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Polymorphous Forms III And IV Of N-Benzoyl - Staurosporine

A technology of benzoyl star and crystal form, which is applied in the direction of medical preparations containing active ingredients, antibacterial drugs, drug combinations, etc., and can solve problems such as difficult application of melt extrusion

Inactive Publication Date: 2014-12-17
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, the melting points of these polymorphs are close to the decomposition temperature of N-benzoylstaurosporine, which makes their application difficult for melt extrusion for the preparation of pharmaceutical compositions

Method used

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  • Polymorphous Forms III And IV Of N-Benzoyl - Staurosporine
  • Polymorphous Forms III And IV Of N-Benzoyl - Staurosporine
  • Polymorphous Forms III And IV Of N-Benzoyl - Staurosporine

Examples

Experimental program
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Embodiment 1

[0087] In Example 1, Form III of N-benzoylstaurosporine was prepared by GAS recrystallization. The X-ray diffraction pattern of the crystal form III is in figure 1 , and the X-ray diffraction patterns of Form III and Form II disclosed in WO 2006 / 048296 are in figure 2 displayed in .

Embodiment 2

[0089] In Example 2, crystalline form IV of N-benzoylstaurosporine was prepared by GAS recrystallization. The X-ray diffraction pattern of crystal form IV is in image 3 , and the X-ray diffraction patterns of Form IV and Form II disclosed in WO 2006 / 048296 are in Figure 4 displayed in .

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PUM

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Abstract

The present invention relates to a crystalline form III and a crystalline form IV of N-benzoyl staurosporine.

Description

[0001] This application is a divisional application of PCT application PCT / EP2010 / 068359 filed on November 29, 2010, entitled "Polymorphic forms III and IV of N-benzoyl-staurosporine", said PCT The date of application to enter the Chinese national phase is May 30, 2012, and the application number is 201080054097.4. technical field [0002] The present invention relates to novel crystalline forms of N-benzoylstaurosporine and processes for the preparation of these crystalline forms. Background technique [0003] Protein kinase C (abbreviated as PKC hereinafter) is one of the key enzymes in the cell signal transduction pathway, and it plays a key role in the control of cell proliferation and differentiation. PKC is a family of serine / threonine kinases. [0004] At least 12 isoforms of PKC have been identified, which are generally divided into three classes based on their structure and substrate requirements. Promising results have recently been obtained in a clinical trial i...

Claims

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Application Information

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IPC IPC(8): C07D498/22A61K31/553A61P35/00A61P35/02A61P29/00A61P31/04A61P9/10A61P25/00
CPCC07D498/22A61P9/00A61P9/10A61P25/00A61P29/00A61P31/00A61P31/04A61P35/00A61P35/02A61P43/00A61K31/00A61K31/553C07B2200/13
Inventor R·塔库尔
Owner NOVARTIS AG
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