Ketorolac derivatives with considerably reduced gastro-intestina

Details Ketorolac derivatives with considerably reduced gastro-intestina Ketorolac derivatives with considerably reduced gastro-intestina

1994-01-07

1996-04-16

Siegal, Alan

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

A61K 3140

Patent

active

055083013

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.

REFERENCES:
patent: 4089969 (1978-05-01), Muchowski et al.
Lombardino, "Nonsteroidal Antiinflammatory Drugs." Otterness and Bliven, Chapter 3, pp. 228-231. John Wiley and Sons (1985).
The Merck index, Merck & Co., Inc., pp. 836, No. 5186 (1989).
"Salts of Four Analgesic/Antiinflammatory Agents with the Sodium Salts and the Free Acids." Pharmaceutical Research, vol. 2, No. 3, pp. 255-257 (1987).
Muchowski et al., "Synthesis and Antiinflammatory and Analgesic Activity of 5-Aroyl-1, 2-dihydro-3H-pyrrolo[1, 2-a]pyrrole-1-carboxylic Acids and Related Compounds," J. med. Chem., vol. 28, pp. 1037-1049 (1985).
Gu et al., "Preformulation Salt Selection, Physical Property Comparisons of the Tris(hydroxymethyl)aminomethane" (THAM) (1984).

Affiliated with

Also associated with

Rating

Ketorolac derivatives with considerably reduced gastro-intestina does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Ketorolac derivatives with considerably reduced gastro-intestina, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Ketorolac derivatives with considerably reduced gastro-intestina will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-325456