FORFARANDE FOR FRAMSTELLNING AV SULFAMOYL-BENSENSULFONAMIDER MED TERAPEUTISKA EGENSKAPER

摘要

1280418 Sulphonamides MERCK & CO Inc 21 Sept 1970 [26 Sept 1969] 44897/70 Heading C2C Novel compounds I (including salts thereof) where R is alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, haloalkyl, aryl, aralkyl, dialkylsulphamoyl-substituted aryl or a 5- or 6- membered heterocycle bonded either directly via a nuclear carbon or indirectly via a methylene radical to Z (the heterocycle contains a single hetero atom, i.e. O, N or S), Z is CO or SO 2 , R1 is H, alkyl, or cycloalkyl and R2 is alkyl or cycloalkyl or -NR1R2 is a 5- or 6-membered heterocyclic ring, X is halo, C 1-6 alkyl, NO 2 , trihalomethyl, CN or CO 2 H or two Xs on adjacent carbon atoms may constitute a hydrocarbylene chain containing 3 or 4 carbons between their points of attachment and m is 0 to 4, are made by standard methods utilizing compounds II to XIV, some of which are prepared and described (X3 and X5 are halogen, Y is alkanoylamino, R6 is alkyl and X‹ is nitro or sulphamoyl). Pharmaceutical preparations effective as uricosuric agents and useful in treating gout and gouty arthritis and also capable of inhibiting penicillin excretion contain I as active ingredient. Administration may be orally or parenterally.