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

US8067456B2 · kind B2 · utility

Assignee

• Aeterna Zentaris, Inc. · DE

Inventors

• Klaus Paulini · Maintal, DE
• Matthias Gerlach · Wächtersbach, DE
• Eckhard Gunther · Offenbach, DE
• Emmanuel Polymeropoulos · Frankfurt, DE
• Silke Baasner · Schöneck, DE
• Peter Schmidt · Straubing, DE
• Ronald Kühne · Berlin, DE
• Arvid Söderhäll · Spånga, SE

Key dates

• Filing date: Feb 14, 2008
• Grant date: Nov 29, 2011
• Expiry date: Jul 3, 2029

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D209/82
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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.