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Preparation and application of a gefitinib idebenone conjugate

A technology of idebenone and gefitinib, which is applied in the field of preparation of idebenone analogue conjugates of gefitinib, can solve problems such as difficult onset of brain tumors and limited drug delivery efficiency, and achieve oral Effect of good bioabsorption, good inhibitory activity, and good pharmacokinetic profile

Active Publication Date: 2021-03-23
广州初曲科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The blood-brain barrier refers to the barrier between plasma and brain cells formed by brain capillary walls and glial cells, and the barrier between plasma and cerebrospinal fluid formed by the choroid plexus, which can limit the efficiency of drug administration and make it difficult for ordinary drugs to treat brain tumor onset

Method used

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  • Preparation and application of a gefitinib idebenone conjugate
  • Preparation and application of a gefitinib idebenone conjugate
  • Preparation and application of a gefitinib idebenone conjugate

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Synthesis of decyl 10-(4,5-dimethoxy-2-methyl-3,6-dioxocyclohexa-1,4-dien-1-yl)methanesulfonate

[0031]

[0032] Weigh 2-(10-hydroxydecyl)-5,6-dimethoxy-3-methylcyclohexa-2,5-diene-1,4-dione (1.69g, 5mmol) into the circle In the bottom flask, add 20mL of dichloromethane, weigh triethylamine (0.61g, 6mmol) into the reaction system, stir the reaction system, cool down to 0-5°C, weigh methanesulfonyl chloride (0.62g, 5.5 mmol) was added dropwise to the system, after the drop was completed, the temperature was controlled at 0-5°C and the reaction was continued for 3 hours. After the reaction was detected by TLC, the temperature was naturally raised to room temperature, and an appropriate amount of saturated sodium chloride solution was added, and continued to stir for 15 minutes. Wash the organic phase twice with saturated sodium chloride solution, dry the organic phase with anhydrous sodium sulfate, filter, and concentrate to obtain 10-(4,5-dimethoxy-2-methyl-3,6-dioxo...

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Abstract

The invention discloses a gefitinib idebenone analogue conjugate and application thereof. The gefitinib idebenone analogue conjugate provided by the present invention has good inhibitory activity on cancer cells with mutant EGFR or EGFR mutation, can penetrate the blood-brain barrier, and has the effect on the growth of various brain tumor cells. Good inhibitory activity. It has good pharmacokinetic characteristics and good oral bioabsorption. Specifically, the present invention relates to a conjugate represented by general formula I and a pharmaceutical composition containing the conjugate of formula I, which can be used to prepare drugs for treating and preventing EGFR-related diseases, or inhibiting EGFR. In formula I, R 1 is one of methyl, ethyl, isopropyl or propyl; R 2 is one of methoxy, ethoxy, propoxy or isopropoxy; R 3 It is one of methoxy, ethoxy, propoxy or isopropoxy; n is 2‑10.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to the preparation and application of a gefitinib idebenone analogue conjugate. Background technique [0002] In the known technology, cancer, also known as malignant tumor, is a large class of diseases characterized by abnormal proliferation and metastasis of cells. It has the characteristics of high morbidity and mortality, and is one of the malignant diseases that threaten human health and cause death. [0003] Gefitinib is a first-generation tyrosine kinase inhibitor (TKIs), and it is one of the most effective inhibitory drugs in certain patients with advanced non-small cell lung cancer (NSCLC). These patients had recurrent somatic activating mutations in the exons encoding the epidermal growth factor receptor (EGFR) domain. Patients with tumors harboring these activating mutations (EGFRm+) represent approximately 10% to 17% of Western populations and 30% to 50% of Asian populations....

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G63/91C08G63/20
CPCC08G63/20C08G63/916C08G2230/00C08G2390/00
Inventor 欧机智
Owner 广州初曲科技有限公司
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