5,6-dihydropyrone derivatives as protease inhibitors and antivir

Organic compounds -- part of the class 532-570 series – Organic compounds – Sulfur containing

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549437, C07C32126, C07D31744

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active

059361280

ABSTRACT:
The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.

REFERENCES:
patent: 3206476 (1965-09-01), Collins
patent: 3818046 (1974-06-01), Harris et al.
patent: 3931235 (1976-01-01), Harris et al.
Brinkworth et al., "Flavones are inhibitors of HIV-1 proteinase", Biochemical and Biophysical Research Communications, vol. 188, No. 2, 1992, pp. 631-637.
Thaisrivongs et al., "Structure-Based Design of HIV Protease Inhibitors: 4-Hydroxycoumarins and 4-Hydroxy-2-pyrones as Non-peptidic Inhibitors", J. Med. Chem., vol. 37, 1994, pp. 3200-3204.
Ruwart et al., "Solubility and permeability determine bioavailability of HIV protease", American Association of Pharmaceutical Scientists, San Diego, CA, Nov. 6-10, 1994, Abstract PDD 7290.
PCT International Search Report, PCT/US94/12234.
Richman, "Therapy--HIV", 45.sup.th Symposium of the Society for General Microbiology, , 1990, pp. 261-313.
Toh et al., "Retroviral protease-like sequence in the yeast transposon Ty1", Nature, vol. 315, 1985, p. 691.
Kay and Dunn, "Viral proteinases: weakness in strength", Biochimica et Biophysica Acta, 1048, 1990, pp. 1-18.
Cameron et al., "Comparison of the Substrate-binding Pockets of the Rous Sarcoma Virus and Human Immunodeficiency Virus Type 1 Proteases", Journal of Biological Chemistry, vol. 268, No. 16, 1993, pp. 11711-11720.
Graves, "Human Immunodeficiency Virus Proteinase: Now, Then, What's Next?", Structure and Function of the Aspartic Proteinases, Ed. Dunn, Plenum Press, NY, 1991, pp. 395-405.
Peng et al., "Role of Human Immunodeficiency Virus Type 1-Specific Protease in Core Protein Maturation and Viral Infectivity", Journal of Virology, vol. 63, No. 6, 1989, pp. 2550-2556.
Kohl et al., "Active human immunodeficiency virus protease is required for viral infectivity", Proc. Natl. Acad. Sci. USA, vol. 85, 1988, pp. 4686-4690.
Craig et al., "Antiviral properties of Ro 31-8959, an inhibitor of human immunodeficiency virus (HIV) protease", Antiviral Research, vol. 16, 1991, pp. 295-305.
Tomasselli et al., "The complexities of AIDS: as assessment of the HIV protease as a therapeutic target", Chimicaoggi, 1991, pp. 6-27.
Meek, "Inhibitors of HIV-1 protease", J. Enzyme Inhibition, vol. 6, 1992, pp. 65-98.
Bourinbaiar et al., "Effect of the oral anticoagulant, warfarin, on HIV-1 replication and spread", AIDS, vol. 7, No. 1, 1993, pp. 129-130.

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