Metabotropic glutamate receptor antagonists

US7629468B2 · kind B2 · utility

Assignee

• Janssen Pharmaceuticals, Inc. · BE

Inventors

• Dominique Jean-Pierre Mabire · La Saussaye, FR
• Marc Venet Gaston · Le Mesnil-Esnard, FR
• Sophie Coupa · Saint-Étienne-du-Rouvray, FR
• Alain Philippe Poncelet · Bayeux, FR
• Anne Simone Josephine Lesage · Zoersel, BE

Key dates

• Filing date: May 20, 2005
• Grant date: Dec 8, 2009
• Expiry date: Dec 5, 2026

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F7/0812
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention concerns compounds of formula. In a preferable embodiment, X represents O; R1 represents C1-6alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl-moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1-6alkyloxy, aryl, halo or thienyl; R2 represents hydrogen; halo; C1-6alkyl or amino; R3 and R4 each independently represent hydrogen or C1-6alkyl; or R2 and R3 may be taken together to form —R2—R3—, which represents a bivalent radical of formula -Z4-CH2—CH2—CH2— or -Z4-CH2—CH2— with Z4 being O or NR11 wherein R11 is C1-6alkyl; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R3 and R4 may be taken together to form a bivalent radical of formula —CH2—CH2—CH2—CH2—; R5 represents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. The invention also relates to the use of a compound according to the invention as a medicament and in the manufacture of a medicament for treating or preventing glutamate-induced diseases of the central nervous system, as well as formulations comprising such a compound and processes for preparing such a compound…