2,4-disubstituted triazine derivatives

US6638932B1 · kind B1 · utility

Assignee

• Janssen Pharmaceutica NA · BE

Inventors

• Bart De Corte · Southampton, US
• Marc René de Jonge · Tilburg, NL
• Jan Heeres · Vosselaar, BE
• Paul Adriaan Jan Janssen · Vosselaar, BE
• Robert W. Kavash · Glenside, US
• Lucien Maria Henricus Koymans · Retie, BE
• Michael Joseph Kukla · Masontown, US
• Donald Ludovici · Quakertown, US
• Koen Jeanne Alfons Van Aken · Kortrijk, BE

Key dates

• Filing date: Aug 2, 2001
• Grant date: Oct 28, 2003
• Expiry date: Aug 2, 2021

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S977/915
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein —a1═a2—a3═a4— forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl or substituted C1-6alkyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR4, —NH—S(═O)pR4, —C(═O)R4, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R4, —C(═NH)R4 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl, or pyridazinyl; X is —NR1—, —NH&…