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NOVEL TRIAZOLE DERIVATIVES WITH IMPROVED RECEPTOR ACTIVITY AND BIOAVAILABILITY PROPERTIES AS GHRELIN ANTAGONISTS OF GROWTH HORMONE SECRETAGOGUE RECEPTORS
专利权人:
Gilbert Mueller;Klaus Paulini;Lars Blumenstein;Anne-Laure Blayo;Matthias Gerlach;Jean Martinez;Jean-Alain Fehrentz;Babette Aicher;Peter Schmidt;Michael Teifel
发明人:
Babette Aicher,Gilbert Mueller,Klaus Paulini,Lars Blumenstein,Peter Schmidt,Matthias Gerlach,Michael Teifel,Jean Martinez,Jean-Alain Fehrentz,Anne-Laure Blayo
申请号:
US13235116
公开号:
US20120083494A1
申请日:
2011.09.16
申请国别(地区):
US
年份:
2012
代理人:
摘要:
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).
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