618439-82-0Relevant articles and documents
Preparation of novel 2,3,8-trisubstituted pyrido[3,4-b]pyrazines and pyrido[2,3-b]pyrazines
Antoine, Maud,Czech, Michael,Gerlach, Matthias,Guenther, Eckhard,Schuster, Tilmann,Marchand, Pascal
experimental part, p. 794 - 806 (2011/04/16)
A four-step synthesis of 8-bromo-2,3-disubstituted pyrido[3,4-b]pyrazines and a six-step synthesis of 8-amino-2,3-disubstituted pyrido[3,4-b]pyrazines have been developed. A particularly valuable feature of this synthetic route is the possibility to build
Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor
Vera, Matthew D.,Lundquist IV, Joseph T.,Chengalvala, Murty V.,Cottom, Joshua E.,Feingold, Irene B.,Garrick, Lloyd M.,Green, Daniel M.,Hauze, Diane B.,Mann, Charles W.,Mehlmann, John F.,Rogers, John F.,Shanno, Linda,Wrobel, Jay E.,Pelletier, Jeffrey C.
supporting information; scheme or table, p. 2512 - 2515 (2010/07/06)
Antagonism of the gonadotropin releasing hormone (GnRH) receptor has resulted in positive clinical results in reproductive tissue disorders such as endometriosis and prostate cancer. Following the recent discovery of orally active GnRH antagonists based on a 4-piperazinylbenzimidazole template, we sought to investigate the properties of heterocyclic isosteres of the benzimidazole template. We report here the synthesis and biological activity of eight novel scaffolds, including imidazopyridines, benzothiazoles and benzoxazoles. The 2-(4-tert-butylphenyl)-8-(piperazin-1-yl)imidazo[1,2-a]pyridine ring system was shown to have nanomolar binding potency at the human and rat GnRH receptors as well as functional antagonism in vitro. Additional structure-activity relationships within this series are reported along with a pharmacokinetic comparison to the benzimidazole-based lead molecule.
7-SUBSTITUTED IMIDAZO[4,5-C]PYRIDINE ANTAGONISTS OF GONADOTROPIN RELEASING HORMONE RECEPTOR
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Page/Page column 13; 19, (2008/06/13)
The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists.
Diaminopyridine compounds and methods of use
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, (2008/06/13)
The present invention relates to compositions and method for inhibiting nonenzymatic cross-linking (protein aging) which contain diaminopyridines and derivates thereof. Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.