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Crystalline forms of kinase inhibitors

A form, crystallization technique, applied in the field of crystalline forms of kinase inhibitors

Inactive Publication Date: 2013-03-27
ABBVIE INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Certain polymorphic forms can exhibit excellent stability and shelf life, leading to improved shelf-life of pharmaceutical products

Method used

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  • Crystalline forms of kinase inhibitors
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0163] N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl )-N'-(3-fluorophenyl)urea free base solid (100 mg) was suspended in THF / water mixture (80 / 20 v / v, 500 μL). The solid was collected by centrifugation after equilibrating at ambient conditions for three days.

[0164] Table 1. PXRD peak list: N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridine-3- Base}phenyl)-N'-(3-fluorophenyl)urea malonate type I

[0165] Peak position (° 2θ) 6.136 9.363 10.696 11.684 12.280 13.297 16.321 16.543 16.966 18.474 19.538 21.217 21.498 22.177 23.137 23.456 23.684 24.001

[0166] Example 2

Embodiment 2

[0168] N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl )-N'-(3-fluorophenyl)urea L-bitartrate solid (30 mg) was dissolved in THF / water mixture (80 / 20 v / v, 500 μl). Single crystals were observed after six weeks of equilibration at ambient conditions.

[0169] Table 2. PXRD peak list: N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridine- 3-yl}phenyl)-N'-(3-fluorophenyl)urea L-tartrate type II

[0170] Peak position (° 2θ) 6.205 8.879 10.277 10.644 11.958 12.436 12.763 15.933 18.479 19.181 20.581 21.155 21.382 21.745 22.504 22.861 23.855 24.500 24.916

[0171] Example 3

Embodiment 3

[0173] N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridine- 3-yl}phenyl)-N'-(3-fluorophenyl)urea free base solid (27 mg) was suspended in 2-propanol (750 μl). Hydrochloric acid (60 μl, 1 N) was diluted with 2-propanol (250 μl). The hydrochloric acid solution was then slowly added to the A-968660 free base suspension under magnetic stirring at 40°C. Crystallization was observed shortly after complete addition of the HCl solution. The solid was collected by centrifugation.

[0174] Example 4

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Abstract

Salts of N-(4- {4-amino-7-[ 1 -(2-hydroxyethyl)- 1 H-pyrazol-4-yl]thieno[3,2-c]pyridin- 3-yl}phenyl)-N'-(3-fluorophenyl)urea and crystalline forms thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application No. 61 / 353,170, filed June 09, 2010, the entire contents of which are incorporated herein by reference. field of invention [0003] The present invention relates to N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridine-3 in crystalline form Salts of -yl}phenyl)-N'-(3-fluorophenyl)ureas, methods of preparing crystalline forms, pharmaceutical formulations thereof, and methods of treating cancer. Background of the invention [0004] Mitosis is the process by which the replicated complete copy of the chromosome set separates into two daughter cells by the microtubule-spindle apparatus. Aurora-kinase, a key mitotic regulator required for genome stability, was found to be overexpressed in human tumors. Accordingly, there remains a need in the therapeutic art for compounds that inhibit Aurora-kinase, compositions comprising the inhibitor, and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D495/04A61K31/4365A61P35/00
CPCC07D495/04A61P35/00A61P35/02A61P43/00
Inventor G.G.Z.张P.J.布拉克迈尔A.Y.谢赫
Owner ABBVIE INC
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