883001-24-9Relevant articles and documents
QUINOXALINE DERIVATIVES
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Page/Page column 27, (2021/07/24)
The present invention relates to compounds according to general formula (I), which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
FURTHER SUBSTITUTED TRIAZOLO QUINOXALINE DERIVATIVES
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Paragraph 0192-0194, (2020/02/08)
The present invention relates to compounds according to general formula (I) which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
SUBSTITUTED TRIAZOLO QUINOXALINE DERIVATIVES
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Page/Page column 44, (2020/02/14)
The present invention relates to compounds according to general formula (I) which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
Design, synthesis and biological evaluation of renin inhibitors guided by simulated annealing of chemical potential simulations
Cloudsdale, Ian S.,Dickson, John K.,Barta, Thomas E.,Grella, Brian S.,Smith, Emilie D.,Kulp, John L.,Guarnieri, Frank,Kulp, John L.
, p. 3947 - 3963 (2017/07/05)
We have applied simulated annealing of chemical potential (SACP) to a diverse set of ~150 very small molecules to provide insights into new interactions in the binding pocket of human renin, a historically difficult target for which to find low molecular
Development of a scalable process for DG-041, a potent EP3 receptor antagonist, via tandem heck reactions
Zegar, Siead,Tokar, Christopher,Enache, Livia A.,Rajagopol, Venkat,Zeller, Wayne,O'Connell, Matthew,Singh, Jasbir,Muellner, Frank W.,Zembower, David E.
, p. 747 - 753 (2012/12/29)
DG-041 is a small molecule antagonist of the EP3 receptor for prostaglandin E2 that is in clinical development for treatment of peripheral artery disease (PAD). Originally produced using a six-step synthetic procedure, process optimization led to development of a four-step sequence that is readily scalable. The key step in the optimized sequence contains two sequential Heck reactions, involving an intramolecular Heck cyclization followed by an intermolecular Heck coupling, performed in one pot to produce a highly substituted indole core.
7-(ACRYLOYL) INDOLE COMPOSITIONS AND METHODS FOR MAKING AND USING SAME
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, (2010/11/29)
The present invention is directed to pharmaceutical compositions of 7-(acryloyl) indoles, such as 4,5-Dichloro-thiophene-2-sulfonic acid [(E)-3-[1-(2,4-dichlorophenylmethyl)-5-fluoro-3-methyl-1H-indol-7-yl]-acryloyl]amide (DTSI). The invention is also dir
PROCESS FOR PREPARING 7-(ACRYLOYL)INDOLES
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Page/Page column 8-9, (2008/06/13)
The present invention involves a process for preparing substituted indoles, such as DTSI involving two sequential cross-coupling reactions.
Sulfonamide peri-substituted bicyclics for occlusive artery disease
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Page/Page column 54, (2008/06/13)
Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is: