Pyrimidinyl methyl indole derivatives with antibacterial...

C - Chemistry – Metallurgy – 07 – D

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C07D 403/06 (2006.01) A61K 31/505 (2006.01) C07D 209/04 (2006.01) C07D 209/08 (2006.01) C07D 209/30 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01)

Patent

CA 2405607

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.

La présente invention concerne des dérivés d'indole répondant à la formule générale (1) dans laquelle R?1¿ représente un alkyle, alcényle, alkynyle, cycloalkyle, cycloalkylalkyle, alkylsulfonyle, cycloalkylsulfonyle, cycloalkylalkylsulfonyle, dialkylsulfamoyle, N-cycloalkyl-N-alkylsulfamoyle, hétérocyclylalkyle ou phénylylalkyle; R?2¿ représente un hydrogène, halogène, alkyle, alkanoyle, phényle, phénylalkyle, ou hétérocyclylalkyle; R?3¿ représente un hydrogène, alkyle; et R?4¿ représente un alkyle, alcényle, alkynyle, cycloalkyle, cycloalkylalkyle, alkylsulfonyle, cycloalkylkylsulfonyle, cycloalkylalkylsulfamoyle, dialkylsulfamoyle, N-cycloalkyl-N-alkylsulfamoyle, hétérocyclylalkyle, ou phénylalkyle; et des sels d'addition acide pharmaceutiquement acceptables de ces composés, leur utilisation comme substances thérapeutiques actives ; des médicaments à base de ces substances, facultativement combinés avec des sulfamides, et leur production ; l'utilisation de ces substances comme médicaments et dans la production de médicaments à activité antibactérienne ; ainsi que la fabrication des composés de la formule (1) et de leurs sels d'addition acide pharmaceutiquement acceptables et leurs intermédiaires de fabrication.

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