Difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists

A -NO2, alkyl technology, applied in the field of difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists, can solve problems such as limitations

Inactive Publication Date: 2017-05-31
RUGEN HLDG CAYMAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, NR2B antagonists described to date generally exhibit disadvantag

Method used

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  • Difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists
  • Difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists
  • Difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists

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example

[0342] As depicted in the Examples below, in certain exemplary embodiments, chemical entities were prepared according to the following procedures. It should be appreciated that although the general methods illustrate the synthesis of certain chemical entities of the present invention, the following methods and others known to those skilled in the art are applicable to all chemical entities and subclasses and species of each of these chemical entities, as described in this article.

[0343] Temperatures are given in degrees Celsius. If not stated otherwise, all evaporations are performed under reduced pressure, preferably between about 15 mmHg and 100 mmHg. The structures of intermediates and final products were confirmed by standard analytical methods such as mass spectrometry and NMR spectroscopy.

[0344] abbreviation:

[0345] aq water-based

[0346] Boc tert-butoxycarbonyl

[0347] Cbz benzyloxycarbonyl

[0348] DCM dichloromethane

[0349] DCE 1,2-Dichloroethane

...

example 1

[0372] Example 1. Chemical entity.

example 1A

[0373] Example 1.A. Intermediates.

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Abstract

Disclosed are chemical entities of formula (I) wherein X, Y, Z, R1, R3, R4, R5 and R6 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of formula I.

Description

Background technique [0001] Nonselective NMDA receptor antagonists originally developed in stroke and head trauma have recently shown clinical efficacy in the treatment of depression. The nonselective NMDA receptor antagonist ketamine has been shown to have rapid onset and efficacy in depression resistant to standard monoamine reuptake inhibitor therapy (Mathews and Zarate, 2013 , J. Clin. Psychiatry 74:516-158). However, non-selective NMDA receptor antagonists such as ketamine have a range of undesired pharmacological activities that limit their use in humans. In particular, dissociative or psychoactive side effects are particularly pronounced for non-selective NMDA receptor antagonists. Recently, NR2B subtype-selective NMDA receptor antagonists have demonstrated potential in a broad range of clinical indications. In particular, NR2B antagonists have also demonstrated antidepressant activity in early clinical trials (Ibrahim et al., 2012, J.Clin.Psychopharmacol. 32, 551-55...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/519A61P25/24A61P25/28A61P25/16
CPCA61K31/519A61P9/00A61P17/02A61P25/00A61P25/04A61P25/06A61P25/08A61P25/14A61P25/16A61P25/24A61P25/28A61P43/00C07D487/04
Inventor 吉迪恩·夏皮罗
Owner RUGEN HLDG CAYMAN
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