Carboxamide compounds and their use as calpain inhibitors V

US9051304B2 · kind B2 · utility

Assignees

• Abb Vie Deutschland Gmbh & Co. KG · DE
• Abb Vie Inc. · US

Inventors

• Andreas Kling · Mannheim, DE
• Katja Jantos · Ludwigshafen, DE
• Helmut Mack · Ludwigshafen, DE
• Achim Möller · Bad Kötzting, DE
• Wilfried Hornberger · Wiesbaden, DE
• Gisela Backfisch · Dossenheim, DE
• Yanbin Lao · Libertyville, US
• Marjoleen Nijsen · Libertyville, US

Key dates

• Filing date: Dec 20, 2010
• Grant date: Jun 9, 2015
• Expiry date: Jul 28, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D417/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.The carboxamide compounds are compounds of the general formula Iin which R1, R2, R3 R4, R5, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R1 is optionally substituted phenyl-C1-C2-alkyl or hetaryl-C1-C2-alkyl, R2 is optionally substituted aryl, hetaryl, aryl-C1-C6-alkyl, aryl-C2-C6-alkenyl or hetaryl-C1-C4-alkyl, R3 is C1-C3-alkyl, C1-C3-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, or phenyl-C1-C3-alkyl, R4 and R5 independently of one another are halogen, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-alkoxy, and m and n independently of one another are 0 or 1.