Centre National De La Recherche Scientifique

Merck Patent Gmbh

Aeterna Zentaris Gmbh

University of Montpellier I

University of Montpellier Ii

Æterna Zentaris Gmbh

Anne-Laure Blayo

Matthias Gerlach

Jean Martinez

Michael Teifel

Stephan Schann

Klaus Paulini

Stanislas Mayer

Peter Schmidt

Jean-Alain Fehrentz

Babette Aicher

Gilbert Mueller

Lars Blumenstein

Camille Amalric

Thomas Catelain

Ismet Dorange

Baptiste Manteau

Mickaël Fer

Gilbert MÜLLER

The present invention relates to novel 5-azaindazole derivatives of formula (I), as described and defined herein, and pharmaceutically acceptable salts, solvates and prodrug thereof, as well as pharmaceutical compositions comprising such compounds. The 5-azaindazole derivatives according to the invention have been found to be highly effective dual A/Aadenosine receptor antagonists, and can thus be used as therapeutic agents, particularly in the treatment or prevention of hyperproliferative or infectious diseases or disorders.

5-azaindazole derivatives as adenosine receptor antagonists

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

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Credin, France

Anne-Laure Blayo