U.S. patents available from 1976 to present.
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Aspartyl protease inhibitors

Patent 5883252 Issued on March 16, 1999. Estimated Expiration Date: Icon_subject January 26, 2016. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

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Retroviral protease inhibiting compounds
Patent #: 5354866
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HIV protease inhibitors useful for the treatment of AIDS
Patent #: 5413999
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Inventor: Vacca, et al.

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Inventors

Assignee

Application

No. 592777 filed on 01/26/1996

US Classes:

544/71, Spiro oxazine544/231, Spiro diazine544/336, 1,4-diazines544/384, Chalcogen bonded directly to piperazine ring carbon548/127, 1,2,3-thiadiazoles (including hydrogenated)548/206, 1,2-thiazoles (including hydrogenated)548/311.1, Additional hetero ring attached directly or indirectly to the diazole ring by nonionic bonding (e.g., 1,3-dioxolan-2-yl methyl-imidazole, etc.)548/323.5, Chalcogen attached indirectly to the diazole ring by acyclic nonionic bonding548/324.1, The chalcogen, X, is in a -C(=X)- group548/550Nitrogen attached directly or indirectly to the five-membered hetero ring by acyclic nonionic bonding

Examiners

Primary: Higel, Floyd D.

Attorney, Agent or Firm

Foreign Patent References

  • 0 264 795 EP. 04/20/1988
  • 0 541 168 EP. 05/20/1993
  • 0 560 268 EP. 09/20/1993
  • 0 560 269 EP. 09/20/1993
  • 2288801 GB. 11/20/1995
  • WO 94/19329 WO. 09/20/1994
  • WO 84/26717 WO. 11/20/1994
  • WO 95/24385 WO. 09/20/1995

International Classes

C07D 307/20
C07D 319/06
C07D 493/04
C07D 211/60
C07D 241/04
C07D 277/06

Abstract

This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of 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 aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.

Other References

  • Marquez et al., J. Org. Chem., vol. 37, No. 16, pp. 2558 to 2561 (1972)
  • J.C. Craig et al., "Antiviral Synergy Between Inhibitors of HIV Proteinase and Reverse Transcriptase", Antiviral Chem. and Chemotherapy, 4(3), pp. 161-166 (1990)
  • J.R. Huff, "HIV Protease: A Novel Chemotherapeutic Target for AIDS", Journal of Medicinal Chemistry, 34(8), pp. 2305-2314 (1991)
  • M. Miller et al., "Structure of Complex of Synthetic HIV-1 Protease with a Substrate-Based Inhibitor at 2.3 Å Resolution", Science, 246, pp. 1149-1152 (1989)
  • K.H.M. Murthy et al., "The Crystal Structures at 2.2-Å Resolution of Hydroxyethylene-Based Inhibitors Bound to Human Immunodeficiency Virus Type 1 Protease Show That the Inhibitors Are Present in Two Distinct Orientations", J. Biol. Chem., 267, pp. 22770-22778 (1992)
  • N.A. Roberts et al., "Rational Design of Peptide-Based HIV Proteinase Inhibitors", Science, 248, pp. 358-361 (1990)
  • S. Scharpe et al., "Proteases and Their Inhibitors: Today and Tomorrow", Biochimie, 73, pp. 121-126 (1991
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