Glaxosmithkline Istrazivacki Centar Zagreb D.o.o.

Pliva-Istrazivacki Institut D.o.o.

Glaxosmithkline Istrazivacki Centar Zagreb

Glaxo Group Limited

Linda Tomaskovic

Milan Mesic

Mladen Mercep

Stribor Markovic

Boska Hrvacic

Marijana Komac

Sulejman Alihodzic

Visnja Poljak

Martina Bosnar

Ognjen Culic

Nikola Marjanovic

Boris Mildner

Oresta Makaruha

The present invention relates to new macrolide compounds represented by the general structure I, wherein M is a macrolide, P is a photo-affinity group bearing subunit containing biotin, and L is a linking molecule, and to their pharmaceutically acceptable salts and solvates, to processes and intermediates for their preparation and to the use of these compounds for the macrolide target identification.

Macrolide compounds containing biotin and photo-affinity group for macrolide target identification

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 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 (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

Linda Tomaskovic