Title:
7-FLUORODIBENZO(B,F)THIEPIN DERIVATIVES
Document Type and Number:
Japanese Patent JPS5788176
Kind Code:
A
Abstract:
7-Fluoro-dibenzo[b,f]thiepin derivatives of formula: -in which n is 0, 1, 2, 3 or 4; Z is thio, sulfinyl, or sulfonyl; A is 5-tetrazolyl, 3-hydroxy-1,2,5-thiadiazol-4-yl, 4-hydroxy-2,5-dioxo- DELTA <3>-pyrrolin-3-yl, or -CO-R2, where R2 is hydroxy, lower alkyl, lower alkoxy, amino or 2-amino-3-methylthiazoline, or certain substituted amino or lower alkoxy radicals, and the dotted line indicates either an olefinic bond or saturation at the 10,11-position; and the pharmaceutically acceptable salts thereof are novel. They are used in the treatment and control of allergic conditions such as allergic asthma and are made into pharmaceutical compositions for this purpose. Certain specific derivatives, for example, 7-fluoro-dibenzo-[b,f]thiepin-3-carboxylic acid-5-oxides, exist as racemic mixtures and are readily into the respective enantiomers one of which possesses greater bioactivity than the racemic mixture from which it is derived. The compounds are prepared by a number of suitable methods, including hydrolysis of the corresponding 3-cyano compounds and dehydration of a corresponding 11-alcohol to form the 10,11-unsaturated compound.
Inventors:
JIYOSHIYUA ROKATSUCHI
KURARENSU ESU RUUNII
EDOWAADO JIEE KURAGOO JIYUNIYA
KURARENSU ESU RUUNII
EDOWAADO JIEE KURAGOO JIYUNIYA
Application Number:
JP7156081A
Publication Date:
June 01, 1982
Filing Date:
May 14, 1981
Export Citation:
Assignee:
MERCK & CO INC
International Classes:
A61K31/38; A61P37/08; C07D337/14; C07D409/04; C07D409/06; C07D417/04; C07D417/06; (IPC1-7): A61K31/38; C07D337/14