Non-nucleoside reverse transcriptase inhibitors

US7642277B2 · kind B2 · utility

Assignee

• Boehringer Ingelheim International GmbH · DE

Inventors

• Bruno Simoneau · Laval, CA
• Anne-Marie Faucher · Oka, CA
• Serge R. Landry · Kitchener, CA
• Jeffrey O'Meara · Laval, CA
• Bounkham Thavonekham · Longueuil, CA
• Christiane Yoakim · Laval, CA

Key dates

• Filing date: Nov 21, 2003
• Grant date: Jan 5, 2010
• Expiry date: Dec 27, 2025

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D409/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed herein are compounds of formula Ar1—X—W—Ar2 wherein Ar1 and Ar2 represent aryl groups characterized generally as aromatic heterocycles (e.g. imidazolyl or tetrazolyl) or carbocycles (e.g. phenyl or naphthalenyl); the aryl groups are optionally substituted or fused with other heterocycles or carbocycles; the aryl groups can bear substituents such as alkyl, halo or O-alkyl. X is a heteroatom, a valence bond or an optionally substituted divalent methylene, and W represents a spacer; typical spacers include divalent alkylene or alkylene-amido, -amido or -oxy radicals, which may optionally be substituted (e.g. hydroxyl or oxo). A typical compound is a derivative of 2-(N-napthalenyltetrazolylthio)-N-(2-nitrophenyl)acetamide. The compounds have inhibitory activity against Wild Type and single or double mutant strains of HIV.