9-Oxo-11-alpha methyl prosta-13-enoic acid derivs - as selective anti-ulcer agents without hypotensive or intestinal-contracting side effects

摘要

Prostenoic acid derivs. of formula (I) and their pharmaceutically acceptable salts are new: (where A = 4-8 C alkylene, esp. hexamethylene; R1 = 1-5C alkyl, esp. n-propyl; R2 and R3 are H or 1-4 C alkyl; R4 = H or 1-4 C alkyl). They are prepd. from corresp. 9-(protected oxo)-15-oxo cpd. by redn. then deprotection. (I) are anti-ulcer agents with little or no hypotensive or intestinal-contracting side effects. Thus, in the rat, 9-oxo-11 alpha 16, 16-trimethyl-15 alpha-hydroxyprost-13-trans-enoic acid has ED50 against indomethacin-(30 mg./kg.) induced ulcer of 0.16 mg./kg. Usual dose is 0.5-100 mg./day for adults e.g., as 3-4 tablets.