1-Sulphonyl-methyl-prostan-1-one derivs. - useful e.g. as selective and long lasting luteolytics, bronchodilators, hypotensives

摘要

Prostaglandin derivs. of formula (I) are new. In (I) R1 is alkyl, cycloalkyl, aralkyl, opt. substd. aryl or heterocyclic; R2 is H or opt. branched 1-5C alkyl, or R1+R2 are together linear or branched 2-5C alkylene, opt. substd. by 1-4C alkyl; R3 is H or opt. functionally-modified OH; R4 is alkyl (opt. halogenated), cycloalkyl, opt. substd. aryl or heterocyclic; A is CH2CH2 or cis-CH=CH; Z is CO or alpha or beta-OH; B is CH2CH2, trans-CH=CH or C tripled bond C; W is opt. functionally-modified CH2OH or C(is approx. CH3)(is approx. OH); alpha or beta-OH; D and E are together a direct bond or D is opt. branched 1-5C alkylene and E is O, S or direct bond. (I) are prepd. by reacting the corresp. methyl ethers with MCHR2.SO2R1 (M = alkali metal). (I) are variously useful as luteolytics, for inducing abortion, labour or menstruation, for synchronising oestrus in animals, as bronchodilators, gastric acid inhibitors, hypotensives, diuretic and antiarrythmics. Compared with natural PG's they are more selective, longer lasting and effective at lower doses, and can be administered orally.