Patent number: 6121240
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.
Type:
Grant
Filed:
December 20, 1996
Date of Patent:
September 19, 2000
Assignee:
Chiron Corporation
Inventors:
Steven Rosenberg, Kerry L. Spear, Eric J. Martin