Non-nucleoside reverse transcriptase inhibitors

US6806265B2 · kind B2 · utility

Assignee

• Boehringer Ingelheim International GmbH · DE

Inventors

• Bruno Simoneau · Laval, CA
• Serge R. Landry · Kitchener, CA
• Eric Malenfant · Rosemère, CA
• Julie Naud · Blainville, CA
• Jeffrey O'Meara · Laval, CA
• Bounkham Thavonekham · Longueuil, CA
• Christiane Yoakim · Laval, CA

Key dates

• Filing date: May 6, 2003
• Grant date: Oct 19, 2004
• Expiry date: May 6, 2023

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds represented by formula I: whereinR2 is selected from the group consisting of H, (C1-4)alkyl, halo, haloalkyl, OH, (C1-6)alkoxy, NH(C1-4alkyl) or N(C1-4alkyl)2; R4 is H or Me; R5 is H or Me; R11 is H, (C1-4)alkyl, (C3-4)cycloalkyl and (C1-4)alkyl-(C3-4)cycloalkyl; A is a connecting chain of (C1-3)alkyl; B is O or S; n is 0 or 1; wherein when n is 0:Ring C is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted;and E is CONR12R13; CONHNR14R15; NR16COR17; NR18SO2(C1-6)alkyl; SO2NR19R20; or SO2R21; orwhen n is 1: Ring C is as defined above and E is a single bond or a connecting group; andRing D is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted with from 1 to 5 substituents;or a salt or a prodrug thereof are provided as inhibitors of HIV reverse transcriptase.