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    • 5. 发明公开
    • SUBSTITUTED AROMATIC COMPOUNDS AND RELATED METHOD FOR THE TREATMENT OF FIBROSIS
    • 取代芳香族化合物及其治疗纤维化的相关方法
    • EP2970089A1
    • 2016-01-20
    • EP14764458.7
    • 2014-03-14
    • ProMetic BioSciences Inc.
    • ZACHARIE, BoulosABBOTT, ShaunGAGNON, LyneLAURIN, PierreGROUIX, Brigitte
    • C07C59/52A61K31/192A61P19/04C07C57/32
    • C07C53/134A61K31/192C07C57/30C07C57/58C07C59/52Y02A50/423
    • The present invention relates to compounds of: or a pharmaceutically acceptable salt thereof, wherein A is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(0)-(CH2)n-CH3 or CH(OH)—(CH2)n-CH3 wherein n is 3 or 4; R1 is H, F or OH; R2 is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(0)-(CH2)n-CH3 or CH(OH)—(CH2)n-CH3 wherein n is 3 or 4; R3 is H, F, OH or CH2Ph; R4 is H, F or OH; Q is 1) (CH2)mC(0)OH wherein m is 1 or 2, 2) CH(CH3)C(0)OH, 3) C(CH3)2C(0)OH, 4) CH(F)—C(0)OH, 5) CF2-C(0)OH, or 6) C(0)-C(0)OH; and compositions comprising the same and the method using the same for the prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis, renal fibrosis, pancreas fibrosis, systemic sclerosis, cardiac fibrosis or macular degeneration.
    • 本发明涉及以下化合物或其药学上可接受的盐,其中A为C 5烷基,C 6烷基,C 5烯基,C 6烯基,C(O) - (CH 2)n -CH 3或CH( OH) - (CH 2)n -CH 3其中n是3或4; R 1是H,F或OH; R 2是C 5烷基,C 6烷基,C 5烯基,C 6烯基,C(O) - (CH 2)n -CH 3或CH(OH) - (CH 2)n -CH 3,其中n是3 或4; R 3是H,F,OH或CH 2 Ph; R 4是H,F或OH; Q是1)(CH 2)mC(O)OH,其中m是1或2,2,2)CH(CH 3)C(O)OH,3)C(CH 3)2 C(O)OH,4)CH F)-C(O)OH,5)CF 2 -C(O)OH,或6)C(O)-C(O)OH; 和组合物,其包括相同的,并且使用用于各种纤维变性疾病和病症的受试者,包括肺纤维化,肝纤维化,皮肤纤维化,肾纤维化,胰纤维化,系统性硬化症,心脏纤维化或黄斑变性的预防或治疗的相同的方法。