Abstract: Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.
Abstract: A process is disclosed for the preparation of (.+-.)-6-cyano-3,4-dihydro-2,2-dimethyl-trans-4-(2-oxo-1-pyrrol idino)-2H-1-benzopyran-3-ol of the Formula (VI) ##STR1## from 4-cyanophenol of the Formula (I) ##STR2## which comprises reacting 4-cyanophenol of the Formula (I) with isoprene, followed with bromination and dehydrobromination steps with formation of intermediates to react with 2-pyrrolidone resulting in obtaining the compound of the Formula (VI).
Type:
Grant
Filed:
June 25, 1990
Date of Patent:
September 8, 1992
Assignee:
Alkaloida Vegyeszeti Gyar
Inventors:
Tibor Timar, Tibor Eszenyi, Peter Sebok, Vilmos Galamb, Julia Fazekas nee Kozak, Terezia Istvan nee Katona, Eva Kovach nee Lakatos, Erika Nagy nee Csaki