A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/401 (2006.01) A61K 31/405 (2006.01) A61P 31/20 (2006.01) A61P 43/00 (2006.01)
Patent
CA 2569729
The patent describes new peptidomimetic inhibitors of retroviral proteases, in particular of human immunodeficiency virus (HIV) protease. These inhibitors comprise as the core structure a new diaminodiol isostere of the dipeptide Phe- Pro having four stereogenic centres. The inhibitors of the invention have been shown to inhibit HIV protease and can therefore be usefully employed as antivirals for post-exposure prophylaxis and as a therapy for viral infections by a retrovirus, in particular HIV. The syntheses processes of the isosteres and inhibitors are also described.
La présente invention a trait à de nouveaux inhibiteurs peptidomimétiques des protéases rétrovirales, notamment de la protéase du virus immunodéficitaire humain (VIH). Ces inhibiteurs comportent en tant que structure central un nouvel isostère diaminodiol du dipeptide Phe-Pro comprenant quatre centres stéréogènes. Il a été démontré que les inhibiteurs de l'invention assurent l'inhibition de la protéase du HIV et peuvent donc être utilisés de manière utile en tant qu'antiviraux pour la prophylaxie post-exposition et comme thérapie pour des infections virales causées par un rétrovirus, en particulier le VIH. L'invention a également trait à des procédés de synthèse des isostères et des inhibiteurs.
Benedetti Fabio
Berti Federico
Campaner Pietro
Dinon Francesca
Tossi Alessandro
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Universita' Degli Studi Di Trieste
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