Preparation of hiv protease inhibitors

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 317/48 (2006.01) A61K 31/18 (2006.01) A61K 31/47 (2006.01) A61P 31/18 (2006.01) C07C 323/60 (2006.01) C07D 215/36 (2006.01)

Patent

CA 2459868

The present invention is concerned with novel HIV protease Inhibitors of formula (I), as individual isomers, racemates, non-racemic mixtures or mixtures of diastereoisomers; wherein A is a group formulas (II, III), n, R1, R2, R3 and R4 are as defined in the description or pharmaceutically acceptable salts thereof. The compounds of formula (I) are peptide mimetics which act as inhibitors of the HIV aspartyl protease, an essential enzyme in the replicative life cycle of HIV.

La présente invention concerne de nouveaux inhibiteurs de la protéase du VIH de la formule (I) utilisés comme isomères individuels, racémates, mélanges non racémiques ou mélanges de diastéréoisomères. Dans ladite formule, A est un groupe des formules (II et III); n, R?1¿, R?2¿, R?3¿ et R?4¿ sont tels que définis dans le mémorandum descriptif ou des sels pharmaceutiquement acceptables desdits composés. Les composés de la formule (I) sont des peptides mimétiques qui agissent comme inhibiteurs de l'aspartyle protéase du VIH, une enzyme essentielle dans le cycle de vie réplicatif du VIH.

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