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Title:
SALT OF MORPHOLINE DERIVATIVE AND CRYSTALLINE FORM THEREOF, AS WELL AS PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE OF THE SAME
Document Type and Number:
WIPO Patent Application WO/2017/114456
Kind Code:
A1
Abstract:
The present invention provides a novel, pharmaceutically acceptable salt of a morpholine derivative, including malate salt, tartrate salt, hydrochloride salt, acetate salt and naphthalene diphosphate salt. The tartrate salt has three crystalline salt forms: crystalline form A, crystalline form B and a dihydrate. The malate salt, hydrochloride salt and acetate salt each have a crystalline salt form. The naphthalene diphosphate salt is amorphous. Compared to a known free alkali of the morpholine derivative, the present invention affords one or more improved properties, such as a better crystalline state with significantly increased water solubility, light stability and thermal stability. The present invention further provides a preparation method of the salt of the morpholine derivative and the crystalline forms thereof, as well as a pharmaceutical composition and use of the same.

Inventors:
XIA GUANGXIN (CN)
XIE JIANSHU (CN)
JIA GUOHUI (CN)
HAN JIANSHENG (CN)
UEDA NAOKO (JP)
IIJIMA TORU (JP)
Application Number:
PCT/CN2016/112966
Publication Date:
July 06, 2017
Filing Date:
December 29, 2016
Export Citation:
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Assignee:
SHANGHAI PHARMACEUTICALS HOLDING CO LTD (CN)
MITSUBISHI TANABE PHARMA CORP (JP)
International Classes:
C07D471/04; A61K31/5377; A61P3/10; A61P9/00; A61P9/12; A61P13/12; C07C51/41; C07C51/43; C07C53/10; C07C59/245; C07C59/255; C07C309/35
Foreign References:
CN103562191A2014-02-05
Other References:
BERGE, S.M. ET AL.: "Pharmaceutical Salts", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 66, no. 1, 31 January 1977 (1977-01-31), pages 1 - 19, XP002675560
See also references of EP 3398946A4
Attorney, Agent or Firm:
KINGSOUND & PARTNERS (CN)
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