WO2026017128 - CYCLOALKENE DERIVATIVE ACTING AS OREXIN RECEPTOR AGONIST, AND COMPOSITION AND USE THEREOF
National phase entry is expected:
Publication Number
WO/2026/017128
Publication Date
22.01.2026
International Application No.
PCT/CN2025/109166
International Filing Date
17.07.2025
Title **
[English]
CYCLOALKENE DERIVATIVE ACTING AS OREXIN RECEPTOR AGONIST, AND COMPOSITION AND USE THEREOF
[French]
DÉRIVÉ DE CYCLOALCÈNE AGISSANT EN TANT QU'AGONISTE DU RÉCEPTEUR DE L'OREXINE, COMPOSITION ET UTILISATION ASSOCIÉES
[Chinese]
作为食欲素受体激动剂的环烯烃衍生物及其组合物和用途
Applicants **
JIANGSU NHWA PHARMACEUTICAL CO., LTD
No.18, Yangshan Road, Economic Development Zone
Xuzhou, Jiangsu 221000, CN
Inventors
LI, Qinan
No.18, Yangshan Road, Economic Development Zone
Xuzhou, Jiangsu 221000, CN
MA, Zhen
No.18, Yangshan Road, Economic Development Zone
Xuzhou, Jiangsu 221000, CN
LI, Guoxing
No.18, Yangshan Road, Economic Development Zone
Xuzhou, Jiangsu 221000, CN
LI, Zhiming
No.18, Yangshan Road, Economic Development Zone
Xuzhou, Jiangsu 221000, CN
CAO, Shinian
No.18, Yangshan Road, Economic Development Zone
Xuzhou, Jiangsu 221000, CN
ZHANG, Xiangrui
No.18, Yangshan Road, Economic Development Zone
Xuzhou, Jiangsu 221000, CN
WANG, Wei
No.18, Yangshan Road, Economic Development Zone
Xuzhou, Jiangsu 221000, CN
ZHU, Yongchao
No.18, Yangshan Road, Economic Development Zone
Xuzhou, Jiangsu 221000, CN
XU, Xiangqing
No.18, Yangshan Road, Economic Development Zone
Xuzhou, Jiangsu 221000, CN
Priority Data
202410956321.2
17.07.2024
CN
202411920329.X
25.12.2024
CN
202510528880.8
25.04.2025
CN
Application details
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International Searching Authority |
CNIPA
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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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| Translation |
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing | 1925 | |
| EPO | Filing, Examination | 10270 | |
| Japan | Filing | 597 | |
| South Korea | Filing | 640 | |
| USA | Filing, Examination | 3160 |
Total: 16592 USD
Abstract[English]
The present invention relates to a cycloalkene derivative having an orexin 2 receptor (OX2R) agonistic activity. Specifically, the present invention relates to a compound as represented by general formula (I), a stereoisomer thereof, a tautomer thereof, a pharmaceutically acceptable salt thereof, and pharmaceutically acceptable salts of said stereoisomer and tautomer. The present invention further relates to a pharmaceutical composition containing the compound, a preparation method therefor, and the use thereof as an orexin 2 receptor (OX2R) agonist in the prevention or treatment of diseases associated with the orexin 2 receptor (OX2R) agonistic effect, such as narcolepsy, hypersomnia, sleep apnea, post-anesthesia recovery or respiratory inhibition amelioration, wherein each substituent in the general formula (I) is the same as that defined in the description.[French]
La présente invention concerne un dérivé de cycloalcène ayant une activité agoniste du récepteur de l'orexine 2 (OX2R). Plus particulièrement, la présente invention concerne un composé tel que représenté par la formule générale (I), un stéréoisomère, un tautomère, un sel pharmaceutiquement acceptable de celui-ci, et des sels pharmaceutiquement acceptables dudit stéréoisomère et tautomère. La présente invention concerne en outre une composition pharmaceutique contenant le composé, son procédé de préparation et son utilisation en tant qu'agoniste du récepteur de l'orexine 2 (OX2R) dans la prévention ou le traitement de maladies associées à l'effet agoniste du récepteur de l'orexine 2 (OX2R), telles que la narcolepsie, l'hypersomnie, l'apnée du sommeil, la récupération après anesthésie ou l'amélioration de l'inhibition respiratoire, chaque substituant dans la formule générale (I) étant le même que celui défini dans la description.[Chinese]
本发明涉及一种具有食欲素受体2(OX2R)激动活性的环烯烃衍生物。特别地，本发明涉及通式(I)所示的化合物、其立体异构体、其互变异构体、其药学上可接受的盐，以及上述立体异构体和互变异构体的药学上可接受的盐。本发明还涉及含有该化合物的药物组合物，其制备方法，以及其作为食欲素受体2(OX2R)激动剂在预防或治疗发作性睡病、嗜睡症、睡眠呼吸暂停、麻醉恢复、或呼吸抑制改善等与食欲素受体2(OX2R)激动作用相关疾病的用途。其中，通式(I)中的各取代基与说明书中的定义相同。