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Modified amino acid derivatives for the treatment of neurological diseases and selected psychiatric disorders

A neurodegenerative and disease technology, used in neurological diseases, drug combinations, organic active ingredients, etc.

Pending Publication Date: 2021-12-07
JAGIELLONIAN UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Currently, there is no such preparation in medicine

Method used

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  • Modified amino acid derivatives for the treatment of neurological diseases and selected psychiatric disorders
  • Modified amino acid derivatives for the treatment of neurological diseases and selected psychiatric disorders
  • Modified amino acid derivatives for the treatment of neurological diseases and selected psychiatric disorders

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Example 1 Preparation of compounds according to the invention.

[0061] Analytical method:

[0062] Using a JEOL-500 spectrometer (JEOL USA, Inc.MA, USA), the proton magnetic resonance ( 1 H NMR) and carbon NMR ( 13 C NMR) spectrum. With respect to TMSδ=0 ( 1 H) Delta values ​​(ppm) report chemical shifts. J values ​​are expressed in Hertz (Hz). deuterated chloroform (CDCl 3 ) is used as a solvent. The following signal abbreviations have been used in spectral descriptions: s (singlet), br s (broad singlet), d (doublet), t (triplet), q (quartet), m (multiplet). The UPLC / MS analysis system consists of the following: Waters The apparatus (Waters Corporation, Milford, MA, USA) was coupled to a Waters TQD mass spectrometer operating in electrospray ionization (ESI) mode. Chromatographic separation was performed using an Acquity UPLC BEH C18 (2.1 x 100 mm, 1.7 μm) column. The column was kept at 40 °C and eluted with a gradient of eluent A from 95% to 0% in 10 min a...

Embodiment 2

[0095] Example 2 Biological activity of compounds according to the invention.

[0096] in vivo studies

[0097] This study was performed on male Swiss albino mice (CD-1) weighing 18-26 g. After obtaining appropriate institutional approval, implement all procedures in accordance with applicable Polish and international ethical guidelines for animal testing. Substances 1-2 were administered intraperitoneally (i.p.) 30 minutes before a given test, after suspension in 1% aqueous Tween 80 solution, as a single injection in a volume of 10 ml / kg body weight. Compound 1 was also evaluated for its anticonvulsant activity after intragastric (p.o.) administration to mice and its effect on motor coordination in the rotarod test. In these studies, after compound 1 was dissolved in a mixture of DMSO, PEG 400, water for injection (10 / 40 / 50, v / v / v), 10 ml / Compound 1 was administered in a volume of kg. The anticonvulsant activity of compound 1 was also tested as part of the US screening...

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PUM

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Abstract

2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2-oxopyrrolidin-1-yl)propanamide derivatives with R-configuration at the stereogenic center are disclosed, showing broad- spectrum protective activity in animal models of epileptic seizures, pain, depression and anxiety that are simultaneously devoid of undesirable sedative effects. Additionally, the disclosed derivatives have neuroprotective effects in the in vitro and in vivo studies.

Description

technical field [0001] The present invention relates to chemical compounds which are structurally modified amino acid derivatives and their use as active substances in various dosage forms of medicaments. [0002] The disclosed compounds exhibit broad protective activity in animal models of seizures, pain models, depression and anxiety models and, crucially, are deprived of the well known sedative effects characteristic of antiepileptic drugs. Results of in vivo studies suggest their potential use in the treatment of neurological disorders (epilepsy, neuropathic pain, and migraine) and psychiatric disorders (including anxiety and depression). Given the wide range of therapeutic indications for antiepileptic drugs, these compounds may be useful for the treatment of withdrawal syndromes, schizophrenia, schizoaffective disorder, personality and nutritional disorders, and post-traumatic stress, among others. The disclosed compound can also effectively treat neurodegenerative dise...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/27C07D207/404C07D207/416A61P25/28A61K31/4015
CPCC07D207/404C07D207/27C07D207/416A61P25/28
Inventor 克日什托夫·卡米斯基米哈尔·阿布拉姆马尔桑·雅库别茨安娜·拉帕茨斯泽潘·莫吉尔斯基格尼沃米尔·拉塔茨玛尔塔·斯特鲁格
Owner JAGIELLONIAN UNIVERSITY
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