Novel phosphorylmuramyl peptides and processes for the manufacture thereof

Claim 1

Pharmaceutical preparation with antiobiotic activity for parenteral or enteral administration which contains an antibiotically effective combination of at least one antibiotic and an amount sufficient to enhance the activity of said antibiotic of at least one phosphorylmuramyl peptide of the formula ##STR37## wherein X represents carbonyl, R 1 represents lower alkyl unsubstituted or substituted by hydroxy, lower alkoxy or halogen, or represents phenyl unsubstituted or substituted by hydroxy, lower alkoxy, lower alkyl or halogen, R 2 , R 4 or R 6 independently of one another represent hydrogen or lower alkyl, R 3 represents hydrogen or lower alkyl, R 5 represents hydrogen, lower alkyl having from 1 to 3 carbon atoms unsubstituted or substituted by hydroxy, lower alkoxy, mercapto, lower alkylthio, amino or halogen, or represents cycloalkyl or cycloalkyl-lower alkyl in which the lower alkyl radical contains from 1 to 3 carbon atoms, and in each of which the cycloalkyl radical contains from 4 to 6 carbon atoms, phenyl or phenyl-lower alkyl having from 1 to 3 carbon atoms in the lower alkyl radical and each unsubstituted or substituted by hydroxy, lower alkoxy or halogen, or heterocyclyl or heterocyclyl-lower alkyl having from 1 to 3 carbon atoms in the lower alkyl radical, and each containing one or two nitrogen atoms and having 5 or 6 ring members, or R 4 and R 5 together alternatively represent alkylene having 3 to 4 carbon atoms, R 7 represents hydrogen, and one of the radicals A 1 and A 2 represents a radical of the formula ##STR38## in which T represents HN or O, Y represents lower alkylene which is unsubstituted or substituted by hydroxy, lower alkoxy, lower alkanoyloxy, halogen, mercapto, lower alkylthio, lower alkanoylthio, amino-lower alkyl, mono- or di- lower alkylamino-lower alkyl, lower alkanoylamino-lower alkyl, aminocarbonyl, lower alkyl, cycloalkyl having 5 or 6 carbon atoms, a phenyl or a phenyl-lower alkyl radical, or by heterocyclyl or heterocyclyl-lower alkyl having from 1 to 3 carbon atoms in the lower alkyl radical and each containing one or two nitrogen atoms and having 5 or 6 ring members or a radical of one of the formulae ##STR39## in which Y 1 and Y 2 each represents lower alkylene which is unsubstituted or substituted by hydroxy, lower alkoxy, lower alkanoyloxy, halogen, mercapto, lower alkylthio, lower alkanoylthio, amino-lower alkyl, mono- or di-lower alkylamino-lower alkyl, lower alkanoylamino-lower alkyl, aminocarbonyl, lower alkyl, cycloalkyl having 5 or 6 carbon atoms, a phenyl or a phenyl-lower alkyl radical, or by heterocyclyl or heterocyclyl-lower alkyl having from 1 to 3 carbon atoms in the lower alkyl radical and each containing one or two nitrogen atoms and having 5 or 6 ring members and R 8 represents hydrogen, W represents an alkyl or alkenyl group having from 7 to 30 carbon atoms which is unsubstituted or substituted by hydroxy, lower alkoxy, lower alkanoyloxy, halogen, amino, lower alkylamino, lower alkanoylamino or oxo or represents a cycloalkyl or cycloalkenyl radical having from 10 to 30 carbon atoms which is unsubstituted or substituted by one or more alkyl radicals having from 1 to 8 carbon atoms, and the other of the radicals A 1 and A 2 represents hydroxy, lower alkoxy, amino or lower alkylamino, or represents aminocarbonyl-lower alkylamino unsubstituted or substituted in the lower alkyl radical by hydroxy, carboxy or amino groups, or a pharmaceutically acceptable salt thereof together with a significant amount of a pharmaceutically acceptable carrier.