A novel series of 1-aryl-4,5,6,7-tetrahydro-1H-indazole-5-carboxylic acids and 2-aryl-4,5,6,7-tetrahydro-2H-indazole-5-carboxylic acids were synthesized via condensation between a phenylhydrazine and a 2-(hydroxymethylene)cyclohexanone-4-carboxylate, and the antiinflammatory activity was determined. In the carrageenan edema test, 1-aryl-4,5,6,7-tetrahydro-1H-indazole-5-carboxylic acids exhibited fairly high antiinflammatory activity. However, the 2-aryl isomers were far less active than the former. The most active compound of the series was 1-phenyl-4,5,6,7-tetrahydro-1H-indazole-5-carboxylic acid, which had an ED50 value of 3.5 mg/kg.

The anti-platelet aggregating action of minidose aspirin and its combined effect with dilazep were examined in healthy male volunteers. A quantitative and dose-dependent decrease in platelet aggregability was observed on a single oral administration of 30 mg, 100 mg and 300 mg of aspirin and also on the repeated oral administration of 10 mg and 30 mg three times a day for 5 days. Administration of 100 mg of dilazep in combination with 30 mg or 100 mg of aspirin produced an anti-platelet effect equivalent to a 3-fold dose of aspirin alone. In the repeated administration test, the t. i. d. admin istration of aspirin 10 mg+ dilazep 100 mg was confirmed to be close to the ideal in the balance between anti-platelet action and the reduced production of PGI2.

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