| 摘要 |
<p>Tetrahydroperimidines (I) of tautomeric formulae (Ia) and (Ib) and their pharmaceutically acceptable salts, in racemic or optically active form, are new (R is H or halogen; n is 1 or 2; R1 is H, alkyl or aryl; R2 is H, alkyl, alkenyl, cycloalkyl, aryl, acyl, amino, alkylamino, dialkylamino, arylamino or heteroarylamino; the aryl gps. in R2 are opt. substd. by halogen, NO2, alkyl, alkoxy, amino or acylamino; the alkyl gps. in R2 are opt. substd. by opt. substd. phenyl pyridyl or a 5-7 membered opt. unsatd. ring opt. contg. 1 or 2 same or different O, S or NR1 gps.; R1 is H, alkyl, aryl, aralkyl or acyl; or R1 and R2 together form alkylene opt. interrupted by O, S, SO, SO2 or NR2; R2 is H, alkyl, aryl, heteroaryl, aralkyl, COR3, CSR3, C(=NH)R3 or SO2R3; R3 is alkyl, cycloalkyl, aryl, aralkyl, alkoxy, NH2, alkylamino, dialkylamino, arylamino or 5-or 6-membered opt. unsatd. heterocyclyl contg. 1 S or 1 or 2 O, NH or N-alkyl gps.; aryl in R2 is opt. substd. by amino, acylamino, halogen, alkyl, alkoxy, CN or NO2). (I) have antihypertensive, coronary vasodilatory, vascular smooth muscle tone reducing (vascular spasmolytic) and muscular spasmolytic activity. the vascular spasmolytic activity may affect the whole system or be localised, e.g. in the CNS. The muscular spasmolytic activity affects the smooth muscles of the gastrointestinal, urogenital and respiratory tracts. (I) are used in human or veterinary medicine, esp. for treating circulatory disorders, in daily doses of 0.01-50 mg/kg. i.v. or 0.1-200 mg/kg. p.o., opt. in combination with other drugs.</p> |
