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Positive allosteric modulators of mGluR3

A technology of tautomers and solvates, applied in the field of substituted pyridine derivatives, can solve problems such as abnormal regulation of output activity

Inactive Publication Date: 2015-09-30
PRESTWICK CHEM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thus, in the diseased brain, dopamine deficiency leads to dysregulation of the output activity of direct and indirect pathways

Method used

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  • Positive allosteric modulators of mGluR3
  • Positive allosteric modulators of mGluR3
  • Positive allosteric modulators of mGluR3

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Experimental program
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Embodiment Construction

[0201] I. Synthesis of Selected Compounds of the Invention

[0202] The following compounds were synthesized and / or characterized. However, it is within the knowledge of those skilled in the art to prepare and / or characterize these compounds differently.

[0203] Step 1 - IS08641-042

[0204] 1-isopropyl-3-oxo-2,3,5,6,7,8-hexahydroisoquinoline-4-carbonitrile

[0205]

[0206] To a solution of 2-isobutyrylcyclohexanone (13 g, 0.0772 mol) in ethanol (250 mL) was added 2-cyanoacetamide (6.5 g, 0.0772 mol) and a catalytic amount of piperidine (3 mL ). After the reaction was complete (by LCMS), the precipitated solid was collected by filtration and dried under vacuum. This was slurried with ethyl acetate to give the title compound (10 g, 59%) as a white solid.

[0207] 1 H NMR (400MHz, DMSO-d 6 ) δ 11.87 (s, 1H), 3.17-3.10 (m, 1H), 2.74 (s, 2H), 2.50-2.47 (m, 2H), 1.66 (s, 4H), 1.19-1.17 (d, J = 7.0 Hz, 6H).

[0208] Step 2 - FS08641-051

[0209] 1-isopropyl-3-morphol...

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Abstract

The present invention relates to novel substituted pyridine derivatives as positive allosteric modulators for modulating metabotropic giutamate receptor subtype 3 (mGluR3) and / or altering giutamate level or glutamatergic signalling.

Description

technical field [0001] The present invention relates to novel substituted pyridine derivatives as positive allosteric agents for modulating metabotropic glutamate receptor subtype 3 (mGluR3) and / or altering glutamate levels or glutamatergic signaling Conditioner. Background technique [0002] Glutamate is the major amino acid transmitter in the mammalian central nervous system (CNS). Glutamate plays an important role in many physiological functions, such as learning and memory as well as sensory perception, development of synaptic plasticity, motor control, respiration, and regulation of cardiovascular function. Furthermore, glutamate is at the center of several different neurological and psychiatric disorders where there is an imbalance in glutamatergic neurotransmission. [0003] Glutamate mediates synaptic neurotransmission through activation of ionotropic glutamate receptor channels (iGluRs), namely NMDA, AMPA, and kainate receptors, which are responsible for fast exci...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/85C07D217/26C07D491/052C07D495/04A61K31/4365A61K31/436A61K31/5377A61K31/472A61P25/00A61P35/00A61P3/10
CPCC07D491/052C07D495/04C07D213/85C07D217/26A61K31/438A61K31/472A61K31/5377A61P1/04A61P3/00A61P3/10A61P7/02A61P9/10A61P25/00A61P25/04A61P25/06A61P25/08A61P25/14A61P25/16A61P25/18A61P25/22A61P25/24A61P25/30A61P27/02A61P29/00A61P35/00A61P43/00
Inventor J.波特尼克
Owner PRESTWICK CHEM
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