Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-11-20
1995-06-27
Ivy, C. Warren
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
549285, A61K 3135
Patent
active
054280591
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
The present invention relates to a novel benzopyran derivative and its physiologically acceptable salts as well as an anti-allergic agent of low toxicity and superior medical value possessing as its active ingredients a benzopyran derivative and its physiologically acceptable salts.
Relevant Art
A large number of benzopyran derivatives are known from relevant arts, however benzopyran derivative publications such as that of the present invention in which three oxygen atoms are directly linked to the benzopyran derivative skeleton, have been extremely rare.
The benzopyran derivative possessing anti-coagulant action, namely anti-thrombus action, is published in the British Journal of Pharmocology, Volume 20, pages 29-35, 1963, by R. B. Arrola, et. al.
As well, a similar derivative possessing anti-thrombus action has been published by Donald T. Witink, et. al. in the Journal of Medical Chemistry, Volume 31, pages 1473-1445, 1988, and in U.S. Pat. No. 4,845,121.
A derivative with a methyl group combined with the position-3 oxygen atom has been published by V. K. Ahluwalia, et. al. in the Indian Journal of Chemistry, 13B(8), pages 791-794, 1975 and in the Indian Journal of Chemistry, Sect. B, 14B(11), pages 858-860, 1976. Additionally, research done by NMR Analysis on a similar compound is noted by Nakayama in Journal of Science, Hiroshima University, Ser. A-2, Volume 33(2), pages 205-211, 1969. As a naturally occurring isolated compound, a similar derivative has been published by Wang Ming-Shi in Chung Ts'ao Yao, Volume 11(2), pages 49-54, 1980. Additionally, a similar naturally occurring isolated example has been published by S. Q. Yan in Yaoxue Xuebao, Volume 24 (10) , pages 744-748, 1989.
However, in these documents, nothing is stated nor even suggested in regards to the benzopyran derivative, the novel compound of the present invention, with anti-allergic action having the formula below (II). ##STR2## (In the formula R.sup.1, R.sup.2 are hydrogen atoms, acyl groups, alkyl groups, or alkenyl groups; when one of R.sup.3, R.sup.4, R.sup.5, R.sup.6 is a hydroxyl group or a protected hydroxyl group, the remaining groups are hydrogen atoms.)
On one hand, extensive research is being carried out on the development of an anti-allergic agent, and currently various superior anti-allergic agents are being developed. However, Tranilast, a common name for a representative example of an anti-allergic agent currently being sold, has the disadvantages that in spite of the need to administer the drug in comparatively high doses to patients, the acute toxic value (LD.sub.50) is low, in the range of 680-780 mg/Kg, the difference between the effective concentration and toxic concentration is small, the safety range is narrow, and much care must be exercised during use. Additionally, another anti-allergic agent sold under the common name Disodium Cromoglicate, (DSCG) is satisfactory. In regards to toxicity, can be applied by spray absorption, and when orally administered, is difficult to absorb into the living body. However, from the problems of active time life in the living body and of the ability to easily administer the drug, the development of a drug which can be easily administered orally is desirable.
As a result, recently as anti-allergic agents, a large number of compounds are being published. However, these compounds always possess various problems which are (1) the anti-allergic action being insufficient, (2) the effective and toxic dosage amounts being too close, resulting in the safety of the drug in the living body being poor, or (3) the absorption into the living body being poor, and therefore the administration method is limited.
SUMMARY OF THE INVENTION
The inventors of the present invention have undertaken intensive research of a large number of novel compounds in order to provide a compound possessing low toxicity and anti-allergic action which can be orally administrated. As a result, a benzopyran derivative possessing both low toxic character and superior allergic action wh
REFERENCES:
patent: 4845121 (1989-07-01), Witiak et al.
Nakayama, Journal of Science of the Hiroshima University, Ser. A-II, vol. 33, No. 2, pp. 205-211, Sep. 1969.
Chemical Abstracts, vol. 94, No. 8, 23 Feb. 1981, Columbus, Ohio, US; Abstract No. 52760h.
Chemical Abstracts, vol. 112, No. 9, 26 Feb. 1990, Columbus, Ohio, US; Abstract No. 73872b.
Witiak et al, J. Med. Chem., vol. 31, No. 7, pp. 1437-1445. Jul. 1988.
Ahluwalia et al, Indian Journal of Chemistry, vol. 13, Aug. 1975, pp. 791-794.
Ahluwalia et al, Indian Journal of Chemistry, vol. 14B, Nov. 1976, pp. 85-860.
Abe Masayoshi
Inazawa Kazuhiko
Kimura Nobuyuki
Sakai Mitsuru
Takagaki Hidetsugu
Dainippon Ink & Chemicals Inc.
Ivy C. Warren
Owens A. A.
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