CARBACYCLINS, PROCESS FOR THEIR PRODUCTION AND THEIR USE AS MEDICAMENTS

摘要

The invention provides compounds of the general formula < IMG > (I), in which X is oxygen or -CH2-; A is CH2-CH2; trans-CH=CH- or -C?C- , W is -CH(OR); -D-E-R2 has the structure < IMG > wherein Y2 and Y3 are independently each H or C1-4-alkyl and < IMG > represents < IMG > < IMG > < IMG > or < IMG > wherein Y4 is C1-5-alkyl; and Y5 is H or C1-5-alkyl and is different from R2;,R1 is OR; R2 is H, C1-10-alkyl, C2-10-alkenyl; C1-10-alkyl or C2-10-alkenyl, each substituted by C6-10-aryl or substituted C6-10-aryl as defined below; C4-10-cycloalkyl; C4-10-cycloalkyl substituted by C1-4-alkyl, C6-10-aryl, C6-10-aryl substituted by 1 to 3 halogen atom, a phenyl group, 1 to 3 alkyl groups each of 1 to 4 carbon atoms, or a chloromethyl, fluoromethyl, trifluoromethyl, carboxyl, C1-C4-alkoxy or hydroxy group; or an aromatic heterocycle or 5 or 6 ring atoms, one of which is O, N or S, the remainder being carbon atoms; and R is H or tetrahydropyranyl, tetrahydrofuranyl, .alpha.ethoxyethyl, trimethylsilyl, dimethyl-tert-butylsilyl, tribenzylsilyl, C1-4-alkanoyl, benzoyl or an acyl group of a C1-15-hydro-carbon sulfonic acid. The compounds have hyptotensive and bronchodilative properties. Furthermore, they can be used for the prophylaxis and therapy of cardiac infarct and for the treatment of stroke. They may be prepared by reducing the corresponding 1carboxylic acid derivatives.