Substituted oxazole derivatives and their use as tyrosine kinase inhibitors

A technology of oxazole and substituents, applied in the field of substituted oxazole derivatives, can solve problems that have not been reported

Inactive Publication Date: 2008-07-09
AB SCIENCE +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] None of the above compounds have been reported as...

Method used

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  • Substituted oxazole derivatives and their use as tyrosine kinase inhibitors
  • Substituted oxazole derivatives and their use as tyrosine kinase inhibitors
  • Substituted oxazole derivatives and their use as tyrosine kinase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0137] 017: 1-[4-Methyl-3-(5-pyridin-4-yl-oxazol-2-ylamino)-phenyl]-3-phenyl-propan-1-one

[0138]

[0139] m.p.=138℃

[0140] 018: 4-[2-(5-Acetyl-2-methyl-phenylamino)-oxazol-5-yl]-benzonitrile

[0141]

[0142] m.p.=240℃

[0143] 019: 4-(2-{5-[3-(4-fluoro-phenyl)-propionyl]-2-methyl-phenylamino}-oxazol-5-yl)-benzonitrile

[0144]

[0145] m.p.=175℃

[0146] 020: 4-{2-[2-Methyl-5-(3-phenyl-propionyl)-phenylamino]-oxazol-5-yl}-benzonitrile

[0147]

[0148] m.p.=138℃

[0149] 021: 4-(2-{5-[3-(3-fluoro-phenyl)-propionyl]-2-methyl-phenylamino}-oxazol-5-yl)-benzonitrile

[0150]

[0151] m.p.=157℃

[0152] 022: 4-[2-(5-Acetyl-2-methyl-phenylamino)-oxazol-5-yl]-benzamide

[0153]

[0154] m.p.>260℃

[0155] Among the specific compounds of the general formula I, the compounds referred to in the present invention are shown in the following general formula IV:

[0156]

[0157] Pass IV

[0158] G is oxygen, sulfur, N(R11) or (CH2) n , where n is 1 or 2...

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PUM

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Abstract

The present invention relates to novel compounds selected from substituted oxazole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl and Flt-3 inhibitors.

Description

technical field [0001] The present invention relates to substituted oxazole derivatives which selectively modulate, modulate and / or inhibit signal transduction mediated by certain native and / or mutant tyrosine kinases present in various human and animal diseases, such as cell proliferation, metabolism, allergies and genetic diseases. Notably, these compounds are potent and selective inhibitors of c-kit, bcr-abl and Flt-3. Background technique [0002] Tyrosine kinases are receptor-type or non-receptor-type proteins that transfer the terminal phosphate group of ATP to protein tyrosine residues, thereby activating or inactivating signal transduction pathways. These proteins are thought to be involved in a variety of cellular mechanisms that, when disrupted, cause abnormal cell proliferation, migration, and inflammation. [0003] So far, there are about 58 receptor tyrosine kinases. Including the well-known VEGF receptor (Kim et al. Nature 362, pp.841-844, 1993), PDGF recept...

Claims

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Application Information

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IPC IPC(8): A61K31/421A61K31/427A61K31/4439C07D263/48C07D413/04C07D413/12C07D413/14C07D417/12A61P35/00A61P37/00A61P29/00
CPCC07D263/48C07D263/46C07D413/04C07D413/14C07D417/12C07D413/12C07D263/58A61P1/00A61P1/04A61P11/02A61P11/06A61P13/12A61P17/00A61P17/04A61P17/06A61P19/02A61P25/00A61P27/14A61P29/00A61P35/00A61P35/02A61P37/00A61P37/06A61P37/08A61P43/00A61P9/00A61K31/421
Inventor D·格里尔森A·贝尼亚哈德A·穆西M·克鲁瓦西
Owner AB SCIENCE
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