3-substituted-1,5-diarly-2-alkyl-pyrroles highly selective and orally effective COX-2 inhibitors

US7906551B2 · kind B2 · utility

Assignee

• Rottapharm SpA · IT

Inventors

• Andrea Cappelli · Civitella Marittima, IT
• Maurizio Anzini · Pianella, IT
• Mariangela Biava · Siena, IT
• Francesco Makovec · Monza, IT
• Antonio Giordani · Pavia, IT
• Gianfranco Caselli · L'Aquila, IT
• Lucio Claudio Rovati · Monza, IT

Key dates

• Filing date: Aug 3, 2006
• Grant date: Mar 15, 2011
• Expiry date: Aug 3, 2026

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D207/337
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention relates to 3-substituted-1,5-diaryl-2-alkyl-pyrroles of Formula I, pharmaceutical compositions containing them, and to their use for the pharmacological treatment of pain and COX-2 over-activation associated disorders. Compounds of this invention are new pyrrole derivatives bearing in position -3 of the pyrrole ring, several variously functionalized, not aliphatic, side chains which confer to the compounds a relevant COX-2 potency and selectivity along with a remarkable oral efficacy. Phenyl rings in position -1 and -5 are variously substituted, but compounds of particular interest are those substituted in position -5 with 4-methylsulphonyl-phenyl or with 4-aminosulphonyl-phenyl groups.