| 摘要 |
N-6 SUBSTITUTED ADENOSINE DERIVATIVES AS CARDIAC VASODILATORS New, N-6 monosubstituted adenosine derivatives are disclosed which have significant cardiac vasodilatory effect. The compounds of the invention include 6-(cyclo-butyl amino) - 9 - (?-D-ribofuranosyl) - 9H - purine, 6 - (2 - methyl - 2 phenyl hydrazino) - 9 - (?-D-ribofuranosyl) - 9H - purine, and compounds of the general formula: wherein R1 is H, lower alkyl, lower alkoxy, alkylamino, or arylamino, R2 is H, lower alkyl, hydroxymethyl, phenyl or substituted phenyl, R3 is H, lower alkyl, phenyl, substituted phenyl, R3 is H, lower alkyl, phenyl, substituted phenyl, 2or 3-thienyl, or 2- or 3-pyridyl, R4 is H or lower alkyl, and R5 is H or lower acyl. Particularly active as a cardiac vasodilator is the compound (-) - 6 - (R - 1 - phenyl - 2 butyl amino) - 9 - (? D-ribofuranosyl) - 9H - purine. Compounds of the invention having a cardiovascular vasodilatory effect in mammals are prepared by a process including the step of incorporating into a pharmaceutically acceptable carrier for oral, topical or intravenous application in the proportion required for an effective dosage thereof a compound of the formulas described above. |
