WO2026021410 - CRYSTAL FORMS OF AROMATIC FUSED-RING NAV1.8 INHIBITOR AND SALT THEREOF, PHARMACEUTICAL COMPOSITION, AND USE
National phase entry is expected:
Publication Number
WO/2026/021410
Publication Date
29.01.2026
International Application No.
PCT/CN2025/109732
International Filing Date
22.07.2025
Title **
[English]
CRYSTAL FORMS OF AROMATIC FUSED-RING NAV1.8 INHIBITOR AND SALT THEREOF, PHARMACEUTICAL COMPOSITION, AND USE
[French]
FORMES CRISTALLINES D'UN INHIBITEUR DE NAV1.8 À CYCLE CONDENSÉ AROMATIQUE ET SEL DE CELUI-CI, COMPOSITION PHARMACEUTIQUE ET UTILISATION
[Chinese]
一种芳香并环类NAV1.8抑制剂及其盐的晶型、药物组合物和用途
Applicants **
CHENGDU KANGHONG PHARMACEUTICAL CO LTD
Inventors
KE, Xiao
ZENG, Xueyao
ZENG, Xia
WU, Zhuan
XIONG, Xinnuo
YAN, Jun
LIU, Ting
Priority Data
202410991336.2
23.07.2024
CN
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International Searching Authority |
CNIPA
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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 | 1877 | |
| EPO | Filing, Examination, Granting | 12958 | |
| Japan | Filing, Examination, Granting | 2216 | |
| South Korea | Filing, Examination, Granting | 2270 | |
| USA | Filing, Examination, Granting | 7740 |
Total:
27,061
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Abstract[English]
The present invention relates to the field of pharmaceutical crystal forms, and specifically relates to crystal forms of 2-(4,4-difluoroazepin-1-yl)-N-(2-sulfamoylpyridin-4-yl)quinoline-3-carboxamide and a salt thereof, a pharmaceutical composition, and a use. The crystal forms of a compound of formula (I) and a salt thereof which are obtained in the present invention have excellent physical stability and chemical stability, and compared with free base crystal form K1 of the compound of formula (I), have significantly improved solubility, hygroscopicity and bioavailability, and are more conducive to clinical applications. Also disclosed in the present invention is a use of the crystal forms of the compound of formula (I) and the salt thereof as sodium ion channel Nav1.8 inhibitors for treating a wide range of pain.[French]
La présente invention relève du domaine des formes cristallines pharmaceutiques, et concerne en particulier des formes cristallines de 2-(4,4-difluoroazépin-1-yl)-N-(2-sulfamoylpyridin-4-yl)quinoléine-3-carboxamide et un sel de celui-ci, une composition pharmaceutique et une utilisation. Les formes cristallines d'un composé de formule (I) et un sel de celui-ci qui sont obtenues selon la présente invention présentent une excellente stabilité physique et une excellente stabilité chimique, et par comparaison avec la forme cristalline de base libre K1 du composé de formule (I), ont une solubilité, une hygroscopicité et une biodisponibilité significativement améliorées, et sont plus favorables à des applications cliniques. La présente invention concerne également l'utilisation des formes cristallines du composé de formule (I) et du sel de celui-ci en tant qu'inhibiteurs de Nav1.8 à canal ionique sodique pour le traitement d'une large gamme de douleurs.[Chinese]
本发明涉及药物晶型领域，具体涉及2-(4,4-二氟氮杂䓬-1-基)-N-(2-氨磺酰基吡啶-4-基)喹啉-3-甲酰胺及其盐的晶型，药物组合物和用途。本发明所得的式(I)化合物及其盐的晶型具备优良的物理稳定性和化学稳定性，相较于式(I)化合物的游离碱晶型K1，具有明显改善的溶解性、引湿性及显著提升的生物利用度，更利于临床应用。本发明还公开式(I)化合物及其盐的晶型作为钠离子通道Nav1.8的抑制剂的作用，用于治疗广泛疼痛。