Patent ID: 6133261
Filing Date: 2000-10-17
Classification: A61K,A61P

Abstract:
A therapeutic method comprising treating a human afflicted with, or at risk of stroke, by administering thereto an effective amount of a compound of formula (I):R--NH--[--C(.dbd.Q)--C(R.sub.2)(R.sub.3)--NH--].sub.n --C(.dbd.A)R.sub.1(I)wherein;R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl, aryl (lower alkyl), heterocyclic, heterocyclic (lower alkyl), (lower alkyl) heterocyclic, lower cycloalkyl, or lower cycloalkyl (lower alkyl), and R is unsubstituted or is substituted with at least one electron withdrawing group, or electron donating group;R.sub.1 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl (lower alkyl), aryl, heterocyclic, (lower alkyl) heterocyclic, heterocyclic (lower alkyl), lower cycloalkyl, or lower cycloalkyl (lower alkyl), each unsubstituted or substituted with an electron donating group or an electron withdrawing group andR.sub.2 and R.sub.3 are independently hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl (lower alkyl), aryl, heterocyclic, heterocyclic (lower alkyl), (lower alkyl) heterocyclic, lower cycloalkyl, lower cycloalkyl (lower alkyl), SO.sub.3.sup.-, or Z--Y wherein R.sub.2 and R.sub.3 may be unsubstituted or substituted with at least one electron withdrawing group or electron donating group;Z is O, S, S(O).sub..alpha., NR.sub.4, PR.sub.4 or a chemical bond;Y is hydrogen, lower alkyl, aryl, aryl (lower alkyl), lower alkenyl, lower alkynyl, halo, heterocyclic, heterocyclic (lower alkyl), (lower alkyl)heterocyclic; cycloalkyl or cycloalkyl (lower alkyl) and Y may be unsubstituted or substituted with an electron donating group or an electron withdrawing group, provided that when Y is halo, Z is a chemical bond;or ZY taken together is NR.sub.4 NR.sub.5 R.sub.7, NR.sub.4 OR.sub.5, ONR.sub.4 R.sub.7, OPR.sub.4 R.sub.5, PR.sub.4 OR.sub.5, SNR.sub.4 R.sub.7, NR.sub.4 SR.sub.7, SPR.sub.4 R.sub.5, PR.sub.4 SR.sub.7, NR.sub.4 PR.sub.5 R.sub.6, PR.sub.4 NR.sub.5 R.sub.7, NR.sub.4 C(O)R.sub.5, SC(O)R.sub.5, NR.sub.4 CO.sub.2 R.sub.5, SCO.sub.2 R.sub.5, NR.sub.4 C(O)R.sub.5 R.sub.6, NR.sub.4 C(O)NR.sub.5 S(O).sub.a R.sub.6, NR.sub.4 C(S)R.sub.5 R.sub.6, NR.sub.4 C(.dbd.Q)MNR.sub.5 C(.dbd.A)OR.sub.6, or C(S)NH.sub.2 ;R.sub.4, R.sub.5 and R.sub.6 are independently hydrogen, lower alkyl, aryl, aryl (lower alkyl), lower alkenyl, or lower alkynyl, wherein R.sub.4, R.sub.5 and R.sub.6 may be unsubstituted or substituted with an electron withdrawing group or an electron donating group;R.sub.7 is R.sub.6, COOR.sub.8, or C(O)R.sub.8 ;R.sub.8 is hydrogen, lower alkyl, or aryl (lower alkyl), and the aryl or alkyl group may be unsubstituted or substituted with an electron withdrawing group or an electron donating group;A and Q are independently O or S;M is an alkylene chain containing up to 6 carbon atoms or a chemical bond;n is 1-4; anda is 1-3;or a pharmaceutically acceptable salt thereof.