Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists

Abstract

Compounds of formula (II), wherein X, Y, and Z are independently selected from N, O, S, C, and CO, and at least one of X, Y, and Z is a heteroatom; Ar1 ​​and Ar2 are independently selected from heterocycles base or fused heterocyclyl and aryl groups; the compounds act as metallotropic glutamate receptor antagonists and can be used to treat neurological diseases and disorders.

Description

field of invention [0001] The present invention provides compounds that are active at metabotropic glutamate receptors and are useful in the treatment of neurological and psychiatric diseases and disorders. Background of the invention [0002] Recent advances in elucidating the neurophysiological roles of metallotropic glutamate receptors have established these receptors as promising drug targets in the treatment of acute and chronic neurological and psychiatric disorders and diseases. However, a major challenge in achieving this goal is the development of metallotropic glutamate receptor subtype-selective compounds. [0003] Glutamate is the major excitatory neurotransmitter in the mammalian central nervous system (CNS). Glutamate exerts its effects on central neurons by binding to and thereby activating cell surface receptors. These receptors have been divided into two classes, ionotropic and metallotropic glutamate receptors, based on the structu...

AI Technical Summary

Problems solved by technology

[0017] From the above description, it is clear that currently available mGluR agonists and antagonists are of limited value due to lack of potency and selectivity

Furthermore, most currently available compounds are amino acids or amino acid derivatives with very limited bioavailability, which hinders in vivo studies to evaluate the physiology, pharmacology and therapeutic potential of mGluRs

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