Glaxo Group Limited

Pliva, Farmaceutska Industrija, Dionicko Drustvo

Pliva D.d.

Glaxosmithkline Istrazivacki Centar Zagreb D.o

Glaxosmithkline Istrazivacki Center Zagret D.o.o.

Stjepan Mutak

Gorjana Lazarevski

Gabrijela Kobrehel

Sergio Lociuro

Antun Hutinec

Zorica Marusic-Istuk

Andrea Berdik

Suleman Alihodzic

Daniele Andreotti

Stefano Biondi

Drazen Pavlovic

Miljenko Dumic

Jessica Tibasco

Andrea Fajdetic

Federica Damiani

Alfonso Pozzan

Francesca Cardullo

Natasa Marsić

Marko Djerek

Marko Derek

Alfredo Paio

Vlado Stimac

Ilaria Bientinesi

Manuela Ciraco

Vesna Erakovic

Anna Quaglia

Wolfgang Schoenfeld

Nedjelko Kujundzić

Sulejman Alihodzi&cacute;

The present invention relates to the new 3-decladinosyl derivatives of 9-de-oxo-9a-aza9a-homoerythromycin A 9a,11-cyclic carbamate of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, wherein Rindividually stands for hydrogen, hydroxyl or a group of the formula (II), wherein X individually stands for C-Calkyl group, C-Calkenyl group or X individually stands for C-Calkyl group with at least one incorporated O, S or N atom or X individually stands for (CH)&#x2014;Ar or X individually stands for (CH)-heterocycloalkyl, wherein (CH)individually stands for alkyl, wherein n is 1-10, with or without incorporated atom O, S or N, wherein Ar individually stands for 5-10-membered monocyclic or bycyclic aromatic ring with 0-3 atom O, S or N, unsubstituted or substituted with 1-3 group, which are selected independently from halogen, OH, OMe, NO, NH, amino-C-Calkyl or amino-C-Cdialkyl, CN, SONH, C-Calkyl, and heterocycloalkyl stands for unaromatic, partially or completely saturated 3-10-membered monocyclic or bicyclic ring system, which includes 3-8-membered monocyclic or bicyclic ring, which includes 6-membered aromatic or heteroaromatic ring connected with a unaromatic ring with or without incorporated O, S or N atom, unsubstituted or substituted with 1-4 group, which are selected independently from halogen, OH, OMe, NO, NH, amino-C-Calkyl or amino-C-Cdialkyl, CN, SONH, CCalkil, &#x2014;C(O)&#x2014;, COOH or Rtogether with Rstands for ketone, Rindividually stands for hydrogen or together with Rstands for ketone or together with Rstands for ether, Rindividually stands for hydroxyl, a group of the formula &#x2014;OX or together with Rstands for ether, Rindividually stands for hydrogen, C-Calkyl group or C-Calkenyl group, and Rindividually stands for hydrogen or hydroxyl protected group, to intermediates for synthesis of other macrolide compounds with antibacterial activity, to the process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to the process for the preparation of pharmaceutical compositions, as well as the use of pharmaceutical compositions for treating bacterial infections 

Present invention relates to the new 3-decladinosyl derivatives of 9-deoxo-9a-aza9a-homoerythromycin a 9a, 11-cyclic carbamates

The invention relates to novel semi-synthetic macrolides of formula (I) having antibacterial activity. More particularly this invention relates to derivatives of 8a-aza-8a-homoerythromycin A, to processes for their preparation, to compositions containing them and to their use in medicine 

Macrolides

The present invention relates to 14 or 15 membered macrolides substituted at the 4' position of formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body 

The invention relates to halo derivatives of 9a-N-(N'-arylcarbamoyl)- and 9a-N-(N&#x2032;-arylthiocarbamoyl)-9-deoxo-9a-aza-9a-homoerythromycin A of the general formula (I)wherein R has the meaning of a substituted aryl group of the formula (II)wherein substituents a, b, c, d and e are the same or different and at least one of them has the meaning of halo, a (C-C)haloalkyl or a (C-C)haloalkoxy group, whereas the remaining ones have the meaning of hydrogen, halo, a (C-C)alkyl or a (C-C)alkoxy group, and X has the meaning of oxygen or sulfur, and pharmaceutically acceptable addition salts thereof with inorganic or organic acids, to a process for their preparation, to a process for the preparation of pharmaceutical compositions comprising them and to the use of these pharmaceutical compositions for the treatment or prevention of bacterial infections.

Halo derivatives of 9-deoxo-9a-aza-homerythromycin A

8a- and 9a-15-membered lactams

Growing community of inventors

Zagreb, Croatia

Stjepan Mutak