Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/519 (2006.01) A61P 31/18 (2006.01) C07D 221/00 (2006.01) C07D 223/00 (2006.01) C07D 239/00 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2509554

Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula (A): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Cette invention concerne des tétrahydro-4H-pyrido[1,2-a]pyrimidines et des composés connexes représentés par la formule (A) convenant comme inhibiteurs de l'intégrase du VIH et comme inhibiteurs de la réplication du VIH. Dans la formule A, n est un entier égal à 0, 1, 2 ou 3, et R?1¿, R?3¿, R?4¿, R?12¿, R?14¿, R?16¿, R?30¿, R?32¿, R?34¿ et R?36¿ ont la notification ci-définie. Ces composés sont utiles pour la prévention et le traitement de l'infection par le VIH et pour la prévention, le retard de l'apparition et le traitement du SIDA. Ils s'utilisent contre les infections par le VIH et le SIDA tels quels ou sous forme de sels pharmceutiquement acceptables. Les composés et leurs sels peuvent être utilisés en tant que principes actifs dans des compositions pharmaceutiques, voire en association avec d'autres antiviraux, immunomodulateurs, antibiotiques ou vaccins.

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