Hydroxyphosphonate peptidomimetics as inhibitors of aspartyl proteases
AssigneePharmacopeia, Inc.
InventorsCarolyn DiIanni Carroll, Roland Ellwood Dolle, III, Yvonne Class Shimshock, Timothee Felix Herpin
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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.
Claims7
A compound of Formula I ##STR70## wherein:
- R.sup.1 is chosen from the group consisting of alkyl, --(CH.sub.2).sub.n -cycloalkyl, --(CH.sub.2 CH.sub.2).sub.n NHC(O)-alkyl, and arylalkyl, wherein n=1-3;
- R.sup.2 is H or
- .sup.S--C(O)--L--, wherein .sup.S is a solid support, and --L-- is a linker;
- R.sup.7 is H, alkyl, arylalkyl, or --(CH.sub.2).sub.n -cycloalkyl;
- and
- R.sup.8 is alkyl, arylalkyl, or aryl.
Dependencies are inferred from the claim text.