Glaxo Group Limited

Pliva-Istrazivacki Institut

Glaxosmithkline Istrazivacki Centar Zagreb D.o

Fidelta D.o.o.

Selvita D.o.o.

Glaxosmithkline Istrazivacki Centar Zagreb D.o.o.

Andrea Fajdetic

Gordon Saxty

Milan Mesic

Dijana Pesic

Antun Hutinec

Goran Kragol

Dinko Ziher

Visnja Poljak

Ivaylo Jivkov Elenkov

Renata Rupcic

Zorica Marusic Istuk

Ivana Ozimec Landek

Marko Duksi

Sanja Kostrun

Maja Matanovic Skugor

Gorjana Lazarevski

Gabrijela Kobrehel

Desmond John Best

Robert John Sheppard

Andrew Keith Forrest

Stjepan Mutak

Nedjeljko Kujundzic

Sulejman Alihodzic

Kristina Butkovic

Mirjana Bukvic

John Stephen Elder

Mirjana Bukvic Krajacic

Zrinka Ivezic

The present invention relates to seco (opened ring) macrolide compounds, to the process for preparation thereof, to the use of said seco macrolide compounds as intermediates for preparation of macrolide based macrocycles, to macrolide based macrocycles obtained from said seco macrolide compounds, to the process for preparation of macrolide based macrocycles, to the pharmaceutical compositions comprising macrolide based macrocycles, and to the use of macrolide based macrocycles as therapeutic agents.

Seco macrolide compounds

Macrolones&#x2014;amino substituted quinolones

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

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Zagreb, Croatia

Andrea Fajdetic