Trisubstituted 1,3,5-triazine derivatives

US6774235B2 · kind B2 · utility

Assignee

• Janssen Pharmaceutica NA · BE

Inventors

• Frederik Frans Desiré Daeyaert · Beerse, BE
• Bart De Corte · Southampton, US
• Marc René de Jonge · Tilburg, NL
• Jan Heeres · Vosselaar, BE
• Chih Yung Ho · Lansdale, US
• 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

Key dates

• Filing date: Feb 5, 2002
• Grant date: Aug 10, 2004
• Expiry date: Feb 5, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D403/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0, 1, 2, 3 or 4; R1 and R2 are each independently selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each of the aforementioned C1-12alkyl groups may optionally and each individually be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl; and each R4 independently is hydroxy, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is —X—R5 or —X—Alk—R6; wherein R5 and R6 each independently are indanyl, indolyl or phenyl; each of said indanyl, indolyl or phenyl may be substituted; and X is —NR3—, —NH—NH—, —N═N—, —O—, —S —, —S(═O…