| 摘要 |
Disclosed are benzothiazine derivatives represented by the following formula (I):wherein the dashed line indicates the presence or absence of a bond; Z represents one of the following groups:in which R1 and R2 individually represent alkyl, aralkyl or the like, R3 represents H, alkyl or the like, R4 represents H, aralkyl or the like, X1, X2 and X3 individually represent O or S, and G represents substituted or unsubstituted ethylene, trimethylene or the like; Q1 and Q2 individually represent H, OH, halogen, alkoxy or the like; A represents alkylene, alkenylene or the like; Y represents CH, C= or N; when Y is CH, m stands for 0 or 1, n stands for 1 or 2, B represents O, S, carbonyl or the like, when Y is C=, m stands for 1, n stands for 1 or 2, B represents:in which the double bond is linked to Y, R6 represents substituted or unsubstituted aryl or the like; when Y is N, m stands for 0 or 1, n stands for 2 or 3 and B represents carbonyl, sulfonyl or the like, E1 and E2 individually represent H or lower alkyl; and D represents an aromatic hydrocarbon group or an aromatic heterocyclic group; and salts thereof.The benzothiazine derivatives (I) and their salts according to the present invention have strong serotonin-2 blocking action, have excellent selectivity to this action against alpha1 blocking action and have high safety. Accordingly, the present invention has made it possible to provide pharmaceuticals making use of antagonistic action against serotonin-2 receptors, for example, therapeutics for various circulatory diseases such as ishemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.
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