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1. 发明申请

WO2010142934A1 INDOLE DERIVATIVES AS LIGANDS OF CRTH2 RECEPTORS 审中-公开
标题翻译：作为CRTH2受体配体的衍生物
公开(公告)号：WO2010142934A1
公开(公告)日：2010-12-16
申请号：PCT/GB2009/050671
申请日：2009-06-12
申请人： PULMAGEN THERAPEUTICS (ASTHMA) LIMITED , HYND, George , MONTANA, John Gary , FINCH, Harry , ARIENZO, Rosa , AHMED, Shahadat
发明人： HYND, George , MONTANA, John Gary , FINCH, Harry , ARIENZO, Rosa , AHMED, Shahadat
IPC分类号： C07D209/10 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , A61P37/00 , A61K31/4439 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/06 , C07D417/14 , A61K31/4178 , A61K31/422 , A61K31/404
CPC分类号： C07D417/14 , C07D209/10 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： The following compounds are CRTH2 antagonists, useful in treatment of respiratory disease: {3-[3-chloro-4-(pyridine-2-sulfonyl)isothiazol-5-ylmethyl]-5-fluoro-2- methylindol-1-yl}acetic acid, [3-(5-benzenesulfonyl-3-methyl-3H-imidazol-4-ylmethyl)-5-fluoro-2- methylindol-1-yl]acetic acid, [3-(5-benzenesulfonyloxazol-4-ylmethyl)-5-fluoro-2-methylindol-1-yl]acetic acid, [3-(3-benzenesulfonyl-4-met ylthiophen-2-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, {5-fluoro-2-methyl-3-[2-(pyridin-2-ylsulfamoyl)benzyl]indol-1-yl}acetic acid, {5-fluoro-2-methyl-3-[4-methyl-3-(pyridine-2-sulfonyl)thiophen-2- ylmethyl]indol-1-yl}acetic acid, {5-fluoro-2-methyl-3-[3-methyl-5-(pyridine-2-sulfonyl)-3H-imidazol-4- ylmethyl]indol-1-yl}acetic acid, {5-fluoro-3-[2-(3-fluorophenylsulfamoyl)pyridin-3-ylmethyl]-2-methylindol-1- yl}acetic acid, [3-(4-benzenesulfonyloxazol-5-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, {3-[2-(3-cyanophenylsulfamoyl)benzyl]-5-fluoro-2-methylindol-1-yl}acetic acid, [3-(4-benzenesulfonylthiazol-5-ylmethyl)-5-chloro-2-methyl-indol-1-yl]acetic acid, [3-(4-benzenesulfonyl-2-methylthiazol-5-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, and [3-(4-benzenesulfonyl-3-methylisothiazol-5-ylmethyl)-5-fluoro-2- methylindol-1-yl]acetic acid.
摘要翻译：以下化合物是可用于治疗呼吸系统疾病的CRTH2拮抗剂：{3- [3-氯-4-（吡啶-2-磺酰基）异噻唑-5-基甲基] -5-氟-2-甲基吲哚-1-基} 乙酸，[3-（5-苯磺酰基-3-甲基-3H-咪唑-4-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸[3-（5-苯磺酰基恶唑-4-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸，[3-（3-苯磺酰基-4-甲基噻吩-2-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸， {5-氟-2-甲基-3- [2-（吡啶-2-基氨磺酰基）苄基]吲哚-1-基}乙酸{5-氟-2-甲基-3- [4-甲基-3- （吡啶-2-磺酰基）噻吩-2-基甲基]吲哚-1-基}乙酸{5-氟-2-甲基-3- [3-甲基-5-（吡啶-2-磺酰基）咪唑-4-基甲基]吲哚-1-基}乙酸，{5-氟-3- [2-（3-氟苯基氨磺酰基）吡啶-3-基甲基] -2-甲基吲哚-1-基}乙酸[3 - （4-苯磺酰氧基-5-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸{3- [2-（3-氰基苯基氨磺酰基）苄基] -5-氟-2-甲基吲哚-1-基] 乙酸，[3- （4-苯磺酰基噻唑-5-基甲基）-5-氯-2-甲基 - 吲哚-1-基]乙酸[3-（4-苯磺酰基-2-甲基噻唑-5-基甲基）-5-氟-2- 甲基吲哚-1-基]乙酸和[3-（4-苯磺酰基-3-甲基异噻唑-5-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸。

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