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Novel naphthyridine derivatives and the use thereof as kinase inhibitors

A derivative, naphthyridine technology, applied in the field of new naphthyridine derivatives and their use as kinase inhibitors, can solve the problems of cell death, uncontrolled cell growth and the like

Inactive Publication Date: 2012-09-12
AETERNA ZENTARIS GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The consequences of this excessive kinase activation are, for example, uncontrolled cell growth and reduced cell death

Method used

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  • Novel naphthyridine derivatives and the use thereof as kinase inhibitors
  • Novel naphthyridine derivatives and the use thereof as kinase inhibitors
  • Novel naphthyridine derivatives and the use thereof as kinase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0191] Example 1 (reaction according to scheme 1, step 1):

Embodiment 111 and Embodiment 11

[0192] Example 1.1.1 and Example 1.1.2: 3-bromo-[1,5]naphthyridine-5-oxide and 3-bromo-1,5-naphthyridine-1-oxide

[0193]

[0194] 4.43 g (21.2 mmol, 1 equivalent) of 3-bromo-1,5-naphthyridine (W. Czuba, Recueil des Travaux Chimiques des Pays-Bas 1963, 82, 988-996) were introduced into 165 mL of dichloromethane. Then 5.23 g (21.2 mmol, 1 equiv) of m-chloroperbenzoic acid were added portionwise at 0°C. The mixture was stirred at room temperature for 18 h. The mixture was washed with 1M aqueous NaOH and water. The organic layer was washed with Na 2 SO 4 Dry, filter and evaporate to dryness. The residue was purified by column chromatography using dichloromethane and then dichloromethane / ethanol:98 / 2 as eluents. The solvent was evaporated to dryness to give 3.08 g of 3-bromo-1,5-naphthyridine-5-oxide (pale yellow powder, 64% yield) and 1.00 g of 3-bromo-1,5-naphthyridine- 1-oxide (yellow powder, 21% yield).

[0195] 3-Bromo-[1,5]naphthyridine-5-oxide

[0196] Yield: 3.0...

Embodiment 2

[0205] Example 2 (reaction according to scheme 1, step 2):

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Abstract

The present invention relates to kinase modulators of the naphthyridine type and to the preparation and use thereof as medicaments for the modulation of misdirected cellular signal transduction processes, in particular for influencing the function of tyrosine and serine / threonine kinases and for the treatment of malignant or benign tumours and other disorders based on pathological cell proliferation, such as, for example, restenosis, psoriasis, arteriosclerosis and cirrhosis of the liver.

Description

technical field [0001] The present invention relates to naphthyridine kinase modulators, their preparation and use as medicaments for regulating misdirected cell signal transduction processes, in particular for affecting tyrosine and serine-threonine kinases Function and use in the treatment of malignant or benign tumors and other diseases based on pathological cell proliferation, for example, restenosis, psoriasis, arteriosclerosis and liver cirrhosis. Background technique [0002] Activation of protein kinases is a central event in cellular signal transduction. Aberrant kinase activation is observed in various pathological states. Therefore, targeted inhibition of kinases is an essential therapeutic goal. [0003] Phosphorylation of proteins is often initiated by extracellular signals and represents a general mechanism for the control of various cellular events such as metabolic processes, cell growth, cell migration, cell differentiation, membrane trafficking, and apopt...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61K31/4745A61P35/00
CPCC07D471/04A61P1/16A61P17/06A61P35/00A61P43/00A61P9/10A61K31/4375C07B55/00C07D403/04C07B2200/13
Inventor T·舒斯特M·格拉齐I·塞佩尔特E·波利莫罗普洛斯G·穆勒E·京特P·马尔尚J·德福
Owner AETERNA ZENTARIS GMBH
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