公开(公告)号：US20100311749A1

公开(公告)日：2010-12-09

申请号：US12739462

申请日：2008-10-24

申请人： Laura Jane Chambers ,  Katharine Laura Collis ,  David Kenneth Dean ,  Jorge Munoz-Muriedas ,  Jon Graham Anthony Steadman ,  Daryl Simon Walter

发明人： Laura Jane Chambers ,  Katharine Laura Collis ,  David Kenneth Dean ,  Jorge Munoz-Muriedas ,  Jon Graham Anthony Steadman ,  Daryl Simon Walter

IPC分类号： A61K31/5377 ,  C07D241/08 ,  A61K31/495 ,  C07D413/10 ,  C07D401/06 ,  A61K31/496 ,  C07D405/06 ,  C07D403/10 ,  A61P29/00 ,  A61P25/28 ,  A61P19/02

CPC分类号： C07D241/08 ,  C07D401/06 ,  C07D401/10 ,  C07D403/10 ,  C07D407/06

摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: A is C1-6alkyl, C3-6cycloalkyl, —CH2—R6, —CHMe-R7, —CMe2-R7, or optionally substituted aryl; wherein, when A is optionally substituted aryl, said aryl group is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of halogen, C1-6alkyl, —CF3, C1-4alkoxy, C1fluoroalkoxy, cyano, NR8R9, and pyridyl wherein the pyridyl is optionally substituted by one methyl; R1 is chlorine, fluorine, —CF3, cyano or C1-6alkyl; R2, R3 and R5 independently are hydrogen, fluorine, chlorine, —CF3, cyano or C1-6alkyl, such that at least one of R2, R3 and R5 is other than hydrogen; R4 is hydrogen. These compounds and salts are thought to be P2X7 receptor antagonists. The invention also provides for the treatment of pain, inflammation, rheumatoid arthritis, osteoarthritis, or a neurodegenerative disease.

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C 1-6烷基，C 3-6环烷基，-CH 2 -R 6，-CHMe-R 7，-CMe 2 -R 7或任选取代的芳基; 其中当A是任选取代的芳基时，所述芳基任选地被1至3个选自卤素，C 1-6烷基，-CF 3，C 1-4烷氧基，C 1-6烷氧基， 氰基，NR8R9和吡啶基，其中吡啶基任选被一个甲基取代; R1是氯，氟，-CF3，氰基或C1-6烷基; R2，R3和R5独立地是氢，氟，氯，-CF3，氰基或C1-6烷基，使得R2，R3和R5中的至少一个不是氢; R4是氢。 这些化合物和盐被认为是P2X7受体拮抗剂。 本发明还提供治疗疼痛，炎症，类风湿性关节炎，骨关节炎或神经变性疾病。