PURPOSE: To obtain the subject antiinflammatory agent useful for the treatment of inflammatory diseases, allergic diseases and circulatory system diseases by using a specific pyrimidobenzothiazine derivative having lipoxygenase- inhibiting action as an active component.
CONSTITUTION: The objective medicine contains the pyrimidobenzothiazine derivative of formula I or II (R1 and R2 are H or methyl) or its salt, e.g. 1,5- dihydro-2H-pyrimido[4,5b] [,14]benzothiazine-2,4(3H)dione, as an active component. The compound of formula I can be produced, e.g. by successively adding and reacting bromine and an ice-cooled saturated NaHCO3 solution to an aqueous solution of a compound of formula III, and successively reacting the obtained compound of formula IV with N-bromosuccinimide and a 2- aminobenzenethiol derivative of formula V. The compound of formula II is produced by reacting the compound of formula I with an oxidizing agent such as diethyl azodicarboxylate.
SAKAKIBARA MINORU
HAYAKAWA TAKAKO
SHISHIDO YUJI