摘要 |
Disclosed are substituted bis(4-aminophenyl)-sulfones of general formula <IMAGE> (I) wherein R1 is hydrogen, alkyl or cycloalkyl; group, R2 is hydrogen or C1-C3 alkyl, R3 is nitrile, C1-C3 alkylaminocarbonyl, di C1-C3 alkylaminocarbonyl, C3-C7 N-cycloalkyl-C1-C3 alkylaminocarbonyl C1-C3 alkylamino, C1-C3, di alkylaminocarbonyl alkoxy, alkylaminosulfonyl, di C1-C3 alkylaminono, diC1-C3 alkylaminosulfonyl, hydroxy C1-C3 alkyl, C1-C3 alkylcarbonyl, amino C1-C3 alkyl or C1-C3 alkoxy C1-C3 alkyl group or, when R1 and R2 are each hydrogen, R3 can be hydroxy, hydroxycarbonyl C1-C3 alkoxy or di C1-C3 aminocarbonylalkoxy; or, when R1 is C1-C3 alkyl or C1-C3 cycloalkyl and R2 is hydrogen or C1-C3 alkyl, R3 can also be halogen, trifluoromethyl, nitro, amino, aminosulfonyl, aminocarbonyl, C1-C3 alkyl, carboxy or C1-C3 alkoxycarbonyl; and R4 is hydrogen or, when R1 and R2 are each hydrogen and R3 is halogen or hydroxy, R4 can also be halogen, hydroxy or C1-C3 alkoxy; or a nontoxic, pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions comprising such compounds alone and in combination with dihydrofolic acid-reductase inhibitors. The compounds and compositions are useful for their inhibiting effect on bacteria, mycobacteria and plasmodia. |
申请人 |
DR. KARL THOMAE GESELLSCHAFT MIT BESCHRAENKTER HAFTUNG |
发明人 |
SEYDEL, JOACHIM KARL;PIEPER, HELMUT;KRUEGER, GERD;NOLL, KLAUS;KECK, JOHANNES;LECHNER, UWE |