Unlock instant, AI-driven research and patent intelligence for your innovation.

A kind of pteridine derivative and its pharmaceutical composition

A derivative, pteridine technology, applied in the field of medicine, can solve problems such as uncontrollable cell division, and achieve the effects of inhibiting the growth of tumor cells, easy to prepare, and rich in synthetic raw materials

Inactive Publication Date: 2019-07-19
李柱来
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Increased expression and activity of EGFR can eventually lead to uncontrolled cell division

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A kind of pteridine derivative and its pharmaceutical composition
  • A kind of pteridine derivative and its pharmaceutical composition
  • A kind of pteridine derivative and its pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] The preparation of embodiment 1 compound

[0050] (1) Synthesis of the compound with the chemical structural formula shown in formula II

[0051] 1.1 Synthesis of 3-aminopyrazine-2-carboxamide

[0052] Add 15.4 g (about 0.1 mol) of methyl 3-aminopyrazine-2-carboxylate and 120 mL of concentrated ammonia water to a 250 mL three-necked flask equipped with magnetic stirring and a reflux condenser (with a dry end adapter), respectively, Stir for 10 h, filter, wash with water, and dry at 60°C to obtain 12.5 g of a yellow solid, namely 3-aminopyrazine-2-carboxamide. Yield: 90.6%; Melting point: 237.9~238.3°C (Reference: Design, Synthesis and Anticancer Activity of Pteridine Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors, PhD Thesis of Shandong University, Duan Chonggang, 2008) .

[0053] 1.2 Synthesis of 3-amino-6-bromopyrazine-2-carboxamide

[0054] Add 11.04g (0.08mol) 3-aminopyrazine-2-carboxamide and 120mL For glacial acetic acid, add dropwise a solution...

Embodiment 2

[0082] Example 2 In vitro cell inhibitory activity experiment

[0083] 1 reagent preparation

[0084] Preparation of medium: (1) RPMI-1640 medium (Lossway Parker Memorial Institute, No. 1640 medium, containing 10% fetal bovine serum). Weighing NaHCO with an electronic balance 3 Put 2.0 g into a large beaker, add 1000 mL of double-distilled water, and add 1 bag of culture medium under stirring to dissolve it completely; adjust the pH to 7.1; add penicillin-streptomycin (final concentrations are 100 μg / mL, 100 U / mL, respectively mL); in a clean bench, use a 0.45 μm membrane filter to remove impurities, and then use a 0.2 μm membrane filter to remove bacteria; seal the filtered medium and store it in a refrigerator at 4°C. (2) DMEM (high sugar) medium. Add 3.7g NaHCO 3 , the operation steps are the same as above.

[0085] Preparation and use of thiazolium blue staining agent (abbreviated as MTT): Weigh 0.5 g of MTT, dissolve it with phosphate buffered solution (PBS) medium,...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
melting pointaaaaaaaaaa
melting pointaaaaaaaaaa
melting pointaaaaaaaaaa
Login to View More

Abstract

On one hand, the invention provides a pteridine derivative and a pharmaceutically acceptable salt thereof. The pteridine derivative and the pharmaceutically acceptable salt thereof have obvious restraining effect on tumor cell generation and breeding, and can be used for medicines for treating cancers and tumors.

Description

technical field [0001] The application relates to a pteridine derivative and a pharmaceutical composition containing it, belonging to the field of medicine. Background technique [0002] The combination of Epidermal Growth Factor (EGF for short) and Epidermal Growth Factor Receptor (EGFR for short) can activate the activity of tyrosine kinase and thus activate the response leading to cell proliferation. Increased expression and activity of EGFR can eventually lead to uncontrolled cell division. Epidermal growth factor receptor tyrosine kinase (abbreviated as EGFR-TK) is the earliest discovered protein tyrosine kinase, which is widely distributed on the cell membrane of various tissues in the human body. Cell lung cancer, ovarian cancer, breast cancer, gastric cancer, esophageal cancer, etc.), the intracellular region of EGFR has a binding site for adenosine triphosphate (abbreviated as ATP), and EGFR inhibitors can competitively bind to the ATP binding site , thereby inhib...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07D475/00A61K31/519A61P35/00
CPCC07D475/00
Inventor 李柱来王艰许秀枝
Owner 李柱来