Title:
BENZOTHIAZINE DERIVATIVE
Document Type and Number:
WIPO Patent Application WO/1995/018117
Kind Code:
A1
Abstract:
A benzothiazine derivative represented by general formula (I) or a salt thereof, wherein the broken line indicates the presence or absence of a bond; Z represents any of the groups (a), (b), (c), (d), (e), (f), (g) and (h); (wherein R1 represents alkyl, aralkyl, etc.; R2 represents alkyl, aralkyl, etc.; R3 represents H, alkyl, etc.; R4 represents H, aralkyl, etc.; X1, X2 and X3 represent each O or S; and G represents optionally substituted ethylene, trimethylene, etc.); A represents alkylene, alkenylene, etc.; Y represents CH, C= or N, provided when Y is CH, then m represents O or 1, n represents 1 or 2, and B represents O, S, carbonyl, etc., when Y is C=, then m represents 1, n represents 1 or 2, and B represents (i) (wherein the double bond is bound to Y, and R6 represents optionally substituted aryl, etc.), and when Y is N, then m represents O or 1, n represents 2 or 3, and B represents carbonyl, sulbonyl, etc.; E1 and E2 represent each H or lower alkyl; and D represents an aromatic hydrocarbon group, aromatic heterocyclic group, etc. The benzothiazine derivatives and salts thereof have a potent serotonin 2 blocker activity and an excellent 'alpha'1 blocker activity selectivity and are highly safe, thus providing drugs utilizing a serotonin 2 receptor antagonism, for example, remedies for circulatory diseases such as ischemic heart diseases, cerebrovascular diseases and peripheral circulation disorder.
Inventors:
MIZUNO AKIRA (JP)
SHIBATA MAKOTO (JP)
IWAMORI TOMOE (JP)
INOMATA NORIO (JP)
SHIBATA MAKOTO (JP)
IWAMORI TOMOE (JP)
INOMATA NORIO (JP)
Application Number:
PCT/JP1994/002194
Publication Date:
July 06, 1995
Filing Date:
December 22, 1994
Export Citation:
Assignee:
SUNTORY LTD (JP)
MIZUNO AKIRA (JP)
SHIBATA MAKOTO (JP)
IWAMORI TOMOE (JP)
INOMATA NORIO (JP)
MIZUNO AKIRA (JP)
SHIBATA MAKOTO (JP)
IWAMORI TOMOE (JP)
INOMATA NORIO (JP)
International Classes:
C07D279/02; C07D417/06; C07D513/10; (IPC1-7): C07D279/02; C07D417/06; C07D513/10; A61K31/54
Domestic Patent References:
| WO1993016073A1 | 1993-08-19 |
Foreign References:
| FR2675801A1 | 1992-10-30 | |||
| JPH01311059A | 1989-12-15 | |||
| JPH0267274A | 1990-03-07 | |||
| JPH03255063A | 1991-11-13 |
Other References:
Eur. J. Pharmacol., Vol. 204, No. 1, 1991, ROGER GODBOUT et al., pp. 97-100.
J. Med. Chem., Vol. 36, Apr. 1993, JEAN-LUC MALLERON et al., pp. 1194-1206.
J. Med. Chem., Vol. 34, 1991, JEAN-LUC MALLERON et al., pp. 2477-2483.
J. Med. Chem., Vol. 36, Apr. 1993, JEAN-LUC MALLERON et al., pp. 1194-1206.
J. Med. Chem., Vol. 34, 1991, JEAN-LUC MALLERON et al., pp. 2477-2483.
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