专利号:US-2012095211-A1 优先权日:2010-09-22 标 题 :Substituted proline inhibitors of hepatitis c virus replication 发明人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D 权利人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D; INTERMUNE INC 摘要:The embodiments provide compounds of the general Formulae I, Ia, II, IIa, III, IIIa, IIIb, IV, IVa, IVb, V, Va, Vb, VI, VIa, VIb, and VIc, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. The embodiments also provide methods for the synthesis of subject compounds and intermediates in the synthetic methods.
专利号:US-8987195-B2 优先权日:2012-08-08 标 题:HCV NS3 protease inhibitors 发明人:BARA THOMAS; BHAT SATHESH; BISWAS DIPSHIKHA; BROCKUNIER LINDA; BURNETT DUANE A; CHACKALAMANNIL SAMUEL; CHELLIAH MARIAPPAN V; CHEN AUSTIN; CLASBY MARTIN; COLANDREA VINCE J; GUO ZHUYAN; HAN YONGXIN; JAYNE CHARLES; JOSIEN HUBERT; MARCANTONIO KAREN; MIAO SHOUWU; NEELAMKAVIL SANTHOSH; PINTO PATRICK; RAJAGOPALAN MURALI; SHAH UNMESH; VELAZQUEZ FRANCISCO; VENKATRAMAN SRIKANTH; XIA YAN 权利人:MERCK SHARP & DOHME; MERCK CANADA INC 摘要:The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.
专利号:US-9328138-B2 优先权日:2011-11-15 标题:HCV NS3 protease inhibitors 发明人:RUDD MICHAEL T; MCCAULEY JOHN; LIVERTON NIGEL; GRISÉ-BARD CHRISTIANE; BROCHU MARIE-CHRISTINE; CHARRON SYLVIE; AULAKH VIRENDER; BACHAND BENOIT; BEAULIEU PATRICK; ZAGHDANE HELMI; HAN YONGXIN; FERRARA MARCO; HARPER STEVEN; SUMMA VINCENZO; CHACKALAMANNIL SAMUEL; VENKATRAMAN SRIKANTH; SHAH UNMESH; VELAZQUEZ FRANCISCO 权利人:MERCK SHARP & DOHME; MSD ITALIA SRL; MERCK CANADA INC 摘要:The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
参考文献:10.1055/s-0031-1290373 摘要:Fülöp F, Kiss L, Nonn M. Syntheses of Isoxazoline-Based Amino Acids by Cycloaddition of Nitrile Oxides and Their Conversion into Highly Functionalized Bioactive Amino Acid Derivatives. Synthesis. 2012 Jun 05;44(13):1951–63. doi: 10.1055/s-0031-1290373.