Novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin antagonists of growth hormone secretagogue receptors (WO2012035124): a patent evaluation.
The patent claims triazole compounds as inhibitors of the ghrelin receptor, the growth-hormone secretagogue receptor (GHS-R1a). These compounds are potent GHS-R1a ligands with an improved in vitro antagonistic activity against ghrelin receptors of at least factor 3 compared with a representative compound disclosed in a previous patent, and are expected to possess, on the basis of the results of in vitro assays, improved safety and human oral bioavailability with respect to the lead.
Dipartimento di Scienze Farmaceutiche, Università di Modena e R.E, Via Campi 183 41100, Modena, Italy. luca.costantino@unimore.it
Luca
L
Costantino
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D015195:Drug Design; D054439:Ghrelin / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D010330:Patents as Topic; D054440:Receptors, Ghrelin / Q000037:antagonists & inhibitors*; D014230:Triazoles / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology*
D054439:Ghrelin; D008024:Ligands; D054440:Receptors, Ghrelin; D014230:Triazoles