Patent ID: 6313158
Filing Date: 2001-11-06
Classification: A61P,C07D

Abstract:
A 3-heteroarylidenyl-2-indolinone compound having the following chemical structure: ##STR4##wherein,A is selected from the group consisting of nitrogen, oxygen and sulfur;Z is selected from the group consisting of oxygen, sulfur and --NR.sup.11 wherein,R.sup.11 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, aryl, hydroxy, alkoxy, aryloxy, R.sup."" C(O)--, --C(O)OR.sup."", R.sup."" C(O)O--, C-amido, guanyl, sulfonyl and trihalomethanesulfonyl;R.sup.1 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, aryl, hydroxy, alkoxy, --C(O)OR.sup."", C-amido, trihalomethane, R.sup."" C(O)--, trihalomethanesulfonyl and sulfonyl;R.sup.2 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, aryl and halogen;When A is nitrogen,R.sup.3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, aryl, hydroxy, alkoxy, aryloxy, R.sup."" C(O)--, --C(O)R.sup."", R.sup."" C(O)O--, C-amido, guanyl, sulfonyl and trihalomethanesulfonyl;One or two of R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are independently selected from the group consisting of --NR.sup.8 R.sup.9, --J(CH.sub.2).sub.m NR.sup.8 R.sup.9, --JCH.sub.2).sub.m C(.dbd.Y)Q, --N.dbd.CNR.sup.8 R.sup.9 and --NHR.sup.10, wherein,J is selected from the group consisting of oxygen, NH and sulfur;m is 0, 1, 2 or 3;Y is selected from the group consisting of NH and oxygen;Q is selected from the group consisting of hydroxy, alkoxy, aryloxy, amino, N-hydroxylamino, R.sup."" C(O)O--, NR.sup.8 R.sup.9 and N-peptidyl;R.sup.8 and R.sup.9 are independently selected from the group consisting of hydrogen, alkyl, --C(O)OR.sup."", C-peptidyl and, combined, a five-member or 6-member heteroalicyclic group containing at least one nitrogen;R.sup.10 is a polyhydroxyalkyl group;those of R.sup.4, R.sup.5, R.sup.6 and R.sup.7 which are not substituted as noted above are independently selected from the group consisting of hydrogen, alkyl, trihaloalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, heteroalicyclic, hydroxy, alkoxy, aryloxy, thiohydroxy, thioalkoxy, thioaryloxy, sulfinyl, sulfonyl, S-sulfonamido, N-Sulfonamido, trihalomethanesulfonyl, R.sup."" C(O)--, --C(O)OR.sup."", R.sup."" C(O)O--, C-amido, N-amido, cyano, nitro, halo, O-thiocarbamyl, N-thiocarbamyl, guanyl and phosphonyl;R.sup.4 and R.sup.5 may combine to form a six-member cycloalkyl, heteroaryl or heteroalicyclic ring; andR.sup."" is selected from the group consisting of hydrogen, alkyl, cycloalkyl and aryl; or, a physiologically acceptable salt thereof;wherein at least one of the selected chemical substituents is a peptidyl group.