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Pyrimidinylmethylindole derivatives with antibacterial activity

机译:具有抗菌活性的嘧啶基甲基吲哚衍生物

摘要

This invention relates to indole derivatives of the general formula (I) wherein R1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, alkylsulfonyl, cycloalkylsulfonyl, cycloalkylalkylsulfonyl, dialkylsulfamoyl, N-cycloalkyl-N-alkylsulfamoyl, heterocyclylalkyl or phenylalkyl; R2 is hydrogen, halogen, alkyl, alkanoyl, phenyl, phenylalkyl or heterocyclylalkyl; R3 is hydrogen, alkyl; and R4 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, alkylsulfonyl, cycloalkylsulfonyl, cycloalkylalkylsulfonyl, dialkylsulfamoyl, N-cycloalkyl-N-alkylsulfamoyl, heterocyclylalkyl, or phenylalkyl; and pharmaceutically acceptable acid addition salts of these compounds, there use as therapeutically active substances; medicaments based on these substances, optionally in combination with sulphonamides, and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula (I) and their pharmaceutically acceptable acid addition salts and intermediates for their manufacture.
机译:本发明涉及通式(I)的吲哚衍生物,其中R 1为烷基,烯基,炔基,环烷基,环烷基烷基,烷基磺酰基,环烷基磺酰基,环烷基烷基磺酰基,二烷基磺氨酰基,N-环烷基-N-烷基磺氨酰基,杂环基烷基或苯基烷基; R 2为氢,卤素,烷基,烷酰基,苯基,苯基烷基或杂环基烷基; R 3为氢,烷基; R 4是烷基,烯基,炔基,环烷基,环烷基烷基,烷基磺酰基,环烷基磺酰基,环烷基烷基磺酰基,二烷基氨磺酰基,N-环烷基-N-烷基氨磺酰基,杂环基烷基或苯基烷基;这些化合物的药学上可接受的酸加成盐用作治疗活性物质。基于这些物质的药物,及其与磺酰胺的组合,及其生产;这些物质作为药物的用途和用于生产抗菌活性药物的用途;以及制备式(I)化合物及其药学上可接受的酸加成盐和用于制备它们的中间体。

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