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Pharmaceutical composition for treatment of melancholia and neuropathic pain and application thereof

一种组合物、神经性的技术，应用在药物组合、神经系统疾病、非中枢性止痛剂等方向

Active Publication Date: 2019-05-24
UNITED STATES OF AMERICA +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, ketamine treatment is associated with serious side effects due to the drug's narcotic effects and potential for abuse

Method used

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  • Pharmaceutical composition for treatment of melancholia and neuropathic pain and application thereof
  • Pharmaceutical composition for treatment of melancholia and neuropathic pain and application thereof
  • Pharmaceutical composition for treatment of melancholia and neuropathic pain and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0158] Example 1. Synthesis of lysine conjugates of norketamine

[0159]

Embodiment 2

[0160] Example 2. Synthesis of an ester conjugate of 6-hydroxynorketamine

[0161]

Embodiment 3

[0162] Example 3. Synthesis of (+,-)-(2S,6R / 2R,6S)-6-hydroxynorketamine

[0163]

[0164] Synthesis of (+,-)-(Z+E)-6-bromonorketamine. A 50 mL sample of racemic (+,-)-norketamine (free base) (10.0 g, 35.8 mmol) in glacial acetic acid was treated with bromopyridine (16.4 g, 51.3 mmol). The resulting mixture was heated at 130 °C for 1 h using a microwave. The solvent was removed in vacuo and the crude was dissolved in CHCl 3 , with saturated NaHCO 3 Washed, dried in vacuum (Na 2 SO 4 ) and evaporated, leaving 12.4 g of a crude mixture of diastereoisomers (Z+E, 3:1). Using silica gel chromatography with CH varying in concentration from (99.9 / 0 / 0.1) to (98.9 / 1 / 0.1) 2 Cl 2 / MeOH / Et 3 N eluted to afford the pure isolated isomers, (+,-)-(E)-6-bromonorketamine (1.22 g) (9% yield) and (+,-)-(Z) - 6-bromonorketamine (6.6 g) (49% yield).

[0165] Analytical data for (+,-)-(E)-6-bromonorketamine: 1 H NMR: (300MHz, CDCl 3 ):δ7.60(m,1H),7.20-7.10(m,3H),5.17(dd,1H,J=12.0Hz,J=6...

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PUM

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Abstract

The disclosure provides pharmaceutical composition for treatment of melancholia and neuropathic pain and application thereof. Especially, the present invention provides pharmaceutical preparations containing (2R, 6R)-hydroxynorketamine, or (R)- or (S)-dehydronorketamine, or other stereoisomeric dehydro or hydroxylated ketamine metabolite. (2R, 6R)-hydroxynorketamine. The invention also provides novel ketamine metabolite prodrugs. The invention provides methods of treating, bipolar depression, major depressive disorder, neuropathic and chronic pain, including complex regional pain disorder (CRPS) by administering a purified ketamine metabolite or a ketamine metabolite prodrug directly to patients in need of such treatment.

Description

[0001] The application date is October 15, 2012, the application number is 201280062294.X, and the invention name is "(2R,6R)-hydroxynorketamine, (S)-dehydronorketamine and (R,S) - Application of other stereoisomeric dehydrogenated and hydroxylated metabolites of ketamine in the treatment of depression and neuropathic pain" is a divisional application of the invention patent application. [0002] Cross References to Related Applications [0003] This application claims priority to US Provisional Patent Application Serial No. 61 / 547,336, filed October 14, 2011, the entire contents of which are hereby incorporated by reference. [0004] Statement of Government Support [0005] The subject matter of the present disclosure was funded by an in-house research program of the National Institute of Aging and the Nation Institute of Mental Health. The US Government has certain rights in this application. technical field [0006] The present disclosure demonstrates that the active age...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/135A61P25/24A61P25/18A61P25/28A61P25/00A61P29/00
CPCC07C225/20C07C237/04C07B2200/07C07C2601/14C07C2601/16A61K31/137A61K31/165A61K31/222A61K31/24A61K31/265A61K31/4453A61K31/5375A61P21/02A61P25/00A61P25/04A61P25/18A61P25/24A61P25/28A61P29/00A61K31/135A61K45/06C07D295/108C07D295/112C07C229/48C07C237/20C07D295/15C07D295/155
Inventor 欧文·W·魏纳鲁因·莫阿德尔米歇尔·伯尼尔卡洛斯·A·萨拉特马克·C·托尔曼迈克尔·E·戈德堡玛丽·J·坦加
Owner UNITED STATES OF AMERICA
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