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    • 28. 发明申请
    • ISOTHIAZOLIDINE 1,1-DIOXIDE AND TETRAHYDRO-2H-1,2-THIAZINE 1,1-DIOXIDE DERIVATIVES AS P2X7 MODULATORS
    • 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
    • WO2009077362A1
    • 2009-06-25
    • PCT/EP2008/066945
    • 2008-12-05
    • GLAXO GROUP LIMITEDWALTER, Daryl Simon
    • WALTER, Daryl Simon
    • C07D275/02C07D279/02A61K31/41A61K31/54
    • C07D275/03C07D279/02
    • The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof:(formula) wherein: R 1 represents optionally substituted C 1-4 alkyl; X represents -(CR 10 R 11 ) n - in which n represents 1 or 2; R 2 , R 3 and R 4 independently represent H, F or Me; and R 5 , R 6 ; R 7 ; R 8 and R 9 independently represent hydrogen, halogen, or cyano; or optionally substituted C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl or C 3-6 cycloalkyl, such that at least one of R 5 and R 9 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.
    • 本发明提供式(I)化合物或其药学上可接受的盐:(式)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。