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26 条记录 (耗时 0.241 秒)

    5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine derivatives as P2X7 modulators
    1.
    发明授权
    5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine derivatives as P2X7 modulators 有权
    5,6,7,8-四氢[1,2,4]三唑并[4,3-a]吡嗪衍生物，为P2X7调节剂

    公开(公告)号：US08501946B2

    公开(公告)日：2013-08-06

    申请号：US13266592

    申请日：2010-04-28

    申请人： David Kenneth Dean ,  Jorge Munoz-Muriedas ,  Mairi Sime ,  Jon Graham Anthony Steadman ,  Rachel Elizabeth Anne Thewlis ,  Giancarlo Trani ,  Daryl Simon Walter

    发明人： David Kenneth Dean ,  Jorge Munoz-Muriedas ,  Mairi Sime ,  Jon Graham Anthony Steadman ,  Rachel Elizabeth Anne Thewlis ,  Giancarlo Trani ,  Daryl Simon Walter

    IPC分类号： C07D495/00

    CPC分类号： C07D487/04

    摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.

    摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐：其中A为氢，C 1-4烷基，C 3-6环烷基，C 1-3烷氧基，C 1-3烷氧基C 1-4烷基，C 1-2 - 氟烷基，卤素，NR 6 R 7， 任选取代的杂芳基（Het）或任选取代的苯基，并且R 1，R 2，R 3，R 4，R 5，R 6和R 7如说明书中所定义。 认为化合物或盐可以调节P2X7受体功能，并能够拮抗ATP在P2X7受体上的作用。 本发明还提供了化合物或盐在治疗或预防例如炎性疼痛，神经性疼痛，内脏痛，类风湿性关节炎，骨关节炎或神经变性疾病中的用途。

    Imidazolidine carboxamide derivatives as P2X7 modulators
    6.
    发明授权
    Imidazolidine carboxamide derivatives as P2X7 modulators 失效
    咪唑烷羧酰胺衍生物作为P2X7调节剂

    公开(公告)号：US07932282B2

    公开(公告)日：2011-04-26

    申请号：US12594381

    申请日：2008-04-02

    申请人： Paul John Beswick ,  David Kenneth Dean ,  Robert James Gleave ,  Andrew Peter Moses ,  Daryl Simon Walter

    发明人： Paul John Beswick ,  David Kenneth Dean ,  Robert James Gleave ,  Andrew Peter Moses ,  Daryl Simon Walter

    IPC分类号： A61K31/4164 ,  C07D233/02

    CPC分类号： C07D233/36 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04

    摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.

    摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐：该化合物或盐调节P2X7受体功能并能够拮抗ATP在P2X7受体（P2X7受体拮抗剂）下的作用。 本发明还提供了这样的化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的病症/疾病中的用途，例如疼痛，炎症或神经变性疾病，特别是疼痛，例如炎性疼痛， 神经性疼痛或内脏痛。

    Pyrazole Derivatives as P2X7 Modulators
    9.
    发明申请
    Pyrazole Derivatives as P2X7 Modulators 审中-公开
    吡唑衍生物作为P2X7调节剂

    公开(公告)号：US20100056595A1

    公开(公告)日：2010-03-04

    申请号：US12595099

    申请日：2008-04-10

    申请人： Paul John Beswick ,  David Kenneth Dean ,  Daryl Simon Walter

    发明人： Paul John Beswick ,  David Kenneth Dean ,  Daryl Simon Walter

    IPC分类号： A61K31/415 ,  C07D231/12 ,  A61P25/00

    CPC分类号： C07D231/16 ,  C07D231/12

    摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 represents C1-6 alkyl or C3-6 cycloalkyl, either of which is optionally substituted with 1, 2 or 3 halogen atoms; and R2 represents hydrogen, halogen, C1-6 alkyl or C3-6 cycloalkyl; and either of said C1-6 alkyl or C3-6 cycloalkyl is optionally substituted with 1, 2 or 3 halogen atoms. The pyrazole compounds of formula (I) or salts thereof modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also relates to the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease.

    摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐：其中R1表示C1-6烷基或C3-6环烷基，其任一个任选被1,2或3个卤素原子取代; 并且R 2表示氢，卤素，C 1-6烷基或C 3-6环烷基; 并且所述C 1-6烷基或C 3-6环烷基中的任一个任选被1,2或3个卤素原子取代。 式（I）的吡唑化合物或其盐调节P2X7受体功能，并且能够拮抗ATP在P2X7受体（P2X7受体拮抗剂）下的作用。 本发明还涉及这些化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的疾病/疾病中的用途，例如疼痛，炎症或神经变性疾病。

    Pyridine substituted furan derivatives as Raf kinase inhibitors
    10.
    发明授权
    Pyridine substituted furan derivatives as Raf kinase inhibitors 失效
    吡啶取代的呋喃衍生物作为Raf激酶抑制剂

    公开(公告)号：US07375105B2

    公开(公告)日：2008-05-20

    申请号：US10488650

    申请日：2002-09-05

    申请人： David Kenneth Dean ,  Andrew Kenneth Takle ,  David Matthew Wilson

    发明人： David Kenneth Dean ,  Andrew Kenneth Takle ,  David Matthew Wilson

    IPC分类号： A61K31/5377 ,  A61K31/4545 ,  A61K31/443 ,  C07D413/14 ,  C07D211/32 ,  C07D405/04

    CPC分类号： C07D405/04 ,  C07D405/14

    摘要： Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. Wherein X is O, CH2 CO, S or NH, or the moiety X—R1 is hydrogen; Y1 and Y2 independently represent CH or N; Ar is a mono- or fused bicyclic aromatic or heteroaromatic group which may be optionally substituted; one of X1 and X2 is selected from O, S or NR11 and the other is CH, wherein R11 is hydrogen, C1-6alkyl, aryl or arylC1-6alkyl.

    摘要翻译： 化合物及其作为药物的用途，特别是用作治疗神经创伤性疾病，癌症，慢性神经变性，疼痛，偏头痛和心脏肥大的Raf激酶抑制剂。 其中X是O，CH 2 CO，S或NH，或者X-R 1部分是氢; Y 1和Y 2独立地表示CH或N; Ar是可以任选取代的单或二稠合双环芳族或杂芳族基团; X 1和X 2之一选自O，S或NR 11，另一个是CH，其中R 11， / SUP>是氢，C 1-6烷基，芳基或芳基C 1-6烷基。