113984-76-2Relevant articles and documents
Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors
Waldschmidt, Helen V.,Bouley, Renee,Kirchhoff, Paul D.,Lee, Pil,Tesmer, John J.G.,Larsen, Scott D.
, p. 1507 - 1515 (2018)
G protein-coupled receptor (GPCR) kinases (GRKs) regulate the desensitization and internalization of GPCRs. Two of these, GRK2 and GRK5, are upregulated in heart failure and are promising targets for heart failure treatment. Although there have been several reports of potent and selective inhibitors of GRK2 there are few for GRK5. Herein, we describe a ligand docking approach utilizing the crystal structures of the GRK2–Gβγ·GSK180736A and GRK5·CCG215022 complexes to search for amide substituents predicted to confer GRK2 and/or GRK5 potency and selectivity. From this campaign, we successfully generated two new potent GRK5 inhibitors, although neither exhibited selectivity over GRK2.
Therapeutic Aryl-Amido-Aryl Compounds and Their Use
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Page/Page column 101, (2012/06/18)
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as “AAA compounds”), which, inter alia, a
PYRIMIDINE AND QUINAZOLINE DERIVATIVES
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Page/Page column 86, (2008/06/13)
This invention is concerned with compounds of the formula ( l ) wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.