Polymorphic substances of 4-aminopyridine, and preparation and application thereof

A technology of aminopyridine and polymorphs, applied in medical preparations containing active ingredients, drug combinations, active ingredients of heterocyclic compounds, etc., can solve the problems that there are no reports of polymorphs of 4-aminopyridine

Inactive Publication Date: 2012-05-09
TIANJIN HEMAY BIO TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] However, there is no polymorphic report of 4-aminopyridine

Method used

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  • Polymorphic substances of 4-aminopyridine, and preparation and application thereof
  • Polymorphic substances of 4-aminopyridine, and preparation and application thereof
  • Polymorphic substances of 4-aminopyridine, and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Embodiment 1, polymorph I

[0076] Add 1.6 g of 4-aminopyridine to a mixture of 15 mL of toluene and 6 mL of pyridine, heat to 95°C to dissolve the clear liquid, leave it to cool to room temperature for 3 hours, filter with suction, and dry the filter cake in the air. Crystal form I was obtained with a melting point of 151.8-152.2°C.

Embodiment 2

[0077] Example 2: Polymorph II

[0078] Method a: Add 3 grams of 4-aminopyridine into a mixture of 2 mL of acetone and 2 mL of water, heat to 80 ° C to dissolve, let it stand to cool to room temperature, let it stand for 2 hours, filter with suction, and dry the obtained filter cake in the air. Crystal form II was obtained with a melting point of 160-160.8°C.

[0079] Method b: Add 4.5 grams of 4-aminopyridine to a mixture of 3 mL of ethanol and 3 mL of water, heat to 85 ° C to dissolve, and the colorless clear liquid is left to cool to 5 ° C, kept for 3 hours, and filtered with suction. The cake was dried in air to obtain the crystal form II.

Embodiment 3

[0080] Example 3: Polymorph III

[0081] Method a: Add 2.2 g of 4-aminopyridine into a mixture of 20 mL of carbon tetrachloride and 5 mL of isopropanol, heat to 86°C to reflux to dissolve the liquid, let stand to cool to 5°C, keep for 20 minutes, and filter with suction. The obtained filter cake was dried in air to obtain the crystal form III with a melting point of 159.8-160.2°C.

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Abstract

The invention discloses polymorphic substances I-VIII of 4-aminopyridine or solvate thereof, and a preparation method and application thereof as active ingredients of medicaments. The polymorphic substances of 4-aminopyridine or solvate thereof provide a better active medical substance state other than the amorphous state, thereby providing optimal selection for the preparation of agents for improving the walking speed of patients with multiple sclerosis and simultaneously relieving other symptoms of multiple sclerosis.

Description

Field of invention: [0001] The invention discloses a polymorphic form of 4-aminopyridine or its solvate and its preparation and application. technical background: [0002] Multiple sclerosis is a chronic and disabling autoimmune disease. According to statistics from the International Multiple Sclerosis Society, more than 2.5 million people have been diagnosed with the disease worldwide, and 400,000 patients in the United States alone suffer from it. The clinical manifestations of multiple sclerosis mainly include progressive difficulty in walking, easy fatigue, loss of body coordination, vision and memory decline, accompanied by heat sensitivity. Among all the onset types of multiple sclerosis, the most common is the relaxation type, which is mainly manifested as a sudden acute attack followed by a period of months to years of remission, without any new symptoms. The second is the persistent type, that is, from the time of onset, the disease is progressively exacerbated wi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/73A61K31/4409A61P37/00A61P25/00
CPCC07D213/73A61K31/44A61P25/00A61P37/00
Inventor 张和胜陈鑫
Owner TIANJIN HEMAY BIO TECH CO LTD
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