Patent ID: 6150362
Filing Date: 2000-11-21
Classification: A61P,C07D

Abstract:
A method of ameliorating angiogenic diseases comprising administering an effective therapeutic amount of a compound having Formula I, ##STR13## or pharmaceutically acceptable salts or prodrugs thereof, wherein R.sub.1, R.sub.2, R.sub.3, and are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.20 alkyl, and C.sub.1 -C.sub.20 alkanoyl; orR.sub.1 and R.sub.2 together with the nitro gen atom to which they are attached form a ring independently selected from the group consisting of morpholine, piperidine, piperazine, and pyrrolidine; orR.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form a ring independently selected from the group consisting of morpholine, piperidine, piperazine, and pyrrolidine;A is selected from the group consisting of heterocycle, (hetero gvcle)--C.sub.1 -C.sub.20 -alkyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.6 -C .sub.15 spiroalkyl, and --B--L--Y;B and Y are independently aryl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.4 -C.sub.10 cycloalkenyl, heterocycle, or C.sub.6 -C.sub.15 spiroalkyl;L is a covalent bond, --C(.dbd.W)--, C.sub.1 -C.sub.20 alkylene, --NR.sub.5 --, --NR.sub.6 C(X)NR.sub.7 --, C.sub.2 -C.sub.20 alkynylene, C.sub.2 -C.sub.20 alkenylene, --O--, --S(O).sub.t --, --NR.sub.6 C(X)--, --C(X)NR.sub.6, --NR.sub.6 SO.sub.2 NR.sub.7 --, --NR.sub.6 SO.sub.2 --, SO.sub.2 NR.sub.6 --, SO.sub.2 NR.sub.6 --, or --O-- C(R.sub.100)(R.sub.200)--;R.sub.5 is hydrogen, C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkanoyl, and C.sub.1 -C.sub.20 arylalkyl;R.sub.6 and R.sub.7 are independently hydrogen, C.sub.1 -C.sub.20 alkyl, and aryl-C.sub.1 -C.sub.20 -alkyl;R.sub.100 and R.sub.200 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.20 alkyl, and C.sub.1 -C.sub.20 alkanoyl;W is O, S, or (.dbd.N--O--R.sub.6) ;X is O or S;t is 0-2;each L is shown with its left end attached to B and its right end attached to Y; andat each occurrence, aryl, cycloalkyl, cycloalkenyl, heterocycle, spiroalkyl, alkylene, and (heterocele)alkyl may be optionally substituted with 1-3 substituents independently selected from C.sub.1 -C.sub.20 alkoxy, C.sub.1 -C.sub.20 alkyl, amino, aryl, azido, cyano, halo, C.sub.1 -C.sub.20 haloalkyl, heterocycle, nitro, or ##STR14## wherein A and D are independently oxygen or S(O).sub.t and n is 2-3, with the proviso that when B and Y are unsubstituted phenyl and L is a covalent bond, then at least one of R.sub.1, R.sub.2 ;R.sub.3, and R.sub.4 is other than hydrogen, andwith the proviso that when L is a covalent bond and one of B or Y is unsubstituted imidazole and the other is unsubstituted phenyl, then at least one of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 is other than hydrogen.