157665-52-6Relevant articles and documents
STAT INHIBITORY COMPOUNDS AND COMPOSITIONS
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Paragraph 0269, (2021/09/11)
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for the inhibition of Signal Transducer and Activator of Transcription 5a and 5b (STAT5). Furthermore, the subject compounds and compositions are usefu
COMPOUNDS, COMPOSITIONS, AND METHODS FOR MODULATING FERROPTOSIS AND TREATING EXCITOTOXIC DISORDERS
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Paragraph 0164; 0180, (2020/06/19)
The present disclosure provides, inter alia, a compound having the structure (1). Also provided are compositions containing a pharmaceutically acceptable carrier and one or more compounds according to the present disclosure. Further provided are methods f
GLP-1 Agonists and Uses Thereof
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Paragraph 0436, (2018/07/05)
Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, 7-aza- and 4,7-diaza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
Allosteric Inhibitors, Crystallography, and Comparative Analysis Reveal Network of Coordinated Movement across Human Herpesvirus Proteases
Acker, Timothy M.,Gable, Jonathan E.,Bohn, Markus-Frederik,Jaishankar, Priyadarshini,Thompson, Michael C.,Fraser, James S.,Renslo, Adam R.,Craik, Charles S.
supporting information, p. 11650 - 11653 (2017/09/07)
Targeting of cryptic binding sites represents an attractive but underexplored approach to modulating protein function with small molecules. Using the dimeric protease (Pr) from Kaposi's sarcoma-associated herpesvirus (KSHV) as a model system, we sought to dissect a putative allosteric network linking a cryptic site at the dimerization interface to enzyme function. Five cryogenic X-ray structures were solved of the monomeric protease with allosteric inhibitors bound to the dimer interface site. Distinct coordinated movements captured by the allosteric inhibitors were also revealed as alternative states in room-temperature X-ray data and comparative analyses of other dimeric herpesvirus proteases. A two-step mechanism was elucidated through detailed kinetic analyses and suggests an enzyme isomerization model of inhibition. Finally, a representative allosteric inhibitor from this class was shown to be efficacious in a cellular model of viral infectivity. These studies reveal a coordinated dynamic network of atomic communication linking cryptic binding site occupancy and allosteric inactivation of KHSV Pr that can be exploited to target other members of this clinically relevant family of enzymes.
NOVEL PYRROLOY2,3-d¨PYRIMIDINE COMPOUND
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Page/Page column 63, (2011/12/12)
Disclosed is a novel pyrrolo[2,3-d]pyrimidine compound represented by formula [I] or a pharmacologically acceptable salt thereof, which has a GPR119 receptor agonistic activity and is useful for a pharmaceutical. In formula [I], E represents a group repre
BENZIMIDAZOLECARBOXAMIDES AS INHIBITORS OF FAK
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Page/Page column 107, (2010/11/17)
This invention relates to benzimadolecarboxamides of formula (I) which are inhibitors of focal adhesion kinase, and as such are useful for treating proliferative diseases
BENZIMIDAZOLONE CHYMASE INHIBITORS
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Page/Page column 189, (2009/01/20)
Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase.
4-Acetylamino-3-(imidazol-1-yl)-benzoic acids as novel inhibitors of influenza sialidase
Howes, Peter D.,Cleasby, Anne,Evans, Derek N.,Feilden, Helen,Smith, Paul W.,Sollis, Steven L.,Taylor, Neil,Wonacott, Alan J.
, p. 225 - 234 (2007/10/03)
Two methods for the synthesis of 4-acetylamino benzoic acids substituted at the 3-position with imidazoles are described. Many of the compounds are inhibitors of influenza virus sialidases with levels of activity similar to the recently described 4-acetylamino-3-guanidino-benzoic acid (BANA 113).
Novel prodrugs of alkylating agents derived from 2-fluoro- and 3- fluorobenzoic acids for antibody-directed enzyme prodrug therapy
Springer,Niculescu-Duvaz,Pedley
, p. 2361 - 2370 (2007/10/02)
The synthesis of six novel fluorinated potential prodrugs for antibody- directed enzyme prodrug therapy is described. The [2- and 3-fluoro-4-[bis(2- chloroethyl)amino]benzoyl]-L-glutamic acid (9 and 21), their bis(mesyloxy)ethyl derivatives (7 and 19), an