Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-11-16
1999-12-14
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540575, C07D24308, A61K 3138, A61K 3155
Patent
active
060018275
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.
REFERENCES:
patent: 3284450 (1966-11-01), Kraaijeveld et al.
patent: 3770733 (1973-11-01), Sianesi et al.
patent: 5130313 (1992-07-01), Comte 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.
Inomata Norio
Iwamori Tomoe
Mizuno Akira
Shibata Makoto
Kifle Bruck
Shah Mukund J.
Suntory Limited
LandOfFree
Benzothiazine derivative does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Benzothiazine derivative, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Benzothiazine derivative will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-863569