1028252-15-4Relevant academic research and scientific papers
The discovery of asunaprevir (BMS-650032), an orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection
Scola, Paul M.,Sun, Li-Qiang,Wang, Alan Xiangdong,Chen, Jie,Sin, Ny,Venables, Brian L.,Sit, Sing-Yuen,Chen, Yan,Cocuzza, Anthony,Bilder, Donna M.,D'Andrea, Stanley V.,Zheng, Barbara,Hewawasam, Piyasena,Tu, Yong,Friborg, Jacques,Falk, Paul,Hernandez, Dennis,Levine, Steven,Chen, Chaoqun,Yu, Fei,Sheaffer, Amy K.,Zhai, Guangzhi,Barry, Diana,Knipe, Jay O.,Han, Yong-Hae,Schartman, Richard,Donoso, Maria,Mosure, Kathy,Sinz, Michael W.,Zvyaga, Tatyana,Good, Andrew C.,Rajamani, Ramkumar,Kish, Kevin,Tredup, Jeffrey,Klei, Herbert E.,Gao, Qi,Mueller, Luciano,Colonno, Richard J.,Grasela, Dennis M.,Adams, Stephen P.,Loy, James,Levesque, Paul C.,Sun, Huabin,Shi, Hong,Sun, Lucy,Warner, William,Li, Danshi,Zhu, Jialong,Meanwell, Nicholas A.,McPhee, Fiona
, p. 1730 - 1752 (2014/04/03)
The discovery of asunaprevir (BMS-650032, 24) is described. This tripeptidic acylsulfonamide inhibitor of the NS3/4A enzyme is currently in phase III clinical trials for the treatment of hepatitis C virus infection. The discovery of 24 was enabled by employing an isolated rabbit heart model to screen for the cardiovascular (CV) liabilities (changes to HR and SNRT) that were responsible for the discontinuation of an earlier lead from this chemical series, BMS-605339 (1), from clinical trials. The structure-activity relationships (SARs) developed with respect to CV effects established that small structural changes to the P2* subsite of the molecule had a significant impact on the CV profile of a given compound. The antiviral activity, preclincial PK profile, and toxicology studies in rat and dog supported clinical development of BMS-650032 (24).
TRIPEPTIDES INCORPORATING DEUTERIUM AS INHIBITORS OF HEPATITIS C VIRUS
-
, (2013/02/27)
Hepatitis C virus inhibitors having the general formula (I) [INSERT CHEMICAL STRUCTURE HERE] are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
CRYSTALLINE FORMS OF N-(TERT-BUTOXYCARBONYL)-3-METHYL-L-VALYL-(4R)-4-((7-CHLORO-4-METHOXY-1-ISOQUINOLINYL)OXY)-N-((1R,2S)-1-((CYCLOPROPYLSULFONYL)CARBAMOYL)-2-VINYLCYCLOPROPYL)-L-PROLINAMIDE
-
Page/Page column 25, (2009/08/14)
The present disclosure generally relates to crystalline forms of N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-((7-chloro-4-methoxy-1-isoquinolinyl)oxy)-N-((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-L-prolinamide. The present disclosure also generally relates to a pharmaceutical composition comprising one or more of the crystalline forms, as well of methods of using the crystalline forms in the treatment of Hepatitis C virus (HCV) and methods for obtaining such crystalline forms.
Hepatitis C Virus Inhibitors
-
Page/Page column 37-38, (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.
Hepatitis C Virus Inhibitors
-
Page/Page column 17; 19, (2009/12/05)
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.
