| 摘要 |
<p>The invention comprises compounds of formula <FORM:1033268/C2/1> wherein R1 and R2 are C1- 7 groups optionally substituted by a hydroxyl group or a di-(C1- 7 alkyl) amino group or in combination form a C1- 7 alkylene, monooxa-C1- 7 alkylene or monoaza-C1- 7 alkylene group whose aza-atom may be substituted by a C1- 7 alkyl or C1- 7 hydroxyalkyl group, R3 and R4 are C1- 7 alkyl groups, R5 is a hydrogen or halogen atom or a C1- 7 alkyl C1- 7 alkoxy or trifluoromethyl group and R6 is a hydrogen atom or an acyl group derived from a C1- 10 aliphatic, araliphatic or aromatic carboxylic acid, acid addition salts thereof, and their preparation by (a) reaction of a simple or mixed anhydride of a 5-dialkylsulphamyl-anthranili acid or an inner anhydride of an N-acyl-S-dialkylsulphamyl-anthranilic acid, i.e. a 6-(dialkylsulphamyl)-4(H)-3:1-benzoxazine-4-one, with an amine of formula HNR1R2, (b) reduction of a nitro group to an amino group -NHR6, or (c) acylation or hydrolysis of the group -NHR6. Nitro-starting materials wherein the group -NHR6 is replaced by a nitro group are prepared by formation of the group -CONR1R2 by conversion of the corresponding acid to its chloride and reaction with the appropriate amine. S - Diethylsulphamyl - 2 - nitro - benzoic acid is prepared by reaction of 5-chlorosulphonyl-2-nitro-benzoic acid with diethylamine. 6 - Dimethylsulphamyl - 2 - methyl - 4 - (H)-3:1 - benzoxazine - 4 - one is prepared by heating 5 - dimethylsulphamyl - anthranilic acid with acetic anhydride. 5 - Dimethylsulphamyl - isatoic anhydride is prepared by refluxing 2-amino-5-dimethyl-sulphamyl-benzoic acid with ethyl chloroformate. The compounds of the invention have anti-inflammatory, anti-allergic and blood-pressure lowering activity and may be used in pharmaceutical compositions in combination with a carrier, for example in forms suitable for oral, topical or parenteral administration.</p> |
