发明名称 Cyclosporin analogues for preventing or treating hepatitis C infection
摘要 The present invention relates to novel cyclosporine analogs having antiviral activity against HCV and useful in the treatment of HCV infections. More particularly, the invention relates to novel cyclosporine analog compounds, compositions containing such compounds and methods for using the same, as well as processes for making such compounds.
申请公布号 US9616099(B2) 申请公布日期 2017.04.11
申请号 US201514948876 申请日期 2015.11.23
申请人 Enanta Pharmaceuticals, Inc. 发明人 Or Yat Sun;Wang Guoqiang;Long Jiang;Kim In Jong
分类号 A61K45/06;A61K38/13;C07K7/64;A61K38/21;A61K38/00 主分类号 A61K45/06
代理机构 Elmore Patent Law Group, P.C. 代理人 Harlan Edgar W.;Elmore, Esq. Carolyn S.;Elmore Patent Law Group, P.C.
主权项 1. A compound represented by the formula:or a pharmaceutically acceptable salt thereof, wherein R1 is C1-C5-alkyl-Y or C2-C5-alkenyl-Y, where Y is H; optionally substituted aryl, optionally substituted heterocyclyl; —OC(O)R5; NR5R6; OH; —O—(CH2)n—W, where n is 1 to 4 and W is heterocyclyl; —OC(O)NR5R6; —C(O)H; —CH═NOZ, where Z is H, or alkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, each optionally substituted; —CH(OR5)2; —SC(O)R5; —SH; —OSO2R5; —C(O)OH; or —C(O)N(R8)OH, where R8 is hydrogen or C1-C4-alkyl; N3; —CN; or halogen; A is (a) C3-C4-alkyl-X, where X is H; OH; optionally substituted phenyl; optionally substituted —O-phenyl; optionally substituted —S-phenyl; optionally substituted 5-membered heteroaryl; optionally substituted —O-5-membered heteroaryl; optionally substituted —S-5-membered heteroaryl; —OC(O)NR5R6, —NHC(O)OR5, C(O)OR7, —OC(O)OR7, —CN, —N3, —C(O)NR5R6, —C(O)R5, optionally substituted —OSO2-phenyl, —NHC(O)R5 or —NR5R6; or (b) C3-C4-alkenyl-X′, where X′ is OH; optionally substituted phenyl; optionally substituted —O-phenyl; optionally substituted —S-phenyl; optionally substituted 5-membered heteroaryl; optionally substituted —O-5-membered heteroaryl; optionally substituted —S-5-membered heteroaryl; —OC(O)NR5R6, —NHC(O)OR5, C(O)OR7, —OC(O)OR7, —CN, —N3, —C(O)NR5R6, —C(O)R5, optionally substituted —OSO2-phenyl, —NHC(O)R5, or —NR5R6; each R5 and R6 is independently H; optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; alternatively, R5, R6 and the nitrogen atom to which they are attached form an optionally substituted heterocyclic; R7 is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; andR2, R3 and R4 are independently selected from: hydrogen and methyl.
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