Substituted bicyclic heteroaryl compounds and their use as integrin antagonists

US6706738B2 · kind B2 · utility

Assignee

• AVENTIS PHARMA LIMITED · GB

Inventors

• David Edward Clark · Harlow, GB
• Paul Robert Eastwood · Romford, GB
• Neil Victor Harris · Tilbury, GB
• Clive McCarthy · Woodstock, GB
• Andrew David Morley · Cambridge, GB
• Stephen Pickett · West Malling, GB

Key dates

• Filing date: Oct 11, 2001
• Grant date: Mar 16, 2004
• Expiry date: Jun 11, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention is directed to physiologically active compounds of general formula (I):R1Z1—Het—L1—Ar1—L2—Y  (I)wherein Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring containing at least one heteroatom selected from O, S or N; R1 is optionally substituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; Z1 represents a direct bond, an alkylene chain, NR4, O or S(O)n; L1 is an a —R5—R6— linkage where R5 is alkylene, alkenylene or alkynylene and R6 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, —C(═Z3)—NR4—, —NR4—C(═Z3)—, —Z3—, —C(═O)—, —C(═NOR4)—, —NR4—, —NR4—C(═Z3)—NR4—, —SO2—NR4—, —NR4—SO2—, —O—C(═O)—, —C(═O)—O—, —NR4—C(═O)—O— or —O—C(═O)—NR4—; L2 is a direct bond; an optionally substituted alkylene, alkenylene, alkynylene, cycloa…