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Title:
DIMETHYLAMINO GLAUCOCALYXIN A HYDROCHLORIDE SALT AND CRYSTALLINE FORM THEREOF
Document Type and Number:
WIPO Patent Application WO/2016/150206
Kind Code:
A1
Abstract:
Disclosed is a glaucocalyxin A derivative -- dimethylamino glaucocalyxin A hydrochloride salt -- and two crystalline forms thereof. The dimethylamino glaucocalyxin A hydrochloride salt provided by the present invention has good water solubility and high oral bioavailability; the two crystalline forms of the dimethylamino glaucocalyxin A hydrochloride salt are readily soluble in water, reducing the time required for dissolving and decreasing product degradation; the invention is not prone to produce electrostatic charges, which is advantageous to the preparation of subsequent formulation products; futhermore, the filtration operation during the process of preparation is simple, the product is easy to dry, and the properties of the crystal are stable during drying; the purification effect during the preparation process is obvious, crystal purity is high, and the invention is suitable for industrial production.

Inventors:
LI, Yunsen (Floor 5, Building No. 5 DongFang Industrial District C, No. 1 Huayun Road, Suzhou Industrial Par, Suzhou Jiangsu 0, 215000, CN)
CHEN, Zijun (Floor 5, Building No. 5 DongFang Industrial District C, No. 1 Huayun Road, Suzhou Industrial Par, Suzhou Jiangsu 0, 215000, CN)
DENG, Shiping (Floor 5, Building No. 5 DongFang Industrial District C, No. 1 Huayun Road, Suzhou Industrial Par, Suzhou Jiangsu 0, 215000, CN)
FENG, Haimei (Floor 5, Building No. 5 DongFang Industrial District C, No. 1 Huayun Road, Suzhou Industrial Par, Suzhou Jiangsu 0, 215000, CN)
LI, Yong (Floor 5, Building No. 5 DongFang Industrial District C, No. 1 Huayun Road, Suzhou Industrial Par, Suzhou Jiangsu 0, 215000, CN)
LIU, Qian (Floor 5, Building No. 5 DongFang Industrial District C, No. 1 Huayun Road, Suzhou Industrial Par, Suzhou Jiangsu 0, 215000, CN)
Application Number:
CN2015/097691
Publication Date:
September 29, 2016
Filing Date:
December 17, 2015
Export Citation:
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Assignee:
SUZHOU PHARMAVAN CANCER RESEARCH CENTER CO., LTD. (Floor 5, Building No. 5 DongFang Industrial District C, No. 1 Huayun Road, Suzhou Industrial Par, Suzhou Jiangsu 0, 215000, CN)
International Classes:
C07C225/12; A61K31/133; A61P35/00; A61P37/00; C07C221/00
Foreign References:
CN104817464A2015-08-05
CN104761460A2015-07-08
CN101851273A2010-10-06
Other References:
YANG, JING ET AL.: "Synthesis and Biological Evaluation of Glaucocalyxin A Derivatives as Potential Anticancer Agents", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 86, 31 August 2014 (2014-08-31), pages 235 - 241, XP029048580, ISSN: 0223-5234
Attorney, Agent or Firm:
BEYOND ATTORNEYS AT LAW (F6 Xijin Centre, 39 Lianhuachi East Rd. Haidian District, Beijing 6, 100036, CN)
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