EP 1937655 A1 20080702 - HIV-1 PROTEASE INHIBITORS, AND METHODS OF MAKING AND USING THEM
Title (en)
HIV-1 PROTEASE INHIBITORS, AND METHODS OF MAKING AND USING THEM
Title (de)
INHIBITOREN DER HIV-1-PROTEASE UND VERFAHREN ZU IHRER HERSTELLUNG UND VERWENDUNG
Title (fr)
INHIBITEURS DE LA PROTEASE DU VIH-1, ET LEURS PROCEDES DE FABRICATION ET D'UTILISATION
Publication
Application
Priority
- US 2006024109 W 20060621
- US 69313405 P 20050622
- US 74990205 P 20051212
- US 81023406 P 20060602
Abstract (en)
[origin: WO2007002173A1] One aspect of the invention relates to the design, synthesis and biological activity of novel HIV-1 protease inhibitors incorporating N-phenyloxazolidine-5-carboxamides into the (hydroxyethylamino)sulfonamide scaffold as P2 ligands. For example, the present invention relates to inhibitors with variations at the P2 phenyloxazolidine and the P2' phenylsulfonamide moieties. Remarkably, compounds with an (S)-enantiomer of substituted phenyloxazolidines at P2 show highly potent inhibitory activities against wild-type HIV-1 protease. In certain embodiments, the inhibitors of the invention have Ki values in low picomolar (pM) range. In certain embodiments, the inhibitors of the invention were shown to be active against a variety of multi-drug resistant (MDR) HIV-1 proteases, each representing different paradigm of drug resistance.
IPC 8 full level
C07D 263/24 (2006.01); A61K 31/421 (2006.01); A61P 31/18 (2006.01)
CPC (source: EP)
A61P 31/12 (2017.12); A61P 31/18 (2017.12); C07D 263/24 (2013.01); C07D 413/12 (2013.01); C07D 417/12 (2013.01)
Citation (search report)
See references of WO 2007002173A1
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI SK TR
DOCDB simple family (publication)
WO 2007002173 A1 20070104; AU 2006262275 A1 20070104; CA 2667449 A1 20070104; EP 1937655 A1 20080702; JP 2008546790 A 20081225
DOCDB simple family (application)
US 2006024109 W 20060621; AU 2006262275 A 20060621; CA 2667449 A 20060621; EP 06785253 A 20060621; JP 2008518348 A 20060621