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Quinoline derivative for treating non-small cell lung cancer

A non-small cell lung cancer and drug technology, applied in the field of medicine, can solve the problems of treatment differences in NSCLC patients

Pending Publication Date: 2022-06-24
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinical application in recent years has found that EGFR-TKI has individual differences in the treatment of NSCLC patients

Method used

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  • Quinoline derivative for treating non-small cell lung cancer
  • Quinoline derivative for treating non-small cell lung cancer
  • Quinoline derivative for treating non-small cell lung cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 11

[0058] Example 1 1-[[[4-(4-Fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl] Cyclopropylamine dihydrochloride

[0059]

[0060] 1-[[[4-(4-Fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl was prepared by referring to the method of Example 24 in WO2008112407 ]oxy]methyl]cyclopropylamine, followed by the preparation of the salt form examples in the specification to prepare the title compound.

Embodiment 21

[0061] Example 2 1-[[[4-(4-Fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl] Preparation of capsules of cyclopropylamine dihydrochloride (dihydrochloride of compound I)

[0062]

[0063]Pulverize the dihydrochloride of compound I, pass through an 80 mesh sieve; then mix with mannitol and hydroxypropyl cellulose; then add the microcrystalline cellulose of the recipe quantity, mix well, pass through a 0.8mm sieve; finally add the recipe quantity of magnesium stearate, mix well and fill the capsules.

Embodiment 3

[0065] Randomized, randomized, pathologically confirmed patients with measurable disease, pathologically confirmed advanced non-small cell lung cancer, second-line or higher therapy or intolerable, and receiving other cytotoxic drugs, radiotherapy, or surgery for more than four weeks Double-blind, placebo-controlled, multicenter Phase II clinical trial study. In this study, the efficacy of compound I dihydrochloride capsules in the treatment of advanced non-small cell lung cancer was preliminarily evaluated compared with placebo. The primary outcome measure was progression-free survival (PFS). Of the 117 patients enrolled in the study, 57 were randomized to the placebo group and 60 to the hydrochloride group, aged 18-70 years.

[0066] The above-mentioned eligible non-small cell lung cancer patients received Compound I dihydrochloride / placebo for clinical trials. The dose of 12 mg / 0 mg once a day, continuous medication for 2 weeks and then 1 week off, that is, 3 weeks (21 da...

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PUM

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Abstract

The invention provides a quinoline derivative for treating non-small cell lung cancer. 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl) oxy-6-methoxyquinolin-7-yl] oxy] methyl] cyclopropylamine or a pharmaceutically acceptable salt thereof provided in the present application can be used for treating non-small cell lung cancer patients who are not suitable for EGFR-TKI treatment, and can be used for treating non-small cell lung cancer patients who are not suitable for EGFR-TKI treatment. The progression-free lifetime of a non-small cell lung cancer patient which is not suitable for EGFR-TKI treatment can be obviously improved.

Description

[0001] This application is a part of a Chinese patent application with the application number of 201580066135.0 (the international application number is PCT / CN2015 / 096770), the application date is December 09, 2015, and the invention title is "quinoline derivatives for the treatment of non-small cell lung cancer". case application. [0002] CROSS-REFERENCE TO RELATED APPLICATIONS [0003] This application claims priority to and the benefit of Chinese Patent Application No. 201410747455.X filed with the State Intellectual Property Office of China on December 09, 2014, the disclosure of which is incorporated herein by reference in its entirety. technical field [0004] The present application belongs to the technical field of medicine, and relates to the use of quinoline derivatives for anti-tumor. In particular, the present application relates to the use of quinoline derivatives for the treatment of non-small cell lung cancer. Background technique [0005] Non-small cell lu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4709A61P11/00A61P35/00A61P35/04
CPCA61K31/4709
Inventor 王训强缪亚东周敏王善春杨玲施伟
Owner CHIA TAI TIANQING PHARMA GRP CO LTD