公开(公告)号：US11524930B2

公开(公告)日：2022-12-13

申请号：US16780316

申请日：2020-02-03

申请人： LIMINAL BIOSCIENCES LIMITED

发明人： Boulos Zacharie ,  Shaun Abbott ,  Lyne Gagnon ,  Pierre Laurin ,  Brigitte Grouix

IPC分类号： C07C53/134 ,  C07C57/30 ,  C07C57/58 ,  A61K31/192 ,  C07C59/52

摘要： 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(O)—(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(O)—(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(O)OH wherein m is 1 or 2, 2) CH(CH3)C(O)OH, 3) C(CH3)2C(O)OH, 4) CH(F)—C(O)OH, 5) CF2—C(O)OH, or 6) C(O)—C(O)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.