POLYMORPHIC FORM OF NEPICASTAT ACID ADDITION SALT, PREPARATION METHOD THEREFOR AND USE THEREOF

Title:

POLYMORPHIC FORM OF NEPICASTAT ACID ADDITION SALT, PREPARATION METHOD THEREFOR AND USE THEREOF

Document Type and Number:

WIPO Patent Application WO/2024/056079

Kind Code:

A1

Abstract:

The present invention relates to a polymorphic form of a nepicastat acid addition salt, a preparation method therefor and a use thereof. The acid addition salt is selected from hydrochloride, sulfate, phosphate, mesylate, benzenesulfonate, p-toluenesulfonate, hydrobromate, maleate, tartrate, citrate, and fumarate, preferably hydrochloride. The nepicastat acid addition salt has high polymorphic form stability, high solubility, high plasma concentration, high bioavailability, and excellent pharmacological action, and therefore is suitable for pharmaceutical preparations.

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Inventors:

GUO YUSHEN (CN)
HE XIAOQING (CN)
XU MIAOHUAN (CN)
ZHOU LANPING (CN)

Application Number:

PCT/CN2023/119143

Publication Date:

March 21, 2024

Filing Date:

September 15, 2023

Export Citation:

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Assignee:

JIANGSU YAHONG MEDITECH CO LTD (CN)
ASIERIS PHARMACEUTICALS SHANGHAI CO LTD (CN)

International Classes:

C07D233/84; A61K31/417; A61P9/04; A61P9/12; A61P25/18; A61P29/00; A61P35/00; A61P37/00

Domestic Patent References:

WO2008115706A1

2008-09-25

Foreign References:

CN1151735A

1997-06-11

Attorney, Agent or Firm:

GE CHENG & CO., LTD. (CN)

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