Gruenenthal Gmbh

Elbion Gmbh

Lothar Heinisch

Ute Moellmann

Ernst Roemer

Walter Werner

Rolf Reissbrodt

Matthias Schnabelrauch

Hildegard Poppe

Thomas Kronbach

Norbert H&ouml;fgen

Regina Draheim

Udo Graefe

Christiane Cuny

Udo Gr&auml;fe

Wolfgang Haas

Peter J&uuml;tten

Steffen Wittmann

Wolfgang Witte

Use of maduraohtalazine derivatives as inhibitors of proinflammatory cytokines

Synthetic catechol derivatives, method for production and use thereof

Polycyclic phthalazine compounds and their use

This invention relates to new benzoxazinedione derivatives corresponding to the formula I: ##STR1## wherein R.sup.1 =H or carboxyalkyl, R.sup.2 =H, alkyl or phenyl, and R.sup.3 represents different acid groups derived from amino acids, dipeptides and hydrazones or conjugates thereof with active ingredients, e.g. antibiotics. The compounds may be present as free acids, in the form of their salts or as readily cleavable esters. The compounds according to the invention constitute heterocyclically protected catechol derivatives and are effective as siderophores against gram-negative bacterial strains, particularly against Pseudomonads and strains of E. coli and Salmonella. In the form of their conjugates with active ingredients, e.g. antibiotics (as 'siderophore-antibiotic conjugates'), they can transport the latter into bacterial cells and can improve or extend the antibacterial effect thereof, sometimes even in relation to bacterial strains which are resistant to other .beta.-lactams. In addition, said compounds, as potential prodrug forms for iron chelating agents, are suitable for use against diseases which are caused by a disorder of the iron metabolism. The invention can be employed in pharmaceutical research and in the pharmaceutical industry, and in agriculture.

Benzoxazinedione derivatives, method of producing them and uses thereof

Growing community of inventors

Jena, Germany

Lothar Heinisch