Aryl phosphate derivatives of d4T having anti-HIV activity

US6030957A · kind A · utility

Assignee

• Wayne Hughes Institute · US

Inventors

• Fatih M. Uckun · White Bear Lake, US
• Rakesh Vig · Little Canada, US

Key dates

• Filing date: Jun 30, 1998
• Grant date: Feb 29, 2000
• Expiry date: Jun 30, 2018

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07H19/20
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.