Bioversys Ag

Marcel Tigges

Peter Schneider

Marc Gitzinger

Daniel Gygax

Martin Fussenegger

Wilfried Weber

Ronald Schoenmakers

Rainer Riedl

Michel Pieren

Assaf Levi

Mark Sephton

Birgit Schellhorn

Patrik Zueger

Michael Brand

Peter Spies

The invention relates to compounds and pharmaceutical compositions useful in combination with tetracyclines in the treatment of bacterial infections caused by Gram-positive and Gram-negative pathogens, with particular efficacy in tetracycline resistant strains. These compounds specifically bind to TetR and therefore prevent the transcriptional activation of tet resistance genes. The compounds have a potentiating effect on the activity of members of the tetracycline family, in particular of tetracycline, minocycline, doxycycline and tigecycline, in the treatment of tetracycline susceptible, intermediate and tetracycline resistant pathogens.

Composition for treatment of pathogens that are resistant to tetracyclines

The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein Ris optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; Ris (CH)wherein n is 0, 1, 2, 3 or 4; Ris (CH)Rwherein m is 0, 1, 2, 3 or 4, and Ris methyl, isopropyl, tert-butyl, OCH, OH, optionally substituted phenoxy, C&#x2261;CH, C&#x2261;N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing Xwith the meaning O, S, NH, N(CH) or CH; and Xis O, S or NH; and a compound of formula (2) wherein Ris optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, &#x2014;NRR; or &#x2014;NH&#x2014;N&#x2550;CH&#x2014;R; and substituents Rto Rhave the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis. 

Composition for treatment of tuberculosis

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Reinach, Switzerland

Marcel Tigges