HIV protease inhibitors

Details HIV protease inhibitors HIV protease inhibitors

1998-03-12

1999-12-14

Northington Davis, Zinna

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546146, C07D21720, A61K 3147

Patent

active

060018518

ABSTRACT:
HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

REFERENCES:
patent: 5063208 (1991-11-01), Rosenberg et al.
patent: 5142056 (1992-08-01), Kempe et al.
patent: 5157041 (1992-10-01), Handa et al.
patent: 5196438 (1993-03-01), Martin et al.
patent: 5204471 (1993-04-01), Negele et al.
patent: 5235039 (1993-08-01), Heath, Jr. et al.
patent: 5434265 (1995-07-01), Fritz et al.
patent: 5463104 (1995-10-01), Vazquez et al.
patent: 5484926 (1996-01-01), Dressman
patent: 5514802 (1996-05-01), Fritz et al.
patent: 5527829 (1996-06-01), Kalish
patent: 5705647 (1998-01-01), Babu et al.
patent: 5714518 (1998-02-01), Reich et al.
Kong-Teck Chong et al., "Peptidomimetic HIV Protease Inhibitors: Phosphate Prodrugs with Improved Biological Activities," J. Med. Chem., 36:2575-2577 (1993).
Arun K. Ghosh et al., "3-Tetrahydrofuran and Pyran Urethanes as High-Affinity P.sub.2 -Ligands for HIV-1 Protease Inhibitors," J. Med. Chem., 36:292-294 (1993).
Arun K. Ghosh et al., "Cyclic Sulfolanes as Novel and High Affinity P.sub.2 Ligands for HIV-1 Protease Inhibitors," J. Med. Chem., 36:924-927 (1993).
Arun K. Ghosh et al., "Potent HIV Protease Inhibitors: The Development of Tetrahydrofuranylglycines as Novel P.sub.2 -Ligands and Pyrazine Amides as P.sub.3 -Ligands," J. Med. Chem., 36:2300-2310 (1993).
Jenny C. Gilbert et al., "NMR Studies of Four Isomers of Decahydroisoquinoline-3(S)-carboxylic Acid and a Potent HIV Proteinase Inhibitor Incorporating the (S,S,S) Isomer," J. Chem. Soc. Perkin Trans. 2,, pp. 475-479 (1993).
Ioannis N. Houpis et al., "Towards the Synthesis of HIV-Protease Inhibitors. Synthesis of Optically Pure 3-Carboxyl-decahydroisoquinolines," Tetrahedron Letters, vol. 34, No. 16, pp. 2593-2596 (1993).
Joel R. Huff, "HIV Protease: A Novel Chemotherapeutic Target for AIDS," J. Med. Chem., vol. 34, No. 8, pp. 2305-2314 (1991).
J.V.N. Vara Prasad et al., "P.sub.3 and P.sub.3 ' substituted analogs of hydroxyethylamine inhibitors of HIV protease," Peptides: Chemistry & Biology, pp. 721-722 (1991).
Daniel H. Rich et al., "Effect of Hydroxyl Group Configurations in Hydroxyethylamine Dipeptide Isosteres on HIV Protease Inhibition. Evidence for Multiple Binding Modes," J. Med. Chem., 34:1222-1225 (1991).
Noel A. Roberts et al., "Rational Design for Peptide-Based HIV Proteinase Inhibitors," Science, vol. 248, pp. 358-361 (1990).
Tim F. Tam et al., "Intriguing Structure--Activity Relations Underlie the Potent of HIV Protease by Norstatine-Based Peptides," J. Med. Chem., 35:1318-1320 (1992).
Suvit Thaisrivongs et al., "Inhibitors of the Protease from Human Immunodeficiency Virus: Design and Modeling of a Compound Containing a Dihydroxyethylene Isostere Insert with High Binding Affinity and Effective Antiviral Activity," J. Med. Chem., 34:2344-2356 (1991).
Wayne J. Thompson et al., "3'-Tetrahydrofuranylglycine as a Novel, Unnatural Amino Acid Surrogate for Asparagine in the Design for Inhibitors of the HIV Protease," J. Am. Chem. Soc., 115:801-803 (1993).
T.A. Lyle, et al., "Benzocycloalkyl Amines as Novel C-Termini for HIV Protease Inhibitors," J. Med. Chem., 34:1228-1230 (1991).
Steven D. Young et al., "HIV-1 Protease Inhibitors Based on Hydroxyethylene Dipeptide Isosteres: An Investigation into the Role of the P.sub.1 ' Side Chain on Structure-Activity," J. Med. Chem., 35:1702-1709 (1992).
Rich, Chemical Abstracts, vol. 114, No. 15 Abstract No. 114:143998 (1991).
Abstract for Japanese Patent Appln. No. 95-248183 to Inaba, et al., dated Apr. 1997.
Abstract for Japanese Patent Appln. No. 95-248184 to Deason, et al., dated Apr. 1997.
Ratner, et al., "Complete Nucleotide Sequence of the AIDS Virus, HTLV-III," Nature, vol. 313 (1985), pp. 277-284.
Rose, et al., "Regulation of Autoproteolysis of the HIV-1 and HIV-2 Proteases with Engineered Amino Acid Substitutions," The Journal of Biological Chemistry, vol. 268, No. 16 (1993), pp. 11939-11945.
Menge, et al., "Structure-Function Analysis of the Mammalian DNA Polymerase .beta. Active Site: Role of Aspartic Acid 256, Arginine 254, and Arginine 258 in Nucleotidyl Transfer," Biochemistry, vol. 34, (1995), pp. 15934-15942.
Celis, "Chain-terminating Mutants Affecting a Periplasmic Binding Protein Involved in the Active Transport of Arginine and Ornithine in Escherichia coli," The Journal of Biological Chemistry, vol. 256, No. 2 (1981), pp. 773-779.
Morrison, "Kinetics of the Reversible Inhibition of Enzyme-Catalysed Reactions by Tight-Binding Inhibitors," Biochemica et Biophysica Acta, vol. 185 (1969), pp. 269-286.
Alley, et al., "Feasibility of Drug Screening with Panels of Human Tumor Cell Lines Using a Microculture Tetrazolium Assay," Cancer Research, vol. 48 (1988), pp. 589-601.
Longer, et al., "Preformulation Studies of a Novel HIV Protease Inhibitor, AG1343," Journal of Pharmaceutical Sciences, vol. 84, No. 9, Sep. 1995, pp. 1090-1093.

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