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Protein kinase inhibitor and application thereof

A protein kinase inhibitor, low-level technology, applied in the field of drug application, can solve problems such as time-consuming and labor-intensive

Inactive Publication Date: 2012-07-25
CGENETECH (SUZHOU CHINA) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This is undoubtedly time-consuming and labor-intensive.

Method used

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  • Protein kinase inhibitor and application thereof
  • Protein kinase inhibitor and application thereof
  • Protein kinase inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] The chemical structural formula of the protein kinase inhibitor synthesized in the present embodiment is as follows:

[0055]

[0056] [5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl][2,6-difluoro-3-(pyrimidine base-2-ylamino)phenyl] ketone

[0057] (5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl)(2,6-difluoro-3-(pyrimidin-2-ylamino)phe nyl)methanone

[0058] The synthesis process of the protein kinase inhibitor of this embodiment is shown as follows:

[0059]

[0060] Concrete synthetic steps are:

[0061] 1) Dissolve 18.7 grams of (1) in 200 ml of dioxane, add 9.6 grams of sodium tert-butoxide, stir at room temperature for half an hour, then add 15.9 grams of (2) and 1 gram of PdCl 2 (dppf) and refluxed under nitrogen protection for 8 hours, cooled, spin-dried and column chromatography (petroleum ether / ethyl acetate=2:1) ​​to obtain 15.11 g of product, yield 57%.

[0062] 2) After dissolving 5.3 grams of (3) in 50 milliliters of ethanol, add 40 millilite...

Embodiment 2

[0067] The chemical structural formula of the protein kinase inhibitor synthesized in the present embodiment is as follows:

[0068]

[0069] [5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl][2,6-difluoro-3-(thiazol-2-ylamino)phenyl]methyl ketone

[0070] (5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl)(2,6-difluoro-3-(thiaz ol-2-ylamino)phenyl)methanone

Embodiment 3

[0072]

[0073] N-3-[5-(4-chlorophenyl)-1H-pyrrole[2,3-b]pyridin-3-yl)deutero(carbonyl)methyl]-2,4-difluorophenyl]- Ammonium propane-1-sulfonate

[0074] N-3-((5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl)deutero(hydroxy)methyl)-2,4-difluorophenyl)propane-1-sulfonamide

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PUM

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Abstract

The invention discloses a protein kinase inhibitor which is in a mode of a compound shown in a general formula I or pharmaceutically acceptable salt and prodrug thereof, and an isomer and polycrystalline or metamict crystal mode. The invention also relates to a method for preparing a medicament for treating cell excessive multiplification diseases by applying the protein kinase inhibitor.

Description

technical field [0001] The invention relates to a protein kinase inhibitor and its application as a medicine for treating cell overgrowth diseases. Background technique [0002] Protein kinases are used to regulate important signal transduction channels, and their functions cover key signal transduction cascades, control or participate in the control of excess physiological functions, etc., including cell growth and proliferation, cell differentiation, cell development, cell division, stress response , transcriptional regulation, mitotic disorders, and more. Thus, abysmal regeneration of protein kinases is associated with different specific disease states. Diseases particularly associated with unregulated protein kinases include various cancers, leukemia, senile dementia, amyotrophic lateral sclerosis, arthritis, asthma, arteriosclerosis, and atopic dermatitis, among others. In the process of treating the above diseases, additional compounds are required to regulate recept...

Claims

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Application Information

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IPC IPC(8): C07D471/04C07F9/6561A61K31/506A61K31/437A61K31/675A61K31/444A61P35/00A61P35/02A61P25/28A61P21/00A61P19/02A61P11/06A61P9/10A61P17/00A61P37/08A61P37/00A61P31/00A61P9/00A61P11/00A61P3/10A61P15/00A61P25/00A61P13/12A61P25/16A61P19/10A61P29/00A61P17/06
Inventor 余强王彤
Owner CGENETECH (SUZHOU CHINA) CO LTD
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