Use of divalent cations for inhibiting erythrocyte...

A - Human Necessities – 61 – K

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A61K 31/40 (2006.01) A61K 31/00 (2006.01) A61K 31/4015 (2006.01) A61K 31/4025 (2006.01) A61K 31/555 (2006.01)

Patent

CA 2308854

The present invention provides a chemical class of active agents to be used as efficacious drugs in preventing erythrocyte dehydration, thus helping ameliorate the symptoms of certain hemoglobinopathies. The active agents include a class of compounds that can deliver to an erythrocyte in vivo a divalent cation. Increased intracellular concentrations of the divalent cation in the erythrocyte block K-Cl cotransport preventing dehydration of the erythrocyte, thus improving erythrocyte survival. These agents are to be administered by any preferred route of administration including oral, intravenous and parenteral routes. These agents may be co-administered with any other antihemoglobinopathic compounds. The methodology is effective for both long term and short term therapy; may be employed prophylactically and/or therapeutically; and may be used in acute crisis clinical situations.

La présente invention concerne une classe chimique de principes actifs destinés à être utilisés en tant que médicaments permettant de prévenir efficacement la déshydratation érythrocytaire, contribuant ainsi à traiter les symptômes de certaines hémoglobinoses. Ces principes actifs comprennent une classe de composés pouvant apporter un cation bivalent à un érythrocyte in vivo. Une hausse des concentrations intracellulaires de ce cation bivalent dans le cotransport du bloc erythrocytaire K-C1 permet de prévenir toute déshydratation érythrocytaire, ce qui favorise la survie des érythrocytes. Ces principes actifs peuvent par ailleurs être administrés selon n'importe quelle voie d'administration préférée, notamment par voie orale, intraveineuse, et parentérale. Ces principes peuvent en outre être administrés conjointement à d'autres composés d'hémoglobinose. Cette méthode, qui est efficace dans un traitement à court ou à long terme, peut être suivie de manière prophylactique et/ou thérapeutique et dans des situations cliniques graves.

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