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Novel imidazopyrazines as cyclin dependent kinase inhibitors

a cyclin-dependent kinase inhibitor and imidazopyrazines technology, applied in the field ofimidazo1, can solve the problems of increased cdk2 activity and poor overall survival

Inactive Publication Date: 2007-07-05
SCHERING CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention provides a novel class of compounds that inhibit cyclin dependent kinases (CDKs) and methods of preparing and using them. These compounds can be used to treat and prevent diseases associated with CDKs such as cancer, inflammation, and arthritis. The compounds can also be used to treat neurodegenerative diseases such as Alzheimer's disease. The invention provides a wide range of compounds that can be used as protein kinase inhibitors."

Problems solved by technology

Their altered expression has been shown to correlate with increased CDK2 activity levels and poor overall survival.

Method used

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  • Novel imidazopyrazines as cyclin dependent kinase inhibitors
  • Novel imidazopyrazines as cyclin dependent kinase inhibitors
  • Novel imidazopyrazines as cyclin dependent kinase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparative Example 1

[0140]

[0141] A mixture of 1-methylimidazole-2-carboxamide (1 equiv.) and bromoacetone (1.2 eq) in anhydrous CH3CN is stirred and refluxed under N2 for 1 day. The solvent is evaporated and the pure product is obtained after column chromatography on silica gel with CH2Cl2:7 N NH3 in MeOH.

examples 2-5

Preparative Examples 2-5

[0142]

[0143] These compounds are prepared by essentially same procedure set forth in Preparative Example 1.

example 6

Preparative Example 6

[0144]

[0145] A mixture of the product from Preparative Example 1 (1 eq.) and imidazole (25 eq.) is stirred under N2 at 175° C. for 20 hr. The imidazole is distilled off in a vacuum and the residue is purified by column chromatography on silica gel with CH2Cl2:7 N NH3 in MeOH. Pure product is obtained.

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Abstract

In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Description

FIELD OF THE INVENTION [0001] The present invention relates to imidazo[1,2-a]pyrazine compounds useful as protein kinase inhibitors (such as for example, the inhibitors of the cyclin-dependent kinases, mitogen-activated protein kinase (MAPK / ERK), glycogen synthase kinase 3(GSK3beta) and the like), pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases such as, for example, cancer, inflammation, arthritis, viral diseases, neurodegenerative diseases such as Alzheimer's disease, cardiovascular diseases, and fungal diseases. This application claims the benefit of priority from U.S. provisional patent application Ser. No. 60 / 1412,906, filed Sep. 23, 2002. BACKGROUND OF THE INVENTION [0002] Protein kinase inhibitors include kinases such as, for example, the inhibitors of the cyclin-dependent kinases (CDKs), mitogen activated protein kinase (MAPK / ERK), glycogen synthase kinase 3 (GSK3beta), and the like. The cy...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/498C07D487/02C07D487/04
CPCC07D487/04A61P1/00A61P1/16A61P1/18A61P11/00A61P13/00A61P13/08A61P13/12A61P15/00A61P17/00A61P19/00A61P21/00A61P25/00A61P35/00A61P35/02A61P43/00A61P7/00
Inventor PARUCH, KAMILGUZI, TIMOTHY J.DWYER, MICHAEL P.DOLL, RONALD J.GIRIJAVALLABHAN, VIYYOOR M.
Owner SCHERING CORP
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