93349-99-6Relevant academic research and scientific papers
PYRAZOLYL-SUBSTITUTED PYRIDONE COMPOUNDS AS SERINE PROTEASE INHIBITORS
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Paragraph 00277-00278, (2016/04/09)
There are provided inter alia pyrazolyl-substituted pyridone compounds, which exhibit biological activity, e.g., inhibitory action, against serine proteases, including thrombin and various kallikreins. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of serine proteases, including thrombin and various kallikreins.
Design and structural analysis of aromatic inhibitors of type II dehydroquinase from mycobacterium tuberculosis
Howard, Nigel I.,Dias, Marcio V.B.,Peyrot, Fabienne,Chen, Liuhong,Schmidt, Marco F.,Blundell, Tom L.,Abell, Chris
, p. 116 - 133 (2015/04/14)
3-Dehydroquinase, the third enzyme in the shikimate pathway, is a potential target for drugs against tuberculosis. Whilst a number of potent inhibitors of the Mycobacterium tuberculosis enzyme based on a 3-dehydroquinate core have been identified, they generally show little or no in vivo activity, and were synthetically complex to prepare. This report describes studies to develop tractable and drug-like aromatic analogues of the most potent inhibitors. A range of carbon-carbon linked biaryl analogues were prepared to investigate the effect of hydrogen bond acceptor and donor patterns on inhibition. These exhibited inhibitory activity in the high-micromolar range. The addition of flexible linkers in the compounds led to the identification of more potent 3-nitrobenzylgallate- and 5-aminoiso-phthalate-based analogues.
AROMATIC RING COMPOUND
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Paragraph 0549; 0550, (2015/01/18)
Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
CYCLOALKENYL ARYL DERIVATIVES FOR CETP INHIBITOR
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Paragraph 0042; 0562; 0563, (2014/02/16)
The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same.
SUBSTITUTED PYRIDINE COMPOUNDS AS CRAC MODULATORS
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Page/Page column 40-41, (2013/11/19)
The present invention relates to compounds described herein Formula (I) and pharmaceutical acceptable salts thereof, which modulate the activity of calcium release- activated calcium (CRAC) channel. The invention also describes the compounds of Formula (I)and pharmaceutical compositions containing such compounds thereof for treating, managing, and/or lessening the severity of diseases, disorders, syndromes or conditions associated with the modulation of calcium release-activated calcium (CRAC) channel.
HYDROXAMIC ACID DERIVATIVES AS GRAM-NEGATIVE ANTIBACTERIAL AGENTS
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Page/Page column 75-76, (2010/09/18)
The invention relates to chemical compounds of formula (IB): or a salt thereof. In some embodiments, the invention relates to inhibitors of UDP-3-0 — (R-S-hydroxymyristoyl)-N-acetylglucosamine deacetylase (LpxC). In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein and their use in the prevention and/or treatment of Gram- negative bacterial infections.
A General Synthesis of 5-Arylnicotinates
Thompson, Wayne J.,Gaudino, John
, p. 5237 - 5243 (2007/10/02)
Arylboronic acids have been found to couple efficiently with 5-bromonicotinates to yield 5-arylnicotinates.The reaction is considerably more sensitive to steric inhibition in the arylboronic acid component than in the pyridyl bromide 4.The dianion salt of the boronic acid is implicated as the reactive intermediate responsible for the facile coupling reaction.Pure arylboronic acids are best prepared by using triisopropyl borate as the transmetalating agent.
