Ketorolac derivatives with considerably reduced gastro-intestinal irritation and ulceration
AssigneeRoemmers S.A.I.C.F.
InventorsCarlos E. A. Monti, Gustavo Enrique Aldoma
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Abstract
The present invention concerns compounds of formula (I) which is the novel 2-(1-pyrrolidinyl)ethylester of (.+-.)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxyl- or ketorolac-acid, the pharmaceutically acceptable addition salts thereof, preferably oxalate. It is known that the commercially available ketorolac (trometamole salt) exhibits undesired side effects (gastro-intestinal irritation and ulceration). Surprisingly, when applying the compounds according to the invention there are considerably less undesired effects which render them potentially of great advantage as analgetic/antiphlogistic agent.
Claims5
A pharmaceutical composition comprising in a therapeutically effective amount 2-(1-pyrrolidinyl)ethylester of (+)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid of formula (I) ##STR2## and pharmaceutically acceptable addition salts thereof;
- and appropriate amounts of pharmaceutically acceptable excipients appropriate for galenic formulations for oral or parenteral administration.
Dependencies are inferred from the claim text.