Abstract:
Basically substituted 4-piperazino-benzene-1,3-disulfonamides, their non toxic salts and a process for their manufacture which process comprises introducing either the piperazino radical in 4position or the basic group in 6-position into corresponding 1,3benzene sulfonamides having an appropriate group in 4- or 6position in usual manner or by oxidizing compounds containing an allyl group which is interrupted by an S or an SO-group.
Abstract:
1437023 Benzene-1,3-disulphonamides HOECHST AG 13 Aug 1973 [12 Aug 1972 7 July 1973] 38246/73 Heading C2C [Also in Division A5] The invention comprises compounds having the general formula wherein R is C 1 to C 6 alkyl; R 1 and R 2 are hydrogen, methyl or ethyl; R 3 is hydrogen or C 1 to C 6 alkyl; and R 4 is hydrogen, optionally substituted allyl, C 1 to C 6 alkyl which may be interrupted by oxygen, sulphur, -SO-, -SO 2 - or -N-alkylthe nitrogen atom of which may be a member of a 5- or 6-membered heterocyclic ring, C 3 to C 8 cycloalkyl or cycloalkylalkyl, or aralkyl (optionally substituted by one or two halogen atoms or alkyl, alkoxy, bismethylene-oxy, or mono- or di-alkylamino groups) or 2-furylmethyl, 2-tetrahydrofurylmethyl or pyridylmethyl, or the group represents pyrrolidyl, piperidyl or morpholinyl which may be alkyl substituted, hexamethyleneimino or 4-alkyl-piperazin-1-yl. They may be prepared by (a) reacting a compound of the formula where X is halogen, alkyl or arylsulphonyloxy with an amine of the formula or (b) reacting a compound of formula with a piperazine derivative of the formula or (c) methylating a compound of Formula I in which at least one of R 1 to R 4 is hydrogen, or (d) oxidizing a compound of the Formula I in which R 4 is an alkyl radical interrupted by a sulphur atom or a -SO- group. The compounds of the invention exhibit hypotensive properties and may be administered by the intraduodenal and intravenous routes optionally as their physiologically tolerable salts, alone or in admixture with pharmaceutically acceptable diluents or carriers.
Abstract:
Antihypertensively-active 3-sulfamoyl-4-piperazinyl-benzoic acids, optionally substituted in the 2-position by halogen or alkyl, and the esters, amides, and nitriles of these acids are disclosed, as is a method for making these compounds by the reaction of the corresponding 4-halogeno- or 4-alkyl-(or 4-aryl-) sulfonyloxy-benzoic acids (or their esters etc.) with piperazines.