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Purpose of pyrazolopyrimidine derivative for preparation of medicine for treating diseases

A pyrazolopyrimidine and disease-treating technology, which is applied in the field of pyrazolopyrimidine derivatives in the field of preparing medicines for treating diseases, and achieves an obvious inhibitory effect

Pending Publication Date: 2019-04-02
GUANGXI WUZHOU PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there are only reports about pyrazolopyrimidine derivatives in the treatment of acute myeloid leukemia and psoriasis

Method used

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  • Purpose of pyrazolopyrimidine derivative for preparation of medicine for treating diseases
  • Purpose of pyrazolopyrimidine derivative for preparation of medicine for treating diseases
  • Purpose of pyrazolopyrimidine derivative for preparation of medicine for treating diseases

Examples

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Effect test

Embodiment 1

[0018] Example 1 In vitro human tumor cell proliferation inhibition experiment of pyrazolopyrimidine derivatives of the present invention

[0019] (1) Experimental materials: The cell lines used in this experiment were purchased from ATCC Company of the United States or the cell bank of the Type Culture Collection Committee of the Chinese Academy of Sciences, and the culture conditions were in accordance with the instructions. Pyrazolopyrimidine derivatives were synthesized by the inventors.

[0020] (2) Experimental method: collect the cells to be tested in the logarithmic growth phase, and fix the number in each well (depending on the cells, the suspension cells are generally 1 × 10 4 -4×10 4 The number of cells / well, the adherent cells are generally 2×10 3 -4×10 3 The number of cells / well) was seeded in a 96-well plate and cultured overnight in a cell culture incubator at 37°C and 5% CO2. On the next day, dilute sorafenib and pyrazolopyrimidine derivatives to correspond...

Embodiment 2

[0026] Embodiment 2 intends in vivo anti-glioma experiment

[0027] (1) Experimental materials: rat C6 glioma cell line (Cell Resource Center, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences); healthy male SD rats, SPF grade. Pyrazolopyrimidine derivatives were synthesized by the inventors.

[0028] (2) Experimental method:

[0029] Establishment of the rat glioma model: SD rats were injected with 1% pentobarbital sodium (40mg / kg) into the tail vein, and the hair on the top of the head of the rat was removed. The scalp was cut to expose the sign of the blanche skull, and a bone hole was drilled with a self-made dental drill at 1 mm anterior to the midpoint of the breech and 3 mm beside the sagittal suture, and 10 μL of C6 cell suspension was extracted with a micro-syringe and fixed vertically on the test bench. Insert the needle 6 mm below the dura mater at the original bone hole, retreat 1 mm, inject the cell suspension within 10 minutes (2 μL / min),...

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Abstract

The invention relates to the technical field of a medicine, and especially relates to a purpose of pyrazolopyrimidine derivative for preparation of medicine for treating diseases. The diseases includemyelodysplastic syndrome, ovarian cancer, testicular cancer, skin squamous cell carcinoma, bladder cancer, cancer of biliary duct, prostate cancer, glioma, nasopharyngeal carcinoma, renal cancer, tongue squamous carcinoma, squamous cell lung carcinoma, maxicell lung cancer, renal cell adenocarcinoma, choriocarcinoma, and placental villus cancer. The pyrazolopyrimidine derivative of the inventionhas obvious inhibitory effects on various tumor cells, especially the tumor cell inhibiting effect of glioma, and the inhibition effect on some tumor cells is better than that of sorafenib.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to the use of pyrazolopyrimidine derivatives in the preparation of medicines for treating diseases. Background technique [0002] Sorafenib is a widely used FLT3 inhibitor in clinical practice, but there is no report about the use of sorafenib in brain glioma. [0003] The pyrazolopyrimidine derivative (Formula I) is a small-molecule inhibitor targeting FLT3 kinase, which is a new type of compound independently developed by the applicant, and the compound patent has been authorized at present. [0004] At present, there are only reports about pyrazolopyrimidine derivatives in the treatment of acute myeloid leukemia and psoriasis. [0005] Contents of the invention [0006] In order to overcome the shortcomings of the prior art, the present invention provides the use of pyrazolopyrimidine derivatives in the preparation of medicines for treating diseases. [0007] The purpose...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61P35/00
CPCA61K31/519
Inventor 钟杰敏赖树生欧阳静波陈焕展黄宇声刘冠萍
Owner GUANGXI WUZHOU PHARMA GRP
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