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16 条记录 (耗时 0.024 秒)

    SUBSTITUTED PIPERAZINE DERIVATIVES
    4.
    发明申请
    SUBSTITUTED PIPERAZINE DERIVATIVES 审中-公开
    替代哌嗪衍生物

    公开(公告)号：WO1997019943A1

    公开(公告)日：1997-06-05

    申请号：PCT/GB1996002870

    申请日：1996-11-21

    申请人： MERCK SHARP & DOHME LIMITED ,  LADDUWAHETTY, Tamara ,  MACLEOD, Angus, Murray ,  ROWLEY, Michael

    发明人： MERCK SHARP & DOHME LIMITED

    IPC分类号： C07D403/14

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： A compound of formula (I), or a salt or prodrug thereof, wherein L is selected from (A) wherein G represents oxygen or sulphur; M represents halogen or C1-6 alkyl; R represents aryl or heteroaryl, either of which groups may be optionally substituted; (B) wherein Ar is a six-membered aromatic ring optionally containing one or two nitrogen atoms, which ring is optionally substituted; and (C) wherein R is phenyl, optionally substituted. R and R are independently selected from hydrogen, C1-6 alkyl, C2-6 alkyl, C2-6 alkenyl, C2-6 alkynyl and halogen, R and R , together with the carbon atom to which they are attached, form a C3-7 cycloalkyl group; processes for its preparation and its use in the treatment of conditions for which the administration of an agonist selective for the 5-HT1Dalpha receptor subtype is indicated, such as migraine.

    摘要翻译： 式（I）化合物或其盐或前药，其中L选自（A）其中G表示氧或硫; M表示卤素或C 1-6烷基; R 1表示芳基或杂芳基，其中任一个可以任选被取代; （B）其中Ar是任选含有一个或两个氮原子的六元芳环，该环任选被取代; 和（C）其中R 8是苯基，任选被取代。 R 9和R 10独立地选自氢，C 1-6烷基，C 2-6烷基，C 2-6烯基，C 2-6炔基和卤素，R 9和R 10，以及 它们所连接的碳原子形成C 3-7环烷基; 其制备方法及其用于治疗指示给予5-HT1Dalpha受体亚型选择性激动剂的条件，例如偏头痛。

    SPIRO-SUBSTITUTED AZACYCLIC DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
    5.
    发明申请
    SPIRO-SUBSTITUTED AZACYCLIC DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
    螺旋取代的亚氨基衍生物及其作为治疗剂的用途

    公开(公告)号：WO1996005203A1

    公开(公告)日：1996-02-22

    申请号：PCT/GB1995001867

    申请日：1995-08-07

    申请人： MERCK SHARP & DOHME LIMITED ,  LADDUWAHETTY, Tamara ,  LEWIS, Richard, Thomas ,  MACLEOD, Angus, Murray ,  MERCHANT, Kevin, John

    发明人： MERCK SHARP & DOHME LIMITED

    IPC分类号： C07D471/10

    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 C1-6alkyl, C1-6alkoxy, hydroxy, halogen, cyano, trifluoromethyl, SO2C1-6alkyl, NR R , NR COR or CONR R , where R and R are each H, C1-6alkyl, phenyl or trifluoromethyl; R represents phenyl optionally substituted by 1, 2 or 3 of C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, -O(CH2)pO- (where p is 1 or 2), halogen, cyano, nitro, trifluoromethyl, trimethylsilyl, OR , SR , SOR , SO2R , NR R , NR COR , NR CO2R , COR , CO2R or CONR R ; naphthyl; benzhydryl; or benzyl, where the naphthyl group or each phenyl moiety of benzyl and benzhydryl may be substituted by C1-6alkyl, C1-6alkoxy, halogen or trifluoromethyl; R represents hydrogen, a substituent as defined for R or heteroaryl selected from indazolyl, thienyl, furanyl, pyridyl, thiazolyl, tetrazolyl and quinolinyl; wherein each heteroaryl may be substituted by C1-6alkyl, C1-6alkoxy, halogen or trifluoromethyl; R and R are each H or C1-6alkyl or R and R together are linked so as to form a C1-3alkylene chain; R represents H, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenylC1-4alkyl, CO2R , CONR R , SOR or SO2R , wherein the phenyl moiety may be substituted by C1-6alkyl, C1-6alkoxy, halogen or trifluoromethyl; X and Y are each H, or together represent =O; and Z represents a bond, O, S, SO, SO2, NR , or -(CR R )- where R is H or C1-6alkyl; 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： 本发明涉及式（I）化合物，其中n为0,1,2或3; R表示C 1-6烷基，C 1-6烷氧基，羟基，卤素，氰基，三氟甲基，SO 2 C 1-6烷基，NR a R b，NR a COR b或CONR a R b，其中 R a和R b各自为H，C 1-6烷基，苯基或三氟甲基; R 1表示任选被1,2或3个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，-O（CH 2）p O--（其中p为1或 2），卤素，氰基，硝基，三氟甲基，三甲基甲硅烷基，OR a，SR a，SOR a，SO 2 R a，NR a R b，NR a COR b， ，NR a CO 2 R b，COR a，CO 2 R a或CONR a R b; 萘; 二苯甲基; 或苄基，其中苄基和二苯甲基的萘基或每个苯基部分可被C 1-6烷基，C 1-6烷氧基，卤素或三氟甲基取代; R 2表示氢，R 1所定义的取代基或选自吲唑基，噻吩基，呋喃基，吡啶基，噻唑基，四唑基和喹啉基的杂芳基; 其中每个杂芳基可以被C 1-6烷基，C 1-6烷氧基，卤素或三氟甲基取代; R 3和R 4各自为H或C 1-6烷基或R 3和R 4一起连接形成C 1-3亚烷基链; R 5表示H，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基C 1-4烷基，CO 2 R a，CONR a R b，SOR a或SO 2 R a，其中 苯基部分可以被C 1-6烷基，C 1-6烷氧基，卤素或三氟甲基取代; X和Y各自为H，或一起表示= O; 和Z表示键，O，S，SO，SO 2，NR 6或 - （CR 6 R 6） - ，其中R 6是H或C 1-6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。

