Quinoline derivative for treatment of triple-negative breast cancer

Patent metadata

Field	Value
Publication number	US-11554115-B2
Application number	US-201916980786-A
Country	US
Kind code	B2
Filing date	Mar 13, 2019
Priority date	Mar 14, 2018
Publication date	Jan 17, 2023
Grant date	Jan 17, 2023

Abstract

The present invention provides a quinoline derivative for treating triple-negative breast cancer and use thereof in preparing a pharmaceutical composition for treating a tumor. Specifically, the present invention relates to use of quinoline derivative 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinoline-7-yl]oxy]methyl]cyclopropylamine in the treatment of triple-negative breast cancer,

First claim

What is claimed is:

1. A method of treating triple-negative breast cancer in a patient, the method comprising administering to the patient in need thereof a therapeutically effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof,

2. The method of claim 1 , wherein the triple-negative breast cancer is advanced or metastatic triple-negative breast cancer.

3. The method of claim 1 , wherein the triple-negative breast cancer is refractory to prior treatment.

4. The method of claim 1 , wherein the triple-negative breast cancer is refractory to radiotherapy and/or chemotherapy.

5. The method of claim 3 , wherein the prior treatment comprises at least one treatment selected from the group consisting of radiotherapy, chemotherapy, and targeted therapy.

6. The method of claim 5 , wherein the prior treatment is at least one of an anthracycline, a taxane, ara antimetabolite, and a platinum-based therapy.

7. The method of claim 1 , wherein the pharmaceutically acceptable salt is a salt formed by the compound of formula I and an acid selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, acetic acid, trifluoroacetic acid, propionic acid, hexanoic acid, heptanoic acid, cypionic acid, glycolic acid, pyruvic acid, lactic acid, malonic acid, succinic acid, malic acid, maleic acid, fumaric acid, tartaric acid, citric acid, benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, 1,2-ethanedisulfonic acid, 2-hydroxyethanesulfonic acid, benzenesulfonic acid, p-chlorobenzenesulfonic acid, p-toluenesultbnic acid, 3 phenylpropionic acid, trimethylacetic acid, t-butylacetic acid, dodecyl sulfuric acid, gluconic acid, glutamic acid, hydroxynaphthoic acid, salicylic acid, and stearic acid.

8. The method of claim 1 , wherein the pharmaceutically acceptable salt is a hydrochloride or a maleate salt.

9. The method of claim 1 , wherein the compound of formula I or the pharmaceutically acceptable salt thereof is administered via oral, parenteral, intraperitoneal, intravenous, intra-arterial, transdermal, sublingual, intramuscular, rectal, buccal, intranasal, inhalational, vaginal, intraocular, topical, subcutaneous, intralipid, intra-articular, intraperitoneal or intrathecal route.

10. The method of claim 1 , wherein the compound of formula I or the pharmaceutically acceptable salt thereof is administered orally.

11. The method of claim 1 , wherein the daily dose of the compound of Formula I or the pharmaceutically acceptable salt administered is selected from the group consisting of 3 mg to 30 mg, 5 mg to 20 mg, 8 mg to 16 mg, 8 mg to 14 mg, 8 mg, 10 mg. and 12 mg.

12. The method of claim 1 , wherein the daily dose of the compound of Formula I or the pharmaceutically acceptable salt administered is 8 mg, 10 mg, or 12 mg.

13. The method of claim 1 , wherein the compound of Formula I or the pharmaceutically acceptable salt thereof is administered by an intermittent regimen including treatment periods and rest periods, and the ratio of the treatment period to the rest period in days is 2:0.5˜2:5, 2:0.5˜2:3, 2:0.5˜2:2, or 2:0.5˜2:1.

14. The method of claim 1 , wherein the compound of Formula I or the pharmaceutically acceptable salt thereof is administered by an intermittent regimen selected from the group consisting of: 2-week treatment period/2-week rest period, 2-week treatment period/1-week rest period, and 5-day treatment period/2-day rest period.

15. The method of claim 1 , wherein the compound of Formula I or the pharmaceutically acceptable salt thereof is administered by an intermittent regimen, wherein the treatment is administered for two weeks, and rested for 1 week.

16. The method of claim 1 , wherein a second active ingredient is administered concurrently or sequentially with the compound of Formula I or the pharmaceutically acceptable salt thereof.

17. The method of claim 16 , wherein the second active ingredient is a chemotherapeutic drug.

18. The method of claim 17 , wherein the chemotherapeutic drug is selected from the group consisting of an anthracycline, a taxane, a platinum-based drug, capecitabine, and cyclophosphamide.

19. The method of claim 1 , wherein the patient is a human.

20. The method of claim 3 , wherein the triple-negative breast cancer has progressed or relapsed after the prior treatment selected from the group consisting of Baa anthracycline, a taxane, an antimetabolite, and a platinum-based therapy.

Assignees

• Chia Tai Tianqing Pharmaceutical Group Co Ltd

Inventors

• Tian Xin
• Lv Peng
• Yang Ling
• Wang Xiangjian
• Zhang Xiquan
• Wang Shanchun
• Wang Xunqiang
• Jiang Hai

Classifications

• A61K31/675 Primary

  having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61K31/337

  having four-membered rings, e.g. taxol · CPC title

• A61K9/4858

  Organic compounds · CPC title

• A61K31/4709 Primary

  Non-condensed quinolines and containing further heterocyclic rings · CPC title