Substituted imidazolopyrazine and triazolopyrazyne...

A - Human Necessities – 01 – N

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A01N 43/58 (2006.01) A01N 43/60 (2006.01) A61K 31/495 (2006.01) A61K 31/50 (2006.01) C07D 471/00 (2006.01) C07D 487/00 (2006.01) C07D 491/00 (2006.01) C07D 495/00 (2006.01) C07D 497/00 (2006.01)

Patent

CA 2524376

Compounds of Formula (I) are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8, and Ar in the above Formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) 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 GABAA receptors (e.g., receptor localization studies).

L'invention concerne des composés de formule (I) et des procédés de préparation de ceux-ci. Les variables Z¿1?, Z¿2?, Z¿3?, R¿4?, R¿5?, R¿6?, R¿7?, R¿8?, et Ar dans la formule (I) sont définis dans la description. De tels composés peuvent être utilisés pour moduler la liaison des ligands aux récepteurs GABA<SB>A</SB> <i>in vivo</i> ou <i>in vitro</i> et sont particulièrement utiles dans le traitement d'une pluralité de troubles du système nerveux central (SNC) chez des êtres humains, des animaux de compagnie domestiqués et du bétail. Les composés selon l'invention peuvent être administrés seuls ou conjointement avec un ou plusieurs autres agents du SNC, afin de potentialiser les effets des autres agents du SNC. L'invention concerne également des compostions pharmaceutiques et des méthodes de traitement de tels troubles, ainsi que des procédés d'utilisation de tels ligands aux fins de détection des récepteurs GABA<SB>A</SB> (<i>par exemple</i>, des études de localisation des récepteurs).

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