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27 条记录 (耗时 0.048 秒)

    Morpholine derivatives, compositions containing them and their use as therapeutic agents
    14.
    发明授权
    Morpholine derivatives, compositions containing them and their use as therapeutic agents 失效
    吗啉衍生物，含有它们的组合物及其作为治疗剂的用途

    公开(公告)号：US5877316A

    公开(公告)日：1999-03-02

    申请号：US913566

    申请日：1997-09-16

    申请人： Karen Elizabeth Haworth ,  Simon Neil Owen ,  Eileen Mary Seward

    发明人： Karen Elizabeth Haworth ,  Simon Neil Owen ,  Eileen Mary Seward

    IPC分类号： A61K31/535 ,  A61P1/08 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P43/00 ,  C07D413/06 ,  C07D417/06

    CPC分类号： C07D413/06

    摘要： The present invention relates to compounds of formula (I), wherein R.sup.1 and R.sup.4 represent hydrogen, halogen, 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, C.sub.1-6 alkoxy, C.sub.1-4 alkyl substituted by a hydroxy or C.sub.1-4 alkoxy group, OCF.sub.3, hydroxy, trifluoromethyl, trimethylsilyl, nitro, CN, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, COR.sup.a, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b, where R.sup.a and R.sup.b are each independently hydrogen or C.sub.1-4 alkyl; R.sup.2, R.sup.3 and R.sup.5 represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-4 alkoxy substituted by a C.sub.1-4 alkoxy group, or trifluoromethyl; R.sup.6 represents C.sub.1-6 alkyl, optionally substituted by oxo, substituted by a 5-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, oxadiazole and thiadiazole, wherein each heteroaromatic ring is substituted at the available carbon atom by a group of the formula: ZNR.sup.7 R.sup.8. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.

    摘要翻译： PCT No.PCT / GB96 / 00587 Sec。 371日期：1997年9月16日 102（e）1997年9月16日PCT PCT 1996年3月13日PCT公布。 公开号WO96 / 29328 日期：1996年9月26日本发明涉及式（I）化合物，其中R 1和R 4表示氢，卤素，C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-7环烷基，C 3-7环烷基C 1-4烷基， C6烷氧基，被羟基或C1-4烷氧基取代的C1-4烷基，OCF3，羟基，三氟甲基，三甲基甲硅烷基，硝基，CN，SRa，SORa，SO2Ra，CORa，CO2Ra或CONRaRb，其中Ra和Rb各自独立地为氢或C1- 4个烷基; R2，R3和R5表示氢，卤素，C1-6烷基，被C1-4烷氧基取代的C1-4烷氧基或三氟甲基; R 6表示任选被氧代取代的，被选自恶唑，噻唑，异恶唑，异噻唑，恶二唑和噻二唑的5元杂芳环取代的C 1-6烷基，其中每个杂芳环在可用的碳原子上被一个式 ：ZNR7R8。 该化合物特别用于治疗疼痛，炎症，偏头痛和呕吐。

    Aralkoxy and aralkylthio substituted azacyclic compounds as tachykinin antagonists
    16.
    发明授权
    Aralkoxy and aralkylthio substituted azacyclic compounds as tachykinin antagonists 失效

    公开(公告)号：US5665883A

    公开(公告)日：1997-09-09

    申请号：US676157

    申请日：1996-09-26

    申请人： Raymond Baker ,  Angus Murray MacLeod ,  Eileen Mary Seward ,  Christopher John Swain

    发明人： Raymond Baker ,  Angus Murray MacLeod ,  Eileen Mary Seward ,  Christopher John Swain

    IPC分类号： A61K31/4427 ,  A61K31/445 ,  A61K31/451 ,  A61P1/00 ,  A61P1/08 ,  A61P9/00 ,  A61P11/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/08 ,  A61P43/00 ,  C07D211/42 ,  C07D211/54 ,  C07D401/06

    CPC分类号： C07D401/06 ,  C07D211/42 ,  C07D211/54

    摘要： The present invention relates to compounds of formula (I) wherein n is 3 and where any carbon atom of (CH.sub.2).sub.n may be substituted by R.sup.4 and/or R.sup.5 ; X represents O or S; R.sup.1 represents (CH.sub.2).sub.q phenyl, wherein q is 0, 1 , 2 or 3 which may be optionally substituted in the phenyl ring; R.sup.2 represents aryl selected from phenyl and naphthyl; heteroaryl selected from indazolyl, thienyl, furyl, pyridyl, thiazolyl, tetrazolyl and quinolyl; benzhydryl; or benzyl; wherein each aryl or heteroaryl moiety may be substituted; R.sup.4 and R.sup.5 each independently represent H, halo, C.sub.1-6 alkyl, oxo, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b ; R.sup.6 represents H or C.sub.1-6 alkyl; R.sup.7 represents trifluoromethyl, C.sub.2-6 alkenyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, (CH.sub.2).sub.p NR.sup.9 R.sup.10, CO.sub.2 R.sup.16, CONR.sup.9 R.sup.10, (CH.sub.2).sub.p CO.sub.2 R.sup.16, (CH.sub.2).sub.p CONR.sup.9 R.sup.10, (CH.sub.2).sub.p NR.sup.9 COR.sup.16, (CH.sub.2).sub.p NHSO.sub.2 R.sup.11, (CH.sub.2).sub.p OR.sup.16, (CH.sub.2).sub.p OC(O)R.sup.9 or (CH.sub.2).sub.p OC.sub.1-4 alkylCOR.sup.17 or C.sub.1-6 alkyl substituted by a hydroxy group; R.sup.8 repents H, COR.sup.a, CO.sub.2 R.sup.a, COCONR.sup.a R.sup.b, COCO.sub.2 R.sup.a, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, C.sub.1-6 alkyl optionally substituted by a group selected from (CO.sub.2 R.sup.a, CONR.sup.a R.sup.b, hydroxy, cyano, COR.sup.a, NR.sup.a R.sup.b, C(NOH)NR.sup.a R.sup.b, CONHphenyl(C.sub.1-4 alkyl), COCO.sub.2 R.sup.a, CONHNR.sup.a R.sup.b, C(S)NR.sup.a R.sup.b, CONR.sup.a C.sub.1-6 alkylR.sup.12, CONR.sup.13 C.sub.2-6 alkynyl, CONR.sup.13 C.sub.2-6 alkenyl, COCONR.sup.a R.sup.b, CONR.sup.a C(NR.sup.b)NR.sup.a R.sup.b, CONR.sup.a heteroaryl, and optionally substituted phenyl or C.sub.1-6 alkyl, optionally substituted by oxo, substituted by an optionally substituted aromatic heterocycle; R.sup.a and R.sup.b each independently represent H, C.sub.1-6 alkyl, trifluoromethyl or phenyl optionally substituted by C.sub.1-6 alkyl, halo or trifluoromethyl. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.