Hiv integrase inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 487/04 (2006.01) A61K 31/4985 (2006.01) A61P 31/18 (2006.01)

Patent

CA 2625673

Substituted hydroxytetrahydropyrrolopyrazinone and substituted hydroxytetrahydro-pyrazolopyrazinone compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein R1, R2, R3, R4; R5, X, ring A, and Q are as defined herein. The 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.

La présente invention se rapporte à des composés d'hydroxytétrahydro-pyrrolopyrazinone substituée et d'hydroxytétrahydropyrazolopyrazinone substituée, qui sont représentés par la formule (I). Lesdits composés sont des inhibiteurs de l'intégrase du VIH et des inhibiteurs de la réplication du VIH. Dans ladite formule, R1, R2, R3, R4, R5, X, le cycle A et Q sont tels que définis dans le descriptif de l'invention. Les composés selon l'invention sont utiles pour prévenir et traiter l'infection par le VIH, et pour prévenir, retarder et traiter le SIDA. Lesdits composés sont utilisés contre l'infection par le VIH et le SIDA en tant que tels ou sous forme de sels pharmaceutiquement acceptables. Lesdits composés et leurs sels peuvent servir d'ingrédients dans des compositions pharmaceutiques, éventuellement en combinaison avec d'autres antiviraux, immunomodulateurs, antibiotiques ou vaccins.

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