669008-25-7Relevant articles and documents
P2-quinazolinones and bis-macrocycles as new templates for next-generation hepatitis C virus NS3/4a protease inhibitors: Discovery of MK-2748 and MK-6325
Rudd, Michael T.,Butcher, John W.,Nguyen, Kevin T.,McIntyre, Charles J.,Romano, Joseph J.,Gilbert, Kevin F.,Bush, Kimberly J.,Liverton, Nigel J.,Holloway, M. Katharine,Harper, Steven,Ferrara, Marco,Difilippo, Marcello,Summa, Vincenzo,Swestock, John,Fritzen, Jeff,Carroll, Steven S.,Burlein, Christine,Dimuzio, Jillian M.,Gates, Adam,Graham, Donald J.,Huang, Qian,McClain, Stephanie,McHale, Carolyn,Stahlhut, Mark W.,Black, Stuart,Chase, Robert,Soriano, Aileen,Fandozzi, Christine M.,Taylor, Anne,Trainor, Nicole,Olsen, David B.,Coleman, Paul J.,Ludmerer, Steven W.,McCauley, John A.
supporting information, p. 727 - 735 (2015/04/14)
With the goal of identifying inhibitors of hepatitis C virus (HCV) NS3/4a protease that are potent against a wide range of genotypes and clinically relevant mutant viruses, several subseries of macrocycles were investigated based on observations made during the discovery of MK-5172. Quinazolinone-containing macrocycles were identified as promising leads, and optimization for superior cross-genotype and mutant enzyme potency as well as rat liver and plasma concentrations following oral dosing, led to the development of MK-2748. Additional investigation of a series of bis-macrocycles containing a fused 18- and 15-membered ring system were also optimized for the same properties, leading to the discovery of MK-6325. Both compounds display the broad genotype and mutant potency necessary for clinical development as next-generation HCV NS3/4a protease inhibitors.
Novel Compound for the Treatment of Hepatitis C
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Paragraph 0072; 0073, (2013/05/08)
The present invention provides (1aR,12bS)-8-cyclohexyl-11-fluoro-N-((1-methylcyclopropyl)sulfonyl)-1a-((3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl)-1,1a,2,12b-tetrahydrocyclopropa[d]indolo[2,1-a][2]benzazepine-5-carboxamide (formula I), including pharmaceutically acceptable salts, as well as compositions and methods of using the compound. The compound has activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
HEPATITIS C VIRUS INHIBITORS
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, (2009/12/02)
Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.