WO2026138869 - RIPK1 INHIBITOR AND USE THEREOF
National phase entry is expected:
Publication Number
WO/2026/138869
Publication Date
02.07.2026
International Application No.
PCT/CN2025/145091
International Filing Date
24.12.2025
Title **
[English]
RIPK1 INHIBITOR AND USE THEREOF
[French]
INHIBITEUR DE RIPK1 ET SON UTILISATION
[Chinese]
RIPK1抑制剂及其用途
Applicants **
TIANJIN TIANYAO PHARMACEUTICALS CO., LTD
Inventors
WANG, Wenzhi
SUN, Shuangyong
LU, Juan
YUAN, Yi
ZHAO, Xinying
WANG, Mengmeng
LIU, Ting
LI, Mingxin
ZHANG, Jie
LIU, Dengke
Priority Data
202411929843.X
26.12.2024
CN
Application details
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International Searching Authority |
CNIPA
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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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| 译文 |
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing, Examination, Granting | 1755 | |
| EPO | Filing, Examination, Granting | 12238 | |
| Japan | Filing, Examination, Granting | 2057 | |
| South Korea | Filing, Examination, Granting | 1851 | |
| USA | Filing, Examination, Granting | 5340 |
Total:
23,241
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Abstract[English]
The present invention belongs to the technical field of medicinal chemistry, and specifically relates to an RIPK1 inhibitor and the use thereof. Specifically provided are compounds represented by formula (I), formula (II), formula (III) or formula (IV), isomers thereof and pharmaceutically acceptable salts thereof. The RIPK1 inhibitor provided by the present invention has good in vitro activity, can significantly increase the survival rate of mice in an LPS-induced sepsis model, can significantly increase the body temperature of mice in an LPS-induced inflammation model, and reduce the level of TNF-αin plasma. In addition, the compounds provided by the present invention have good pharmacokinetic properties.[French]
La présente invention relève du domaine technique de la chimie médicale, et concerne en particulier un inhibiteur de RIPK1 et son utilisation. L'invention concerne en particulier des composés représentés par la formule (I), la formule (II), la formule (III) ou la formule (IV), des isomères de ceux-ci et des sels pharmaceutiquement acceptables de ceux-ci. L'inhibiteur de RIPK1 fourni par la présente invention a une bonne activité in vitro, peut augmenter significativement le taux de survie de souris dans un modèle de septicémie induite par LPS, peut augmenter significativement la température corporelle de souris dans un modèle d'inflammation induit par LPS, et réduire le niveau de plasma de TNF-αin. De plus, les composés selon la présente invention présentent de bonnes propriétés pharmacocinétiques.[Chinese]
本发明属于药物化学技术领域，具体涉及一种RIPK1抑制剂及用途，具有式(I)、式(II)、式(III)或式(IV)所示的化合物、其异构体以及药学上可接受的盐。本发明提供的RIPK1抑制剂，具有良好的体外活性，在LPS诱导的脓毒血症模型中能显著提高小鼠存活率，并且在LPS诱导的炎症模型中能显著提高小鼠体温，降低血浆内的TNF-α水平。此外，本发明提供的化合物具有良好的药代动力学性质。