71590-32-4Relevant articles and documents
Industrial preparation method of 6-bromonaphthalene-1, 2-diamine
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Paragraph 0004-0005; 0013, (2021/04/21)
The invention discloses an industrial preparation method of 6-bromonaphthalene-1, 2-diamine. The method comprises the following steps of: S1, making a compound III react with acetic anhydride in the presence of alkali and a catalyst to obtain a compound IV; S2, in the presence of acetic anhydride and nitric acid, taking acetic acid as a reaction solvent, performing reacting and purifying on the compound IV obtained in the step S1 to generate a compound V; S3, adding the compound V obtained in the above step into a solvent for dissolving the compound V, then adding a metal reducing agent and an ammonium chloride solution, heating to carry out a reaction for 6h, performing centrifugal filtering after finishing the reaction to obtain a filtrate, washing the filtrate with a sodium chloride solution, and performing concentrating to obtain a compound VI; and S4, adding the compound VI obtained in the previous step into a methanol solution, dropwise adding strong acid, replacing the solvent after finishing the reaction, performing crystallizing and filtering to obtain a compound 8. According to the method, the process is optimized, large-scale production can be achieved, applied materials are all commercial reagents, the cost is reduced, and the operation convenience is improved.
Discovery of potent macrocyclic HCV NS5A inhibitors
Yu, Wensheng,Vibulbhan, Bancha,Rosenblum, Stuart B.,Martin, Gregory S.,Vellekoop, A. Samuel,Holst, Christian L.,Coburn, Craig A.,Wong, Michael,Selyutin, Oleg,Ji, Tao,Zhong, Bin,Hu, Bin,Chen, Lei,Dwyer, Michael P.,Jiang, Yueheng,Nair, Anilkumar G.,Tong, Ling,Zeng, Qingbei,Agrawal, Sony,Carr, Donna,Rokosz, Laura,Liu, Rong,Curry, Stephanie,McMonagle, Patricia,Ingravallo, Paul,Lahser, Fred,Asante-Appiah, Ernest,Fells, James,Kozlowski, Joseph A.
, p. 3793 - 3799 (2016/07/21)
HCV NS5A inhibitors have demonstrated impressive in vitro virologic profiles in HCV replicon assays and robust HCV RNA titer reduction in the clinic making them attractive components for inclusion in an all oral fixed-dose combination (FDC) regimen for the treatment of HCV infection. Merck's effort in this area identified MK-4882 and MK-8325 as early development leads. Herein, we describe the discovery of potent macrocyclic NS5A inhibitors bearing the MK-8325 or MK-4882 core structure.
COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS AND PHARMACEUTICAL USES THEREOF
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Paragraph 00248; 00249, (2016/09/26)
The invention provides compounds as hepatitis C virus inhibitors and pharmaceutical uses thereof. Specifically, the invention provides compounds of Formula (I) or a stereoisomer, a tautomer, an enantiomer, an N-oxide, a hydrate, a solvate, a metabolite, a
FUSED TRICYCLIC SILYL COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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, (2015/12/08)
no abstract published
FUSED TRICYCLIC COMPOUNDS AND DERIVATIVES THEREOF USEFUL FOR THE TREATMENT OF VIRAL DISEASES
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, (2011/06/23)
The present invention relates to novel fused tricyclic compounds, compositions comprising at least one fused tricyclic compound, and methods of using fused tricyclic compounds for treating or preventing a viral infection or a virus-related disorder in a patient.
FUSED TRICYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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, (2011/08/04)
The present invention relates to novel Fused Tricyclic Compounds, compositions comprising at least one Fused Tricyclic Compound, and methods of using Fused Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient.
Discovery of novel Tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats
Shen, Hong C.,Ding,Deng, Qiaolin,Wilsie, Larissa C.,Krsmanovic, Mihajlo L.,Taggart, Andrew K.,Carballo-Jane, Ester,Ren, Ning,Cai,Wu,Wu, Kenneth K.,Cheng, Kang,Chen, Qing,Wolff, Michael S.,Tong, Xinchun,Holt, Tom G.,Waters, M. Gerard,Hammond, Milton L.,Tata, James R.,Colletti, Steven L.
supporting information; experimental part, p. 2587 - 2602 (2010/01/15)
Tricyclic analogues were rationally designed as the high affinity niacin receptor G-protein-coupled receptor 109A (GPR109A) agonists by overlapping three lead structures. Various tricyclic anthranilide and cycloalkene carboxylic acid full agonists were di
NIACIN RECEPTOR AGONISTS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Page/Page column 37; 86, (2010/11/30)
The present invention relates to niacin receptor agonists of formula: (I); as well as pharmaceutically acceptable salts and solvates. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and triglycerides, and raising HDL levels. Pharmaceutical compositions and methods of treatment are also included.