Thiazepine inhibitors of HIV-1 integrase

US7015212B1 · kind B1 · utility

Assignee

• The United States of America, as represented by the Department of Health and Human Services · US

Inventors

• Nouri Neamati · Ann Arbor, US
• Yves Pommier · Bethesda, US
• Antonio Garofalo · Siena, IT
• Vito Nacci · Siena, IT

Key dates

• Filing date: May 10, 2000
• Grant date: Mar 21, 2006
• Expiry date: May 10, 2020

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P31/18
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention discloses non-catechol compounds, such as thiazolothiazepines, and analogs and derivatives thereof, which are anti-integrase inhibitors. The compounds, which are useful as treatments for HIV disease, include compounds (I), (II), (III), or pharmaceutically acceptable salts thereof wherein A is thiazole, benzene, naphthalene, pyridine, pyrimidine, pyrazine, or quinoline; R is one or more of H, halogen, lower alkyl, lower alkoxy, NO2, lower ester or carboxylic acid; X—Y is CH2—S, S—CH2, CH2—O, CH2—S(O). S(O)—CH2, CH2—CH2, CH2—CH2—CH2, or CH2—CH2—CH2—CH2; R4 is H or hydroxy; R5 is H, phenyl, or alkylamine; W is S or O; and R6 is H, substituted or unsubstituted alkyl or amine; and Z is S, O, CH2, CH2CH2, or C═O.