565459-90-7Relevant academic research and scientific papers
Highlights of the Structure-Activity Relationships of Benzimidazole Linked Pyrrolidines Leading to the Discovery of the Hepatitis C Virus NS5A Inhibitor Pibrentasvir (ABT-530)
Wagner, Rolf,Randolph, John T.,Patel, Sachin V.,Nelson, Lissa,Matulenko, Mark A.,Keddy, Ryan,Pratt, John K.,Liu, Dachun,Krueger, A. Chris,Donner, Pamela L.,Hutchinson, Douglas K.,Flentge, Charles,Betebenner, David,Rockway, Todd,Maring, Clarence J.,Ng, Teresa I.,Krishnan, Preethi,Pilot-Matias, Tami,Collins, Christine,Panchal, Neeta,Reisch, Thomas,Dekhtyar, Tatyana,Mondal, Rubina,Stolarik, Deanne F.,Gao, Yi,Gao, Wenqing,Beno, David A.,Kati, Warren M.
, p. 4052 - 4066 (2018/05/14)
Curative interferon and ribavirin sparing treatments for hepatitis C virus (HCV)-infected patients require a combination of mechanistically orthogonal direct acting antivirals. A shared component of these treatments is usually an HCV NS5A inhibitor. First generation FDA approved treatments, including the component NS5A inhibitors, do not exhibit equivalent efficacy against HCV virus genotypes 1-6. In particular, these first generation NS5A inhibitors tend to select for viral drug resistance. Ombitasvir is a first generation HCV NS5A inhibitor included as a key component of Viekira Pak for the treatment of patients with HCV genotype 1 infection. Since the launch of next generation HCV treatments, functional cure for genotype 1-6 HCV infections has been achieved, as well as shortened treatment duration across a wider spectrum of genotypes. In this paper, we show how we have modified the anchor, linker, and end-cap architecture of our NS5A inhibitor design template to discover a next generation NS5A inhibitor pibrentasvir (ABT-530), which exhibits potent inhibition of the replication of wild-type genotype 1-6 HCV replicons, as well as improved activity against replicon variants demonstrating resistance against first generation NS5A inhibitors.
BIARYL DERIVATIVE AS GPR120 AGONIST
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Paragraph 0228; 0252, (2017/11/17)
The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.
PROCESS FOR THE PREPARATION OF PHOSPHORIC ACID MONO- (L-{4- [(S) -5- (ACETYLAMINOMETHYL) - 2 - OXO - OXAZOLIDIN- 3 - YL] - 2, 6 - DIFLUOROPHENYL} - 4 -METHOXYMETHYLPIPERIDIN- 4 - YL) ESTER
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Page/Page column 10-11, (2012/05/20)
The invention relates to a process to prepare pharmacologically active phosphoric acid mono-(1-{4-[(S)-5-(acetylamino-methyl)-2-oxo-oxazolidin-3-yl]-2,6-difluoro phenyl}-4-methoxy methyl-piperidin-4-yl) ester.
SUBSTITUTED PIPERIDINO PHENYLOXAZOLIDINONES
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Page/Page column 7, (2010/04/23)
The present invention relates to certain substituted piperidino phenyloxazolidinones. Specifically, the invention relates to geminally disubstituted piperidino phenyloxazolidinones having antimicrobial activity with improved pharmacokinetic profile. The i
A distal methyl substituent attenuates mitochondrial protein synthesis inhibition in oxazolidinone antibacterials
Renslo, Adam R.,Atuegbu, Andy,Herradura, Prudencio,Jaishankar, Priyadarshini,Ji, Mingzhe,Leach, Karen L.,Huband, Michael D.,Dermyer, Michael R.,Wu, Luping,Vara Prasad,Gordeev, Mikhail F.
, p. 5036 - 5040 (2008/03/13)
Oxazolidinone analogs bearing substituted piperidine or azetidine C-rings are described. Analogs with a methyl group at the 3-position of the azetidine ring or the 4-position of the piperidine ring exhibited reduced mitochondrial protein synthesis inhibition while retaining good antibacterial potency.
NOVEL TRIAZOLE COMPOUNDS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Page/Page column 39-40, (2010/02/11)
The present invention relates to novel triazole compounds of formula (I), their prodrugs, their pharmaceutically acceptable salts and their stereoisomers thereof. The present invention also relates to a process for the preparation of the novel compound of
N-aryl-2-oxazolidinone-5-carboxamides and their derivatives
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Page 77, (2010/02/07)
The present invention provides antibacterial agents having the formulae I, II, and III described herein.
ANTIMICROBIAL 1-ARYL DIHYDROPYRIDONE COMPOUNDS
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Page 37, (2010/02/06)
The present invention provides antibacterial agents of formula (I), or a pharmaceutically acceptable salt thereof, wherein A is a structure (i), (ii), (iii) or (iv); X is (a) NHC(=O)R1, (b) NHC(=S)R1, (c) NH-het1/sup
N-ARYL-2-OXAZOLIDINONE-5-CARBOXAMIDES AND THEIR DERIVATIVES AND THEIR USE AS ANTIBACTERIALS
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Page/Page column 158, (2010/02/07)
Compounds of formula B-C-A-CO-NH-R1, wherein A is structure i, ii or iii: formulae (I), (II), (III). C is optionally substituted aryl or heteroaryl, and B is a specified cyclic moiety, or C and B together are a heterobicyclic moiety, are useful as antibacterial agents.
