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Title:
MEDICINAL SALT OF CARIPRAZINE AND CRYSTAL FORM THEREOF, PHARMACEUTICAL COMPOSITION THEREOF, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/160583
Kind Code:
A1
Abstract:
Disclosed are 1-hydroxy-2-naphthoate or bis-hydroxynaphthenate of cariprazine, a new solid form thereof, a pharmaceutical composition thereof, and a preparation method therefor and the use thereof. The cariprazine salt and the solid form thereof, especially 1-hydroxy-2-naphthoate of cariprazine in an insoluble salt of cariprazine has the advantages of a long-acting sustained-release preparation, can be developed into a suspension injection, can also solve the problems of the risk of the dissociation or the lack of sustained release effect of existing salt types such as cariprazine hydrochloride, can achieve the effect of long-acting administration, and greatly improves the compliance of a patient and the bioavailability and medication safety of a drug.

Inventors:
CHEN ZHIXIANG (CN)
ZHANG XIAN (CN)
ZHU TAO (CN)
FU JUN (CN)
GUO ZHEN (CN)
WANG TINGTING (CN)
YING SHUHUAN (CN)
Application Number:
PCT/CN2023/077671
Publication Date:
August 31, 2023
Filing Date:
February 22, 2023
Export Citation:
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Assignee:
SHANGHAI YONSUN BIOTECHNOLOGY CO LTD (CN)
International Classes:
A61K9/16; C07D295/135; A61K31/496; A61P25/18; A61P25/28
Domestic Patent References:
WO2021041730A12021-03-04
WO2005016261A22005-02-24
Foreign References:
CN110769815A2020-02-07
CN108261394A2018-07-10
CN102596172A2012-07-18
CN106831594A2017-06-13
CN114195740A2022-03-18
Other References:
CYSEWSKI PIOTR: "In silico screening of dicarboxylic acids for cocrystallization with phenylpiperazine derivatives based on both cocrystallization propensity and solubility advantage", JOURNAL OF MOLECULAR MODELING, SPRINGER BERLIN HEIDELBERG, BERLIN/HEIDELBERG, vol. 23, no. 4, 27 March 2017 (2017-03-27), Berlin/Heidelberg, pages 1 - 11, XP036211489, ISSN: 1610-2940, DOI: 10.1007/s00894-017-3287-y
Attorney, Agent or Firm:
BEIJING ORIGINTELLIGENCE IP LAW FIRM (CN)
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