| 摘要 |
Novel heterocyclically substituted 5-sulphamoylbenzoic acid derivatives of the accompanying formula I, in which the symbols R<1>, R<2>, X and A have the meaning given in Patent Claim 1, are prepared by introducing the radical X into appropriate 3-nitro-5-sulphamoylbenzoic acids or their esters, which carry a halogen atom in the 4-position and whose 5-sulphamoyl group is protected, reducing the reaction product to the corresponding 3-amino compound, reacting this with dicarboxylic acid derivatives, reducing the 3-imido or 3-amido compounds thus obtained and hydrolysing the reaction product thus obtained to remove the protective group B and the ester group R<3>. The alkyl radicals R<2> can then be introduced by alkylation. Starting from the compounds of the formula I prepared according to the invention, in which X denotes a -SR<4> group, the corresponding compounds in which X denotes a -SOR<4> or -SO2R<4> group are obtained by oxidation. The novel compounds are highly active saluretics and diuretics. They are used mainly for the treatment of oedematous diseases of various origins. <IMAGE>
|
