C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 239/46 (2006.01) A61K 31/505 (2006.01) A61P 31/18 (2006.01) C07D 239/48 (2006.01) C07D 401/12 (2006.01)
Patent
CA 2407754
The present invention concerns compounds of the formula (I): (A1)(A2)N-R1, the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; -S(=O)-R8; -S(=O)2-R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1- 6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N- is the covalently bonded form of the corresponding intermediate of the formula (A1)(A2)N-H, which is a HIV replication inhibiting pyrimidine of formula (II).
La présente invention concerne des composés de formule (I): (A1)(A2)N-R<1>, leurs formes N-oxyde, leurs sels d'addition, acceptables d'un point de vue pharmaceutique, leurs amines quaternaires, ainsi que leurs formes stéréoisomères. Dans cette formule, R<1> représente alkyle C1-6 substitué; -S(=O)-R<8>; -S(=O)2-R<8>; alkylcarbonyle C7-12; alkylcarbonyle C1-6 d'alkyloxycarbonyle C1-6 éventuellement substitué; R<8> étant alkyle C1-6, aryle<1> ou Het<1>; (A1)(A2)N- représente la forme à liaison covalente du produit intermédiaire correspondant, de formule (a): (A1)(A2)N-H, qui est une pyrimidine inhibant la réplication du VIH, de formule (II).
de Corte Bart Lieven Daniel
de Jonge Marc Rene
Heeres Jan
Janssen Paul Adriaan Jan
Kavash Robert W.
Gowling Lafleur Henderson Llp
Janssen Pharmaceutica N.v.
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