1-hydroxy naphthyridine compounds as anti-hiv agents

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/4375 (2006.01) A61K 31/5513 (2006.01) A61P 31/18 (2006.01) C07D 471/14 (2006.01) C07D 495/14 (2006.01) C07D 498/14 (2006.01)

Patent

CA 2657287

1-Hydroxy naphthyridine compounds (e.g., 1-hydroxy naphthyridin-2(1H)-one compounds of Formula I are inhibitors of HIV integrase and/or HIV RNase H and inhibitors of HIV replication: (I) wherein X and R1-R6 are as defined herein. The compounds are useful in the prophylaxis and treatment of infection by HIV and in the prophylaxis, 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 anti-HIV agents such as HIV antivirals, immunomodulators, antibiotics and vaccines.

L'invention concerne des composés de 1-hydroxynaphtyridine (par exemple des composés de 1-hydroxy naphtyridin-2(1H)-one représentés par la Formule I) qui sont des inhibiteurs de la VIH intégrase et/ou de la VIH RNase H et des inhibiteurs de la réplication de VIH : (I) où X et R1-R6 sont tels que définis présentement. Les composés sont utiles dans la prophylaxie et le traitement de l'infection par VIH et dans la prophylaxie, le retard dans l'apparition et le traitement du SIDA. Les composés sont employés contre l'infection par le VIH et le SIDA en tant que composés en eux-mêmes ou sous la forme de sels pharmaceutiquement acceptables. Les composés et leurs sels peuvent être employés comme ingrédients dans des compositions pharmaceutiques, facultativement en combinaison avec d'autres agents anti-VIH tels qu'agents antiviraux, immunomodulateurs, antibiotiques et vaccins contre le VIH.

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