1007882-58-7Relevant academic research and scientific papers
Enantioselective synthesis of an HCV NS5a antagonist
Mangion, Ian K.,Chen, Cheng-Yi,Li, Hongmei,Maligres, Peter,Chen, Yonggang,Christensen, Melodie,Cohen, Ryan,Jeon, Ingyu,Klapars, Artis,Krska, Shane,Nguyen, Hoa,Reamer, Robert A.,Sherry, Benjamin D.,Zavialov, Ilia
, p. 2310 - 2313 (2014)
A concise, enantioselective synthesis of the HCV NS5a inhibitor MK-8742 (1) is reported. The features of the synthesis include a highly enantioselective transfer hydrogenation of an NH imine and a dynamic diastereoselective transformation. The synthesis of this complex target requires simple starting materials and nine linear steps for completion.
Impact of lead impurities in zinc dust on the selective reduction of a dibromoimidazole derivative
Yin, Jianguo,Maguire, Courtney K.,Yasuda, Nobuyoshi,Brunskill, Andrew P. J.,Klapars, Artis
, p. 94 - 97 (2017)
A low level of lead in zinc dust was identified as the causative agent responsible for inhibiting selective reduction of a dibromoimidazole derivative via metal agglomeration and lead deposition on the zinc surface.
Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 1: C2-Symmetric inhibitors with diyne and biphenyl linkers
Giroux, Simon,Bilimoria, Darius,Cadilhac, Caroline,Cottrell, Kevin M.,Denis, Francois,Dietrich, Evelyne,Ewing, Nigel,Henderson, James A.,L'Heureux, Lucille,Mani, Nagraj,Morris, Mark,Nicolas, Olivier,Reddy, T. Jagadeeswar,Selliah, Subajini,Shawgo, Rebecca S.,Xu, Jinwang,Chauret, Nathalie,Berlioz-Seux, Francoise,Chan, Laval C.,Das, Sanjoy K.,Grillot, Anne-Laure,Bennani, Youssef L.,Maxwell, John P.
, p. 936 - 939 (2015)
The discovery of C2-symmetric bis-thienoimidazoles HCV NS5A inhibitors is herein reported. Two straightforward approaches to access the requisite diyne and biphenyl linker moieties are described. This study revealed the paramount importance of the aromatic character of the linker to achieve high genotype 1a potency.
Compounds for inhibiting HCV (hepatitis C virus), pharmaceutical composition and application of compounds or pharmaceutical composition
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Paragraph 0104; 0105; 0108; 0109, (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.
INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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Paragraph 0753-0754, (2019/05/15)
The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
5,5-FUSED ARYLENE OR HETEROARYLENE HEPATITIS C VIRUS INHIBITORS
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Paragraph 0306; 0308, (2018/08/20)
Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
As hepatitis c inhibitor spiro compound and its use in medicine
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Paragraph 0809; 0816; 0817, (2017/12/28)
The invention provides a spiro compound serving as a hepatitis c inhibitor and application thereof in a medicine. The compound is a compound as shown in a formula (I) or a stereisomer, a geometric isomer, a tautomer, nitric oxide, an aquo-complex, a solvate, a metabolite, pharmaceutically acceptable salt or prodrug of the compound as shown in the formula (I). The invention also provides a pharmaceutical composition containing the compound, application of the compound and the pharmaceutical composition in inhibition of HCV (Hepatitis C Virus) copy and HCV virus protein, as well as the application of the compound and the pharmaceutical composition in prevention, handling, treatment or relieving of HCV infection or hepatitis c disease for a patient. The formula I is as shown in the specification.
Structure–activity relationships of proline modifications around the tetracyclic-indole class of NS5A inhibitors
Tong, Ling,Yu, Wensheng,Coburn, Craig A.,Chen, Lei,Selyutin, Oleg,Zeng, Qingbei,Dwyer, Michael P.,Nair, Anilkumar G.,Shankar, Bandarpalle B.,Kim, Seong Heon,Yang, De-Yi,Rosenblum, Stuart B.,Ruck, Rebecca T.,Davies, Ian W.,Hu, Bin,Zhong, Bin,Hao, Jinglai,Ji, Tao,Zan, Shuai,Liu, Rong,Agrawal, Sony,Carr, Donna,Curry, Stephanie,McMonagle, Patricia,Bystol, Karin,Lahser, Frederick,Ingravallo, Paul,Chen, Shiying,Asante-Appiah, Ernest,Kozlowski, Joseph A.
, p. 5354 - 5360 (2016/10/30)
We describe the impact of proline modifications, in our tetracyclic-indole based series of nonstructural protein 5A (NS5A) inhibitors, to their replicon profiles. This work identified NS5A inhibitors with an improved and flattened resistance profiles.
9,9,10,10-TETRAFLUORO-9,10-DIHYDROPHENANTHRENE HEPATITIS C VIRUS INHIBITOR AND APPLICATION THEREOF
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Paragraph 0116-0118, (2016/10/31)
The present invention belongs to the field of chemical pharmaceuticals, and specifically relates to compounds represented by formula I having a 9,9,10,10-tetrafluoro-9,10-dihydrophenanthrene structure and being able to inhibit hepatitis C virus activity, or a pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug of said compounds, a pharmaceutical composition containing said compounds, and an application of said compounds or composition in the preparation of a drug. The compounds of the present invention have a good HCV inhibitory effect.
Fused tricyclic hepatitis virus inhibitor and application thereof
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Paragraph 0452; 0453; 0454; 0455, (2016/12/26)
The invention belongs to the field of medical chemistry, relates to a fused tricyclic hepatitis virus inhibitor and application thereof, and particularly, provides a compound of the general formula I or pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug thereof, and a medicine composition containing the compounds and application of the compounds or the composition in medicine preparation. The compound has the good inhibiting activity on hepatitis C virus, meanwhile has the low toxicity on host cells, and is high in effectiveness, good in safety and likely to become the medicine for treating and/or preventing diseases relevant to HCV infection.
