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Compositions containing kinase inhibitors

A kind of composition and medicine technology, applied in the field of treatment of diseases

Inactive Publication Date: 2014-08-13
ABBVIE INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] For example, the very low water solubility of the compounds disclosed in '783 poses challenges to formulators due to the need to dissolve the compounds for administration to patients, especially for the manufacture of formulations for intravenous administration

Method used

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  • Compositions containing kinase inhibitors
  • Compositions containing kinase inhibitors
  • Compositions containing kinase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Example 1: N -(4-{4-amino-7-[1-(2-hydroxyethyl)-1 H -pyrazol-4-yl]thieno[3,2- c ]pyridin-3-yl}phenyl)- N Solubility of '-(3-fluorophenyl)urea free base in various media

[0099] Table 1:

[0100] Solvent / medium Solubility Water (in physiological pH range) < 30ng / mL

Embodiment 2

[0101] Example 2: Visual Inspection of Excipients at Different Cremophor EL / PEG-300 / Ethanol Ratio

[0102] Table 2:

[0103]

[0104] Mixtures containing PEG-300 and Cremophor EL resulted in cloudy excipients for dissolving the drug. Mixtures containing PEG-300, Cremophor EL, and ethanol resulted in clear, single-phase solutions only when PEG-300 and Cremophor EL were present in a 1:1 ratio. In other cases, mixtures containing PEG-300, Cremophor EL and ethanol also resulted in cloudy excipients.

Embodiment 3

[0105] Example 3: N -(4-{4-amino-7-[1-(2-hydroxyethyl)-1 H -pyrazol-4-yl]thieno[3,2- c ]pyridin-3-yl}phenyl)- N Solubility of '-(3-fluorophenyl)urea free base in PEG-300 / Cremophor EL / ethanol excipient

[0106] table 3:

[0107]

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Abstract

A composition comprises a kinase inhibitory compound, e.g., N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N'-(3-fluorophenyl)urea, in a mixture comprising (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. The composition is suitable for dilution with an IV solution for administration to a subject in need thereof for treatment of a cancer.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application Serial No. 61 / 570,679, filed December 14, 2011, the entire contents of which are incorporated herein by reference. field of invention [0003] The present invention relates to solid dispersions comprising compounds that inhibit protein kinases, pharmaceutical dosage forms comprising such dispersions, methods of making such dispersions and dosage forms and methods of using the same in the treatment of disease. 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 meth...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/10A61K47/44A61K9/10A61K31/4365A61P35/00A61K9/14
CPCA61K47/44A61K31/4365A61K47/10A61K9/0019A61K9/146A61P35/00A61K47/02A61K47/28
Inventor 石屹J.M.利帕里B.E.帕登L.E.迪亚斯J.K.思朋斯
Owner ABBVIE INC