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3. 发明公开

EP2327693A1 Indoles and their therapeutic use 有权
标题翻译： Indole und ihre therapeutische Verwendung
公开(公告)号：EP2327693A1
公开(公告)日：2011-06-01
申请号：EP10193389.3
申请日：2008-12-12
申请人： Pulmagen Therapeutics (Asthma) Limited
发明人： Hynd, George , Montana, John Gary , Finch, Harry , Arienzo, Rosa , Avitabile-Woo, Barbara , Domostoj, Mathias
IPC分类号： C07D209/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/14 , C07D417/06 , A61K31/404
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 are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions:

wherein X is -SO 2 - or *-SO 2 NR 3 - wherein the bond marked with an asterisk is attached to Ar 1 ; R 1 is hydrogen, fluoro, chloro, CN or CF 3 ; R 2 is hydrogen, fluoro or chloro; R 3 is hydrogen, C 1 -C 8 alkyl or C 3 -C 7 cycloalkyl; Ar 1 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, C 3 -C 7 cycloalkyl, -O(C 1 -C 4 alkyl) or C 1 -C 6 alkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and Ar 2 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, C 3 -C 7 cyCloalkyl, -O(C 1 -C 4 alkyl) or C 1 -C 6 alkyl, the latter two groups being optionally substituted by one or more fluoro atoms.
摘要翻译：式（I）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 - ，其中标有星号的键连接到Ar 1 ; R 1是氢，氟，氯，CN或CF 3; R 2是氢，氟或氯; R 3是氢，C 1 -C 8烷基或C 3 -C 7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，后两个基团任选地被一个或多个氟原子; 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，其中苯基或杂芳基是任选的被一个或多个独立地选自氟，氯，CN，C 3 -C 7环烷基，-O（C 1 -C 4烷基）或C 1 -C 6烷基的取代基取代，后两个基团任选地被一个或多个更多的氟原子。

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