Hydroxy-amino acid amides

Details Hydroxy-amino acid amides Hydroxy-amino acid amides

1997-12-08

1999-04-06

Richter, Johann

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

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

544390, 544400, 546343, 546348, 548579, 568735, 585409, C07D24104, C07D21170, C07D20706, C07C 1207

Patent

active

058920382

ABSTRACT:
Compounds of Formula I ##STR1## are disclosed as inhibitors of plasmepsin and cathepsin D. The compounds are therefore useful to treat diseases such as malaria. In preferred compounds of formula I, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. Intermediates in the solid phase synthesis of compounds of formula I, in which the compounds are attached to a solid support, are also disclosed.

REFERENCES:
patent: 5120718 (1992-06-01), Goldman et al.
patent: 5734054 (1998-03-01), Dolle, III et al.
Rich et al., "Design and Discovery of Aspartyl Protease Inhibitors Mechanistic and Clinical Implications," In Conformationally Directed Drug Design, Julius A. Vida and Maxwell Gordon, eds. ACS Symposium Series, American Chemical Society, Washington, D.C., Chapter 10, pp. 211-237, 1984 .

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