Diphenylthiazole derivative

Details Diphenylthiazole derivative Diphenylthiazole derivative

1993-08-23

1995-09-12

Gerstl, Robert

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

548195, C07D27744, C07D27752

Patent

active

054497833

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/JP91/00310 filed Mar. 7, 1992.
1. Technical Field
This invention relates to novel diphenylthiazole derivative which are efficacious as a drug having antiinflammatory, analgesic, antiallergic, uricosuric or platelet aggregation inhibiting effects.
2. Background Art
There have been disclosed compounds having an amino group or an amino substituent at the 2-position of a diphenylthiazole parent nucleus in Japanese Patent Laid-Open Gazette No. (Sho) 50-121269 (121269/1978) (hereinafter referred to as the prior reference A), Japanese Patent Laid-Open Gazette No. (Sho) 54-160369 (160369/1979) (hereinafter referred to as the prior reference B), Japanese Patent Laid-Open Gazette No. (Sho) 58-216186 (216186/1983) (hereinafter referred to as the prior reference C) and Japanese Patent Laid-Open Gazette No. (Hei) 3-27370 (27370/1991) (hereinafter referred to as the prior reference D).
For example, compounds including 2-morpholino-4,5-diphenylthiazole, 2-methylamino-4,5-diphenyl-thiazole and 2-(N-methyl-N-acetyl)amino-4,5-diphenylthiazole are described in the prior reference A. Regarding the pharmacological effects of these compounds, the prior reference A states that they have a platelet aggregation inhibiting effect accompanied by a hypocholesterolemic effect but exhibit weak or scarcely any antiinflammatory and analgesic effects.
In the prior reference B, compounds including 2-phenethylamino-4,5-diphenylthiazole, 5-methyl-2-phenethylamino-4-phenylthiazole and 2-furfurylamino-5-methyl-4-phenylthiazole are described. The prior reference B states that these compounds are efficacious as an antiinflammatory agent or an immunomodulator.
The prior reference C describes about guanidinothiazole derivatives. It is stated therein that these compounds are particularly efficacious as chemical affecting lipid metabolism, an antithrombotic drug and as a fungicide.
Furthermore, the prior reference D discloses thiazole compounds having pharmacological effects such as antithrombotic and vasodilating effects, processes for producing these compounds and pharmaceutical compositions containing the same.
However these prior references neither disclose nor suggest any diphenylthiazole derivative which is mono- or disubstituted at the amino group at the 2-position by a substituted sulfonyl residue, an acyl group or a halogen-substituted acyl group, like the compound of the present invention. As a matter of course, it has not been known at all hitherto that such compounds have excellent pharmacological activities relating to antiinflammatory, analgesic, antiallergic, uricosuric or platelet aggregation inhibiting effects.
Although the thiazole compound described in the prior reference D is partly common to the compound of the present invention regarding a fundamental parent nucleus and substituted phenyl groups at the 4 and 5-positions and has a chemical structure relatively similar to that of the compounds of the present invention, the former differs from the latter in the substituent at the 2-position. Namely, the compounds of the prior reference D has a substituent ##STR2## at the 2-position wherein R.sup.3 and R.sup.4 represent each a hydrogen atom, a lower alkyl group optionally having a heterocyclic group or a piperidyl group optionally having appropriate substituents. In contrast, the group A.sup.1 of the compounds of the present invention comprises a substituted sulfonyl group, an acyl group or a halogen-substituted acyl group. Thus the compounds of the present invention differ from the the prior reference D in the employed substituent. Any desired pharmacological effect on a satisfactory level cannot be achieved by using such compounds as the ones described in the prior reference D.
Although acidic nonsteroidal antiinflammatory drugs, typical examples of which include aspirin and indomethacin, have clear effects as compared with basic antiinflammatory drugs, they have side effects of causing, for example, gastrointestinal tract disorders. When these drugs are to be administered to young or aged persons

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