| 摘要 |
<p>Novel s - triazolo[3,4 - a]isoquinolines of the general formula <FORM:1116308/C2/1> wherein R represents hydrogen or a low alkyl radical containing up to 6 carbon atoms, and non-toxic acid addition salts thereof are prepared (a) by reaction of 1-hydrazino-isoquino-line with a compound of the formula R-CO-X, wherein X represents a hydroxyl or low alkoxy group containing at most 6 carbon atoms, a halogen atom or the radical R-CO-O-; or (b), when R represents a low alkyl radical, by reaction of 1-hydrazino-isoquinoline with a ketene of the formula R1-CH = C = O wherein R1 represents hydrogen or an alkyl radical having from 1 to 5 carbon atoms, and cyclization of the resulting alkyl-substituted 1-hydrazino-isoquinoline; followed in either method by optional conversion to a non-toxic acid addition salt of the product. Pharmaceutical compositions, comprising an s-triazolo - [3,4 - a]isoquinoline of the first formula above or a non-toxic acid addition salt thereof together with a pharmaceutically acceptable carrier or diluent, have cardiovascular, and in particular coronary dilating, activities.</p> |
