Methods and uses of quinoline derivatives in the treatment of soft tissue sarcomas and pharmaceutical compositions for treatment of same

Patent metadata

Field	Value
Publication number	US-9968597-B2
Application number	US-201515315647-A
Country	US
Kind code	B2
Filing date	Jun 5, 2015
Priority date	Jun 6, 2014
Publication date	May 15, 2018
Grant date	May 15, 2018

Abstract

The present invention addresses methods and uses of quinoline derivatives in the treatment of tumors and pharmaceutical compositions for treatment of same. Specifically, the present invention involves a method and applications for the use of the quinoline derivative 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopropylamine in the treatment of soft tissue sarcomas and pharmaceutical compositions for treatment of same.

First claim

What is claimed is:

1. A method for treating a soft tissue sarcoma, the method comprising administrating a therapeutically effective amount of Compound I or pharmaceutically acceptable salts thereof to a patient in need of treatment,

2. The method according to claim 1 , wherein the soft tissue sarcoma is an advanced soft tissue sarcoma.

3. The method according to claim 1 , wherein the soft tissue sarcoma is selected from malignant fibrous histiocytoma, fibrosarcoma, liposarcoma, leiomyosaroma of soft tissue, rhabdomyosarcoma, synovial sarcoma, dermatofibrosarcoma protuberans, malignant peripheral nerve sheath tumor, alveolar soft-part sarcoma, clear cell sarcoma, hemangiosarcoma, malignant mesenchymoma, epithelioid sarcoma and undifferentiated sarcoma.

4. The method according to claim 1 , wherein the pharmaceutically acceptable salt comprises a hydrochloride of Compound I.

5. The method according to claim 1 , wherein the daily dosage of the Compound I or pharmaceutically acceptable salts thereof is 2 mg-20 mg.

6. The method according to claim 1 , wherein Compound I or pharmaceutically acceptable salts thereof is administrated by an interval administration, and the interval administration includes administration periods and rest periods, wherein the ratio of the administration periods to the rest periods in days is 2:0.5-5 or 14:7.

7. A method of treating a soft tissue sarcoma, the method comprising administering Compound I

or pharmaceutically acceptable salts thereof to a patient.

8. The method according to claim 7 , wherein the soft tissue sarcoma is an advanced soft tissue sarcoma.

9. The method according to claim 7 , wherein the soft tissue sarcoma is selected from malignant fibrous histiocytoma, fibrosarcoma, liposarcorna, leiomyosaroma of soft tissue, rhabdomyosarcoma, synovial sarcoma, dermatofibrosarcoma protuberans, malignant peripheral nerve sheath tumor, alveolar soft-part sarcoma, clear cell sarcoma, hemangiosarcoma, malignant mesenchymoma, epithelioid sarcoma and undifferentiated sarcoma.

10. The method according to claim 7 , wherein the pharmaceutically acceptable salt comprises a hydrochloride of Compound I.

11. A method of treating a soft tissue sarcoma, the method comprising administering to a patient in need thereof a pharmaceutical composition comprising Compound I or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier,

12. The method according to claim 11 , wherein the soft tissue sarcoma is an advanced soft tissue sarcomas that has been treated with chemotherapy.

13. The method according to claim 11 , wherein said soft tissue sarcoma is selected from malignant fibrous histiocytoma, fibrosarcoma, liposarcorna, leiomyosaroma of soft tissue, rhabdomyosarcoma, synovial sarcoma, dermatofibrosarcoma protuberans, malignant peripheral nerve sheath tumor, alveolar soft-part sarcoma, clear cell sarcoma, hemangiosarcoma, malignant mesenchymoma, epithelioid sarcoma and undifferentiated sarcoma.

14. The method according to claim 11 , wherein the pharmaceutically acceptable salt comprises a hydrochloride of Compound I.

15. The method according to claim 11 , wherein the amount of Compound I or pharmaceutically acceptable salt thereof is 2 mg-20 mg daily.

16. The method according to claim 11 , wherein the pharmaceutical composition is a single dosage comprising 2 mg to 20 mg of Compound I or pharmaceutically acceptable salt thereof.

17. The method according to claim 11 , wherein the composition is administrated by an interval administration, and the interval administration includes administration periods and rest periods, wherein the ratio of the administration periods to the rest periods in days is 2:0.5-5 or 14:7.

18. The method according to claim 1 , wherein the soft tissue sarcoma is an advanced soft tissue sarcoma which has been treated with chemotherapy.

19. The method according to claim 7 , wherein the soft tissue sarcoma is an advanced soft tissue sarcoma which has been treated with chemotherapy.

20. The method according to claim 7 , wherein the pharmaceutically acceptable salt comprises a dihydrochloride of Compound I.

Assignees

• Chia Tai Tianqing Pharmaceutical Group Co Ltd
• Advenchen Laboratories Nanjing Ltd

Inventors

• Zhang Xiquan
• Wang Xunqiang
• Zhan Xiaole
• Dai Jie
• Tian Xin
• Yang Ling

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• A61K9/48

  Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)} · CPC title

• A61K31/4709 Primary

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

• A61K31/4725

  containing further heterocyclic rings · CPC title