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    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

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

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

    IPC: C07D495/00

    CPC classification number: C07D487/04

    Abstract: 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.

    Abstract translation: 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。

    ISOTHIAZOLIDINE 1,1-DIOXIDE AND TETRAHYDRO-2H-1,2-THIAZINE 1,1-DIOXIDE DERIVATIVES AS P2X7 MODULATORS
    6.
    发明申请
    ISOTHIAZOLIDINE 1,1-DIOXIDE AND TETRAHYDRO-2H-1,2-THIAZINE 1,1-DIOXIDE DERIVATIVES AS P2X7 MODULATORS 审中-公开
    作为P2X7调节剂的异噻唑烷1,1-二氧化物和四氢-2H- 2H-1,2-噻唑烷-1,1-二氧化物衍生物

    公开(公告)号：US20100292224A1

    公开(公告)日：2010-11-18

    申请号：US12747995

    申请日：2008-12-05

    Applicant: Daryl Simon Walter

    Inventor： Daryl Simon Walter

    IPC: A61K31/54 ,  C07D275/03 ,  A61K31/425 ,  C07D279/02 ,  A61P29/00 ,  A61P25/28 ,  A61P25/00 ,  A61P25/14

    CPC classification number: C07D275/03 ,  C07D279/02

    Abstract: The present invention provides a compound of formula (1) or a pharmaceutically acceptable salt thereof: wherein R1 represents optionally substituted C1-4 alkyl; X represents —(CR10R11)n— in which n represents 1 or 2; R2, R3 and R4 independently represent H, F or Me; and R5; R6; R7; R8 and R9 independently represent hydrogen, halogen, or cyano; or optionally substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkyl, such that at least one of R5 and R9 represents a group other than hydrogen. 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 prevention of inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis or osteoarthritis.

    Abstract translation: 本发明提供式（1）化合物或其药学上可接受的盐：其中R 1表示任选取代的C 1-4烷基; X表示 - （CR10R11）n-，其中n表示1或2; R2，R3和R4独立地表示H，F或Me; 和R5; R6; R7; R8和R9独立地表示氢，卤素或氰基; 或任选取代的C 1-6烷基，C 2-6烯基，C 2-6炔基或C 3-6环烷基，使得R 5和R 9中的至少一个表示除氢以外的基团。 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炎性疼痛，神经性疼痛，内脏痛，类风湿性关节炎或骨关节炎中的用途。

    Piperidinone Carboxamide Derivatives as P2X7 Modulators
    7.
    发明申请
    Piperidinone Carboxamide Derivatives as P2X7 Modulators 审中-公开
    哌啶酮甲酰胺衍生物作为P2X7调节剂

    公开(公告)号：US20100168171A1

    公开(公告)日：2010-07-01

    申请号：US12593044

    申请日：2008-03-20

    Applicant: Paul John Beswick ,  Robert James Gleave ,  Jon Graham Anthony Steadman ,  Daryl Simon Walter

    Inventor： Paul John Beswick ,  Robert James Gleave ,  Jon Graham Anthony Steadman ,  Daryl Simon Walter

    IPC: A61K31/45 ,  C07D211/78 ,  A61P29/00 ,  A61P25/28

    CPC classification number: C07D211/78

    Abstract: 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 interfering with the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders 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.

    Abstract translation: 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受体功能并能够干扰ATP在P2X7受体上的作用。 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。

    Oxazolidine and Morpholine Carboxamide Derivatives as P2X7 Modulators
    8.
    发明申请
    Oxazolidine and Morpholine Carboxamide Derivatives as P2X7 Modulators 审中-公开
    恶唑烷和吗啉酰胺衍生物作为P2X7调节剂

    公开(公告)号：US20100144727A1

    公开(公告)日：2010-06-10

    申请号：US12593357

    申请日：2008-03-20

    Applicant: Paul John Beswick ,  Daryl Simon Walter

    Inventor： Paul John Beswick ,  Daryl Simon Walter

    IPC: A61K31/421 ,  C07D263/20 ,  C07D265/32 ,  A61K31/5375 ,  A61P25/00 ,  A61P29/00

    CPC classification number: C07D263/24 ,  C07D265/32

    Abstract: The present invention relates to a compound of formula (I): The compounds modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds, or pharmaceutical compositions thereof, in the treatment or prevention of disorders 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.

    Abstract translation: 本发明涉及式（I）化合物：该化合物调节P2X7受体功能并且能够拮抗ATP在P2X7受体上的作用。 本发明还提供了这些化合物或其药物组合物在治疗或预防P2X7受体介导的病症中的用途，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 疼痛。

    Receptor antagonists and their methods of use
    10.
    发明授权
    Receptor antagonists and their methods of use 有权
    受体拮抗剂及其使用方法

    公开(公告)号：US07718693B2

    公开(公告)日：2010-05-18

    申请号：US11772977

    申请日：2007-07-03

    Applicant: Daryl Simon Walter

    Inventor： Daryl Simon Walter

    IPC: A61K31/4015 ,  C07D207/04

    CPC classification number: C07D401/06 ,  C07D207/277

    Abstract: The present invention relates to novel oxo-prolinamide derivatives of formula (I) which modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.

    Abstract translation: 本发明涉及调节P2X7受体功能并能够拮抗ATP在P2X7受体上的作用的式（I）的新型氧代 - 脯氨酰胺衍生物，以及这些化合物或其药物组合物在治疗由 P2X7受体，例如疼痛，炎症和神经变性。

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