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Small molecule inhibitor compound as well as preparation method and application thereof

A technology of small molecule inhibitors and compounds, applied in anti-inflammatory agents, organic chemistry, drug combinations, etc., can solve problems such as insufficient activity, easy drug resistance, and low activity

Inactive Publication Date: 2015-03-11
CHANGZHOU VELOX PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] In view of the fact that the existing drugs only target a single drug target, and at the same time, these drugs have the disadvantages of low activity and easy drug resistance for advanced cancers and cancers with complex mechanisms, the main purpose of the present invention is to provide a drug that can Simultaneously inhibit the small molecule inhibitor compound of VEGFR and EGFR receptor kinase family and preparation method thereof, to solve the above-mentioned problems

Method used

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  • Small molecule inhibitor compound as well as preparation method and application thereof
  • Small molecule inhibitor compound as well as preparation method and application thereof
  • Small molecule inhibitor compound as well as preparation method and application thereof

Examples

Experimental program
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Embodiment

[0022] Dry acetonitrile solution of compound 1 (0.207 g, 1.54 mmol), compound 2 (0.229 g, 1.54 mmol) and 1,8-diazabicycloundec-7-ene (DBU) (0.235 ml, 1.57 mmol) , heat to reflux for 4-6 hours, spin dry the solvent and add EtoAc– H 2 O, the organic layer was washed with water and NaCl solution, anhydrous Na 2 SO 4 After drying, evaporating the solvent and purifying (for example, passing through a column with dichloromethane), 0.356 g of compound 3 was obtained.

[0023] Compound 3 (0.085g, 0.38mmol) and compound 4 (0.056g, 0.38mmol) were dissolved in 2-ethoxyethanol (1mL), heated at 150°C and stirred overnight. The reaction solution was cooled to room temperature, filtered through a syringe filter, and purified by liquid chromatography-mass chromatography. The trifluoroacetic acid salt thus obtained was neutralized with 10% potassium carbonate aqueous solution to obtain 0.016 g of compound 5. The compound 5 was analyzed by mass spectrometry, MS (MH+): 482 m / z C 24 h 21...

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Abstract

The invention discloses a small molecule inhibitor compound as well as a preparation method and application thereof. The compound has a structure in a formula I show in the specification. The small molecule inhibitor compound provided by the invention overcomes the defects that the conventional drug only aims at a single drug target, and for a cancer at a later period and with a complex mechanism, the activity is low, drug tolerance is easy to generate and the activity is relatively low existing in the conventional drug. The small molecule inhibitor compound provided by the invention restrains VEGFR and EGFR receptor kinase families at the same time, has efficient antitumor activity and efficient antiinflammatory activity, and can be used for preparing efficient drugs for resisting tumors, inflammation, neuroinflammation and obesity.

Description

technical field [0001] The invention relates to a small molecule inhibitor compound, in particular to a small molecule inhibitor compound capable of simultaneously inhibiting VEGFR and EGFR receptor kinase family and a preparation method thereof. Background technique [0002] Vascular endothelial growth factor (VEGF) is also known as vascular permeability factor and vascular proliferation factor. So far, VEGF has been confirmed to have a highly specific and effective role in promoting neovascularization. Studies have shown that VEGF not only induces the migration of endothelial cells, but also stimulates a series of protein products to participate in the degradation of extravascular matrix. These functions make VEGF play a major role in regulating angiogenesis under physiological and pathological conditions. [0003] VEGF selectively acts directly on two subtypes of tyrosine kinase receptors Flt-1 (also known as VEGFR-1) and KDR (also known as VEGFR-2) on the membrane of vas...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/12A61K31/506A61P35/00A61P29/00A61P3/04A61P25/00
CPCY02P20/55C07D403/12
Inventor 杨光
Owner CHANGZHOU VELOX PHARMA SCI & TECH CO LTD
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