53313-41-0Relevant academic research and scientific papers
COMPOUNDS AS HEPATITIS C VIRUS (HCV) INHIBITORS AND USES THEREOF IN MEDICINE
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Paragraph 00245, (2016/01/25)
Provided herein are compounds of Formula (I), or a stereoisomer, a geometric isomer, an enantiomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which are used in the treatment of HCV
SULFONAMIDE COMPOUNDS USEFUL AS CYP17 INHIBITORS
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Page/Page column 102, (2012/02/13)
Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists
Yates, Christopher M.,Brown, Peter J.,Stewart, Eugene L.,Patten, Christopher,Austin, Robert J. H.,Holt, Jason A.,Maglich, Jodi M.,Angell, Davina C.,Sasse, Rosemary Z.,Taylor, Simon J.,Uings, Iain J.,Trump, Ryan P.
experimental part, p. 4531 - 4544 (2010/09/04)
Glucocorticoid receptor (GR) agonists have been used for more than half a century as the most effective treatment of acute and chronic inflammatory conditions despite serious side effects that accompany their extended use that include glucose intolerance, muscle wasting, skin thinning, and osteoporosis. As a starting point for the identification of GR ligands with an improved therapeutic index, we wished to discover selective nonsteroidal GR agonists and antagonists with simplified structure compared to known GR ligands to serve as starting points for the optimization of dissociated GR modulators. To do so, we selected multiple chemical series by structure guided docking studies and evaluated GR agonist activity. From these efforts we identified 5-arylindazole compounds that showed moderate binding to the glucocorticoid receptor (GR) with clear opportunities for further development. Structure guided optimization was used to design arrays that led to potent GR agonists and antagonists. Several in vitro and in vivo experiments were utilized to demonstrate that GR agonist 23a (GSK9027) had a profile similar to that of a classical steroidal GR agonist.
Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists
Lee, Jeewoo,Kang, Sang-Uk,Kil, Min-Jung,Shin, Myoungyoup,Lim, Ju-Ok,Choi, Hyun-Kyung,Jin, Mi-Kyoung,Kim, Su Yeon,Kim, Sung-Eun,Lee, Yong-Sil,Min, Kyung-Hoon,Kim, Young-Ho,Ha, Hee-Jin,Tran, Richard,Welter, Jacqueline D.,Wang, Yun,Szabo, Tamas,Pearce, Larry V.,Lundberg, Daniel J.,Toth, Attila,Pavlyukovets, Vladimir A.,Morgan, Matthew A.,Blumberg, Peter M.
, p. 4136 - 4142 (2007/10/03)
The structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues have been investigated as TRPV1 receptor antagonists. The 2-halogen analogues showed enhanced antagonism compared to the prototype antagonist.
