| 摘要 |
<p>PROBLEM TO BE SOLVED: To obtain an antiallergic agent having an action on the control of the release of a chemical transmitter substance but not inhibiting histamine H1 receptors. SOLUTION: This antiallergic agent contains a tranexamic acid amide derivative of the formula (R1 , R2 are each H, a 1-18C alkyl, a 5-8C cycloalkyl, benzyl, phenyl, wherein the phenyl group and the phenyl part of the benzyl group may be substituted by one to three of lower alkyl groups, lower alkoxy groups, OH groups, amino groups or halogen groups) and its salt. The compound of the formula is e.g., N-methyl-trans-4-aminomethylcyclohexane carboxylic acid amide hydrochloride. The compound of the formula is obtained by protecting the amino group of tranexamic acid with a proper protecting group, reacting the product with an amine compound to produce the amide of the protected tranexamic acid, and subsequently removing the protecting group from the amide. The compound is administered at a dose of 1-200mg in one to three portions a day for an adult as an oral administration agent, at a daily dose of 0.01-10mg as an injection agent, or to a diseased part at a dose of 1-500mg once to several times a day as a coating agent or a suppository.</p> |
