Patent ID: 6083986
Filing Date: 2000-07-04
Classification: A61P,C07C

Abstract:
A compound having potassium channel inhibitory activity of the formula: ##STR45## wherein, R.sup.1 is H, alkyl or is selected from the group consisting of an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted heterocyclyl and an optionally substituted carbocycloalkyl;R.sup.2 is selected from the group consisting of alkyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted heterocyclyl and an optionally substituted carbocycloalkyl;R.sup.3 is hydrogen or methyl;R.sup.4 is hydrogen or methyl;X.sup.1 is C.dbd.O, C.dbd.S, or SO.sub.2 ;X.sup.2 is C.dbd.O or SO.sub.2 ;Y.sup.1 is O, (CH.sub.2).sub.p, CH.sub.2 O, HC.dbd.CH or NH; wherein p is 0, 1 or 2;Y.sup.2 is O, (CH.sub.2).sub.q, HC.dbd.CH or NH; wherein q is 0 or 1;Z is H, OR.sup.5 or NR.sup.6 R.sup.7 ;whereinR.sup.5 is H, (CH.sub.2).sub.m --R.sup.8 ; or C(O)--(CH.sub.2).sub.m --R.sup.8 ;m=1 to 5;R.sup.8 is N(R.sup.9).sub.2, N(R.sup.9).sub.3 L or CO.sub.2 R.sup.9 ; wherein each R.sup.9 is independently selected from H or alkyl; and L is a counter ion;R.sup.6 is H or alkyl;R.sup.7 is H, alkyl or CO.sub.2 R.sup.10 ; wherein R.sup.10 is alkyl;or a pharmaceutically acceptable salt or prodrug thereof, wherein said prodrug has a terminal group selected from an ester derivative, an amide derivative and a peptide,with the proviso that when Z is H, then X.sup.1 and X.sup.2 cannot both be C.dbd.O while Y.sup.1 is (CH.sub.2).sub.p with p=0, while Y.sup.2 is (CH.sub.2).sub.q with q=0, and while R.sup.1 and R.sup.2 are both methyl.