Gruenenthal Gmbh

Leibniz-institut Fuer Naturstoff-forschung Und Infektionsbiologie E.v. Hans-knoell-institut

Alere International

Leibniz Institute for Natural Product Research and Infection Biology E.v. Hans-knoell-institut

Ute Moellmann

Lothar Heinisch

Rolf Reissbrodt

Matthias Schnabelrauch

Vadim Albertovich Makarov

Ernst Roemer

Martin Roth

Cole Stewart

Udo Graefe

Walter Werner

Kerstin Herold

Ingrid Groth

Wolfgang Witte

Christiane Cuny

Friedrich Gollmick

Karin Brigitte Charlotte Graefe, Legal Representative

Steffen Wittmann

Andrea Graefe, Legal Representative

A Vadim Makarov

Susanna Graefe, Legal Representative

Stewart T Cole

T Stewart

Vadim A Makarov

The present invention relates to compounds of Formula (I) or salts thereof wherein R, R, R, R, R, R, and other variables enumerated under one or more of same are as defined herein. Compounds of Formula I have activity as antimicrobial agents. Also disclosed are pharmaceutical compositions and methods of treating and preventing microbial infections in mammals, for example, a tuberculosis or leprosy infection, which employ compounds of Formula (I) or salts thereof.

Antimicrobial compounds, their synthesis and their use for treatment of mammalian infections

Disclosed are benzothiazin derivatives of formula (I), preparation methods therefore, and treatment methods employing such compounds as antibacterial agents in treating infectious diseases of mammals caused by bacteria, especially diseases like tuberculosis and leprosy caused by mycobacteria: wherein R, R, R, R, R, and R, and other variables enumerated under one or more of R, R, R, R, R, and Rare as defined.

Benzothiazinone derivatives and their use as antibacterial agents

The invention relates to the novel antibiotic HKI10311129 which has a molecular weight of 1113 and the summation formula CHNO. The invention also relates to a method for producing said antibiotic using the microorganismspec. DSM 13059, and to the use thereof as an antibacterial substance which is especially effective against infections with Gram positive bacteria, especially antibiotic-resistant germs.

HKI10311129, novel antibiotic, method for producing the same and the use thereof

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

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Jena, Germany

Ute Moellmann