104654-66-2Relevant academic research and scientific papers
Discovery of narlaprevir (SCH 900518): A potent, second generation HCV NS3 serine protease inhibitor
Arasappan, Ashok,Bennett, Frank,Bogen, Stephane L.,Venkatraman, Srikanth,Blackman, Melissa,Chen, Kevin X.,Hendrata, Siska,Huang, Yuhua,Huelgas, Regina M.,Nair, Latha,Padilla, Angela I.,Pan, Weidong,Pike, Russell,Pinto, Patrick,Ruan, Sumei,Sannigrahi, Mousumi,Velazquez, Francisco,Vibulbhan, Bancha,Wu, Wanli,Yang, Weiying,Saksena, Anil K.,Girijavallabhan, Viyyoor,Shih, Neng-Yang,Kong, Jianshe,Meng, Tao,Jin, Yan,Wong, Jesse,McNamkra, Paul,Prongay, Andrew,Madison, Vincent,Piwinski, John J.,Cheng, Kuo-Chi,Morrison, Richard,Malcolm, Bruce,Tong, Xiao,Ralston, Robert,Njoroge, F. George
scheme or table, p. 64 - 69 (2010/12/29)
Boceprevir (SCH 503034), 1, a novel HCV NS3 serine protease inhibitor discovered in our laboratories, is currently undergoing phase III clinical trials. Detailed investigations toward a second generation protease inhibitor culminated in the discovery of narlaprevir (SCH 900518), 37, with improved potency (～10-fold over 1), pharmacokinetic profile and physicochemical characteristics, currently in phase II human trials. Exploration of synthetic sequence for preparation of 37 resulted in a route that required no silica gel purification for the entire synthesis.
Acylsulfonamide compounds as inhibitors of hepatitis C virus NS3 serine protease
-
Page/Page column 44, (2008/06/13)
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis C virus NS3 serine protease
-
Page/Page column 125, (2008/06/13)
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
SULFUR COMPOUNDS AS INHIBITORS OF HEPATITIS C VIRUS NS3 SERINE PROTEASE
-
Page/Page column 125, (2010/02/14)
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Preparation of 2,2-disubstituted 3-chloropropionic esters
-
, (2008/06/13)
2,2-Disubstituted 3-chloropropionic esters I STR1 where R1 and R2 are each C1 -C6 -alkyl, C2 -C6 -oxaalkyl, C2 -C6 -alkenyl, C2 -C6 -oxaalkenyl,
EFFICIENT SYNTHESIS OF SOME 2-OXASPIRONONA-1-ONES AS ANISATIN MODELS
Kato, Michiharu,Kitahara, Haruo,Yoshikoshi, Akira
, p. 1785 - 1788 (2007/10/02)
As a model study for the synthesis of anisatin, 2-oxaspirononane and 5-hydroxy-5-methyl-2-oxaspirononane were synthesized from methyl cyclohexanecarboxylate and 2-ethoxycarbonylcyclohexanone, respectively, and these oxenates were submitted to ru
