Nuevolution A/s

Pliva-istrazivacki Institut D.o.o.

Fidelta D.o.o.

Selvita D.o.o.

Visnja Poljak

Milan Mesic

Gordon Saxty

Dijana Pesic

Antun Hutinec

Goran Kragol

Dinko Ziher

Andrea Fajdetic

Ivaylo Jivkov Elenkov

Zorica Marusic Istuk

Renata Rupcic

Ivana Ozimec Landek

Marko Duksi

Kristina Butkovic

Sanja Kostrun

Mirjana Bukvic

Maja Matanovic Skugor

Lene Teuber

Mladen Mercep

Stribor Markovic

Linda Tomaskovic

Tine Titilola Akinlemnu Kronborg

Gitte Friberg

Jimmi Gerner Seitzberg

Oresta Makaruha

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

Disclosed are compounds towards bromodomains, pharmaceutical compositions containing the compounds and use of the compounds in therapy. 

Compounds active towards bromodomains

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.

Compounds, compositions and methods for treatment of inflammatory diseases and conditions

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Copenhagen, Denmark

Visnja Poljak