Glaxosmithkline Istrazivacki Centar Zagreb D.o.o.

Glaxpsmithkline Istrazivacki

Krka, Tovarna Zdravil D.d. Novo Mesto

Davor Kidemet

Milan Mesic

Gorjana Lazarevski

Mladen Mercep

Dijana Pesic

Rok Zupet

Marko Derek

Marina Modric

Marija Leljak

Janez Smodis

Bogdan Stefane

Franc Pozgan

The present disclosure relates to new 11-O-alkyl macrolides and azalides and pharmaceutically acceptable salts and solvates thereof, and to pharmaceutical compositions thereof. The disclosure also relates to a process for the preparation of 11-O-alkyl macrolides and azalides by regioselective 11-O-alkylation of macrolides and azalides having a vicinal diol system, using diazoalkanes in the presence of transition-metal halides or boric acid as catalysts. In another aspect, the disclosure relates to uses of the 11-O-alkyl macrolides and azalides as antibacterial agents or intermediates for the synthesis of other antibacterial agents.

O-alkyl macrolide and azalide derivatives and regioselective process for their preparation

The present invention relates to derivatives of 1-thia-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-&#x3b1; (TNF-&#x3b1;) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

1-thia-3-aza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof

Growing community of inventors

Varazdin, Croatia

Davor Kidemet