Small molecule entry inhibitors

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 311/21 (2006.01) A61K 31/18 (2006.01) A61P 31/12 (2006.01) A61P 31/18 (2006.01)

Patent

CA 2477851

The present invention concerns a compound having the formula (see above formula I a N-oxide form, a stereochemical isomer, racemic mixture, salt prodrug, ester or metabolite thereof. It further relates to processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present entry inhibitors with anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.

La présente invention concerne un composé de formule (I), une forme N-oxyde, un stéréoisomère, un mélange racémique, un sel, un promédicament, un ester ou une métabolite de celui-ci. L'invention a également pour objet : des procédés permettant la préparation de ces composés ainsi que des compositions pharmaceutiques, leurs utilisations en tant que médicaments, et des kits de diagnostic les comprenant ; des combinaisons des ces inhibiteurs de pénétration avec des agents anti-rétroviraux ; leur utilisation dans le cadre d'essais en tant que composés de référence ou que réactifs. Les composés de l'invention conviennent à la prévention ou au traitement de l'infection par le VIH et au traitement du SIDA.

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