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)
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:
Assignee:
SHANGHAI PHARMACEUTICALS HOLDING CO LTD (CN)
MITSUBISHI TANABE PHARMA CORP (JP)
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:
CN103562191A | 2014-02-05 |
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
See also references of EP 3398946A4
Attorney, Agent or Firm:
KINGSOUND & PARTNERS (CN)
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