Modulation of calcium channels

A - Human Necessities – 61 – K

Patent

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A61K 31/445 (2006.01) A61K 31/38 (2006.01) A61K 31/381 (2006.01) A61K 31/40 (2006.01) A61K 31/4025 (2006.01) A61K 31/4453 (2006.01)

Patent

CA 2222739

A method for modulating calcium channels, increasing the density of calcium channels in vascular and cardiac tissue with no changes in inotropic or pressor response, comprising administering to a warm-blooded animal in need thereof a pharmaceutically-effective amount of a compound having formula (I) wherein R1 and R3 are independently hydrogen, C1-C4 alkyl, -CO-(C1-C6 alkyl), or -CH2Ar, -CO-Ar, wherein Ar is phenyl or substituted phenyl; R2 is selected from the group consisting of pyrrolidine, hexamethyleneimino, and piperidino; or a pharmaceutically-acceptable salt thereof.

L'invention concerne un procédé pour moduler les canaux calciques et accroître leur densité dans les tissus vasculaires et cardiaques sans modifier la réponse inotrope ou vasopressive, consistant à administrer à un homéotherme, dont l'état le requiert, une dose pharmaceutiquement efficace d'un composé de formule (I) dans laquelle R?1¿ et R?3¿ sont indépendamment hydrogène, alkyle C¿1?-C¿4?, -CO-(alkyle C¿1?-C¿6?), ou bien -CH¿2?Ar, -CO-Ar, où Ar est phényle ou phényle substitué; R?2¿ est choisi dans le groupe composé de pyrrolidine, hexaméthylèneimino, et pipéridino; ou bien un sel pharmaceutiquement acceptable de ce composé.

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