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39 条记录 (耗时 0.028 秒)

    PIPERIDINE AND MORPHOLINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
    4.
    发明公开
    PIPERIDINE AND MORPHOLINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 失效
    哌啶和吗啉及其用作治疗剂

    公开(公告)号：EP0837858A1

    公开(公告)日：1998-04-29

    申请号：EP96918772.0

    申请日：1996-06-20

    申请人： MERCK SHARP & DOHME LTD.

    发明人： BAKER, Raymond ,  ELLIOTT, Jason ,  STEVENSON, Graeme, Irvine ,  SWAIN, Christopher, John

    IPC分类号： C07D405 ,  A61K31 ,  A61P25

    CPC分类号： C07D405/14

    摘要： The present invention provides compounds of formula (I), wherein R1 is phenyl or a 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur, which aryl or heteroaryl group is optionally substituted; R2 is hydrogen, halogen, C¿1-6?alkyl, C1-6alkoxy, CF3, OCF3, NO2, CN, SR?a, SORa, SO¿2Ra, CO2R?a, CONRaRb, C¿2-6alkenyl, C2-6alkynyl or C1-4alkyl substituted by C1-4alkoxy, where R?a and Rb¿ each independently represent hydrogen or C¿1-4?alkyl; R?4, R5, R6, R9a and R9b¿, A, X, and Y are as defined in the specification; the dotted line is an optional double bond; Q1 is oxygen, sulphur or -NH-; Q2 is -N=, -NH-, -CH= or -CH¿2?-; and m is zero or 1; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.

    ARALKOXY AND ARALKYLTHIO SUBSTITUTED AZACYCLIC COMPOUNDS AS TACHYKININ ANTAGONISTS
    5.
    发明公开
    ARALKOXY AND ARALKYLTHIO SUBSTITUTED AZACYCLIC COMPOUNDS AS TACHYKININ ANTAGONISTS 失效
    芳烷氧基和取代芳氮杂环化合物作为拮抗剂速激肽

    公开(公告)号：EP0743939A1

    公开(公告)日：1996-11-27

    申请号：EP95907110.0

    申请日：1995-02-06

    申请人： MERCK SHARP & DOHME LTD.

    发明人： BAKER, Raymond ,  MACLEOD, Angus, Murray ,  SEWARD, Eileen, Mary ,  SWAIN, Christopher, John

    IPC分类号： A61K31 ,  A61P1 ,  A61P9 ,  A61P11 ,  A61P25 ,  A61P29 ,  A61P35 ,  A61P37 ,  A61P43 ,  C07D211 ,  C07D401

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

    摘要： The present invention relates to compounds of formula (I) wherein n is 1, 2 or 3 and where any carbon atom of (CH2)n may be substituted by R4 and/or R5; X represents O or S; R1 represents (CH¿2?)qphenyl, wherein q is 0, 1, 2 or 3, which may be optionally substituted in the phenyl ring; R?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?4 and R5¿ each independently represent H, halo, C¿1-6?alkyl, oxo, CO2R?a¿ or CONRaRb; R6 represents H or C¿1-6?alkyl; R?7¿ represents trifluoromethyl, C¿2-6?alkenyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, (CH2)pNR?9R10, CO¿2R?16, CONR9R10, (CH¿2)pCO2R16, (CH2)pCONR?9R10, (CH¿2)pNR?9COR16, (CH¿2)pNHSO2R11, (CH2)pOR16, (CH2)pOC(O)R9 or (CH¿2?)pOC1-4alkylCOR?17¿ or C¿1-6?alkyl substituted by a hydroxy group; R?8¿ represents H, CORa, CO2Ra, COCONRaRb, COCO¿2R?a, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, C1-6alkyl optionally substituted by a group selected from (CO2R?a, CONRaRb¿, hydroxy, cyano, COR?a, NRaRb¿, C(NOH)NRaRb, CONHphenyl(C¿1-4?alkyl), COCO2R?a¿, CONHNRaRb, C(S)NR?aRb, CONRaC¿1-6alkylR?12, CONR13C¿2-6alkynyl, CONR13C2-6alkenyl, COCONR?aRb, CONRaC(NRb)NRaRb, CONRa¿heteroaryl, and optionally substituted phenyl or C¿1-6?alkyl, optionally substituted by oxo, substituted by an optionally substituted aromatic heterocycle; R?a and Rb¿ each independently represent H, C¿1-6?alkyl, trifluoromethyl or phenyl optionally substituted by C1-6alkyl, halo or trifluoromethyl. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.

    SPIRO-PIPERIDINE DERIVATIVES AND THEIR USE AS TACHYKININ ANTAGONISTS
    8.
    发明公开
    SPIRO-PIPERIDINE DERIVATIVES AND THEIR USE AS TACHYKININ ANTAGONISTS 失效
    螺哌啶衍生物及其作为速激肽antagoniste

    公开(公告)号：EP1019410A1

    公开(公告)日：2000-07-19

    申请号：EP96938399.1

    申请日：1996-11-20

    申请人： MERCK SHARP & DOHME LTD.

    发明人： BAKER, Raymond ,  HARRISON, Timothy ,  SWAIN, Christopher, John ,  WILLIAMS, Brian, John

    IPC分类号： C07D491/20 ,  A61K31/445 ,  C07D491/22 ,  A61K31/505

    CPC分类号： C07D491/10

    摘要： The present invention relates to compounds of formula (I), wherein R1 represents halogen, hydroxy, C¿1-6?alkyl group optionally substituted by one to three fluorine atoms, C1-6alkoxy group optionally substituted by one to three fluorine atoms, or C1-6alkylthio optionally substituted by one to three fluorine atoms; R?2¿ represents hydrogen, halogen, C¿1-6?alkyl or C1-6alkoxy; or when R?2¿ is adjacent to R1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; R?4, R5, R9 and R10¿ are a variety of substituents; R6 represents hydrogen, CORa, CO2Ra, COCONRaRb, COCO¿2R?a, C1-6alkyl optionally substituted by a group selected from (CO2R?a, CONRaRb¿, hydroxy, CN, COR?a, NRaRb¿, C(NOH)NRaRb, CONHphenyl(C¿1-4?alkyl), COCO2R?a¿, CONHNRaRb, C(S)NR?aRb, CONRaC¿1-6alkylR?12, CONR13C¿2-6alkenyl, CONR13C2-6alkynyl, COCONR?aRb, CONRaC(NRb)NRaRb, CONRa¿heteroaryl, and optionally substituted phenyl) or -CH¿2?C CCH2NR?7R8¿ or C¿1-6?alkyl, optionally substituted by oxo, substituted by an optionally substituted 5-membered or 6-membered heterocyclic ring containing 1, 2 or 3 nitrogen atoms; m is 0-3 and n is 0-3, with the proviso that the sum total of m+n is 2 or 3; p is zero or 1; q is 1 or 2; and when m is 1 and n is 1 or 2, the broken line represents an optional double bond; 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.