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    • 1. 发明申请
    • INDOLE DERIVATIVES AS LIGANDS OF CRTH2 RECEPTORS
    • 作为CRTH2受体配体的衍生物
    • WO2010142934A1
    • 2010-12-16
    • PCT/GB2009/050671
    • 2009-06-12
    • PULMAGEN THERAPEUTICS (ASTHMA) LIMITEDHYND, GeorgeMONTANA, John GaryFINCH, HarryARIENZO, RosaAHMED, Shahadat
    • HYND, GeorgeMONTANA, John GaryFINCH, HarryARIENZO, RosaAHMED, Shahadat
    • C07D209/10C07D401/06C07D401/12C07D401/14C07D403/06A61P37/00A61K31/4439C07D409/06C07D409/14C07D413/06C07D417/06C07D417/14A61K31/4178A61K31/422A61K31/404
    • C07D417/14C07D209/10C07D401/06C07D401/12C07D401/14C07D403/06C07D409/06C07D413/06C07D417/06
    • 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.
    • 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。