SULFONAMIDES AND PHARMACEUTICAL PREPARATION

organic chemistry, pharmacy. SUBSTANCE: invention describes novel compounds sulfonamides of the general formula (I) where R1 is taken among monocyclic five-six-membered S, N and/or O-containing heterocyclic residue, for example, pyridyl, pyrimidinyl, isoxazolyl, thienyl, thazolyl that can be free or substituted with lower alkyl, halogen atom or lower alkanyl; R2 means hydrogen atom, lower alkyl, lower alkoxy-group, lower alkylthio-group, lower alkoxy-lower alkyl, lower alkylsulfonyl-lower alkoxy-group, phenyl, lower alkylphenyl, lower alkoxy- -phenyl, lower alkylenedioxyphenyl, phenyl-lower alkyl, lower alkylphenyl-lower alkyl, lower alkoxyphenyl-lower alkyl, lower alkylenedioxyphenyl-lower alkyl, monocyclic six-membered N and/or O-containing hetercyclic residue, for example, pyrimidinyl, pyridyl, morpholino-group; R3 means lower alkyl, lower alkoxy-group. formyl, halogen-lower alkyl, hydroxy-lower alkyl, amino-lower alkyl or residue -CH2O-A-lower alkyl, or -(CH2)m-O-(CRaRb)n-B-R9 where R4-R8 means hydrogen atom, lower alkoxy-group or halogen atom; R9 means pyridyl, pyrimidinyl; Ra and Rb mean hydrogen atom or lower alkyl; A means ketalated 1,2- -dihydroxyethylene group; B means -OC(O)O-, -OC(O)NH-, -NHC(O)NH- or NHC(O)O-; n = 2, 3 or 4 and m = 0 or 1. Compounds of the formula (I) are inhibitors of endothelin receptors and can be used as biologically active substances in preparing drugs used for treatment of diseases associated with endothelium activity, in part, circulation system, for example, hypertension, ischemia, vessel spasm and stenocardia. EFFECT: new compounds indicated above, valuable medicinal properties. 24 cl, 60 ex