The United States of America As Represented by the Department of Health

National Institutes of Health, a Component of the US Dept. of Health & Human Services

The United States of America As Represented by the Secretary of

Ramnarayan S Randad

John W Erickson

Michael Eissenstat

Lucyna Lubkowska

Talapadi N Bhat

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

The present invention provides 2,5-diamino-3,4-disubstituted-1,6-diphenylhexane (DAD) isosteres comprising benzamide, sulfonamide and anthranilamide subunits, a pharmaceutical composition comprising such compounds, a method of using such compounds to treat retroviral, specifically HIV and more specifically HIV-1 and HIV-2, infections in mammals, particularly humans, a method of synthesizing asymmetric DAD isosteres comprising benzamide, sulfonamide and anthranilamide subunits, and a method of using such compounds to assay new compounds for antiretroviral activity.

2,5-diamino-3,4-disubstituted-1,6-diphenylhexane isosteres comprising

2, 5-diamino-3, 4-disubstituted-1, 6-diphenylhexane isosteres comprising

The present invention provides novel retroviral agents containing anthranilamide, substituted benzamide, amino acid, and other subunits, a pharmaceutical composition comprising such compound, and a method of using such compounds to treat retroviral infections in mammals, specifically HIV and more specifically HIV-1 and HIV-2, in humans.

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Frederick, MD, United States of America

Ramnarayan S Randad