Dihydroxypyrimidine carboxamide inhibitors of hiv integrase

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 417/04 (2006.01) A61K 31/506 (2006.01) A61K 31/513 (2006.01) A61K 31/5355 (2006.01) A61K 31/5377 (2006.01) A61K 31/541 (2006.01) C07D 239/52 (2006.01) C07D 239/557 (2006.01) C07D 401/04 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/04 (2006.01) C07D 403/06 (2006.01) C07D 403/12 (2006.01) C07D 403/14 (2006.01) C07D 405/04 (2006.01) C07D 405/06 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01) C07D 409/04 (2006.01) C07D 409/06 (2006.01) C07D 409/14 (2006.01) C07

Patent

CA 2463975

4,5-Dihydroxypyrimidine-6-carboxamides of formula (I); are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

La présente invention concerne des 4,5-dihydroxypyrimidine-6-carboxamides représentés par la formule générale (I). Ce sont des inhibiteurs de l'intégrase du VIH et des inhibiteurs de la réplication du VIH. Dans cette formule, les groupes R?1¿, R?2¿, R?3¿ et R?4¿ sont tels que définis dans les spécifications. Ces composés convient particulièrement pour prévenir et traiter l'infection par le VIH ainsi que pour prévenir le SIDA, retarder sa survenue, et le traiter. Ces composés s'utilisent contre l'infection par le VIH et le SIDA comme composés utilisés en tant que tels ou sous la forme de sels pharmaceutiquement admis. Les composés et leurs sels peuvent s'employer comme ingrédients de compositions pharmaceutiques, éventuellement en association avec d'autres antiviraux, immunomodulateurs, antibiotiques ou vaccins. L'invention concerne également, d'une part des procédés s'appliquant pour prévenir le SIDA, le traiter ou en retarder la survenir, et d'autre part des procédés applicables en prophylaxie ou en thérapie de l'infection par le VIH.

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