C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 493/04 (2006.01) A61K 31/36 (2006.01) A61K 31/381 (2006.01) A61K 31/4155 (2006.01) A61K 31/427 (2006.01) A61K 31/443 (2006.01) A61K 45/06 (2006.01) A61P 31/18 (2006.01)
Patent
CA 2380858
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors having the structure of formula I: (see formula I) In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
La présente invention concerne une nouvelle classe de sulfonamides, inhibiteurs d'aspartyl protéase. Dans un mode de réalisation, l'invention porte sur une nouvelle classe d'inhibiteurs d'aspartyl protéase du VIH, présentant des caractéristiques structurelles et physico-chimiques spécifiques. Cette invention concerne également des compositions pharmaceutiques contenant ces composés. Les composés et les compositions pharmaceutiques de l'invention conviennent particulièrement à l'inhibition de l'activité protéase du VIH-1 et du VIH-2 et peuvent, par conséquent, être utilisés de façon avantageuse en tant qu'agents antiviraux contre les virus VIH-1 et VIH-2. L'invention concerne en outre des méthodes permettant d'inhiber l'activité aspartyl protéase à l'aide des composés de l'invention, ainsi que des méthodes de criblage de composés ayant une activité anti-VIH.
Brieger Michael Stephen
Furfine Eric Steven
Hale Michael Robin
Jarvis Ashley Nicholas
Kaldor Istvan
Smart & Biggar
Vertex Pharmaceuticals Incorporated
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