- Discovery of Quinoxaline-Based P1-P3 Macrocyclic NS3/4A Protease Inhibitors with Potent Activity against Drug-Resistant Hepatitis C Virus Variants
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The three pan-genotypic HCV NS3/4A protease inhibitors (PIs) currently in clinical use - grazoprevir, glecaprevir, and voxilaprevir - are quinoxaline-based P2-P4 macrocycles and thus exhibit similar resistance profiles. Using our quinoxaline-based P1-P3 m
- Nageswara Rao, Desaboini,Zephyr, Jacqueto,Henes, Mina,Chan, Elise T.,Matthew, Ashley N.,Hedger, Adam K.,Conway, Hasahn L.,Saeed, Mohsan,Newton, Alicia,Petropoulos, Christos J.,Huang, Wei,Kurt Yilmaz, Nese,Schiffer, Celia A.,Ali, Akbar
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supporting information
p. 11972 - 11989
(2021/09/06)
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- HEPATITIS C VIRUS NS3/4A PROTEASE INHIBITORS
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The invention provides novel classes of HCV therapeutics that are orally available, safe and effective HCV NS3/4A protease inhibitors and are less susceptible to drug resistance than existing therapeutics. The invention also relates to pharmaceutical comp
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Paragraph 00133-00134; 00147; 00160
(2020/12/29)
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- 2-ACYLAMIDOMETHYL AND SULFONYLAMIDOMETHYL BENZOXAZINE CARBAMATES FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
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The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, Ra, Rb, Rc, Rd, Rg, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
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Paragraph 0262
(2015/07/07)
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- NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION
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The present invention relates to a compound of Formula (I): wherein: n is 0 or 1; X is O or CH2; R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H
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Page/Page column 34
(2010/11/03)
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- NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION
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The present invention relates to a compound of Formula (I): wherein: R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H or C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents
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Page/Page column 32
(2010/11/04)
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