82110-21-2Relevant articles and documents
Discovery of MK-6169, a Potent Pan-Genotype Hepatitis C Virus NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Substitutions
Yu, Wensheng,Tong, Ling,Selyutin, Oleg,Chen, Lei,Hu, Bin,Zhong, Bin,Hao, Jinglai,Ji, Tao,Zan, Shuai,Yin, Jingjun,Ruck, Rebecca T.,Curry, Stephanie,McMonagle, Patricia,Agrawal, Sony,Rokosz, Laura,Carr, Donna,Ingravallo, Paul,Bystol, Karin,Lahser, Frederick,Liu, Rong,Chen, Shiying,Feng, Kung-I,Cartwright, Mark,Asante-Appiah, Ernest,Kozlowski, Joseph A.
, p. 3984 - 4003 (2018/05/14)
We describe the discovery of MK-6169, a potent and pan-genotype hepatitis C virus NS5A inhibitor with optimized activity against common resistance-associated substitutions. SAR studies around the combination of changes to both the valine and aminal carbon region of elbasvir led to the discovery of a series of compounds with substantially improved potency against common resistance-associated substitutions in the major genotypes, as well as good pharmacokinetics in both rat and dog. Through further optimization of key leads from this effort, MK-6169 (21) was discovered as a preclinical candidate for further development.
TRICYCLIC INHIBITORS OF 5-LIPOXYGENASE
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Page/Page column 89, (2010/11/28)
Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders.
5-lipoxygenase inhibitors quinoxalinyl derivatives
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, (2008/06/13)
The invention concerns a heterocyclic derivative of the formula I STR1 wherein Q is an optionally substituted quinoxalinyl or a hydrogenated derivative thereof X1 is oxy, thio, sulphinyl, sulphonyl or imino; Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms; R1 is (1-6C)alkyl, (3-6C)alkenyl or (3-6C)alkynyl; and R2 and R3 together form a group of the formula --A2 --X2 --A3 -- which, together with the carbon atom to which A2 and A3 are attached, defines a ring having 4 to 7 ring atoms, wherein A2 and A3, which may be the same or different, each is (1-4C)alkylene and X2 is oxy, thio, sulphinyl, sulphonyl or imino; or a pharmaceutically-acceptable salt thereof. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.