Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
2000-02-14
2000-12-12
Krass, Frederick
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514885, 514925, 514926, A61K 31195
Patent
active
061600172
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a medicament useful in preventing and treating ulcerous colitis and/or Crohn's disease.
BACKGROUND ART
Ulcerous colitis and Crohn's disease are designated to specific intractable diseases by the Ministry of Health and Welfare who prescribes, as a treating method for ulcerous colitis, the administration of salazosulfapyridine and prednisolone while adjusting their doses according to the condition of a patient (Annual Report of Refractory Inflammatory Bowel Disease Research Group of Ministry of Health and Welfare, 1988, 38), and as a treating method for Crohn's disease, the massive administration of an adrenocortical hormone for a small intestine type disease and of salazosulfapyridine for a large intestine type disease at an active phase, and the usual administration of salazosulfapyridine at a remissive phase (Annual Report of Refractory Inflammatory Bowel Disease Research Group of Ministry of Health and Welfare, 1990, 34). However, salazosulfapyridine often causes a side effect and hence involves a problem of patients who cannot be tolerant of prolonged administration (intolerant patients). Besides, prednisolone also involves a problem that prolonged administration becomes difficult by a side effect caused by the reason that it is a steroid.
Mesalazine has been developed for alleviating this side effect. However, the incidence rate of the side effect has been somewhat lowered, but not that the side effect has completely vanished. There is no great difference in clinical effect, and so it is hard to say that the problems have been satisfactorily solved. By the way, the results of a double blind test [Japanese Pharmacology & Therapeutics, Vol. 22, supplement, pp. S2555-S2583 (1994)] on mesalazine using salazosulfapyridine as a control were such that the generalized amelioration rate is 68.8% for mesalazine, or 63.5% for salazosulfapyridine, and the incidence rate of the side effect is 11.5% for mesalazine, or 28.1% for salazosulfapyridine.
With respect to the cause of inflammatory intestinal diseases, there have hitherto been many unknown points. However, the cytokine analysis of the tissue of the diseased part of a patient and research on cytokine production by immunocompetent cells have suggested that inflammatory cytokines such as IL-1.alpha., TNF-.alpha., IL-6 and IL-8 strongly participate in the formation and progress of morbidity [Gastroenterology, Vol. 106, pp. 533-539 (1992); Lancet, pp. 2434-2340 (1992)], thus leading to the consideration that the inflammatory intestinal diseases are tissue damages caused by inflammatory cytokines produced at an abnormally high level from immunocompetent cells. In recent years, an anti-cytokine therapy by administration of a TNF-.alpha.-chimera antibody [Gastroenterology, Vol. 109, pp. 129-135 (1995)] or rectal administration of IL-10 [Gastroenterology, Vol. 108, pp. 1434-1444 (1995)] has been attempted as a new attempt. However, this therapy has involved a problem that the treatment is not simple, and high in cost.
Accordingly, it is an object of the present invention to provide an agent for preventing and treating ulcerous colitis and/or Crohn's disease, by which the problem of the side effect attendant on the treatment with salazosulfapyridine or a steroidal agent is overcome, the problems of therapeutic facility and treatment cost in the therapy with the TNF-.alpha.-chimera antibody and the therapy by the rectal administration of IL-10 are solved, and a high therapeutic effect can be achieved.
DISCLOSURE OF THE INVENTION
With the foregoing circumstances in view, the present inventors have made research on various kinds of medicaments using inflammatory intestinal disease models such as i) acetic acid-induced models, ii) trinitrobenzenesulfonic acid-induced models and iii) dextran sulfate-induced models [Scand J Gastroenterol, Vol. 27, pp. 529-537 (1992)]. As a result, it has been found that conagenin is useful as an agent for preventing and treating ulcerous colitis and Crohn's disease, thus leading to com
REFERENCES:
patent: 5952380 (1999-09-01), Ishizuka et al.
Kawatsu, M. et al., "Improvement of intestinal toxicity of 5-fluorouracil by conagenin, a low molecular immunomodulator" Anticancer Res. 1996, vol. 16, No. 5A, pp. 2937 to 2941.
Kawatsu, M. et al., "Modulation by conagenin of inflammatory mediator productions in mice given 5-fluorouracil" Anticancer Res. 1997, vol. 17, No. 2A, pp. 917 to 922.
International Search Report.
Fukushima Masakazu
Ishizuka Masaaki
Maeda Kenji
Shiraishi Tadayoshi
Takeuchi Tomio
Krass Frederick
Taiho Pharmaceutical Co. Ltd.
Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
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