Sulfonamidocarbonyl-pyridine-2-carboxamides and their pyridine-N-oxides, process for their preparation and their use as medicaments.

摘要

Sulphonamidocarbonyl pyridine-2-carboxylic acid amide derivs. of formula (I) and their pyridine N oxides are new. R<1> = OH or 1-6C alkoxy; R<2> and R<3> = H, opt. substd. 1-6C alkyl, 1-6C alkoxy, halogen, (esp. F, Cl or Br), CN, OH or NH2; R<6> = H, 1-6C alkyl or a N-protecting gp. such as 1-8C alkanoyl, 1-6C alkylcarbonyl, 1-6C alkoxycarbonyl, benzyloxycarbonyl, 1-10C acyloxy(1-6C)alkyl(esp. 1-10C alkanoyloxy(1-6C)alkyl, benzoyloxy(1-6C)alkyl, benzyloxycarbonyloxy(1-6C) alkyl or 1-6C alkoxycarbonyloxy(1-6C)alkyl), a 1,2,3 or 4-valent physiologically acceptable cation (esp. Na<+>, K<+>, Mg<2+>, Ca<2+>, Al<3+> or an ammonium ion, opt. substd. with one to three 1-8C alkyl, 1-8C hydroxyalkyl, 1-4C alkoxy(1-8C)alkyl, Ph, benzyl or 1-8C alkyl, itself opt. mono-, di- or tri-substd. with OH or 1-4C alkoxy) or a cation of a basic amino acid deriv. R<7> = a gp. of formula -Y-(C-U)r-D-W (except -SO2H); Y = SO2 or CO; C = a bond or opt. branched aliphatic 1-16C alkane-diyl, cycloaliphatic 3-10C alkanediyl, opt.branched 2-16C alkenediyl, cycloalkenediyl, 2-16C alkynediyl, 2-16C alkenynediyl, each contg. 1 or more C-C multiple bonds; U = a bond, H, CO, OCO, COO, CONR, NRCO, O, SO, SO2, NR; R = 1-3C alkyl or H; r = 1-4; D = a bond, H opt. branched 1-10C alkanediyl, opt.-branched 1-10C alkenediyl, 2-10C alkynediyl, 2-10C alkenynediyl each contg. 1 or more C-C multiple bonds. W = a bond, H, 3-10C cycloaliphatic alkyl, alkenyl, alknynyl or alkenynyl or 6-16C aryl or a 5-6 membered heteroaryl gp.; provided that≥1 of C, D and W is not a bond and U is only a heteroatom gp. if C is not a bond or if D and/or W are not a bond; and C and/or W, if not a bond or H are pref. themselves substd. R<4> = H, 1-6C alkyl, Ph, phenyl (1-4C) alkyl; R<5> = opt. substd. opt. branched aliphatic 1-8C alkyl which has an acidic gp.and is opt. further substd.; n = 0 or 1;