Glaxosmithkline Istrazivacki Centar Zagreb D.o.o.

Glaxo Group Limited

Ognjen Culic

Sulejman Alihodzic

Martina Bosnar

Antun Hutinec

Goran Kragol

Vanja Vela

Nikola Marjanovic

Gorjana Lazarevski

Linda Tomaskovic

Zorica Marusic-Istuk

Zorica Marusic Istuk

Marija Ribic

Boris Mildner

Dubravko Jelic

Vesna Erakovic Haber

Vesna Erakovic

Vanesa Ivetic

Marija Tomaskovic

Berislav Bosnjak

Vesna Munic

The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4&#x2033; 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-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

Macrolides with anti-inflammatory activity

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 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

Growing community of inventors

Zagreb, Croatia

Ognjen Culic