| 摘要 |
<p>Isoureas and isothioureas which are hiatamine H2-antagonists and also have histamine H1-antagonist activity and antiinflammatory activity having the structure <CHEM> in which R<1> and R<2> are hydrogen, lower alkyl, or together with the carbon and two nitrogen atoms shown form a dihydroimidazolyl or tetrahydropyrimidyl group, Y is sulphur or oxygen, n is from 3 to 8, X is oxygen or sulphur, Z is hydrogen or lower alkyl, A is C1-C5 alkylene or -(CH2)pW(CH2)q- where W is oxygen or sulphur and the sum of p and q is 1 to 4, and B is methyl, cycloalkyl, heteroaryl, aryl or, when A is alkylene, hydrogen, are prepared by a process in which a compound of structure <CHEM> where D is HY- or a leaving group is reacted with: (a) when D is HY-, an isothiourea <CHEM> where A is lower alkyl or aryl (lower alkyl), or a cyanamide R<1>HNCN or a carbodiimide R<1>N = C = NR<2> or (b) when D is a leaving group, a urea or thiourea <CHEM> or, when Y is oxygen a compound of structure <CHEM> where G is a lower alkylthio, chlorine, bromine or NO2NH-, is reacted with an isothiourea of Structure <CHEM> </p> |
