Urokinase receptor ligands

US6121240A · kind A · utility

Assignee

• Chiron Corporation · US

Inventors

• Steven A. Rosenberg · Potomac, US
• Kerry L. Spear · Oakland, US
• Eric Martin · Corona, US

Key dates

• Filing date: Dec 20, 1996
• Grant date: Sep 19, 2000
• Expiry date: Dec 20, 2016

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02A50/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds of the invention inhibit urokinase plasminogen activator or uPAR: ##STR1## where R.sub.10 is --CH(R.sub.9)XCH(R.sub.1)(R.sub.11) or a capping group, where X is NR.sub.12, CR.sub.12 R.sub.15, O, S, SR.sub.12, or SR.sub.12 R.sub.15 ; R.sub.1, R.sub.9, R.sub.11, R.sub.12 R.sub.15 are each H, lower alkyl, lower alkenyl, lower alkynyl, aryl, aralkyl, aryl-alkenyl, aryl-alkynyl, aryl-cycloalkyl, substituted with 0-3 halo, OH, NH.sub.2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, CN or NO.sub.2 ; R.sub.16 is --CH(R.sub.5)C(.dbd.O)NH.sub.2, H, lower alkyl, cycloalkyl, or lower alkenyl; R.sub.2 is aryl or aralkyl, unsubstituted or substituted with 1-3 halo, OH, NH.sub.2, CN, NO.sub.2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, or cycloalkyl; R.sub.3 and R.sub.5 are each independently H or lower alkyl; R.sub.4 is --CH.sub.2 C(.dbd.O)NR.sub.13 R.sub.14, where R.sub.13 is H, lower alkyl, phenyl or benzyl, and R.sub.14 is H, aryl, or aralkyl, where R.sub.6 and R.sub.7 are each independently H, OH, NH.sub.2, CN, NO.sub.2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, or cycloalkyl…