Pliva, Farmaceutska, Kemijska, Prehrambena I Kozmeticka Industrija,

Glaxo Group Limited

Pliva, Farmaceutska Industrija, Dionicko Drustvo

Pliva Hrvatska D.o.o.

Glaxosmithkline Istrazivacki Centar Zagreb D.o.o.

Pliva D.d.

Pliva-istrazivacki Institut

Glaxosmithkline Istrazivacki Centar Zagreb D.o

Glaxpsmithkline Istrazivacki

Pliva Pharmaceutical Industry, Incorporated

Pliva, Farmaceutska Industrja, Dioni{haeck Over (c)}ko Dru{haeck Over (s)}tvo

Glaxosmithkline Istrazivacki Center Zagret D.o.o.

Pliva, Farmaceutska, Kemijska, Prehranbena I Kozmeticka Industrija

Gorjana Lazarevski

Gabrijela Kobrehel

Stjepan Mutak

Antun Hutinec

Zeljko Kelneric

Aleksandar Danilovski

Sergio Lociuro

Nedjeljko Kujundzic

Miljenko Dumic

Sulejman Alihodzic

Drazen Pavlovic

Darko Filic

Zorica Marusic-Istuk

Mladen Vinkovic

Dina Pavlovic

Andrea Berdik

Suleman Alihodzic

Katica Lazaric

Marko Derek

Dominik Cincic

Alojz Dumbovic

Ernest Mestrovic

Marina Oresic

Richard Lewis Jarvest

Daniele Andreotti

Andrew Keith Forrest

Stefano Biondi

Amalija Narandja

Jessica Tibasco

Goran Kragol

Vanja Vela

Andrea Fajdetic

Alfonso Pozzan

Federica Damiani

Francesca Cardullo

Zorica Marusic Istuk

Martina Bosnar

Ognjen Culic

Marko Djerek

Miljenko Dumić

Davor Kidemet

Alfredo Paio

Vlado Stimac

Ilaria Bientinesi

Knezevic Zdravka

Slobodan Djokic

Marija Leljak

Zrinka Banic-Tomisic

Gordana Burek

Sulejman Alihodzi&cacute;

Dejan-Kresimir Bucar

Mladen Vinković

Wolfgang Schoenfeld

Anna Quaglia

Vesna Erakovic

Manuela Ciraco

Zdravka Knezevic

Dejan Kresimir Bucar

The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides lacking cladinose sugar substituted at the C-3 position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-&#x3b1;, IL-1, IL-6, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

Decladinosyl-macrolides with anti-inflammatory activity

The present invention relates to 14- or 15-membered macrolides substituted at the 4&#x2033; position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical microbial infections in a human or animal body.

14 and 15 membered ring compounds

Substantially pure isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A having the Formula I: wherein S is an organic solvent which is at least partially miscible with water, x is 1, 1.25, 1.5 or 2, y is 0, 0.5, or 1, the pseudopolymorph being characterized by the monoclinic space group P2and average unit cell parameters comprising: crystal axis lengths of a=15.5-17.0 &#x212b;, b=15.5-17.0 &#x212b;, and c=17.5-19.5 &#x212b;, and angles between the crystal axes of &#x3b1;=&#x3b3;=90&#xb0; and &#x3b2;=106&#xb0;-112&#xb0;. In addition, this disclosure is directed to processes for the preparation of the substantially pure isostructural pseudopolymorphs of Formula I; to pharmaceutical compositions containing substantially pure isostructural pseudopolymorphs of Formula I; and to a method for the treatment of bacterial and protozoan infections, and inflammation-related diseases by administration of a pharmaceutical composition containing the substantially pure isostructural pseudopolymorphs of Formula I.

Isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A

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 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 

Substantially pure amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A. In addition, this disclosure is directed to a process for the preparation thereof from crude 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A via orthorhombic isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A, of the general formula I:wherein S represents a water-miscible or water-immiscible organic solvent, characterized by the orthorhombic space group P222, with average unit cell parameters a=8.2 to 9.7 &#x212b;, b=11.5 to 13.5 &#x212b;, c=44.5 to 47.0 &#x212b;, &#x3b1;=&#x3b2;=&#x3b3;=90&#xb0;, wherein a, b and c represent the crystal axes lengths and &#x3b1;, &#x3b2; and &#x3b3; represent the angles between the crystal axes. In addition, pharmaceutical compositions containing the substantially pure amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A are disclosed, as well as a method for the treatment of bacterial and protozoal infections, and inflammation related diseases in humans and animals by administration of a pharmaceutical composition containing same.

Amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A, process for preparing the same, and uses thereof

8a- and 9a-15-membered lactams

Derivatives from the class of oleandomycin

The invention relates to novel compounds from the class of macrolide antibiotics. Particularly, the invention relates to novel 3,6-heiketals from the class of 9a-azalides, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for their preparation and to the use thereof as antibiotics or as intermediates for the synthesis of other macrolide antibiotics.

3,6-hemiketals from the class of 9A-azalides

The present invention relates to the new 15-membered ketoazalides from the class of 6-O-methyl-8a-aza-8a-homo-and 6-O-methyl-9a-aza-9a-homoerythromycin A with the general formula (I) ##STR1## wherein A represents NH group and B at the same time represents C.dbd.O group, or

Ketolides from the class of 15-membered lactams

The invention relates to novel secomacrolides from the class of erythromycin A, potential intermediates for preparation of novel macrolide antibiotics general formula ##STR1## and its pharmaceuticaly acceptable addition salts with inorganic or organic acids, wherein R.sub.1 represents hydrogen, C.sub.1 -C.sub.4 alkanoyl group, arylcarbonyl group and together with R.sub.2 and carbon atoms to which they are bound, cyclic carbonyl or thiocarbonyl group, R.sub.2 represents hydrogen or together with R.sub.1 and carbon atoms to which they are bound, cyclic carbonyl or thiocarbonyl group, R.sub.3 represents hydrogen, C.sub.1 -C.sub.4 alkanoyl or arylcarbonyl group,

Secomacrolides from class of erythromycins and process for their

The present invention relates to .beta.,.beta.-disubstituted derivatives of 9-deoxo-9a-N-ethenyl-9a-aza-9a-homoerythromycin A, new semisynthetic antibiotics of macrolide class of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are mutually the same or different and represent nitrile, carboxy group of the formula COOR.sup.3, wherein R.sup.3 represents C.sub.1 -C.sub.4 alkyl group, or keto group of the formula COR.sup.4, wherein R.sup.4 represents C.sub.1 -C.sub.4 alkyl group, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for the preparation thereof, to a process for the preparation of pharmaceutical compositions, as well as to the use of the obtained pharmaceutical compositions in the treatment of bacterial infections.

.beta.,.beta.-distributed derivatives of

The invention relates to 9-N-ethenyl derivatives of 9 (S)-erythromycylamine, new semisynthetic antibiotics of the macrolide class of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and represent nitryl, a carboxyl group of the formula COOR.sup.3, wherein R.sup.3 represents a C.sub.1 -C.sub.4 alkyl group, or a keto group of the formula COR.sup.4, wherein R.sup.4 represents a C.sub.1 -C.sub.4 alkyl group, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for their preparation, to a process for the preparation of the pharmaceutical compositions as well as to the use of the obtained pharmaceutical compositions in the treatment of bacterial infections.

9-N-ethenyl derivatives of 9(S)-erythromycylamine

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Zagreb, Croatia

Gorjana Lazarevski