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Quinoline derivatives with antitumor activity

A technology of methoxyquinoline and methyl, which is applied in the field of medicine and can solve the problems of poor prognosis, difficult to remove tumors, and poor efficacy.

Active Publication Date: 2019-04-09
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] For advanced MTC, it is difficult to completely remove the tumor by surgery alone. Because it is not sensitive to radiation, and adjacent organs such as thyroid cartilage, trachea, and spinal cord have low radiation tolerance, the effect of external radiation therapy is generally poor, and some studies even It is believed that the prognosis of patients receiving radiation therapy is actually worse

Method used

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  • Quinoline derivatives with antitumor activity
  • Quinoline derivatives with antitumor activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 11

[0050] Example 11-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]ring Propylamine dihydrochloride

[0051]

Embodiment 2

[0054] Example 2 contains 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxyl]methyl Capsules of ]cyclopropylamine dihydrochloride (dihydrochloride of compound I)

[0055]

[0056] Grind the dihydrochloride of compound I and pass through a 80-mesh sieve; then mix evenly with mannitol and hydroxypropyl cellulose; then add the prescribed amount of microcrystalline cellulose, mix evenly, and pass through a 0.8mm sieve; finally add the prescribed amount The magnesium stearate is mixed well and filled into capsules.

[0057] Capsules with other contents of the dihydrochloride of compound I can be prepared with reference to the same ratio and prescription as above.

Embodiment 3

[0058] Example 3 Study on Tolerance and Preliminary Curative Effect of Dihydrochloride Capsules Treatment of Compound I

[0059] (1) Tolerance study results

[0060] Patients with malignant tumors who have a clear diagnosis and have failed or lacked standard treatment will be treated continuously for 2 weeks with a break of 1 week, that is, 3 weeks (21 days) is a treatment cycle, and at least 2 cycles (42 days) will continue to be treated. Receptivity observation and curative effect observation at the same time.

[0061] 10 mg once a day, 3 patients had adverse reactions including grade III and above fat and amylase elevation in 1 case, grade II fatigue in 1 case, other grade I adverse reactions included hoarseness in 2 cases, diarrhea and abdominal pain in 1 case, high 1 case of blood pressure and so on.

[0062] 16 mg once a day, 1 case of grade III blood pressure elevation and fatigue occurred in each of the 3 patients during the second week of the second cycle.

[0063]...

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PUM

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Abstract

The invention provides a quinoline derivative with antitumor activity and its use in preparing a pharmaceutical composition for treating antitumor. Specifically, the present invention relates to quinoline derivatives 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinoline-7- Base] oxy] methyl] cyclopropylamine in the treatment of medullary thyroid cancer purposes.

Description

technical field [0001] The invention belongs to the field of medicine, and the invention relates to the use of quinoline derivatives in the preparation of pharmaceutical compositions for treating and antitumor. Specifically, the present invention relates to the use of quinoline derivatives in the treatment of medullary thyroid cancer. Background technique [0002] Medullary thyroid carcinoma (MTC) is a tumor originating from thyroid C cells or parafollicular cells, accounting for about 5% to 10% of thyroid malignancies, and its malignancy is between papillary carcinoma and undifferentiated carcinoma It is a moderately malignant tumor. The disease was first described by Hazard et al. in 1959. MTC patients are more common in women than men, and are common in middle-aged and young adults, with local infiltrative growth and early hematogenous lymphatic metastasis. [0003] MTC is clinically divided into two types: hereditary MTC and sporadic MTC. Hereditary MTC accounts for ab...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4709A61P35/00A61P5/14
CPCA61K31/4709A61K31/4725
Inventor 张喜全王训强湛筱乐于鼎田心杨玲
Owner CHIA TAI TIANQING PHARMA GRP CO LTD