Substituted benzothiazine derivative

Details Substituted benzothiazine derivative Substituted benzothiazine derivative

C - Chemistry, Metallurgy

07

D

C07D 513/10 (2006.01) A61K 31/54 (2006.01) A61K 31/55 (2006.01) C07D 275/06 (2006.01) C07D 279/02 (2006.01) C07D 417/06 (2006.01)

Patent

CA 2179679

Disclosed are substituted benzothiazine deriva- tives represented by the following formula (I): Image (I) wherein the dashed line indicates the presence or ab- sence of a bond; Z represents one of the following groups: Image , Image and Image 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 sub- stituted or unsubstituted ethylene, trimethylene or the like; Q1 represents H, OH, halogen, alkoxy or the like; Q2 is similar to Q1 except for the exclusion of H; 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: Image 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, 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 substituted benzothiazine derivatives (I) and their salts according to the present invention have strong serotonin-2 blocking action, have excellent se- lectivity to this action against .alpha.1 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 recep- tors, for example, therapeutics for various circulatory diseases such as ishemic heart diseases, cerebrovas- cular disturbances and peripheral circulatory dis- turbances.

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