[EN] SUBSTITUTED AROMATIC COMPOUNDS AND RELATED METHOD FOR THE TREATMENT OF FIBROSIS<br/>[FR] COMPOSÉS AROMATIQUES SUBSTITUÉS ET PROCÉDÉ ASSOCIÉ POUR LE TRAITEMENT DE LA FIBROSE
申请人:PROMETIC BIOSCIENCES INC
公开号:WO2014138906A1
公开(公告)日:2014-09-18
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的制备:或其药用盐,其中A为C5烷基、C6烷基、C5烯基、C6烯基、C(0)-(CH2)n-CH3或CH(OH)-(CH2)n-CH3,其中n为3或4;R1为H、F或OH;R2为C5烷基、C6烷基、C5烯基、C6烯基、C(0)-(CH2)n-CH3或CH(OH)-(CH2)n-CH3,其中n为3或4;R3为H、F、OH或CH2Ph;R4为H、F或OH;Q为1)(CH2)mC(0)OH,其中m为1或2,2)CH(CH3)C(0)OH,3)C(CH3)2C(0)OH,4)CH(F)-C(0)OH,5)CF2-C(0)OH,或6)C(0)-C(0)OH;以及包含该化合物的组合物和使用该化合物预防或治疗受试者各种纤维化疾病和状况的方法,包括肺纤维化、肝纤维化、皮肤纤维化、肾纤维化、胰腺纤维化、系统性硬化病、心肌纤维化或黄斑变性。