877385-86-9Relevant academic research and scientific papers
THIAZOLE CARBOXAMIDE COMPOUNDS AND USE THEREOF FOR THE TREATMENT OF MYCOBACTERIAL INFECTIONS
-
Page/Page column 33; 34, (2021/04/02)
Provided herein are compounds of Formula (I) and Formula (II) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.
Compounds for inhibiting HCV (hepatitis C virus), pharmaceutical composition and application of compounds or pharmaceutical composition
-
Paragraph 0207; 0208; 0209; 0212; 0213; 0214, (2019/02/04)
The invention discloses compounds for inhibiting HCV (hepatitis C virus), pharmaceutical composition and an application of the compounds or the pharmaceutical composition. The compounds are compoundsshown in formula (I) or a stereoisomer, geometric isomer, a tautomer, an enantiomer, sulfur oxide, nitrogen oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug of the compounds shown in formula (I); the compounds are effective antiviral drugs, especially can be used for inhibiting the function of NS5A protein encoded by the HCV, thereby effectively inhibiting the HCV.The method for preventing and/or treating drugs or diseases associated with the HCV by the compounds or the composition containing the new compounds has good market development prospects.
Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms
Tong, Ling,Yu, Wensheng,Chen, Lei,Selyutin, Oleg,Dwyer, Michael P.,Nair, Anilkumar G.,Mazzola, Robert,Kim, Jae-Hun,Sha, Deyou,Yin, Jingjun,Ruck, Rebecca T.,Davies, Ian W.,Hu, Bin,Zhong, Bin,Hao, Jinglai,Ji, Tao,Zan, Shuai,Liu, Rong,Agrawal, Sony,Xia, Ellen,Curry, Stephanie,McMonagle, Patricia,Bystol, Karin,Lahser, Frederick,Carr, Donna,Rokosz, Laura,Ingravallo, Paul,Chen, Shiying,Feng, Kung-I,Cartwright, Mark,Asante-Appiah, Ernest,Kozlowski, Joseph A.
, p. 290 - 306 (2017/04/26)
We describe the research that led to the discovery of compound 40 (ruzasvir, MK-8408), a pan-genotypic HCV nonstructural protein 5A (NS5A) inhibitor with a "flat" GT1 mutant profile. This NS5A inhibitor contains a unique tetracyclic indole core while maintaining the imidazole-proline-valine Moc motifs of our previous NS5A inhibitors. Compound 40 is currently in early clinical trials and is under evaluation as part of an all-oral DAA regimen for the treatment of chronic HCV infection.
SUBSTITUTED THIAZOLE OR OXAZOLE P2X7 RECEPTOR ANTAGONISTS
-
Page/Page column 37; 38, (2015/09/22)
The present invention refers to novel substituted thiazole and oxazole compounds of formula (I) having P2X7 receptor (P2X7) antagonistic properties. The compounds are useful in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.
HETEROCYCLE-SUBSTITUED TETRACYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES
-
Page/Page column 70, (2014/08/06)
The present invention relates to novel Heterocycle-Substituted Tetracyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, A', R 2 R 3, R 4 and R are as defined herein. The present i
THIAZOLYL-SUBSTITUED TETRACYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES
-
Page/Page column 51, (2014/08/06)
The present invention relates to novel Thiazolyl-Substituted Tetracyclic Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, A', R2R3, R4 and R5 are as defined herein. The present
Convergent, parallel synthesis of a series of β-substituted 1,2,4-oxadiazole butanoic acids as potent and selective α vβ3 receptor antagonists
Boys, Mark L.,Schretzman, Lori A.,Chandrakumar, Nizal S.,Tollefson, Michael B.,Mohler, Scott B.,Downs, Victoria L.,Penning, Thomas D.,Russell, Mark A.,Wendt, John A.,Chen, Barbara B.,Stenmark, Heather G.,Wu, Hongwei,Spangler, Dale P.,Clare, Michael,Desai, Bipin N.,Khanna, Ish K.,Nguyen, Maria N.,Duffin, Tiffany,Engleman, V. Wayne,Finn, Mary Beth,Freeman, Sandra K.,Hanneke, Melanie L.,Keene, Jeffery L.,Klover, Jon A.,Nickols, G. Allen,Nickols, Maureen A.,Steininger, Christina N.,Westlin, Marisa,Westlin, William,Yu, Yi X.,Wang, Yaping,Dalton, Christopher R.,Norring, Sarah A.
, p. 839 - 844 (2007/10/03)
We describe a series of 1,2,4-oxadiazoles, which are potent antagonists of the integrin αvβ3 and, in addition, show selectivity relative to the other β3 integrin αIIbβ3. In whole cells, the majority o
