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Pharmaceutically acceptable salt and polymorphic forms of flupirtine maleate

a technology of flupirtine maleate and polymorphic forms, which is applied in the field of new polymorphic forms of flupirtine maleate, can solve the problems of affecting the quality, safety and efficacy of a drug product, and achieve the effect of improving the safety and efficacy of the drug produ

Inactive Publication Date: 2012-06-07
PLIVA HRVATSKA D O O
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0018]We have now surprisingly found that certain polymorphic forms of flupirtine maleate exhibit beneficial properties and, in particular, provide advantages over commercially available flupirtine maleate.
[0039]Additionally, the polymorphic forms of flupirtine maleate, as provided by the present invention, exert potent cyto- and neuroprotective effects and have utility in the treatment and prevention of neurodegenerative disorders such as Parkinson's disease, dementia including Alzheimer's disease, Huntington's chorea, multiple sclerosis, amyotrophic lateral sclerosis, encephalopathy including AIDS related encephalopathy, Creutzfeldt-Jakob disease including classical and new-variant types and Batten disease.
[0057]There is also provided by the present invention a polymorphic form of flupirtine maleate, substantially as hereinbefore described, for use in the manufacture of a medicament for the treatment of a disease state prevented, ameliorated or eliminated by the administration of a centrally acting non-opioid analgesic, a muscle-relaxant, a functional NMDA antagonist and / or an apoptosis inhibitor, wherein the polymorphic form of flupirtine maleate according to the invention, provides an enhanced therapeutic effect compared to the therapeutic effect provided by the existing polymorphic forms of flupirtine maleate. The present invention also provides a corresponding method of treatment, which comprises administering to a patient a therapeutically effective amount of a polymorphic form of flupirtine maleate, substantially as hereinbefore described, so that the administered polymorphic form of flupirtine maleate according to the present invention, provides an enhanced therapeutic effect to the patient, compared to the therapeutic effect provided by corresponding administration of the existing polymorphic forms of flupirtine maleate.

Problems solved by technology

Thus, polymorphism can affect the quality, safety, and efficacy of a drug product.

Method used

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  • Pharmaceutically acceptable salt and polymorphic forms of flupirtine maleate
  • Pharmaceutically acceptable salt and polymorphic forms of flupirtine maleate
  • Pharmaceutically acceptable salt and polymorphic forms of flupirtine maleate

Examples

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Effect test

example 1

Preparation of Flupirtine Maleate Form I

[0071]250 mg of flupirtine maleate was dissolved in 35 mL of methyl acetate whilst heating. Hot solution was filtered and crystallisation of needle like crystals occurred while cooling the solution to room temperature. The product was collected by filtration and dried overnight at room temperature. 136 mg of a white crystalline product was obtained.

example 2

Preparation of Flupirtine Maleate Form II

[0072]500 mg of flupirtine maleate was placed in 3-neck round bottom flask filled with a mixture of 96% ethanol (15 mL) and dichloromethane (30 mL). The reaction mixture was refluxed for 20 minutes whilst stirring and then cooled in an ice bath to room temperature. Stirring was then continued at room temperature overnight. The product was filtered and dried overnight at room temperature. 314 mg of a white product was obtained.

example 3

Preparation of Flupirtine Maleate Form III

[0073]500 mg of flupirtine maleate was dissolved in 10 mL of 96% ethanol. The solution was heated and the hot solution was filtered and added dropwise to 20 mL of hot methyl acetate. The mixture was stirred at room temperature and precipitation of a crystalline product occurred. The product was filtered. 320 mg of a white product was obtained.

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Abstract

New polymorphic forms of flupirtine maleate are described.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application is a divisional of U.S. Nonprovisional patent application Ser. No. 12 / 309,260, filed Mar. 25, 2011, which is a National Stage Application of PCT / GB2007 / 002647, filed Jul. 13, 2007, which claims benefit of Serial No. 0613928.1, filed Jul. 13, 2006 in Great Britain and which applications are incorporated herein by reference. To the extent appropriate, a claim of priority is made to each of the above disclosured applications.FIELD OF THE INVENTION[0002]The present invention is concerned with new polymorphic forms of flupirtine maleate, processes for preparing the new polymorphic forms, pharmaceutical compositions containing them, therapeutic uses thereof and methods of treatment employing them.BACKGROUND OF THE INVENTION[0003]Flupirtine maleate is chemically designated 2-amino-3-carbethoxyamino-6,4-fluorobenzylamino-pyridine maleate and can be represented by the following structural formula:[0004]Flupirtine is a centrally ac...

Claims

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Application Information

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IPC IPC(8): A61K31/44A61P21/02A61P25/16A61P29/00C07D213/75A61P25/00
CPCC07D213/75A61P21/02A61P25/00A61P25/04A61P25/16A61P25/28A61P29/00
Inventor DANILOVSKI, ALEKSANDARDEVCIC, MAJAMARINKOVIC, MARINAMESTROVIC, ERNESTMUNDORFER, TINATUNJIC, IVA
Owner PLIVA HRVATSKA D O O
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