862119-82-2Relevant academic research and scientific papers
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
MACROCYCLIC INHIBITORS OF HEPATITIS C PROTEASE
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Page/Page column 83-84, (2010/04/25)
The invention provides macrocyclic compounds inhibitory to the Hepatitis C viral protease, compositions and combinations including the compounds, methods of treatment of conditions wherein inhibition of the Hepatitis C viral protease is medically indicated, and methods of treatment of a Hepatitis C viral infection in a human patient.
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
Macrocyclic Inhibitors of Hepatitis C Virus
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Page/Page column 45-46, (2009/02/11)
Compounds of the formula (I): and N-oxides, salts and stereoisomers thereof wherein A is OR1, NHS(═O)pR2, NHR3, NRaRb, C(═O)NHR3 or C(═O)NRaRb wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl; R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl or NRaRb; R3 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl, —OC1-C6alkyl, —OC0-C3alkylenecarbocyclyl, —OC0-C3alkyleneheterocyclyl; wherein any alkyl, carbocyclyl or heterocycylyl in R1, R2 or R3 are optionally substituted p is independently 1 or 2; n is 3, 4, 5 or 6; denotes an optional double bond; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Ry and Ry′ are independently C1-C6alkyl; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; W is —CH2—, —O—, —OC(═O)NH—, —OC(═O)—, —S—, —NH—, —NRa, —NHS(═O)2—, —NHC(=0)NH— or —NHC(═O)—, —NHC(═S)NH— or a bond; R8 is an optionally substituted ring system containing 1 or 2 saturated, partially saturated or unsaturated carbo or heterocyclic rings have utility in the inhibition of NS-3 serine proteases, such as flavivirus infections.
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.
MACROCYCLIC PEPTIDES AS HEPATITIS C VIRUS INHIBITORS
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, (2008/12/05)
Macrocyclic peptides having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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Page/Page column 95-96, (2008/06/13)
The embodiments provide compounds of the general Formula (I), as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments provide compounds of the general Formula (II), as well as compositions, including
Inhibitors of Hepatitis C Virus
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, (2008/12/04)
Macrocyclic peptides are disclosed having the general formula: wherein R3, R3′, R4, R6, R′, X, Q and W are described. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Inhibitors of Hepatitis C Virus
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, (2008/12/04)
Macrocyclic peptides are disclosed having the general formula: wherein R3, R′3, R4, R6, R′, X, Q and W are described. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Process for the preparation of macrocyclic compounds
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Page/Page column 5, (2008/12/04)
The present invention relates to a new process for the preparation of diene compounds of the formula I wherein R1 is an amino protecting group and X is a halogen atom which may serve as intermediates for the manufacture of macrocyclic HCV protease inhibitors.
