Inhibitors of aspartyl protease

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C549S372000, C549S370000

Reexamination Certificate

active

07919523

ABSTRACT:
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. 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.

REFERENCES:
patent: 4629724 (1986-12-01), Ryono et al.
patent: 5723490 (1998-03-01), Tung et al.
patent: 5843946 (1998-12-01), Vasquez et al.
patent: 6143747 (2000-11-01), Freskos et al.
patent: 6617350 (2003-09-01), Hale et al.
patent: 0159156 (1985-10-01), None
patent: 0594540 (1994-04-01), None
patent: WO 94/04492 (1994-03-01), None
patent: WO 94/05639 (1994-03-01), None
patent: WO 94/10136 (1994-05-01), None
patent: WO 95/06030 (1995-03-01), None
patent: WO 95/07269 (1995-03-01), None
patent: WO 95/09843 (1995-04-01), None
patent: WO 95/14016 (1995-05-01), None
patent: WO 95/32185 (1995-11-01), None
patent: WO 96/22287 (1996-07-01), None
patent: WO 96/33184 (1996-10-01), None
patent: WO 96/33187 (1996-10-01), None
A.K. Ghosh et al., “Potent HIV Protease Inhibitors Incorporating High-Affinity P2-Ligands and (R)-(Hydroxyethylamino)sulfonamide Isostere,”Bioorg. Med. Chem. Lett., 8, pp. 687-690 (1998).
S. J. Hays et al., “Synthesis of cis-4-(Phosphonooxy)-2- piperidinecarboxylic Acid, an N-Methyl-D-aspartate Antagonist,”J. Org. Chem., 56, pp. 4084-4086 (1991).
Y. Kiso et al., “‘O□N Intramolecular Acyl Migration’-type Prodrugs of Tripeptide Inhibitors of HIV Protease,”Peptides: Chemistry, Structure and Biology, 61, pp. 157-159 (1996).
A.C. Nair et al., “A Computational Study of the Resistance of HIV-1 Aspartic Protease to the Inhibitors ABT-538 and VX-478 and Design of New Analogues,”Biochem. Biophys. Res. Commun., 242, pp. 545-551 (1998).
J.W. Perich et al., “The Synthesis of Multiple O-Phosphoseryl-Containing Peptides via Phenyl Phosphate Protection,”J. Org. Chem., 53, pp. 4103-4105 (1988).
M.S. Plummer et al., “Design of Peptidomimetic Ligands for the pp60src SH2 Domain,”Bioorganic&Medicinal Chemistry, 5, pp. 41-47 (1997).
S. Yamaguchi et al., “Synthesis of HIV Protease Dipeptide Inhibitors and Prodrugs,”Peptide Chemistry 1996, pp. 297-300 (1997).
Banker et al.,Modern Pharmaceutics, pp. 627-629 (1996).
C.T. Baker et al., “Design, Synthesis and Conformational Analysis of A Novel Series of HIV Protease Inhibitors,”Bioorg. &Med. Chem. Lett., vol. 8, pp. 3631-3636 (1998).

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Inhibitors of aspartyl protease does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Inhibitors of aspartyl protease, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Inhibitors of aspartyl protease will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-2674389

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.