Non-peptide inhibition of t-lymphocyte activation and...

Details Non-peptide inhibition of t-lymphocyte activation and... Non-peptide inhibition of t-lymphocyte activation and...

A - Human Necessities

61

K

A61K 31/415 (2006.01) A61K 31/16 (2006.01) A61K 31/277 (2006.01) A61K 31/40 (2006.01) A61K 31/41 (2006.01) A61K 31/425 (2006.01)

Patent

CA 2396595

Compounds, preparations and methods for immunosuppressive treatment of autoimmune disorders, graft rejection and/or graft/host disease. Therapeutically effective amounts of certain substituted triarylmethane compounds, such as 1-[(2-chlorophenyl)diphenylmethyl]-1H-pyrazole, are administered to mammalian patients to selectively inhibit the calcium- activated K+ channel (IKCa1) in Lymphocytes, monocytes, macrophages, platelets or endothelial cells without concomitant inhibition of P450-dependent enzyme systems, resulting in reduction of antigen-,cytokine-, or mitogen-induced calcium entry through store operated calcium channels in these cells, suppression of cytokine production by these cells, and inhibition of activation of these cells. Such inhibition of the Ca++ activated K+ channel (IKCa1) prevents the pre-Ca++ stage of cell activation and thus causes immunosuppression and an anti-inflammatory response.

L'invention concerne des composés, des préparations, et des méthodes destinés au traitement immunosuppresseur de troubles auto-immunes, de rejet de greffe et/ou de réaction du greffon contre l'hôte. On administre des quantités thérapeutiques efficaces de certains composés de triarylméthane substitués, tels que 1-[(2-chlorophenyl)diphenylmethyl]-1<i>H</i>-pyrazole, à des patients mammifères de façon à inhiber sélectivement le canal K<+> (<i>IKCa1</i>) activé par le calcium dans les lymphocytes, monocytes, macrophages, plaquettes ou cellules endothéliales sans inhibition concomitante des systèmes enzymatiques dépendants de P450, ce qui entraîne la réduction d'entrée de calcium induite par un antigène, une cytokine, ou un mitogène du fait du stockage effectué dans les canaux calciques des cellules, la suppression de la production de cytokine par ces cellules, et l'inhibition de l'activation desdites cellules. L'inhibition du canal K<+> (<i>IKCa1</i>) activé par le Ca<++> inhibe la phase pré-Ca<++> de l'activation cellulaire, et entraîne donc une immunosuppression et une réponse anti-inflammatoire.

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