2,4,5-trisubstituted thiazolyl derivatives and their antiinflammatory activity

US7138403B2 · kind B2 · utility

Assignee

• Janssen Pharmaceutica NA · BE

Inventors

• Christopher John Love · Deurne, BE
• Jean Pierre Frans Van Wauwe · Beerse, BE
• Marc De Brabander · Zoersel, BE
• Roger Clive Moses · Wadebridge, GB
• Mykhalyo Goncharenko · London, CA
• Ludwig Paul Cooymans · Beerse, BE
• Nele Vandermaesen · Olmen, BE
• Gaston Stanislas Marcella Diels · Turnhout, BE
• Anthony William Sibley · Camelford, GB
• Caterina Noula · Southeast 1st Street, GB

Key dates

• Filing date: Aug 9, 2002
• Grant date: Nov 21, 2006
• Expiry date: Aug 9, 2022

Classification

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

Abstract

This invention concerns the use of a compound of formula (I)a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl or C1-6alkyloxy; polyhaloC1-4alkyl; C1-4alkyloxy; cyano; amino; aminocarbonyl; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; H2N—S(═O)2—; mono- or di(C1-6alkyl)amino-S(═O)2; —C(═N—Rx)NRyRz; Q is an optionally substituted carbocycle or an optionally substituted heterocycle; L is substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through TNF-α and/or IL-12.