The United States of America, As Represented by the Secretary, Department of Health and Human Services

Lucyna Lubkowska

Michael Eissenstat

John W Erickson

Ramnarayan S Randad

The present invention provides an aspartic proteinase-inhibiting compound of the formula: wherein a, b, c, d, and e, can be the same or different and each are R, OR, SR, NRR, NHCOR, COR, CN, NO, NH, N, or a halogen, wherein Rand Rare independently H or an alkyl. Substituents Ror Rare each H or an alkyl. Substituent Ris a straight chain or branched alkyl, alkenyl, or alkynyl substituent, or is a cycloalkyl. Substituent A is OH, NH, or SH. Further provided are pharmaceutical compositions, which include a therapeutically effective amount of at least one of the foregoing compounds, and therapeutic methods of using the foregoing compounds.

Aspartic protease inhibitors

The present invention provides a compound of formula (I) wherein a, b, c, d, and e, are R , OR , SR , NR R , NHCOR , CO R , CN, NO , NH , N , or a halogen. R and R are H or alkyl, R and R are H or alkyl, and R is a non-aromatic substituent. Substituent A is OH, NH , or SH. Substituents B and B include amide and sulfonamide groups, which can be cyclic, acyclic, or amino acid derivatives. Alternatively, B and R&prime; together with the nitrogen to which they are bonded, and/or B&prime; and R together with the nitrogen to which they are bonded, define a heterocycle. The present invention further provides a pharmaceutical composition that includes a carrier and a therapeutically effective amount of at least one compound of the present invention. The present invention further provides therapeutic methods that include administering a therapeutically effective amount of at least one compound of the present invention

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Frederick, MD, United States of America

Lucyna Lubkowska