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Pyrazole naphthylurea tyrosine kinase inhibitor and its application

A kind of technology of tyrosine kinase and naphthalene urea, which is applied in the field of pyrazole naphthalene urea tyrosine kinase inhibitor

Inactive Publication Date: 2013-07-24
WUHAN DONGYU BIOLOGICAL MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far, no receptor tyrosine kinase inhibitor has been used clinically to treat patients with age-related macular degeneration or diabetic retinopathy

Method used

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  • Pyrazole naphthylurea tyrosine kinase inhibitor and its application
  • Pyrazole naphthylurea tyrosine kinase inhibitor and its application
  • Pyrazole naphthylurea tyrosine kinase inhibitor and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Synthesis of Example Compounds II-VI

[0033] Example compound II

[0034] 1-[4-(3-Amino-1H-pyrazolo[3,4-b]pyridin-4-yl)-naphthalen-1-yl]-3-m-tolyl-urea(II), 1-[4 -(3-amino-1H pyrazolo[3,4B]pyridine 4 base)naphthalene 1-yl]-3-toluene-urea

[0035]

[0036] Preparation method: the compound naphthylamine borate (1, purchased from Aldrich, 2.7g, 0.01mol) was dissolved in dichloromethane (20mL), and after the obtained solution was cooled to 0°C, the compound m-tolyl isocyanate (6, purchased from in Aldrich, 1.6 g, 0.012 mol). The resulting reaction mixture was gradually warmed to room temperature with stirring and continued to stir at room temperature for 18 hours. Solvent was removed on a rotary evaporator. The resulting mixture was added with 15 mL of a mixed solvent of dichloromethane / n-hexane (1 / 3), stirred for half an hour and then allowed to stand for one hour. The precipitated white solid was filtered and dried to obtain the compound naphthyl-pheny...

Embodiment 2

[0079] Embodiment 2 pharmacological test

[0080] In vitro test of compounds on KDR, PDGFR-β and c-Kit receptor tyrosine kinase activity inhibition

[0081] (1) Experimental method

[0082] Enzyme-Linked Immunosorbent Assay (ELISA)

[0083] main instrument

[0084] Adjustable wavelength microplate microplate reader Molecular DevicesSPECTRAMAX190.

[0085] main reagent

[0086] Test sample: a series of example compounds II-VI of the above-mentioned Example 1, diluted to the required concentration with the solvent DMSO immediately before use; control group: Sorafenib or Su11248;

[0087] Tyrosine kinase VEGFR2 (KDR), c-Kit is expressed by insect baculovirus expression system, obtained by affinity purification with Ni-NTA column, and tested to meet the experimental requirements;

[0088] Tyrosine kinase PDGFRβ was purchased from Millipore;

[0089] The kinase reaction substrate Poly(Glu, Tyr, 4:1) was purchased from Sigma;

[0090] Anti-phosphotyrosine monoclonal antibody ...

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PUM

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Abstract

The invention relates to a pyrazole naphthylurea tyrosine kinase inhibitor. The pyrazole naphthylurea tyrosine kinase inhibitor is compounds having structures represented by general formula I, and medicinal salts thereof. The compounds have tyrosine kinase inhibition activities, and can be used in medicines for treating tyrosine kinase mediated diseases or illnesses as a tyrosine kinase inhibitor.

Description

technical field [0001] The invention belongs to the field of tyrosine kinase inhibitors, in particular to pyrazole-type naphthylurea-type tyrosine kinase inhibitors and applications thereof. Background technique [0002] Tyrosine kinases are a class of proteins with tyrosine kinase activity. They can catalyze the transfer of phosphate groups on ATP to tyrosine residues of many important proteins, phosphorylate them, and activate downstream signal transduction pathways . Protein tyrosine kinases play a very important role in intracellular signal transduction pathways, regulating a series of physiological and biochemical processes such as cell growth, differentiation, and death. Dysregulation of protein tyrosine kinase function can lead to a series of diseases in organisms, including tumors and eye diseases. [0003] The development and metastasis of many tumors and the formation of tumor angiogenesis are closely related to the abnormal expression of tyrosine kinases. In pa...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61K31/437A61P35/00A61P27/02A61P9/10A61P3/10A61P27/06
Inventor 吴飞飞李雁茭刘盛德
Owner WUHAN DONGYU BIOLOGICAL MEDICAL TECH CO LTD
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