Aeterna Zentaris Gmbh

Zentaris Gmbh

Centre National De La Recherche Scientifique

University of Montpellier I

University of Montpellier Ii

Ae Zentaris Gmbh

Æterna Zentaris Gmbh

Peter Schmidt

Silke Baasner

Matthias Gerlach

Klaus Paulini

Emmanuel Polymeropoulos

Tilmann Schuster

Eckhard Günther

Michael Teifel

Eckhard Guenther

Ronald Kühne

Arvid Söderhäll

Jean Martinez

Jean-Alain Fehrentz

Gilbert Mueller

Babette Aicher

Lars Blumenstein

Anne-Laure Blayo

Peter Ernig

Gilbert MÜLLER

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).

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

The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.

Tetrahydrocarbazole derivatives as ligands of G-protein coupled receptors

The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.

Tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCPs)

Tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCRs)

The invention relates to novel N-substituted indolyl-3-glyoxylamides of the general formula I, their preparation and use as medicaments, in particular for the treatment of tumors 

N-substituted indolyl-3-glyoxylamides, their use as medicaments and process for their preparation

The invention relates to indole derivatives which are used as drugs for treating tumor diseases, in particular when there is drug resistance against other active compounds and where there is a metastasizing carcinoma.

Indole derivatives having an apoptosis-inducing effect

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Schöneck, Germany

Peter Schmidt