| 摘要 |
The invention comprises compounds of the formula <FORM:0991574/C2/1> wherein X is a halogen atom, e.g. Cl or Br, or a nitro or halo-lower alkyl group, e.g. ClCH2 or CF3; R, R1 and R2 are each hydrogen, lower alkyl, lower alkenyl, lower alkynyl, phenyl-lower alkyl or halo-lower alkyl; R3 is lower alkyl, lower alkenyl, lower alkynyl, phenyl-lower-alkyl or halo-lower alkyl, e.g. CF3CH2, and R4 and R5 are each hydrogen, lower alkyl, phenyl or phenyl-lower alkyl or are joined together to form an alkylene group of 3-5 carbon atoms (the word "lower" in the above definitions indicating a group of 1-8 carbon atoms). The compounds are prepared by reacting the appropriate 5-substituted-2,4 - disulphamoyl - aniline with a compound of the formula OHC.CH(R4).CHO or an acetal thereof derived from a lower alcohol. 2,4 - Bis - (substituted sulphamyl) - 5 - X - anilines are made by reacting the bis-sulphonyl chloride with an amine R2R3NH. Di - sulphamyl - 5 - X - anilines wherein R, R1, and R2 are hydrogen are made either by alkylating, alkenylating alkynylating or aralkylating a 3 - keto - 7 - sulphamyl - 2H - 1,2,4-benzothiadiazine - 1,1 - dioxide to introduce the group R3 in the 2-position and treating the resulting benzothiadiazine compound with a base to open the ring; or when the 5-substituent is a nitro group, by treating 5-nitro-aniline-2,4-disulphonyl chloride first with ammonia to give the 4-sulphonamide and then an amine R3NH2. Pharmaceutical preparations having diuretic, natriuretic and antihypertensive activity comprise the above compounds of the invention and a carrier, preferably in unit dosage form such as capsules or tablets.
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