Methods of inhibiting vascular permeability and apoptosis

A - Human Necessities – 61 – K

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A61K 31/133 (2006.01) A61P 9/00 (2006.01)

Patent

CA 2529318

Agonist of vascular endothelial sphingosine-1-phosphate receptors are described. Compounds such as FTY720 can be phosphorylated by sphingosine kinase-2 into the phosphorylated froms which serve as sphingosine-1-phosphate receptor agonists. The vascular endothelial sphingosine-1-phosphate receptor agonists are employed in methods of treating a mammal for vascular permeability disorders and unwanted vascular endothelial cell apoptosis, and for the growth of new blood vessels. The sphingosine-1-phosphate receptor agonists can be used for the manufacture of a medicament for treating vascular permeability disorders and unwanted vascular endothelial cell apoptosis, and for the growth of new blood vessels.

Cette invention concerne des agonistes des récepteurs de sphingosine-1-phosphate endothélial vasculaire. Des composés tels que FTY720 peuvent être transformés par phosphorylation par sphingosine kinase-2 sous leurs formes phosphorylées, qui servent alors d'agonistes des récepteurs de sphingosine-1-phosphate. Ces agonistes des récepteurs de sphingosine-1-phosphate endothélial vasculaire sont utilisés dans des procédés destinés à traiter un sujet mammifère contre les troubles de perméabilité vasculaire et contre l'apoptose non désirée des cellules endothéliales vasculaires et dans des procédés destinés à favoriser la croissance de nouveaux vaisseaux sanguins. Ces agonistes des récepteurs de sphingosine-1-phosphate peuvent servir dans la fabrication d'un médicament destiné à traiter les troubles de la perméabilité vasculaire et l'apoptose non désirée des cellules endothéliales vasculaires et à stimuler la croissance de nouveaux vaisseaux sanguins.

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