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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, and n and m are each independently an integer from 1 to 3; and pharmaceutically acceptable acid addition salts thereof.

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First Claim