799274-04-7Relevant articles and documents
PYRIDINE COMPOUND SUBSTITUTED WITH AZOLE
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Paragraph 1277, (2020/07/07)
The present invention provides a compound represented by formula [I] shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme. (in formula [I] above, the structure represented by formula [II] below: represents any of the structures represented by formula group [III] below: R1, R2, R3, and R4 independently represent a hydrogen atom, a fluorine atom, methyl, or the like, R5 represents any of the structures represented by formula group [IV]:
Toward the back-up of Boceprevir (SCH 503034): Discovery of new extended P4-capped ketoamide inhibitors of hepatitis C virus NS3 serine protease with improved potency and pharmacokinetic profiles
Bogen, Stéphane L.,Pan, Weidong,Ruan, Sumei,Nair, Latha G.,Arasappan, Ashok,Bennett, Frank,Chen, Kevin X.,Jao, Edwin,Venkatraman, Srikanth,Vibulbhan, Bancha,Liu, Rong,Cheng, Kuo-Chi,Guo, Zhuyan,Tong, Xiao,Saksena, Anil K.,Girijavallabhan, Viyyoor,Njoroge, F. George
scheme or table, p. 3679 - 3688 (2010/04/05)
Hepatitis C is the most prevalent liver disease. Viral hepatitis C (HCV), a small (+)-RNA virus, infects chronically an estimated 300 million people worldwide. Results of Phase I clinical studies with our first generation HCV inhibitor Boceprevir, SCH 503034 (1), presented at the 56th Annual Meeting of the American Association for the Study of Liver Diseases (AASLD) were encouraging, and thus, additional human clinical studies are underway. In view of the positive data from our first generation compound, further work aimed at optimizing its overall profile was undertaken. Herein, we report that extension of our earlier inhibitor to the P4 pocket and optimization of the P1′ capping led to the discovery of new ketoamide inhibitors of the HCV NS3 serine protease with improved in vitro potency. In addition to being potent inhibitors of HCV subgenomic RNA replication, some of the new P4-capped inhibitors were also found to have improved PK profile.
Inhibitors of HCV replication
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Page/Page column 211, (2010/10/20)
Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.