公开(公告)号：US08394836B2

公开(公告)日：2013-03-12

申请号：US12746104

申请日：2008-12-12

申请人： George Hynd ,  John Gary Montana ,  Harry Finch ,  Rosa Arienzo ,  Barbara Avitabile-Woo ,  Mathias Domostoj

发明人： George Hynd ,  John Gary Montana ,  Harry Finch ,  Rosa Arienzo ,  Barbara Avitabile-Woo ,  Mathias Domostoj

IPC分类号： A61K31/4439 ,  C07D409/12 ,  C07D401/12

CPC分类号： C07D209/12 ,  C07D209/04 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06 ,  C07D417/14

摘要： Compound of formula (I) are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions. Wherein X is —SO2— or *—SO2NR3— wherein the bond marked with an asterisk is attached to Ar1; R1 is hydrogen, fluoro, chloro, CN or CF3; R2 is hydrogen, fluoro or chloro; R3 is hydrogen, C1C8alkyl or C3-C7cycloalkyl; Ar1 is phenyl or a 5- or 6-membered heteroaryl group selected from furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3-C7cycloalkyl, —O(C1-C4alkyl) or C1C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and Ar2 is phenyl or 5- or 6-membered heteroaryl group selected from pyrrolyl, furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3-C3-C7cycloalkyl, —O(C1-C4alkyl) or C1C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms.

摘要翻译： 式（I）的化合物是CRTH2受体的配体，特别用于治疗炎性病症。 其中X是-SO 2 - 或* -SO 2 NR 3 - ，其中用星号附着的键连接到Ar1上; R1是氢，氟，氯，CN或CF3; R2是氢，氟或氯; R3是氢，C1C8烷基或C3-C7环烷基; Ar 1是苯基或选自呋喃基，噻吩基，恶唑基，噻唑基，咪唑基，吡唑基，异恶唑基，异噻唑基，吡啶基，哒嗪基，嘧啶基和吡嗪基的5-或6-元杂芳基，其中苯基或杂芳基任选被一个 或更多个独立地选自氟，氯，CN，C 3 -C 7环烷基，-O（C 1 -C 4烷基）或C 1 -C 6烷基的取代基，后两个基团任选被一个或多个氟原子取代; 并且Ar 2是苯基或选自吡咯基，呋喃基，噻吩基，恶唑基，噻唑基，咪唑基，吡唑基，异恶唑基，异噻唑基，吡啶基，哒嗪基，嘧啶基和吡嗪基中的5-或6-元杂芳基，其中苯基或杂芳基任选被取代 通过一个或多个独立地选自氟，氯，CN，C 3 -C 3 -C 7环烷基，-O（C 1 -C 4烷基）或C 1 -C 6烷基的取代基，后两个基团任选被一个或多个氟原子取代。