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1. 发明申请

US20110136879A1 COMPOUND 有权
标题翻译：复合
公开(公告)号：US20110136879A1
公开(公告)日：2011-06-09
申请号：US12897510
申请日：2010-10-04
申请人： George Kokotos , Berit Johansen , Victoria Magrioti , Michael Tsakos
发明人： George Kokotos , Berit Johansen , Victoria Magrioti , Michael Tsakos
IPC分类号： A61K31/426 , C07D277/24 , C07D277/56 , C07D277/64 , A61K31/428 , A61P29/00 , A61P17/06 , A61P19/02 , A61P17/00 , A61P17/08 , A61P25/00 , A61P1/04 , A61P1/00 , A61P9/00
CPC分类号： C07D277/64 , A61K31/421 , A61K31/423 , A61K31/426 , A61K31/428 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/56
摘要： The invention provides compounds of formula (I) wherein X is O or S; R1 is H, OH, SH, nitro, NH2, NHC1-6alkyl, N(C1-6alkyl)2, halo, haloC1-6alkyl, CN, C1-6-alkyl, OC1-6alkyl, C1-6alkylCOOH, C1-6alkylCOOC1-6alkyl, C2-6-alkenyl, C3-10cycloalkyl, C6-10aryl, C1-6alkylC6-10aryl, heterocyclyl, heteroaryl, CONH2, CONHC1-6alkyl, CON(C1-6alkyl)2, OCOC1-6alkyl, or is an acidic group, such as a group comprising a carboxyl, phosphate, phosphinate, sulfate, sulfonate, or tetrazolyl group; R2 is as defined for R1 or R1 and R2 taken together can form a 6-membered aromatic ring optionally substituted by up to 4 groups R5; R3 is H, halo (preferably fluoro), or CHal3 (preferably CF3), each R5 is defined as for R1; V1 is a covalent bond or a C1-20alkyl group, or C2-20-mono or multiply unsaturated alkenyl group; said alkyl or alkenyl groups being optionally interupted by one or more heteroatoms selected from O, NH, N(C1-6 alkyl), S, SO, or SO2; M1 is absent or is a C5-10 cyclic group or a C5-15 aromatic group; and R4 is H, halo, OH, CN, nitro, NH2, NHC1-6alkyl, N(C1-6alkyl)2, haloC1-6alkyl, a C1-20alkyl group, or C2-20-mono or multiply unsaturated alkenyl group, said C1-20alkyl or C2-20alkenyl groups being optionally interupted by one or more heteroatoms selected from O, NH, N(C1-6 alkyl), S, SO, or SO2; with the proviso that the group V1M1R4 as a whole provides at least 4 backbone atoms from the C(R3) group; or a salt, ester, solvate, N-oxide, or prodrug thereof; for use in the treatment of a chronic inflammatory condition.
摘要翻译：本发明提供式（I）化合物，其中X是O或S; R1是H，OH，SH，硝基，NH2，NHC1-6烷基，N（C1-6烷基）2，卤素，卤代C 1-6烷基，CN，C 1-6 - 烷基，OC 1-6烷基，C 1-6烷基COOH，C 1-6烷基COOC- C 1-6烷基，C 2-6烯基，C 3-10环烷基，C 6-10芳基，C 1-6烷基C 6-10芳基，杂环基，杂芳基，CONH 2，CONHC 1-6烷基，CON（C 1-6烷基）2，OCOC 1-6烷基，或者是酸性基团，例如包括羧基，磷酸根，次膦酸根，硫酸根，磺酸根或四唑基的基团; R2如R1或R1和R2所定义，可以一起形成任选被至多4个R 5基团取代的6元芳环; R 3是H，卤素（优选氟）或CHal 3（优选CF 3），每个R 5定义为R 1; V1是共价键或C 1-20烷基，或C 2-20 - 单或多不饱和烯基; 所述烷基或烯基任选地被一个或多个选自O，NH，N（C 1-6烷基），S，SO或SO 2的杂原子中间化; M1不存在或是C5-10环基或C5-15芳基; 和R 4是H，卤素，OH，CN，硝基，NH 2，NHC 1-6烷基，N（C 1-6烷基）2，卤代C 1-6烷基，C 1-20烷基或C 2-20 - 单或多不饱和烯基， C 1-20烷基或C 2-20烯基任选地被一个或多个选自O，NH，N（C 1-6烷基），S，SO或SO 2的杂原子中间化; 条件是V1M1R4基团作为整体从C（R 3）基团提供至少4个骨架原子; 或其盐，酯，溶剂化物，N-氧化物或前药; 用于治疗慢性炎症性疾病。

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