Benzothiazine derivative

Details Benzothiazine derivative Benzothiazine derivative

1996-06-24

1999-02-23

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

544 49, A61K 3154, C07D27916

Patent

active

058744290

ABSTRACT:
Disclosed are benzothiazine derivatives represented by the following formula (I): ##STR1## 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 ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.

REFERENCES:
patent: 3284450 (1966-11-01), Kraaijeveld et al.
patent: 5563144 (1996-10-01), Damour et al.
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.
Bioorganic & Medical Chemistry Letters, vol. 3, No. 10, 1993, pp. 1913-1918, "New Indole Derivatives as Potent and Selective Serotonin Uptake Inhibitors", Serge Mignani et al.

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