WO2026133162 - NOVEL SALT OF 5-CHLORO-2-FLUORO-4-((4-FLUORO-2-(METHYL(2-(METHYLAMINO)ETHYL)AMINO)PHENYL)AMINO)-N-(THIAZOL-4-YL)BENZENESULFONAMIDE AND PREPARATION METHOD THEREOF
National phase entry is expected:
Publication Number
WO/2026/133162
Publication Date
25.06.2026
International Application No.
PCT/IB2025/063006
International Filing Date
16.12.2025
Title **
[English]
NOVEL SALT OF 5-CHLORO-2-FLUORO-4-((4-FLUORO-2-(METHYL(2-(METHYLAMINO)ETHYL)AMINO)PHENYL)AMINO)-N-(THIAZOL-4-YL)BENZENESULFONAMIDE AND PREPARATION METHOD THEREOF
[French]
NOUVEAU SEL DE 5-CHLORO-2-FLUORO-4-((4-FLUORO-2-(MÉTHYL(2-(MÉTHYLAMINO)ÉTHYL)AMINO)PHÉNYL)AMINO)-N-(THIAZOL-4-YL)BENZÈNESULFONAMIDE ET SON PROCÉDÉ DE PRÉPARATION
Applicants **
IN THERAPEUTICS CO., LTD.
Inventors
LEE, Seung Beom
HWANG, Ye Jin
JEONG, Yoo Seong
KIM, Dong Woo
Priority Data
10-2024-0188619
17.12.2024
KR
Application details
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International Searching Authority |
MOIP
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| Recordal of a Change of the Applicant's Name/Address |
Change of Applicant's Name and Address
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| Type of Assignment |
The Standard Agent's Assignment
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| Applicant's Legal Status |
Legal Entity
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| Entry into National Phase under |
Chapter I
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| Patent Delivery |
Send the Letters Patent by Courier
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing, Examination, Granting | 2482 | |
| EPO | Filing, Examination, Granting | 17717 | |
| Japan | Filing, Examination, Granting | 2558 | |
| South Korea | Filing, Examination, Granting | 2164 | |
| USA | Filing, Examination, Granting | 8340 |
Total:
33,261
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Abstract[English]
The present disclosure provides a novel salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide and a method for preparing the same. The mesylate salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide, which may be prepared using methanesulfonic acid and, without wishing to be bound by theory, can exhibit reduced hygroscopicity and improved physicochemical stability and solubility. In some aspects, the present disclosure provides a pharmaceutical composition for preventing or treating a sodium channel blocker-related disease, comprising the mesylate salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide.[French]
La présente divulgation concerne un nouveau sel de 5-chloro-2-fluoro-4-((4-fluoro-2-(méthyl(2-(méthylamino)éthyl)amino)phényl)amino)-N-(thiazol-4-yl)benzènesulfonamide et son procédé de préparation. Le sel de mésylate de 5-chloro-2-fluoro-4-((4-fluoro-2-(méthyl(2-(méthylamino)éthyl)amino)phényl)amino)-N-(thiazol-4-yl)benzènesulfonamide, qui peut être préparé à l'aide d'acide méthanesulfonique et, sans être lié par la théorie, peut présenter une hygroscopicité réduite ainsi qu'une une stabilité physico-chimique et une solubilité améliorées. Selon certains aspects, la présente divulgation concerne une composition pharmaceutique pour prévenir ou traiter une maladie liée au bloqueur des canaux sodiques, comprenant le sel mésylate de 5-chloro-2-fluoro-4-((4-fluoro-2-(méthyl(2-(méthylamino)éthyl)amino)phényl)amino)-N-(thiazol-4-yl)benzènesulfonamide.