发明名称 Fatty acid COX inhibitor derivatives and their uses
摘要 The invention relates to fatty acid COX inhibitor derivatives; compositions comprising an effective amount of a fatty acid COX inhibitor derivative; and methods for treating or preventing a metabolic, autoimmune, inflammatory, or neurodegenerative disorder comprising the administration of an effective amount of a fatty acid COX inhibitor derivative.
申请公布号 US9216224(B2) 申请公布日期 2015.12.22
申请号 US201113582932 申请日期 2011.03.04
申请人 Catabasis Pharmaceuticals, Inc. 发明人 Milne Jill C.;Jirousek Michael R.;Bemis Jean E.;Vu Chi B.
分类号 A61K47/48 主分类号 A61K47/48
代理机构 Goodwin Procter LLP 代理人 Goodwin Procter LLP
主权项 1. A compound of Formula I:or a pharmaceutically acceptable salt, enantiomer, or stereoisomer thereof; wherein Rn is W1 and W2 are each independently S, NH, or NR; each a, b, c and d is independently —H, -D, —CH3, —OCH3, —OCH2CH3,—C(O)OR, or —O—Z, or benzyl, or two of a, b, c, and d can be taken together, along with the single carbon to which they are bound, to form a cycloalkyl or heterocycle; each n, o, p, and q is independently 0, 1 or 2; each L is independently null, —O—, —S—, —S(O)—, —S(O)2—, —S—S—, —(C1-C6alkyl)-, —(C3-C6cycloalkyl)-, a heterocycle, a heteroaryl, wherein the representation of L is not limited directionally left to right as is depicted, rather either the left side or the right side of L can be bound to the W1 side of the compound of Formula I; R6 is independently —H, -D, —C1-C4 alkyl, -halogen, cyano, oxo, thiooxo, —OH, —C(O)C1-C4 alkyl, —O-aryl, —O-benzyl, —OC(O)C1-C4 alkyl, C2-C3 alkene, C2-C3 alkyne, —C(O)C1-C4 alkyl, —NH2, —NH(C1-C3 alkyl), —N(C1-C3 alkyl)2, —NH(C(O)C1-C3 alkyl), —N(C(O)C1-C3 alkyl)2, —SH, —S(C1-C3 alkyl), —S(O)C1-C3 alkyl, or —S(O)2C1-C3 alkyl; each g is independently 2, 3 or 4; each h is independently 1, 2, 3 or 4; m is 0, 1, 2, or 3; if m is more than 1, then L can be the same or different; m1 is 0, 1, 2 or 3; k is 0, 1, 2, or 3; z is 1, 2, or 3; each R3 is independently H or C1-C6 alkyl, or both R3 groups, when taken together with the nitrogen to which they are attached, can form a heterocycle; each R4 is independently e, H or straight or branched C1-C10 alkyl which can be optionally substituted with OH, NH2, CO2R, CONH2, phenyl, C6H4OH, imidazole or arginine; each e is independently H or any side chain of a naturally occurring amino acid; each Z is independently —H with the proviso that there is at least one  in the compound; each r is independently 2, 3, or 7; each s is independently 3, 5, or 6; each t is independently 0 or 1; each v is independently 1, 2, or 6; R1 and R2 are each independently hydrogen, deuterium, —C1-C4 alkyl, -halogen, —OH, —C(O)C1-C4 alkyl, —O-aryl, —O-benzyl, —OC(O)C1—C4 alkyl, C2-C3 alkene, C2-C3 alkyne, —C(O)C1-C4 alkyl, —NH2, —NH(C1-C3 alkyl), —N(C1-C3 alkyl)2, —NH(C(O)C1-C3 alkyl), —N(C(O)C1-C3 alkyl)2, —SH, —S(C1-C3 alkyl), —S(O)C1-C3 alkyl, —S(O)2C1-C3 alkyl; and each R is independently —H, —C1-C3 alkyl, or straight or branched C1-C4 alkyl optionally substituted with OH, or halogen.
地址 Cambridge MA US
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