The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Aug. 20, 2019

Filed:

Jul. 29, 2016
Applicants:

Chia Tai Tianqing Pharmaceutical Group Co., Ltd., Lianyungang, CN;

Lianyungang Runzhong Pharmaceutical Co., Ltd., Lianyungang, CN;

Centaurus Biopharma Co., Ltd., Beijing, CN;

Inventors:

Feng Gong, Lianyungang, CN;

Xinlu Li, Lianyungang, CN;

Rui Zhao, Lianyungang, CN;

Xiquan Zhang, Lianyungang, CN;

Xinhe Xu, Beijing, CN;

Xijie Liu, Beijing, CN;

Dengming Xiao, Beijing, CN;

Yongxin Han, Beijing, CN;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 401/14 (2006.01); A61K 31/496 (2006.01); A61P 35/00 (2006.01);
U.S. Cl.
CPC ...
C07D 401/14 (2013.01); A61K 31/496 (2013.01); A61P 35/00 (2018.01); C07B 2200/13 (2013.01);
Abstract

The present invention discloses a crystal of citrate salt of pyridine-substituted 2-aminopyridine-based protein kinase inhibitors, in particular, to crystal of 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4'-methoxy-6′-((S)-2-methylpiperazin-1-yl)-3,3′-bipyridin-6-amine citrate salt, a method for preparation thereof, a crystalline composition and a pharmaceutical composition comprising the crystal, and further discloses the use of crystals of citrate salt of the compound of Formula I in protein kinase-related diseases. The crystals of citrate salt according to the present invention are superior to 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4′-methoxy-6′-((S)-2-methylpiperazin-1-yl)-3,3′-bipyridin-6-amine or other salts of 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4′-methoxy-6′-((S)-2-methylpiperazin-1-yl)-3,3′-bipyridin-6-amine in at least one aspect of bioavailability, hygroscopicity, stability, solubility, purity, ease of preparation, and the like.


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