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Polymorphic forms of deferasirox ( icl670a)

A technology of crystal form and type, applied in the field of crystal form A, therapeutic treatment, which can solve problems such as differences

Active Publication Date: 2009-09-23
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is also known that different crystalline forms of the same drug may have very different properties in certain pharmaceutically important

Method used

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  • Polymorphic forms of deferasirox ( icl670a)
  • Polymorphic forms of deferasirox ( icl670a)
  • Polymorphic forms of deferasirox ( icl670a)

Examples

Experimental program
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Effect test

Embodiment 1

[0184] Example 1 : Form A of 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid prepared using THF / ethanol and HXF

Embodiment 2

[0185] Example 2 : Form A of 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid prepared using toluene and THF

Embodiment 3

[0186] Example 3 : Form A of 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid prepared using methanol / THF

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PUM

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Abstract

The invention relates to crystalline forms of 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1- yl]benzoic acid and to its amorphous form, to processes for the preparation thereof, to compositions containing the same and their uses for the manufacture of a medicament for the treatment of the human body.

Description

[0001] The present invention relates to new crystalline forms of 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid, processes for preparing these crystalline forms, combinations containing these crystalline forms and the use of these crystalline forms in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. Background of the invention [0002] The drug 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid is an orally active iron chelator indicated for the treatment of transfusion dependence iron overload in transfusion dependent anemias, particularly thalassemia major, thalassemia intermedia and sickle cell disease, to reduce iron-related morbidity and mortality. 4-[3,5-Bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid is also useful in the treatment of hemochromatosis. In general, the preparation of 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid is known in the art. However, it is also known that differe...

Claims

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Application Information

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IPC IPC(8): C07D249/08A61K31/4196A61P7/00
CPCC07D249/08A61P7/00
Inventor M·马兹
Owner NOVARTIS AG