Novel potassium channel drugs and their uses

Details Novel potassium channel drugs and their uses Novel potassium channel drugs and their uses

A - Human Necessities

61

K

A61K 31/00 (2006.01) A61K 38/00 (2006.01) A61K 39/00 (2006.01) A61K 39/395 (2006.01) A61K 39/44 (2006.01) A61K 47/48 (2006.01) A61K 51/00 (2006.01) C07K 2/00 (2006.01) C07K 4/00 (2006.01) G01N 33/53 (2006.01) G01N 33/543 (2006.01) G01N 33/566 (2006.01)

Patent

CA 2318745

This invention relates to novel multibinding compounds that bind to potassium (K+) channels and modulate their activity. The compounds of this invention comprise 2-10 K+ channel ligands covalently connected by a linker or linkers, wherein the ligands in their monovalent (i.e., unlinked) state bind to one or more types of K+ channel. The manner of linking the ligands together is such that the multibinding agents thus formed demonstrate an increased biologic and/or therapeutic effect as compared to the same number of unlinked ligands made available for binding to the K+ channel. The invention also relates to methods of using such compounds and to methods of preparing them. The compounds of this invention are particularly useful for treating diseases and conditions of mammals that are mediated by K+ channels. Accordingly, this invention also relates to pharmaceutical compositions comprising a pharmaceutically acceptable excipient and an effective amount of a compound of this invention.

La présente invention concerne des composés à liaisons multiples se liant aux canaux potassium (canaux K?+¿) dont ils modulent l'activité. Les composés de l'invention comprennent de 2 à 10 ligands à canal potassium reliés par covalence au moyen d'au moins un lieur. A l'état monovalent, c'est-à-dire non liés, ces ligands se lient à au moins un type de canal potassium. La façon dont ces ligands sont liés fait que les agents à liaisons multiples ainsi constitués font preuve d'une efficacité biologique et/ou thérapeutique accrue par comparaison à ce que donnerait une même quantité de ligands non liés rendus disponibles pour une liaison avec le canal potassium. L'invention concerne également des procédés permettant de préparer et d'utiliser de tels composés. Les composés de l'invention conviennent particulièrement pour le traitement, chez les mammifères, d'états et d'affections à médiation des canaux potassium. L'invention concerne enfin des compositions pharmaceutiques comprenant un excipient pharmaceutiquement admis et une quantité suffisante d'un composé entrant par ailleurs dans le cadre de cette invention.

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