5-Formyl-prostacyclin derivs. - useful as long lasting hypotensives, bronchodilators, diuretics etc.

摘要

Prostane derivs. of formula (I) and their salts with pharmaceutically acceptable bases when R1 = H, are new. In (I), R1 is H or alkyl; B is opt. branched, satd. or unsatd. 2-6C alkylene; A is CH2CH2, trans-vinylene or C triple bond C; W is CH2OH or both opt. functionally modified; D is opt. branched 1-5C alkylene or bond; R2 is alkyl, cycloalkyl or opt. substd. aryl; and R3 is opt. functionally-modified OH. (I) are made by reacting the corresp. 5-H cpd. with a Vilsmeyer-Haack reagent. (I) have the same hypotensive, bronchodilating, antisclerotic, diuretic, antiarrythmic, antisecretory and thrombocyte-aggregation inhibiting activities as PGI2 but are more stable with a longer-lasting effect. They have superior tissue specificity e.g. reduced stimulation of guinea pigileum or isolated rabbit trachea. They can be administered orally or parenterally.