Imines as ion channel modulators

Details Imines as ion channel modulators Imines as ion channel modulators

C - Chemistry, Metallurgy

07

C

C07C 257/14 (2006.01) A61K 31/15 (2006.01) A61K 31/155 (2006.01) A61K 31/44 (2006.01) A61K 31/66 (2006.01) A61P 7/00 (2006.01) C07C 251/40 (2006.01) C07C 251/80 (2006.01) C07C 257/22 (2006.01) C07C 259/12 (2006.01) C07C 259/14 (2006.01) C07D 213/61 (2006.01) C07F 9/02 (2006.01) C07F 9/24 (2006.01)

Patent

CA 2594505

The present invention provides a class of chemical compounds useful in the treatment of sickle cell disease, diseases characterized by unwanted or abnormal cell proliferation and for the treatment of ocular disorders such as glaucoma. The active compounds are tri-(aryl or heteroaryl) methane compounds or analogues thereof which further comprise an imine moiety and where the tertiary carbon atom can be replaced with a different atom such as Si, Ge, N or P. The compounds enhance resistance to degradation in a biological medium, inhibit potassium flux in a cell, reduce mammalian cell proliferation, reduce the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

L'invention porte sur une classe de composés chimiques utiles pour le traitement: de maladies drépanocytaires, de maladies caractérisées par une prolifération de cellules indésirée ou anormale, et pour le traitement de troubles de l'oeil tels que le glaucome. Leur principe actif est constitué de composés tri-(aryl ou hétéroaryl) méthane ou de leurs analogues, et comporte en outre un fragment imine dont l'atome tertiaire de carbone peut être remplacé par un atome différent tel que Si, Ge, N ou P. Ces composés renforcent la résistance aux dégradations de milieux biologiques, inhibent le flux de potassium des cellules, réduisent la prolifération de cellules chez les mammifères, réduisent le canal de Gardos des érythrocytes, réduisent la déshydration des drépanocytes et/ou retardent leur survenue ou leur déformation.

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