Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-10-06
1998-06-23
Bond, Robert T.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546 39, A61K 31435, C07D22122
Patent
active
057706042
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP. 95/00180, filed Feb. 9, 1995, which in turn claims priority of JAPAN 6-47648, filed Feb. 9, 1994.
TECHNICAL FIELD
The present invention relates to a novel compound possessing an aconitine chemical structure and also relates to an antipyretic/analgesic/anti-inflammatory agent containing said compound as an active ingredient. In further detail, the present invention relates to a compound possessing an aconitine chemical structure illustrated by general formula (I), or a salt thereof ##STR2## wherein, R.sub.1 is a hydrogen atom or hydroxyl group;
In addition, the present invention relates to an antipyretic/analgesic/anti-inflammatory agent characterized in that it contains as an active ingredient a novel compound possessing an aconitine chemical structure illustrated by general formula (I), or a salt thereof ##STR3## wherein, R.sub.1 is a hydrogen atom or hydroxyl group;
BACKGROUND ART
Aconitine alkaloids contained in the tuberous root of plants of the genus Aconitium have previously been reported to have potent analgesic and anti-inflammatory activity (e.g., Tohoku J. Exp. Med., 128:175-187 deemed to have a narrow margin of safety.
DISCLOSURE OF INVENTION
As a result of extensive studies in attempts to obtain novel aconitine alkaloid derivatives which are low in toxicity and also retain the analgesic and anti-inflammatory activity of aconitine alkaloids, the present inventor has heretofore succeeded in offering a novel aconitine compound and an analgesic/anti-inflammatory agent (See JP, A, S63-211268, JP, A, S63-211269, JP, A, S64-34965, JP, A, H1-143859 and JP, A, H3-223255). Thereafter, the present inventor succeeded in offering an analgesic/anti-inflammatory agent containing as an active ingredient a novel analgesic/anti-inflammatory agent of 14-O-p-chlorobenzoylaconine, or a salt thereof, which exhibits activity superior to that of compounds having a p-chlorobenzoyloxy group bonded to the position 14 carbon atom of the aconitine chemical structure (See JP, A, H5-17448). As a result of further studies, the present inventor has now discovered that among compounds having a p-chlorobenzoyloxy group bonded to the position 14 carbon atom of the aconitine chemical structure, compounds having an acetyloxy group bonded to the position 15 carbon atom are particularly excellent in their pharmacological effect and are also highly safe.
Tail pressure methods and hot plate methods used for the evaluation of the analgesic activity are experimental methods applied for evaluating the activity of morphine or other such compounds having a powerful analgesic effect. The non-steroidal antipyretic/analgesics aspirin and indomethacin have a weak analgesic activity compared to morphine and are deemed to show no remarkable activity in tail pressure methods and hot plate methods. Additionally, in hot plate methods, the action of a mouse licking its paws in response to the heat stimulus provided is taken to indicate involvement of the higher central nervous system. Thus, in evaluating the analgesic effect of a compound, this method is considered a better reflect pain relief in humans than other experimental methods. In tail pressure methods and hot plate methods employing subcutaneous administration, the compound pertaining to the present invention was found to have an even stronger analgesic effect than 14-O-p-chlorobenzoylaconine and to have an antipyretic effect on rats with yeast-induced fever. Furthermore, in concomitant drug use involving intravenous administration of morphine and subcutaneous administration of the compound pertaining to the present invention, the compound pertaining to the present invention was found to strongly reinforce the analgesic effect of morphine.
Consequently, the compound pertaining to the present invention makes a great contribution to intensely painful illnesses and pyretic and inflammatory illnesses. Furthermore, the analgesic effect of the compound pertaining to the present invention is not suppressed even by concomitant use with a morphine antagon
REFERENCES:
Zhang et al. Sites on Analgesic Action of 3,15-diacteylbenzoylacynine. Acta Pharmacologica Sinica, 15(2) pp. 176-180. English translation also attached, Mar. 1994.
Sato et al., "Pharmacological Actions of Aconitine Alkaloids", Tohoku J. Exp. Med., vol. 128:175-187, (1979).
Bond Robert T.
Sanwa Shoyaku Kabushiki Kaisha
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