Triazole derivatives with improved receptor activity and bioavailability properties as ghrelin antagonists of growth hormone secretagogue receptors

US8546435B2 · kind B2 · utility

Assignees

• Aeterna Zentaris, Inc. · DE
• CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE · FR
• Universite De Montpellier · FR

Inventors

• Babette Aicher · Frankfurt am Main, DE
• Gilbert Mueller · Frankfurt am Main, DE
• Klaus Paulini · Maintal, DE
• Lars Blumenstein · Frankfurt am Main, DE
• Peter Schmidt · Straubing, DE
• Matthias Gerlach · Wächtersbach, DE
• Michael Teifel · Weiterstadt, DE
• Jean Martinez · Caux, FR
• Jean-Alain Fehrentz · Lunel, FR
• Anne-Laure Blayo · North Palm Beach, US

Key dates

• Filing date: Sep 16, 2011
• Grant date: Oct 1, 2013
• Expiry date: Feb 15, 2032

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular alcohol disorder, drug abuse, growth retardation, cachexia, short-, medium-, and/or long term regulation of energy balance, short-, medium-, and/or long term regulation (stimulation and/or inhibition) of food intake, intake of rewarding food, adipogenesis, adiposity and/or obesity, body weight gain and/or reduction, diabetes, diabetes type I, diabetes type II, tumor cell proliferation, inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).