公开(公告)号：US4992430A

公开(公告)日：1991-02-12

申请号：US302158

申请日：1989-01-26

申请人： Joachim K. Seydel ,  Helmut Pieper ,  Gerd Kruger ,  Klaus Noll ,  Johannes Keck ,  Uwe Lechner

发明人： Joachim K. Seydel ,  Helmut Pieper ,  Gerd Kruger ,  Klaus Noll ,  Johannes Keck ,  Uwe Lechner

IPC分类号： C12N9/99 ,  A61K31/135 ,  A61K31/165 ,  A61K31/24 ,  A61K31/275 ,  A61K31/505 ,  A61P31/04 ,  A61P33/00 ,  A61P43/00 ,  C07C67/00 ,  C07C205/26 ,  C07C205/34 ,  C07C313/00 ,  C07C315/04 ,  C07C317/36 ,  C07C317/48

CPC分类号： C07C205/34 ,  C07C205/26 ,  C07C317/00 ,  C07C323/00

摘要： Disclosed are substituted bis(4-aminophenyl)-sulfones of general formula ##STR1## wherein R.sub.1 is hydrogen, alkyl or cycloalkyl; group,R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl,R.sub.3 is nitrile, C.sub.1 -C.sub.3 alkylaminocarbonyl, di C.sub.1 -C.sub.3 alkylaminocarbonyl, C.sub.3 -C.sub.7 N-cycloalkyl-C.sub.1 -C.sub.3 alkylaminocarbonyl C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3, di alkylaminocarbonyl alkoxy, alkylaminosulfonyl, di C.sub.1 -C.sub.3 alkylaminono, diC.sub.1 -C.sub.3 alkylaminosulfonyl, hydroxy C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkylcarbonyl, amino C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy C.sub.1 -C.sub.3 alkyl groupor, when R.sub.1 and R.sub.2 are each hydrogen, R.sub.3 can be hydroxy, hydroxycarbonyl C.sub.1 -C.sub.3 alkoxy or di C.sub.1 -C.sub.3 aminocarbonylalkoxy;or, when R.sub.1 is C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 cycloalkyl and R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl, R.sub.3 can also be halogen, trifluoromethyl, nitro, amino, aminosulfonyl, aminocarbonyl, C.sub.1 -C.sub.3 alkyl, carboxy or C.sub.1 -C.sub.3 alkoxycarbonyl; andR.sub.4 is hydrogen or, when R.sub.1 and R.sub.2 are each hydrogen and R.sub.3 is halogen or hydroxy, R.sub.4 can also be halogen, hydroxy or C.sub.1 -C.sub.3 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.