    PIPERIDINE AND TETRAHYDROPYRIDINE DERIVATIVES
    9.
    发明申请
    PIPERIDINE AND TETRAHYDROPYRIDINE DERIVATIVES 审中-公开
    哌啶和四氢吡啶衍生物

    公开(公告)号：WO1997019073A1

    公开(公告)日：1997-05-29

    申请号：PCT/GB1996002795

    申请日：1996-11-14

    申请人： MERCK SHARP & DOHME LIMITED ,  CHAMBERS, Mark, Stuart ,  HOBBS, Sarah, Christine ,  LADDUWAHETTY, Tamara ,  MACLEOD, Angus, Murray ,  MERCHANT, Kevin, John

    发明人： MERCK SHARP & DOHME LIMITED

    IPC分类号： C07D401/14

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D413/14

    摘要： A class of substituted piperidine and tetrahydropyridine derivatives, linked through the 4-position thereof via an alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 1-position by an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl-alkyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D alpha receptor subtype whilst processing at least a 10-fold selective affinity for the 5-HT1D alpha receptor subtype relative to the 5-HT1D beta subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.

    摘要翻译： 一类通过其4-位通过亚烷基链连接到稠合双环杂芳族部分如吲哚基并在1位被进一步被任选取代的烷基，烯基，炔基，环烷基 - 取代的烷基取代的哌啶和四氢吡啶衍生物， 烷基，芳基 - 烷基或杂芳基 - 烷基部分是5-HT1样受体的选择性激动剂，它是人类5-HT1Dα受体亚型的有效激动剂，同时对5-HT1Dαα进行至少10倍的选择性亲和力 受体亚型相对于5-HT1Dβ亚型; 因此，它们可用于治疗和/或预防临床状况，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比 与非亚型选择性5-HT1D受体激动剂相关的那些。

    MORPHOLINE AND THIOMORPHOLINE TACHYKININ RECEPTOR ANTAGONISTS
    10.
    发明申请
    MORPHOLINE AND THIOMORPHOLINE TACHYKININ RECEPTOR ANTAGONISTS 审中-公开
    吗啉和噻吗啉嘧啶酮受体拮抗剂

    公开(公告)号：WO1995016679A1

    公开(公告)日：1995-06-22

    申请号：PCT/US1994014497

    申请日：1994-12-13

    申请人： MERCK & CO., INC. ,  DORN, Conrad, P. ,  FINKE, Paul, E. ,  HALE, Jeffrey, J. ,  MacCOSS, Malcolm ,  MILLS, Sander, G. ,  SHAH, Shrenik, K. ,  CHAMBERS, Mark, Stuart ,  HARRISON, Timothy ,  LADDUWAHETTY, Tamara ,  WILLIAMS, Brian, John

    发明人： MERCK & CO., INC.

    IPC分类号： C07D265/32

    CPC分类号： C07D265/30 ,  C07D265/32 ,  C07D279/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14

    摘要： Substituted heterocycles of general structural formula (I) or a pharmaceutically acceptable salt thereof, wherein: R is selected from the group consisting of: hydrogen; C1-6 alkyl, unsubstituted or substituted; C2-6 alkenyl, unsubstituted or substituted; C2-6 alkynyl; phenyl, unsubstitued or substituted; X is selected from the group consisting of: -O-, -S-, -SO-, -SO2-; Y is selected from the group consisting of: a single bond, -O-, -S-, -CO-, -CH2, -CHR5- and -CR R ; Z = C1-6 alkyl, are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

    摘要翻译： 取代的通式结构式（I）的杂环或其药学上可接受的盐，其中：R 1选自：氢; 未取代或取代的C 1-6烷基; C 2-6烯基，未取代或取代的; C 2-6炔基; 苯基，未取代或取代的; X选自：-O - ， - S - ， - SO - ， - SO 2 - ; Y选自：单键，-O - ， - S - ， - CO - ， - CH 2，-CHR 5 - 和-CR 15 R 16; Z = C 1-6烷基是可用于治疗炎性疾病，疼痛或偏头痛，哮喘和呕吐的速激肽受体拮抗剂，以及可用于治疗心血管疾病如心绞痛，高血压或缺血的钙通道阻滞剂。