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

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United States of America Patent

PATENT NO 8546435
APP PUB NO 20120083494A1
SERIAL NO

13235116

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Abstract

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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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Patent Owner(s)

Patent OwnerAddress
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE3 RUE MICHEL ANGE 75794 PARIS
AETERNA ZENTARIS GMBH60314 FRANKFURT
UNIVERSITY OF MONTPELLIER IIPLACE EUGENE BATAILLON 34095 MONTPELLIER CEDEX 5
UNIVERSITY OF MONTPELLIER I5 BD HENRI IV CEDEX 1 F-34060 MONTPELLIER

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Aicher, Babette Frankfurt am Main, DE 8 110
Blayo, Anne-Laure Credin, FR 11 42
Blumenstein, Lars Frankfurt am Main, DE 4 11
Fehrentz, Jean-Alain St. Nazaire de Pezan, FR 7 57
Gerlach, Matthias Brachttal, DE 42 212
Martinez, Jean Caux, FR 43 206
Mueller, Gilbert Frankfurt am Main, DE 4 15
Paulini, Klaus Maintal, DE 10 115
Schmidt, Peter Schoeneck, DE 300 3467
Teifel, Michael Weiterstadt, DE 20 160

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