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Sulphonamidocarbonyl pyridine-2-carbonic acid amides and their pyridine-N-oxides, their manufacturing processes and their use as medicinal products

机译:磺酰氨基羰基吡啶-2-碳酸酰胺及其吡啶-N-氧化物,其制备方法和用作医药产品的用途

摘要

Sulphonamidocarbonyl pyridine-2-carboxylic acid amide derivs. of formula (I) and their pyridine N oxides are new. R1 = OH or 1-6C alkoxy; R2 and R3 = H, opt. substd. 1-6C alkyl, 1-6C alkoxy, halogen, (esp. F, Cl or Br), CN, OH or NH2; R6 = 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+, Mg2+, Ca2+, Al3+ 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. R7 = 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. R4 = H, 1-6C alkyl, Ph, phenyl (1-4C) alkyl; R5 = opt. substd. opt. branched aliphatic 1-8C alkyl which has an acidic gp.and is opt. further substd.; n = 0 or 1;
机译:磺酰胺基羰基吡啶-2-羧酸酰胺的衍生物。式(I)的式(I)及其吡啶N氧化物是新的。 R 1 = OH或1-6C烷氧基; R 2和R 3 = H,选择。取代1-6C烷基,1-6C烷氧基,卤素(尤其是F,Cl或Br),CN,OH或NH2; R 6 = H,1-6C烷基或N-保护性gp。如1-8C烷酰基,1-6C烷基羰基,1-6C烷氧基羰基,苄氧基羰基,1-10C烷氧基(1-6C)烷基(特别是1-10C烷酰氧基(1-6C)烷基,苯甲酰氧基(1-6C)烷基,苄氧基羰基氧基(1-6C)烷基或1-6C烷氧基羰基氧基(1-6C)烷基),1,2,3或4价生理上可接受的阳离子(特别是Na +,K +,Mg 2 +,Ca 2 +,Al 3+或铵离子,优选用1至3个1-8C烷基,1-8C羟烷基,1-4C烷氧基(1-8C)烷基,Ph,本身为OH或1-4C烷氧基的单,二或三取代的苄基或1-8C烷基)或碱性氨基酸衍生物的阳离子。 R 7 = gp。式-Y-(C-U)r-D-W(-SO2H除外); Y = SO2或CO; C =债券或期权。支链的脂肪族1-16C链烷二基,脂环族3-10C链烷二基,优选分支的2-16C链烯基,环链烯基,2-16C炔基,2-16C链烯基。 1个或多个C-C多键; U =键,H,CO,OCO,COO,CONR,NRCO,O,SO,SO2,NR; R = 1-3C烷基或H; r = 1-4; D =债券,H选择。续接1-10C链烷二基,任选分支的1-10C链烯基,2-10C炔基,2-10C炔基。 1个或多个C-C多重键。 W =键,H,3-10C环脂族烷基,烯基,炔基或亚炔基或6-16C芳基或5-6元杂芳基gp。前提是C,D和W中的1个不是键,而U只是杂原子gp。如果C不是债券,或者D和/或W不是债券; C和/或W,如果不是键或H,则是优选的。自己取代。 R 4 = H,1-6C烷基,Ph,苯基(1-4C)烷基; R 5 =优化。取代选择。支链的脂肪族1-8C烷基,具有酸性gp.。进一步替换。 n = 0或1;

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