| 摘要 |
Compounds of the formula R1-A1-NH-C(: NH)-Y-R2 and their acid addition salts wherein R1 is a phenyl or thien-2-yl ring optionally substituted by halogen, alkyl or alkoxy, A1 is a straight or branched alkylene group of from 2-6 C and containing one or two O or S atoms (including hydroxy substituted alkylene) provided that there are at least 2 C between each divalent atom and between the divalent atom or atoms and the NH group; Y is O, S or NH and R2 is a group R1 or R1A2 where A2 is a straight or branched alkylene group of 1-3 C, are prepared by reacting a cyanamide R3NHCN with a compound R4YNH where one of R3 and R4 is an R1A1 and the other an R2 group when Y is NH, and wherein R3 is an R1A1 group and R4 an R2 group when Y is O or S; or, where Y is NH, reacting an isourea or isothiourea R5.NH.CR8 : NR6 with a compound R7NH2, wherein one of R5, R6 and R7 is an R1A1 group, one of the remaining two an R2 group and the last is H, and R8 is respectively an alkoxy or aralkoxy group or an alkylthio or aralkylthio group; or, where Y is O or S, reacting a urea or thiourea R1A1.NH.CY.NH2 with a compound R2Z, wherein Z is a reactive group or atom, and, if desired, forming the salt from the base formed or converting one salt into another. Pharmaceutical compositions comprise the compounds of the invention in a form suitable for enteral or parenteral administration. The compounds antagonize the effects of 5-hydroxytryptamine. |
