862119-82-2Relevant articles and documents
Discovery of danoprevir (ITMN-191/R7227), a highly selective and potent inhibitor of hepatitis C virus (HCV) NS3/4A protease
Jiang, Yutong,Andrews, Steven W.,Condroski, Kevin R.,Buckman, Brad,Serebryany, Vlad,Wenglowsky, Steve,Kennedy, April L.,Madduru, Machender R.,Wang, Bin,Lyon, Michael,Doherty, George A.,Woodard, Benjamin T.,Lemieux, Christine,Do, Mary Geck,Zhang, Hailong,Ballard, Joshua,Vigers, Guy,Brandhuber, Barbra J.,Stengel, Peter,Josey, John A.,Beigelman, Leonid,Blatt, Lawrence,Seiwert, Scott D.
, p. 1753 - 1769 (2014/04/03)
HCV serine protease NS3 represents an attractive drug target because it is not only essential for viral replication but also implicated in the viral evasion of the host immune response pathway through direct cleavage of key proteins in the human innate im
Macrocylic Inhibitors of Hepatitis C Virus
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Page/Page column 46, (2009/05/28)
Compounds of the formula I: and N-oxides, salts, and stereoisomers thereof wherein A is OR1, NHS(═O)pR2; wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl;R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl;p is independently 1 or 2;n is 3, 4, 5 or 6; — denotes an optional double bond;L is N or CRz; Rz is H or forms a double bond with the asterisked carbon;Rq is H or when L is CRz, Rq can also be C1-C6alkyl;Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C1-C6 alkyl, C1-C6alkoxy, hydroxyl, halo, haloC1-C6alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C1-C6alkyl-carbonylamino, C0-C3alkylenecarbocyclyl and C0-C3 alkyleneheterocyclyl;R5 is hydrogen, C1-C6alkyl, C1-C6alkoxyC1-C6alkyl or C3-C7cycloalkyl;R6 is hydrogen, C1-C6alkyl, C1-C6alkoxy, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV
Process for the preparation of a macrocycle
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Page/Page column 11-12, (2009/07/10)
The present invention relates to a new process for the preparation of macrocyclic HCV protease inhibitor compounds of the formula wherein R1 is an amino protecting group and X is halogen by way of a ring closing metathesis approach.