Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...
Patent
1981-12-28
1983-05-17
Daus, Donald G.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Bacterium or component thereof or substance produced by said...
544278, C07D51304, A61K 31505
Patent
active
043839967
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel derivative of thiazolo[3,2-a]pyrimidine, a drug which contains it, and a process for the preparation of said derivative of thiazolo[3,2-a]pyrimidine. More particularly, the present invention relates to a novel derivative of thiazolo[3,2-a]pyrimidine having excellent immunoregulating activities which is especially effective in curing such autoimmune diseases as nephritis, rheumatoid arthritis, etc. and a process for the preparation thereof and an immunoregulating drug which contains said derivative as an active ingredient.
BACKGROUND ART
In recent years, immunoregulating therapy has come to be practiced to cure such autoimmune diseases as rheumatoid arthritis, generalized lupus erythematodes, etc. or malignant tumor and a variety of drugs have been developed. As an example of such drugs, the application of levamisole, which is a levorotatory isomer of tetramisole, to the drugs for immunotherapy of cancer and such autoimmune diseases as rheumatoid arthritis has due attention.
Though it has been reported that levamisole has efficacy in said diseases to a certain degree, it has no singularity in its efficacy and does not always display its efficacy satisfactorily either. Many immunoregulating drugs have been developed but most of them not only lack singularity in their remedial activities but also raise a problem of side effects, and no satisfactory drugs of this kind are available as yet.
Meanwhile, it is mentioned in the "Journal of American Chemical Society" vol. 64, pp. 2709-2712, 1942, that a derivative of barbituric acid is obtained from 2-aminothiazoline and diethyl malonate, and that this compound has a hypnotic action and an anesthetic action as well; however, nothing is mentioned in the journal as to other efficacy besides its hypnotic and anesthetic actions.
The inventors of the present invention have prepared a novel thiazolo[3,2-a]pyrimidine derivative which is a novel barbituric acid derivative different from the derivative of barbituric acid mentioned in the above journal and made a focused study of the efficacy of this newly prepared compound. The result is a remarkable finding that it is a compound which has a specific immunoregulating action different from an action owned by levamisole, or the immunoregulating action based on a pharmacological action apart from hypnotic and anesthetic actions, and that, because of its low toxicity, the abovementioned thiazolo[3,2-a]pyrimidine derivative is very useful for curing such autoimmune diseases as rheumatoid arthritis, nephritis, etc., thus producing the present invention.
DISCLOSURE OF INVENTION
The present invention is directed to a derivative of thiazolo[3,2-a]pyrimidine expressed by the following formula (I) ##STR3## (where R indicates a phenyl group or a benzyl group which has a halogen atom, a lower alkyl or lower alkyloxy group as a substituent group, an alicyclic group or an arylethyl group), and a process for the preparation of the derivative of thiazolo[3,2-a]pyrimidine expressed by the following formula (I) ##STR4## (where a definition of R is as same as that given in case of the abovementioned formula (I), comprising cyclizing a compound expressed by the following formula (II) by application of heat ##STR5## (where R indicates a phenyl group or a benzyl group which has a halogen atom, a lower alkyl or lower alkyloxy group as a substituent group, an alicyclic group or an arylethyl group, and R' indicates a halogen atom or lower alkyloxy group), and an immunoregulating drug which contains the derivative of thiazolo[3,2-a]pyrimidine expressed by the abovementioned formula (I) as an active ingredient.
BEST MODE OF CARRYING OUT THE INVENTION
R of the derivative of thiazolo[3,2-a]pyrimidine expressed by the aforementioned formula (I) of the present invention is a phenyl group or a benzyl group which has a halogen atom, a lower alkyl or lower alkyloxy group as a substituent group, an alicyclic group or an arylethyl group.
As a phenyl group or a benzyl group which has a halogen at
REFERENCES:
Masters, E. J., et al., JACS, 64, 2709-2711 (1942).
Bannai Kiyoshi
Hoshina Kenji
Komoriya Keiji
Kurozumi Seizi
Naruchi Tatsuyuki
Daus Donald G.
Gibson Sharon A.
Teijin Limited
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