Macrolides with anti-inflammatory activity

C - Chemistry – Metallurgy – 07 – H

Patent

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Details

C07H 17/00 (2006.01) A61K 31/7048 (2006.01) A61K 31/7052 (2006.01) A61P 29/00 (2006.01) C07H 17/08 (2006.01)

Patent

CA 2594820

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" 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- .alpha., IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

L'invention concerne de nouveaux macrolides semi-synthétiques qui présentent une activité anti-inflammatoire. D'une manière plus spécifique, l'invention concerne des macrolides à 14 ou 15 éléments substitués en position 4", leurs dérivés pharmaceutiquement acceptables, des processus et des intermédiaires pour leur préparation, des compositions pharmaceutiques contenant ces macrolides ainsi que leur activité et leur utilisation dans le traitement de maladies et d'états inflammatoires sur des humains et des animaux, notamment des maladies associées à une sécrétion excessive de TNF-a, IL-1, IL-8, IL-2 ou IL-5 ; et/ou à l'inhibition d'une prolifération lymphocytaire excessive ; et/ou à une dégranulation excessive des granulocytes.

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