Proline derivatives and compositions for their use as inhibitors

Details Proline derivatives and compositions for their use as inhibitors Proline derivatives and compositions for their use as inhibitors

1992-05-15

1994-03-22

Springer, David B.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

548537, C07D20716, C07D40112, A61K 3147, A61K 3140

Patent

active

052966046

ABSTRACT:
The present disclosure describes novel peptidomimetic compounds which contain a novel class of isosteres and which inhibit the proteolytic activity of HIV protease and further describes therapeutic compositions comprising said compounds, a method of treatment for patients having the AIDS virus involving administering a therapeutically effective amount of the novel compounds of the present invention, and a method of preparation for said isosteres.

REFERENCES:
Tamburini et al., 1990, "A Fluorometric Assay for HIV-Protease Activity Using High-Performance Liquid Chromatography", Analytical Biochemistry, 186:363.
Kohl et al., 1988, "Active Human Immuno-deficiency Virus Protease is Required for Viral Infectivity" Proc. Natl. Acad. Sci. USA, 85:4686.
J. R. Huff, 1991, "HIV Protease: A Novel Chemotherapeutic Target for AIDS", J. Med. Chem., 34:2305.

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