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Title:
SACUBITRIL SODIUM SALT, EUTECTIC OF SACUBITRIL FREE ACID AND ACETIC ACID, CRYSTAL FORM THEREOF, METHOD FOR PREPARING CRYSTAL FORM, AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/127994
Kind Code:
A1
Abstract:
The present invention relates to a sacubitril sodium salt as represented by formula IV, a eutectic of sacubitril free acid and acetic acid, a crystal form of the eutectic and a preparation method for the crystal form, and a method for using the eutectic having the described crystal form to prepare LCZ696. The eutectic provided by the present invention may form a stable crystal form and does not easily absorb moisture; the eutectic has good thermal stability, facilitates the purification of sacubitril, is good for storage, and is helpful in synthesizing LCZ696. Moreover, the eutectic provided by the present invention may be directly used for preparing LCZ696 without additional ion exchange, thus being helpful in controlling the type and content of counter cations.

Inventors:
TU, Yongjun (Jiangkou Development Zone, HuangyanTaizhou, Zhejiang 0, 318020, CN)
ZHU, Guorong (Jiangkou Development Zone, HuangyanTaizhou, Zhejiang 0, 318020, CN)
XIE, Wenlong (Jiangkou Development Zone, HuangyanTaizhou, Zhejiang 0, 318020, CN)
DUAN, Zhenghua (Jiangkou Development Zone, HuangyanTaizhou, Zhejiang 0, 318020, CN)
WANG, Zhen (Jiangkou Development Zone, HuangyanTaizhou, Zhejiang 0, 318020, CN)
Application Number:
CN2018/083729
Publication Date:
July 04, 2019
Filing Date:
April 19, 2018
Export Citation:
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Assignee:
ZHEJIANG TIANYU PHARMACEUTICAL CO., LTD. (Jiangkou Development Zone, HuangyanTaizhou, Zhejiang 0, 318020, CN)
International Classes:
C07D257/04; A61K31/216; A61K31/41; A61P9/12; C07C51/43; C07C53/08; C07C231/24; C07C233/47
Domestic Patent References:
WO2017191620A12017-11-09
Foreign References:
CN108530371A2018-09-14
CN107188820A2017-09-22
US5217996A1993-06-08
Attorney, Agent or Firm:
BOSS & YOUNG PATENT AND TRADEMARK LAW OFFICE (5/F, Tower A GT International Center, Jia 3 Yongandongli,Jianguomenwai Ave., Chaoyang District, Beijing 2, 100022, CN)
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