Glaxosmithkline Istrazivacki Centar Zagreb D.o.o.

Pliva-istrazivacki Institut D.o.o.

Glaxosmithkline Istrazivacki Centar Zagreb

Glaxosmithkline LLC

Glaxosmithkline Istrazivacki Center Zagreb D.o.o

Glaxosmithkline Istraziva{hacek Over (c)}ki Centar Zagreb D.o.o.

Glaxosmith Kline Istrazivocki Centar Zagreb, D.o.o.

Mladen Mercep

Milan Mesic

Dijana Pesic

Stribor Markovic

Linda Tomaskovic

Boska Hrvacic

Ivaylo Jivkov Elenkov

Ivica Malnar

Anita Filipovic

Andreja Cempuh Klonkay

Lidija Simicic

Ivana Ozimec

Marijana Komac

Visnja Poljak

Renata Rupcic

Davor Kidemet

Marina Modric

Rudolf Trojko

Iva Benko

Oresta Makaruha

Zeljko Zupanovic

The present invention relates to novel compounds represented by the structure I and pharmaceutical preparations thereof for the treatment of inflammatory diseases in humans and animals. 

Conjugates of immune cell specific macrolide compounds with anti-inflammatory compounds for improved cellular targeting of anti-inflammatory therapy

The present invention relates to new compounds represented by Formula I: wherein M represents a macrolide subunit of the substructure II: L represents the chain of the substructure III:&#x2014;X&#x2014;(CH)-Q-(CH)&#x2014;X&#x2014;&#x2003;&#x2003;IIID represents the steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity; The present invention relates also to pharmaceutically acceptable salts and solvates of such prepared compounds, to process and intermediates for their preparation, as well as to the improved therapeutic action and the use in the treatment of inflammatory diseases and conditions in humans and animals.

Compounds with anti-inflammatory activity

The present invention relates to derivatives of 1,2-diaza-dibenzoazulene, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory actions, especially to the inhibition of tumor necrosis factor-&#x3b1; (TNF-&#x3b1;) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

1,2-Diaza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof

The present invention relates to novel compounds represented by the structure I and pharmaceutical preparations thereof for the treatment of inflammatory diseases in humans and animals.

The present invention relates to compounds of 2-thia-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.

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

The invention relates to novel compounds of the formula (I) including all their tautomers, to pharmaceutically acceptable salts and solvates thereof, to processes and reactive intermediates for the preparation thereof, and to processes and reactive intermediates for the preparation of the compounds of the formula (II) including all their stereoisomers and tautomers to the use of the compounds of the formula (II) as suitable precursors for the preparation of the compounds of the formula (I) as well as to use of the compounds of the formula (I) and of the compounds of the formula (II) as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diesases and conditions in humans.

Substituted furochromenes, preparation thereof and their antiinflammatory action

The present invention relates to 1-aza-dibenzoazulene derivatives, 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-aza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof

The present invention relates to benzonaphthoazulene derivatives of tiophene 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 tumor necrosis factor-&#x3b1; (TNF-&#x3b1;) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

1- or 3-thia-benzonaphthoazulenes as inhibitors of tumor necrosis factor production and intermediates for the preparation thereof

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

The present invention relates to derivatives of 1-oxa-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 actions, 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-oxa-3-aza-dibenzoazulenes as inhibitors of tumor necrosis factor production and intermediates for the production thereof

The present invention relates to novel compounds of the formula (I) including all stereoisomers and tautomers thereof, to the pharmaceutically acceptable salts and solvates thereof, to the processes and reactive intermediates for their preparation and to their use in the prophylaxis and treatment of asthma and other inflammatory diseases and/or conditions in humans.

Substituted furochromene compounds of antiinflammatory action

The present invention relates to 1,3-diaza-dibenzoazulene derivatives, 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 tumor necrosis factor-&#x3b1; (TNF-&#x3b1;) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

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

The present invention relates (a) to new compounds represented by Formula I: wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, V represents an anti-inflammatory steroid or nonsteroid subunit, or an antineoplastic or antiviral subunit and L represents a linking group covalently linking M and V; (b) to their pharmacologically acceptable salts, prodrugs and solvates, (c) to processes and intermediates for their preparation, and (d) to their use in the treatment of inflammatory/neoplastic/viral diseases and conditions in humans and animals.

Compounds, compositions as carriers for steroid/nonsteroid anti-inflammatory; antienoplastic and antiviral active molecules

The present invention relates (a) to new compounds represented by Formula I:wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, D represents a nonsteroidal subunit (nonsteroidal moiety) derived from nonsteroid drug with anti-inflammatory, analgesic and/or antipyretic activity (NSAID) and L represents a linking group covalently linking M and D; (b) to their pharmacologically acceptable salts, prodrugs and solvates, (c) to processes and intermediates for their preparation, and (d) to their use in the treatment of inflammatory diseases and conditions in humans and animals.

Nonsteroidal anti-inflammatory substances, compositions and methods for their use

The present invention relates (a) to new compounds represented by Formula I:wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, S represents a steroid subunit (steroid moiety) derived from steroid drug with anti-inflammatory activity and L represents a linker molecule linking M and S, (b) to their pharmacologically acceptable salts, prodrugs and solvates, (c) to processes and intermediates for their preparation, and (d) to their use in the treatment of inflammatory diseases and conditions in humans and animals. Such compounds inhibit many cytokines and immune mediators involved in immune responses which cause inflammation, allergy, or alloimmunity, including without limitation IL-1, 2, 4, 5, 6, 10, 12, GMCSF, ICAM, and TNF-&#x3b1;. Importantly, anti-inflammatory steroids exert a direct anti-inflammatory effect through binding to the glucocorticosteroid receptor.

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Zagreb, Croatia

Mladen Mercep