Piperazinyl oxoalkyl tetrahydroisoquinolines and related...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 513/04 (2006.01) A61K 31/395 (2006.01) A61P 3/00 (2006.01) A61P 25/00 (2006.01) C07D 217/04 (2006.01) C07D 217/14 (2006.01) C07D 223/16 (2006.01) C07D 401/04 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 413/04 (2006.01) C07D 471/04 (2006.01) C07D 487/04 (2006.01) C07D 495/04 (2006.01) C07D 498/04 (2006.01) G01N 33/566 (2006.01)

Patent

CA 2646023

Piperazinyl oxoalkyl tetrahydroisoquinolines and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).

L'invention concerne des pipérazinyl-oxoalkyl-tétrahydroisoquinoléines et des analogues apparentés de formule : dans laquelle les variables sont telles que décrites dans la description. Ces composés peuvent être utilisés pour moduler la liaison de ligands aux récepteurs histaminiques H3 in vivo ou in vitro et ils sont particulièrement utiles pour traiter divers troubles du système nerveux central (SNC) et autres chez l'homme, les animaux domestiques et le bétail. Les composés de l'invention peuvent être administrés seuls ou en combinaison avec un ou plusieurs autres agents agissant sur le SNC afin de potentialiser les effets dudit ou desdites autres agents agissant sur le SNC. L'invention concerne également des compositions pharmaceutiques et des procédés de traitement de ces troubles, ainsi que des procédés d'utilisation de ces ligands pour la détection des récepteurs histaminiques H3 (par exemple dans des études de localisation de récepteurs).

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