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    N-AROYL CYCLIC AMINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
    72.
    发明申请
    N-AROYL CYCLIC AMINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
    作为OREXIN受体拮抗剂的N-阿洛尔循环胺衍生物

    公开(公告)号：WO2002089800A2

    公开(公告)日：2002-11-14

    申请号：PCT/EP2002/004874

    申请日：2002-05-03

    Applicant: SMITHKLINE BEECHAM P.L.C. ,  GAILLARD, Pascale ,  JOHNSON, Christopher, Norbert ,  NOVELLI, Riccardo ,  PORTER, Roderick, Alan ,  STEMP, Geoffrey ,  THEWLIS, Kevin, Michael

    Inventor： GAILLARD, Pascale ,  JOHNSON, Christopher, Norbert ,  NOVELLI, Riccardo ,  PORTER, Roderick, Alan ,  STEMP, Geoffrey ,  THEWLIS, Kevin, Michael

    IPC: A61K31/445

    CPC classification number: C07D265/30 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14

    Abstract: This invention relates to N-aroyl cyclic amine derivatives of formula (I): wherein: Y represents a bond, oxygen, or a group (CH 2 ) n , wherein n represents 1, 2 or 3 m represents 1, 2 or 3; p represents 0 or 1; X is O,SC=O, SO 2 , or -CH=CH; Ar 1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar 2 represents phenyl or a 5- or 5-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R 1 and further optional substituents; or Ar 2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R 1 represents hydrogen, optionally substituted (C 1-4 )alkoxy, halo, cyano, optionally substituted (C 1-16 )alkyl, optionally substituted 5- or 6-membered heterocyclic ring containing up to 4 heteroatoms selected from N, O and S; or a pharmaceutical acceptable salt thereof; and their use as pharmaceuticals, specifically as orexin receptor antagonists.

    Abstract translation: 本发明涉及式（I）的N-芳酰基环胺衍生物：其中：Y表示键，氧或基团（CH 2）n，其中n表示1,2或3m表示1,2或3; p表示0或1; X是O，SC = O，SO 2或-CH = CH; Ar 1是芳基或含有至多4个选自N，O和S的杂原子的单或双环杂芳基; 任何一个可以任选地被取代; Ar 2表示苯基或含有至多3个选自N，O和S的杂原子的5或5元杂环基，其中苯基或杂环基被R 1取代，另外任选的取代基; 或Ar 2表示含有至多3个选自N，O和S的杂原子的任选取代的双环芳族或双环杂芳族基团; R 1表示氢，任选取代的（C 1-4）烷氧基，卤素，氰基，任选取代的（C 1-6）烷基，任选取代的含有至多4个选自N，O的杂原子的5-或6-元杂环， S; 或其药学上可接受的盐; 以及它们作为药物的用途，特别是作为食欲素受体拮抗剂。

    PYRIMIDINYL-PIPERAZINE DERIVATIVES AND THEIR USE AS MEDICAMENTS
    73.
    发明申请
    PYRIMIDINYL-PIPERAZINE DERIVATIVES AND THEIR USE AS MEDICAMENTS 审中-公开
    哌嗪基哌嗪衍生物及其作为药物的用途

    公开(公告)号：WO1994014779A1

    公开(公告)日：1994-07-07

    申请号：PCT/EP1993003565

    申请日：1993-12-14

    Applicant: SMITHKLINE BEECHAM PLC ,  PORTER, Roderick, Alan

    Inventor： SMITHKLINE BEECHAM PLC

    IPC: C07D239/46

    CPC classification number: C07D239/47

    Abstract: Pyrimidinyl piperazine derivatives of formula (I), wherein R1, R2 and R3 are independently H or C1-C4-alkyl; R4 is optionally substituted phenyl; and n is 1 to 5; or a pharmaceutically acceptable salt, solvate or hydrate thereof.

    Abstract translation: 式（I）的嘧啶基哌嗪衍生物，其中R 1，R 2和R 3独立地为H或C 1 -C 4 - 烷基; R4是任选取代的苯基; n为1〜5; 或其药学上可接受的盐，溶剂合物或水合物。

    TETRAHYDROCARBAZOLE DERIVATIVES AS 5-HT1-LIKE AGONISTS
    74.
    发明申请
    TETRAHYDROCARBAZOLE DERIVATIVES AS 5-HT1-LIKE AGONISTS 审中-公开
    四氢叶酸衍生物作为5-HT1样激动剂

    公开(公告)号：WO1994014773A1

    公开(公告)日：1994-07-07

    申请号：PCT/EP1993003628

    申请日：1993-12-16

    Applicant: SMITHKLINE BEECHAM PLC ,  PORTER, Roderick, Alan ,  VIMAL, Mythily

    Inventor： SMITHKLINE BEECHAM PLC

    IPC: C07D209/88

    CPC classification number: C07D209/88

    Abstract: Compounds of formula (I), wherein R represents halogen, C1-4alkyl, C1-4alkoxy, hydroxy, NO2, -NR R , R R NCO(CH2)m-, R R NSO2(CH2)m-, R CONH(CH2)-m or R SO2NH(CH2)m-; R and R each independently hydrogen or C1-4alkyl or NR<>4 represents a 5- to 7-membered heterocyclic ring; R represents hydrogen or C1-4alkyl; R represents C1-4alkyl; m is zero, 1 or 2; n is zero or 1 to 5; R and R each independently represent hydrogen, C1-6alkyl or benzyl or -NR R represents a pyrrolidino, piperidino or hexahydroazepino ring; and A represents a bond, a C1-5alkylene chain or a C3-5alkenyle chain wherein the double bond is not adjacent the nitrogen atom; and salts thereof have affinity for the 5-HT1-like receptor and are useful e.g. in the treatment of migraine.

