Salts of quinazoline derivative and method for preparing the same

Patent metadata

Field	Value
Publication number	US-10231973-B2
Application number	US-201615560099-A
Country	US
Kind code	B2
Filing date	Mar 18, 2016
Priority date	Mar 20, 2015
Publication date	Mar 19, 2019
Grant date	Mar 19, 2019

Abstract

The present application relates to maleates of a compound of Formula I, methods for preparing the same, pharmaceutical compositions thereof and uses thereof in the treatment of tumors, such as non-small cell lung cancer, breast cancer, and other malignant tumors.

First claim

The invention claimed is:

1. A maleate of a compound of Formula I,

2. The maleate of the compound of Formula I according to claim 1 , wherein a molar ratio of the compound of Formula I to maleic acid is 1:0.5-4.

3. The maleate of the compound of Formula I according to claim 2 , wherein the molar ratio of the compound of Formula I to maleic acid is 1:1 or 1:2.

4. A method for preparing a maleate of a compound of Formula I:

the method comprising: (1) preparing a solution of the compound of Formula I; (2) mixing the solution of the compound of Formula I obtained from step (1) with maleic acid to provide a reaction mixture; and (3) spray-drying the reaction mixture obtained from step (2) to obtain the maleate of the compound of Formula I.

5. The method according to claim 4 , wherein a molar ratio of the amount of the compound of Formula I to that of maleic acid in the reaction mixture is 1:1-20.

6. The method according to claim 4 , wherein in step (1), the compound of Formula I is dissolved in an organic solvent to prepare the solution of the compound of Formula I.

7. The method according to claim 6 , wherein a solvent miscible with the organic solvent is added prior to the spray-drying.

8. A pharmaceutical composition, comprising the maleate of the compound of Formula I according to claim 1 , and a pharmaceutically acceptable carrier, excipient, diluent and/or vehicle.

9. A method for treating non-small cell lung cancer or breast cancer, comprising administering the maleate of the compound of Formula I according to claim 1 to a subject in need thereof.

10. A method for treating non-small cell lung cancer or breast cancer, comprising administering the pharmaceutical composition according to claim 8 to a subject in need thereof.

11. The method according to claim 4 , wherein a molar ratio of the amount of the compound of Formula I to that of maleic acid in the reaction mixture is 1:1-15.

12. The method according to claim 4 , wherein a molar ratio of the amount of the compound of Formula I to that of maleic acid in the reaction mixture is 1:1-10.

13. The method according to claim 6 , wherein the organic solvent is DMF.

14. The method according to claim 7 , wherein the solvent miscible with the organic solvent is water.

Assignees

• Chia Tai Tianqing Pharmaceutical Group Co Ltd
• Centaurus Biopharma Co Ltd
• Lianyungang Runzhong Pharmaceutical Co Ltd
• Chai Tai Tianqing Pharmaceutical Group Co Ltd

Inventors

• Zhang Xiquan
• Tang Song
• Feng Weiwei
• Tian Xin
• Chen Zhilin
• Gu Hongmei
• Xu Hongjiang
• Liu Fei

Classifications

• C07D403/12

  linked by a chain containing hetero atoms as chain links · CPC title

• C07C57/145

  Maleic acid · CPC title

• A61K31/517 Primary

  ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title