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

The United States of America, as Represented by the Secretary, Department of Health and 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