Non-nucleoside reverse transcriptase inhibitors

US6610714B2 · kind B2 · utility

Assignee

• MEDIVIR AB · SE

Inventors

• Christer Sahlberg · Stuvsta-Snättringe, SE
• Dmitry Antonov · Huddinge, SE
• Hans Wallberg · Stuvsta-Snättringe, SE
• Rolf Noreen · Huddinge, SE

Key dates

• Filing date: Mar 5, 2002
• Grant date: Aug 26, 2003
• Expiry date: Mar 5, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D213/85
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds of the formula I: where;R1 is O, S;R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond;R3 is H, C1-C3 alkyl,R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto;X is —(CR8R9)n—R8 and R9 are independently H, C1-C3 alkyl, OH or R8 and R9 together are ═On is 1, 2 or 3and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.