Hydroxypropylamide peptidomimetics as inhibitors of aspartyl pro

Details Hydroxypropylamide peptidomimetics as inhibitors of aspartyl pro Hydroxypropylamide peptidomimetics as inhibitors of aspartyl pro

1998-04-29

1999-11-16

Ramsuer, Robert W.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

544391, C07D29514

Patent

active

059861029

ABSTRACT:
Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathsepsin D. The compounds are useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is a heterocycle, amide, sulfonamide or carbamate and Z is an acyl or a functionalized acyl. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid phase support, are also disclosed.

REFERENCES:
Atsuumi, Shugo et al. "Renin Inhibitors. III. Synthesis and Structure-Activity Relationships of Transition-State Inhibitors Containing Dihydroxyethylene Isotere at the P1-P1 Site", Chem. Pharm. Bull. 42(2) 306-313 (1994).
Cavallaro et al, Chemical Abstracts, vol. 130, No. 324763, 1999.

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