HIV inhibiting pyrimidine derivative

US6197779A · kind A · utility

Assignee

• Janssen Pharmaceuticals, Inc. · BE

Inventors

• Koenraad Jozef Lodewijk Marcel Andries · Beerse, BE
• Bart De Corte · Southampton, US
• Marc René de Jonge · Tilburg, NL
• Jan Heeres · Vosselaar, BE
• Chih Yung Ho · Lansdale, US
• Marcel A. C. Janssen · Vosselaar, BE
• Paul Adriaan Jan Janssen · Vosselaar, BE
• 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: Mar 25, 1999
• Grant date: Mar 6, 2001
• Expiry date: Mar 25, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D401/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

This invention concerns the use of the compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR.sup.4 or N; n is 0 to 4; Q is hydrogen or --NR.sup.1 R.sup.2 ; R.sup.1 and R.sup.2 are selected from hydrogen, hydroxy, C.sub.1-12 alkyl, C.sub.1-12 alkyloxy, C.sub.1-12 alkylcarbonyl, C.sub.1-12 alkyloxycarbonyl, aryl, amino, mono- or di(C.sub.1-12 alkyl)amino, mono- or di(C.sub.1-12 alkyl)aminocarbonyl wherein each C.sub.1-12 alkyl may optionally be substituted; or R.sup.1 and R.sup.2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C.sub.1-12 alkyl)aminoC.sub.1-4 alkylidene; R.sup.3 is hydrogen, aryl, C.sub.1-6 alkylcarbonyl, optionally substituted C.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonyl,; and R.sup.4 is hydroxy, halo, optionally substituted C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R.sup.5 is hydrogen or C.sub.1-4 alkyl; L is optionally substituted C.sub.1-10 alkyl, C.sub.3-10 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl; or L is --X.sup.1 --R.sup.6 or --X.sup.2 -Alk-R.sup.7 …