TRIAZOLO-PYRIDAZINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS

摘要

A class of substituted 1,2,4-triazolo[4,3-b]pyridazine derivatives, formula (I), wherein Y represents hydrogen or C1-6 alkyl; Z represents an optionally substituted tetrahydropyridinyl moiety; R1 represents C¿3-7? cycloalkyl, phenyl, furyl, thienyl or pyridinyl, any of which groups may be optionally substituted; and R?2¿ represents cyano (C¿1-6?)alkyl, hydroxy(C1-6)alkyl, C3-7cycloalkyl(C1-6)alkyl, propargyl, C3-7heterocycloalkylcarbonyl(C1-6)alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted, are selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.