    Abstract translation: 式（I）化合物，其中R 1表示卤素，C 1-4烷基，C 1-4烷氧基，羟基，NO 2，-NR 4 R 5，R 4 R 5 NCO（CH 2）m - ，R 4 R 5 NSO 2（CH 2）m - ，R 6 CONH（CH 2）m或R 7 SO 2 NH（CH 2）m - ; R 4和R 5各自独立地为氢或C 1-4烷基或NR <4 表示5-至7-元杂环; R 6表示氢或C 1-4烷基; R 7表示C 1-4烷基; m为零，1或2; n为0或1〜5; R 2和R 3各自独立地表示氢，C 1-6烷基或苄基或-NR 2 R 3表示吡咯烷子基，哌啶子基或六氢氮杂环环。 A表示键，C1-5亚烷基链或C3-5链烯基链，其中双键不与氮原子相邻; 其盐对5-HT1样受体具有亲和力，并且可用于例如 在治疗偏头痛。

    TRYPTAMINE ANALOGUES AS 5-HT1-LIKE AGONISTS
    76.
    发明申请
    TRYPTAMINE ANALOGUES AS 5-HT1-LIKE AGONISTS 审中-公开
    作为5-HT1型激动剂的三甲酚胺类似物

    公开(公告)号：WO1994014770A1

    公开(公告)日：1994-07-07

    申请号：PCT/EP1993003563

    申请日：1993-12-14

    Applicant: SMITHKLINE BEECHAM PLC ,  PORTER, Roderick, Alan ,  WARD, John, Gerard

    Inventor： SMITHKLINE BEECHAM PLC

    IPC: C07D209/16

    CPC classification number: C07D401/04 ,  C07D209/14 ,  C07D209/16 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

    Abstract: A compound of structure (I), in which A is O, S(O)n in which n is 0, 1 or 2, NR, CH2, or CH(OH); A is a bond or CH2; or A A is CH = CH; R is hydrogen or C1-4alkyl; R is an optionally substituted 6- to 10-membered aryl or heteroaryl ring; suitably R is an optionally substituted 6- or 10-membered aryl ring such as phenyl or naphthyl; suitably R is an optionally substituted 6- to 10-membered heteroaryl ring, containing from 1 to 4 nitrogen atoms; R is hydrogen, halogen, C1-4alkyl, CN, NO2 or CF3; R is C(R )(R )CH2NR R , -CH = NNHC(NH)NH2 or a; R and R are independently hydrogen or C1-4alkyl; R and R are the same or different and are each hydrogen or C1-4alkyl or together with the nitrogen atom to which they are attached form a ring; R is hydrogen, C1-4alkyl, or C3-6alkenyl; the dotted lines represent an optional bond; and q and m are independently 1 or 2; and pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds are 5-HT1-like agonists (or partial agonists) and as such are expected to have utility in medicine in the treatment and/or prophylaxis of migraine, and other conditions associated with cephalic pain, such as cluster headache, headache associated with vascular disorders and other neuralgia. They are also expected to have utility in the treatment or prophylaxis of portal hypertension.

    Abstract translation: 结构（I）的化合物，其中A 1是O，S（O）n，其中n是0,1或2，NR，CH 2或CH（OH）; A 2是键或CH 2; 或A 1 A 2是CH = CH; R是氢或C 1-4烷基; R 1是任选取代的6至10元芳基或杂芳基环; 合适的R 1是任选取代的6-或10-元芳环，例如苯基或萘基; 适当地R 1是含有1至4个氮原子的任选取代的6至10元杂芳基环; R 2是氢，卤素，C 1-4烷基，CN，NO 2或CF 3; R 3是C（R 4）（R 5）CH 2 NR 6 R 7，-CH = NNHC（NH）NH 2或a; R 4和R 5独立地是氢或C 1-4烷基; R 6和R 7相同或不同，各自为氢或C 1-4烷基，或与它们所连接的氮原子一起形成环; R 8是氢，C 1-4烷基或C 3-6烯基; 虚线表示可选的键; q和m独立地为1或2; 及其药学上可接受的盐，溶剂化物和水合物。 化合物是5-HT1样激动剂（或部分激动剂），因此预期在医学中可用于治疗和/或预防偏头痛以及与头痛相关的其它病症，例如丛集性头痛，头痛与 血管疾病等神经痛。 它们也预期可用于治疗或预防门静脉高压。

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