SGLT-2 INHIBITOR SARCOSINE CO-CRYSTAL, PREPARATION METHOD THEREFOR AND USE THEREOF - BEIJING CREATRON INSTITUTE OF PHARMACEUTICAL RES CO LTD

Title:

SGLT-2 INHIBITOR SARCOSINE CO-CRYSTAL, PREPARATION METHOD THEREFOR AND USE THEREOF

Document Type and Number:

WIPO Patent Application WO/2022/067724

Kind Code:

A1

Abstract:

Provided are an SGLT-2 inhibitor sarcosine co-crystal, a preparation method therefor and use thereof. Using sarcosine as a ligand, said co-crystal has higher safety and lower costs; a drug co-crystal has higher stability, and during the production process or storage process of a formulation composition, the crystal form is not easily changed; said co-crystal does not melt when heated, does not stick, aggregate or generate static electricity, and has better mixing uniformity. Said co-crystal has uniform distribution in a prepared pharmaceutical composition, causing that the pharmaceutical composition has better in-vivo release, absorption and efficacy, and has small difference between batches; and the pharmaceutical composition has high stability, and is more conducive to storage and transportation. The present invention has a simple preparation process, has high reproducibility, has short crystallization time, has low process condition requirements, and has higher economic benefits; the present invention does not use an unsafe solvent during the preparation process; and a crude product or intermediate of the SGLT-2 inhibitor can be simultaneously purified.

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Inventors:

JIA HUIJUAN (CN)
HOU WEI (CN)
REN XIAOHUI (CN)
GUO LIANG (CN)
DONG YANYANG (CN)

Application Number:

PCT/CN2020/119547

Publication Date:

April 07, 2022

Filing Date:

September 30, 2020

Export Citation:

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Assignee:

BEIJING CREATRON INSTITUTE OF PHARMACEUTICAL RES CO LTD (CN)
TIANJIN CREATRON BIOTECHNOLOGY CO LTD (CN)

International Classes:

C07H7/04; A61K31/7042; A61P3/10; A61P9/00; A61P13/12; C07D309/10; C07D409/10

Domestic Patent References:

WO2003099836A1	2003-12-04
WO2008002824A1	2008-01-03
WO2014159151A1	2014-10-02

Foreign References:

CN102234260A	2011-11-09
CN103694230A	2014-04-02
CN102167715A	2011-08-31
US20170247356A1	2017-08-31
CN110922372A	2020-03-27
CN100534997C	2009-09-02
US7919598B2	2011-04-05
CN201014792878A
US8513202B2	2013-08-20
CN101573368A	2009-11-04

Other References:

"IDF Diabetes Atlas", INTERNATIONAL DIABETES FEDERATION

Attorney, Agent or Firm:

FAIRSKY LAW OFFICE (CN)

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