Hydroxyphosphonate peptidomimetics as inhibitors of aspartyl pro

Details Hydroxyphosphonate peptidomimetics as inhibitors of aspartyl pro Hydroxyphosphonate peptidomimetics as inhibitors of aspartyl pro

1999-05-26

2000-11-21

Seaman, D. Margaret

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

514478, 558 70, 558170, 558174, A61K 3166, A61K 3127, C07F 907

Patent

active

061503444

ABSTRACT:
Compounds of Formula I ##STR1## are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or .alpha.-hydroxyamide group and Z is an acyl or .alpha.-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.

REFERENCES:
patent: 5565324 (1996-10-01), Still et al.
Rotella, D.P., "Solid Phase Synthesis of Olefin and Hydroxyethylene Peptidomimetics," Journal of the American Chemical Society, vol. 118, pp. 12246-12247 (1996).
Murphy, M.M. et al., "Combinatorial Organic Synthesis of Highly Functionalized Pyrrolidines . . . , " Journal of the American Chemical Society, vol. 117, no. 26, pp. 7029-7030 (1995).
Baldwin, J.J. et al., "Synthesis of a Small Molecule Combinatorial Library Encoded with Molecular Tags," Journal of the American Chemical Society , vol. 117, no. 20, pp. 5588-5599 (1995).
Wang, G.T. et al., "Synthetic Chemical Diversity: Solid Phase Synthesis of Libraries . . . ," Journal of Medicinal Chemistry , vol. 38, no. 16, pp. 2995-3002 (1995).
Kick, E.K. et al., "Expedient Method for the Solid-Phase Synthesis of Aspartic Acid Protease Inhibitors . . . ," Journal of Medicinal Chemistry , vol. 38, No. 9, pp. 1427-1430 (1995).

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