The present invention provides novel triazole derivatives 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 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; 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).

Perrissoud; Daniel

Martinez; Jean

Moulin; Aline

Fehrentz; Jean-Alain

Boeglin; Damien

Demange; Luc

Zentaris GmbH

Le Centre National de la Recherche Scientifique

University of Montpellier I

University of Montpellier II

Triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors

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).

Aicher; Babette

Mueller; Gilbert

Paulini; Klaus

Blumenstein; Lars

Schmidt; Peter

Gerlach; Matthias

Teifel; Michael

Blayo; Anne-Laure

AEterna Zentaris GmbH

Centre National de la Recherche Scientifique

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

Methods of using a stimulator device in the treatment of: gastrointestinal disorders such as dysphagia, gastroesophageal reflux diseases, functional dyspepsia, gastroparesis, postoperative ileus, irritable bowel syndrome, constipation, diarrhea, fecal incontinence, nausea and vomiting; gastrointestinal obstruction or pseudo-obstruction; pain and/or discomfort related to visceral organs; eating disorders, such as obesity, binge eating, bulimia, anorexia, and chemotherapy-induced emesis or emesis of other origin. The stimulator device generally includes a housing, at least two electrodes, and a pulse generator. The housing has an exterior surface and an interior surface defining a sealed interior space. The housing is constructed of bio-compatible materials and sized and shaped for transport through the gastrointestinal tract.

Chen; Jianfeng

Transtimulation Research, Inc.

Method of using a gastrointestinal stimulator device for digestive and eating disorders

ileus

obesidade

obesity

ileus/obesidade

Triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors

Triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors

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

Method of using a gastrointestinal stimulator device for digestive and eating disorders

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