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Application of substituted crotonamide

A technology of ethoxy and ethynylbenzene, which is applied in the application field of substituted crotonamides and can solve unrecorded problems

Pending Publication Date: 2021-05-28
JIANGSU SUZHONG PHARM GRP CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] CN102625797A discloses (E)-N-(3-cyano-7-ethoxyl-4-(3-ethynylphenylamino) quinoline-6-yl)-4-(dimethylamino)butane- The effect of 2-enamide on EGFR common mutants such as EGFR mutant L858R / T790M, EGFR mutant E746-A750, but the effect on rare mutations such as L861Q, G719X, S768I, etc.

Method used

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  • Application of substituted crotonamide
  • Application of substituted crotonamide
  • Application of substituted crotonamide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The IC50 determination of embodiment 1 protein kinase

[0034] The compound tested in this example is (E)-N-(3-cyano-7-ethoxy-4-(3-ethynylphenylamino)quinolin-6-yl)-4-(dimethyl amino) but-2-enamide.

[0035] 1. Experimental Design

[0036] For the IC50 of the test compound on the protein kinase, 10 semi-logarithmic concentrations (1×10 -06 M to 3×10 - 11 M), single hole, IC50 determination.

[0037] 2. Test substance

[0038] The test substance was two solid tubes, and the ProQinase was transferred to -20°C for subsequent use.

[0039] Before the experiment, make up 1×10 with 100% DMSO -03 M stock solution of test substance and further diluted to 1×10 -04 M / 100% DMSO.

[0040] With 100% DMSO, the test substance was half-logarithmically diluted to a 96-well plate, and prepared from 1 × 10 -04 M to 3×10 -09 M. Before use, the test substance was diluted 1:10 with water to obtain 1×10 -05 M to 3×10 -10 M test substance samples, containing 10% DMSO.

[0041] 5...

Embodiment 2

[0063] The above data show that the inhibitory effect of the tested compounds on rare mutations is better than that of general non-rare mutations. Example 2 Exploratory clinical research trials for the treatment of locally advanced or metastatic non-small cell lung cancer

[0064] 1. Subject selection criteria

[0065] 1. Inclusion criteria:

[0066] Age 18-75 (including 18, 75) years old, gender is not limited. Patients with locally advanced or metastatic NSCLC confirmed by histopathology and / or cytology. Expected survival time > 3 months. The patient's EGFR has one or more of L861Q, G719X, and S768I mutations, and does not have T790M primary / de novo mutations, exon 20 insertion mutations, or L858R mutations.

[0067] 2. Exclusion criteria:

[0068] Patients cannot participate in this trial if they meet any of the following conditions:

[0069] (1) Received any epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) anti-tumor therapy before enrollment.

...

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Abstract

The invention relates to application of substituted crotonamide, in particular to application of (E)-N-(3-cyano-7-ethoxy-4-(3-ethynylphenylamino)quinol-6-yl)-4-(dimethylamino)-2-crotonamide and a pharmaceutically acceptable salt and solvent compound thereof in preparation of drugs for treating cancers mediated by rare EGFR mutation.

Description

technical field [0001] The present application relates to the technical field of medicine, in particular to the application of a substituted crotenamide. Background technique [0002] Non-small cell lung cancer (NSCLC) is a malignant tumor that seriously threatens human health. Despite the continuous improvement of surgery and chemotherapy techniques, the prognosis of patients is still poor, and the 5-year survival rate is less than 20%. At present, molecular targeted therapy targeting human epidermal growth factor receptor (EGFR) has become the most important way to treat NSCLC. [0003] EGFR is the expression product of the proto-oncogene C-erbB-1. The gene is located on chromosome 7 and belongs to the transmembrane receptor tyrosine kinase. After EGFR binds to its ligand, it can activate downstream signaling pathways, regulate tumor cell proliferation, differentiation, angiogenesis and apoptosis inhibition, thereby regulating a series of tumor biological behaviors. [0...

Claims

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Application Information

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IPC IPC(8): A61K31/4706A61P35/00
CPCA61K31/4706A61P35/00C07D215/54
Inventor 唐海涛葛海涛易年红张玉强曹苏闽
Owner JIANGSU SUZHONG PHARM GRP CO LTD
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