| 摘要 |
The novel 4-oxocyclic ureas and the pharmaceutically acceptable salts and esters thereof of the present invention are useful as antiarrhythmic and antifibrillatory agents and have following general structure: (I), wherein (a) X is a saturated or unsaturated, 5-, 6-, or 7-membered heterocycle or carbocycle; (b) R is selected from the group consisting of covalent bond, nil, heteroatom, carbonyl, heterocyclic ring, carbocyclic ring, alkyl, alkenyl, alkoxy, alkylamino, arylalkyl, aryloxy, aryl, acyloxy, and acylamino; (c) Y is a substituted or unsubstituted, saturated or unsaturated, 5-, 6-, or 7- membered heterocyclic ring or carbocyclic ring, or is nil; and wherein when R is nil, X and Y are fused ring systems; and when R is a covalent bond, X and Y are ring systems linked through a covalent bond; and when Y is nil, R is a covalent bond, and X is bound to L through R; (d) R1, R2, and R3 are independently selected from the group consisting of nil, Cl, F, Br, NH2, CF3, OH, S03H, CH3SO2NH, COOH, alkoxy; alkyl, alkoxycarbonyl, hydroxyalkyl, carboxyalkyl, aminoalkyl, acylamino and acyloxy; (e) L is selected from the group consisting of alkylamino, alkenylamino, alkylimino, alkenylimino, and acylamino; wherein the nitrogen atom thereof is bound to the nitrogen atom at the 1-position of the 4-oxocyclic urea moiety; (f) R4 is selected from the group consisting of alkyl, alkenyl, alkynyl, alkylacyl, and heteroalkyl; (g) A is a substituted or unsubstituted, saturated or unsaturated, straight-chain or branched, C1-C8 heteroalkyl; or a substituted or unsubstituted, saturated or unsaturated heterocycle having 5-, 6-, or 7-members; and A has one nitrogen atom, which is adjacent to R4; and (h) R5 is a substituted or unsubstituted C1 or C2 alkyl.
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