专利号:US-8591878-B2 优先权日:2008-02-25 标 题:Therapeutic compounds 发明人:MCCAULEY JOHN A; LIVERTON NIGEL J; HARPER STEVEN; MCINTYRE CHARLES J; RUDD MICHAEL T 权利人:MCCAULEY JOHN A; LIVERTON NIGEL J; HARPER STEVEN; MCINTYRE CHARLES J; RUDD MICHAEL T; MERCK SHARP & DOHME; ANGELETTI P IST RICHERCHE BIO 摘要:A class of macrocyclic compounds of formula (I), wherein R 1 , R 3 , R 4 , R a , R b , A, B, Z, M, W and n are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.
专利号:US-9738661-B2 优先权日:2006-10-27 标题:HCV NS3 protease inhibitors 发明人:LIVERTON NIGEL J; SUMMA VINCENZO; HARPER STEVEN; MCCAULEY JOHN A; ROMANO JOSEPH J; RUDD MICHAEL T 权利人:MERCK SHARP & DOHME; MSD ITALIA SRL 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.
参考标题:Screening For Covalent Inhibitors Using Dna-Display Of Small Molecule Libraries Functionalized With Cysteine Reactive Moieties 作者:C. Zambaldo,J.-P. Daguer,J. Saarbach,S. Barluenga,N. Winssinger 摘要:Despite The Resurging Interest In Covalent Inhibitors, Libraries Are Typically Designed With Synthon Filtered Out For Reactive Functionalities That Can Engage A Target Through Covalent Interactions. Herein, We Report The Synthesis Of Two Libraries Containing Michael Acceptors To Identify Cysteine Reactive Ligands. We Developed A Simple Procedure To Discriminate Between Covalent And High Affinity Non-Covalent
合成参考文献
摘要:Gribble, G. W., Science of Synthesis, (2006) 8, 398. 摘要:Larsen, R. D.; Cai, D., Science of Synthesis, (2005) 15, 472.