H or C.sub.1-6 alkyl; 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##

    Aromatic compounds, compositions containing them and their use in therapy
    4.
    发明授权
    Aromatic compounds, compositions containing them and their use in therapy 失效
    芳香族化合物，含有它们的组合物及其在治疗中的应用

    公开(公告)号：US5674889A

    公开(公告)日：1997-10-07

    申请号：US513759

    申请日：1995-08-21

    申请人： Fintan Kelleher ,  Richard Thomas Lewis ,  Angus Murray Macleod

    发明人： Fintan Kelleher ,  Richard Thomas Lewis ,  Angus Murray Macleod

    IPC分类号： C07D209/14 ,  C07D401/12 ,  C07D471/08 ,  A61K31/405 ,  C07D209/10

    CPC分类号： C07D401/12 ,  C07D209/14 ,  C07D471/08

    摘要： The present invention relates to compounds of formula (I) and salts and prodrugs thereof, wherein Q.sup.1 represents a phenyl group substituted by one or more halo optionally substituted naphthyl, optionally substituted indolyl, optionally substituted benzthiophenyl, optionally substituted benzofuranyl, optionally substituted benzyl or optionally substituted fluorenyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; Z.sup.1 represents a group selected from (a) or (b). The compounds are tachykinin antagonists useful for treating pain or inflammation, migraine or emesis.

    摘要翻译： PCT No.PCT / EP94 / 00438 Sec。 371日期1995年8月21日 102（e）日期1995年8月21日PCT 1994年2月15日PCT PCT。 公开号WO94 / 19320 PCT （I）的化合物本发明涉及式（I）的化合物及其盐和前药，其中Q1表示被一个被一个 或更多的卤素任选取代的萘基，任选取代的吲哚基，任选取代的苯硫基苯基，任选取代的苯并呋喃基，任选取代的苄基或任选取代的芴基; R1表示H或C1-6烷基; R 2表示H，C 1-6烷基或C 2-6烯基; Z1表示选自（a）或（b）的基团。 这些化合物是可用于治疗疼痛或炎症，偏头痛或呕吐的速激肽拮抗剂。

    Morpholine derivatives and their use as therapeutic agents
    6.
    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）