摘要 |
<p>PURPOSE:To obtain a new propenoic acid derivative, having antagonistic actions on adenosine A1 and useful as a preventing and a therapeutic agent for renal failure, a diuretic agent, etc. CONSTITUTION:This propenoic acid derivative is expressed by the formula [ring A is an aromatic ring; X, Y and Z are each 0, S, N or C; R<1> is a substitutive alkyl or a substitutive heteroaryl; R<2> to R<4> are each H, an alkyl, an alkenyl, an alkynyl or W-Q (W is a group derived from an alkyl; Q is an aryl, a cycloalkyl, CN, CH, etc.); R' and R' are each H or an alkyl; R<7> and R<8> are each H, an alkyl, an alkoxy, a substitutive aryl, a substitutive arylakyl, carboxyalkyl, etc., which may be protected, or together with N to which they are bound, may form a ring; B is 0 or S] or a salt thereof, e.g. (+)-(E)-N-{1-(3- chlorophenyl)-2-(pyridin-2-yl)ethyl}-3-(3-1H-phenyl pyrazol-4-yl)-2-propenamide.</p> |