The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Dec. 14, 1999
Filed:
Nov. 16, 1998
Akira Mizuno, Kyoto, JP;
Makoto Shibata, Ashikaga, JP;
Tomoe Iwamori, Ibaraki, JP;
Norio Inomata, Mino, JP;
Suntory Limited, Osaka, JP;
Abstract
Disclosed are benzothiazine derivatives represented by the following formula (I): ##STR1## wherein the dashed line indicates the presence or absence of a bond; Z represents one of the following groups: ##STR2## in which R.sub.1 and R.sub.2 individually represent alkyl, aralkyl or the like, R.sub.3 represents H, alkyl or the like, R.sub.4 represents H, aralkyl or the like, X.sub.1, X.sub.2 and X.sub.3 individually represent O or S, and G represents substituted or unsubstituted ethylene, trimethylene or the like; Q.sub.1 and Q.sub.2 individually represent H, OH, halogen, alkoxy or the like; A represents alkylene, alkenylene or the like; Y represents CH, C.dbd. 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.dbd., m stands for 1, n stands for 1 or 2, B represents: ##STR3## in which the double bond is linked to Y, R.sub.6 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, E.sub.1 and E.sub.2 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 .alpha..sub.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 receptors, for example, therapeutics for various circulatory diseases such as ishemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.