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Pyrimidinecarboxamide derivatives as inhibitors of SYK kinase

A technology of drugs and compounds, applied in the direction of anti-inflammatory agents, drug combinations, non-central analgesics, etc., can solve the problem of lack of efficacy of placebos

Inactive Publication Date: 2012-02-08
GLAXO GROUP LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In a further Phase II clinical trial, for allergic rhinitis, R112 was shown to lack efficacy compared to placebo (Clinical Trials.gov Identifier NCT0015089)

Method used

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  • Pyrimidinecarboxamide derivatives as inhibitors of SYK kinase
  • Pyrimidinecarboxamide derivatives as inhibitors of SYK kinase
  • Pyrimidinecarboxamide derivatives as inhibitors of SYK kinase

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-2

[0301] Example 1-2-{[(3R, 4R)-3-aminotetrahydro-2H-pyran-4-yl]amino}-4-[(4-methylphenyl)amino]-5-pyrimidinemethyl Amide

[0302]

[0303] [(3R, 4R)-4-({5-(aminocarbonyl)-4-[(4-methylphenyl)amino]-2-pyrimidinyl}amino)tetrahydro-2H-pyran-3- 1,1-Dimethylethyl carbamate (52.2g) was added to a mixture of hydrogen chloride in isopropanol (5M, 300ml) and ethanol (400ml). The mixture was heated to reflux with stirring and heating was continued for 24 hours with vigorous stirring. The mixture was cooled to room temperature, filtered and the solid was washed with ethanol (100ml) and dried in vacuo. The crude product was suspended in water (900ml) and heated to reflux to give a clear solution. The solution was basified with sodium hydroxide solution (2M, 300ml) and cooled in ice. The precipitated product was collected by filtration, washed with water (2×100 ml) and the beige solid was dried in a vacuum oven at 40° C. for 2 h to give 2-{[(3R,4R)-3-aminotetrahydro- 2H-pyran-4-yl]am...

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Abstract

The compound of formula (I) or a salt, preferably a pharmaceutically acceptable salt, thereof; is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate mast cell activation, for instance allergic and inflammatory diseases, as well of potential use in cancer therapy, specifically heme malignancies.

Description

technical field [0001] The present invention relates to novel compounds having activity against spleen tyrosine kinase (Syk kinase), processes for their preparation, pharmaceutically acceptable formulations containing them and their use in therapy. Background technique [0002] Syk kinases are non-receptor tyrosine kinases involved in coupling activated immune receptors to signaling downstream events that mediate diverse cellular responses including proliferation, differentiation and phagocytosis. Syk kinase is widely expressed in hematopoietic cells. Syk kinase inhibitors have potential anti-inflammatory and immunomodulatory activities. They inhibit Syk kinase-mediated signaling of IgG Fcε and γ receptors and BCR receptors, resulting in inhibition of mast cell, macrophage and B cell activation, and associated inflammatory responses and tissue damage. Accordingly, Syk kinase inhibitors are of interest in several therapeutic areas, including the treatment of rheumatoid arth...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/12A61P35/00A61K31/506
CPCC07D405/12A61P1/00A61P1/04A61P11/00A61P11/02A61P11/04A61P11/06A61P11/16A61P17/00A61P17/02A61P17/04A61P17/06A61P27/14A61P29/00A61P35/00A61P35/02A61P37/08A61P43/00A61K31/506
Inventor F·L·阿特金森V·K·帕特尔
Owner GLAXO GROUP LTD
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