WO2025124488 - CRYSTAL FORMS OF COMPOUND HAVING FUSED FIVE- AND SIX-MEMBERED RINGS, PREPARATION METHOD THEREFOR, AND USE THEREOF
National phase entry:
Publication Number
WO/2025/124488
Publication Date
19.06.2025
International Application No.
PCT/CN2024/138851
International Filing Date
12.12.2024
Title **
[English]
CRYSTAL FORMS OF COMPOUND HAVING FUSED FIVE- AND SIX-MEMBERED RINGS, PREPARATION METHOD THEREFOR, AND USE THEREOF
[French]
FORMES CRISTALLINES D'UN COMPOSÉ AYANT DES CYCLES À CINQ ET SIX CHAÎNONS FUSIONNÉS, LEUR PROCÉDÉ DE PRÉPARATION ET LEUR UTILISATION
[Chinese]
一种五元并六元化合物的晶型、其制备方法及应用
Applicants **
HANGZHOU POLYMED BIOPHARMACEUTICALS, INC.
Inventors
XIANG, Jason Shaoyun
WU, Lei
Priority Data
202311712765.3
13.12.2023
CN
202411656766.5
18.11.2024
CN
Application details
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International Searching Authority |
CNIPA
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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 | 1880 | |
| EPO | Filing, Examination, Granting | 12561 | |
| Japan | Filing, Examination, Granting | 2025 | |
| South Korea | Filing, Examination, Granting | 1815 | |
| USA | Filing, Examination, Granting | 4740 |

Total:
23,021
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Abstract[English]
Provided are crystal forms of a compound having fused five- and six-membered rings, a preparation method therefor, and the use thereof. Particularly provided are a crystal form A, a crystal form B, a crystal form C, a crystal form D, a crystal form F, a crystal form G, a crystal form H, a crystal form I or a crystal form J of said compound represented by formula X. The X-ray powder diffraction pattern of the crystal form A using Cu-Kα radiation and represented by 2θ has diffraction peaks at 6.9±0.2°, 11.2±0.2°, 12.2±0.2°, 13.7±0.2°, 17.3±0.2°, 18.2±0.2° and 24.3±0.2°. The crystal forms of said compound have IRAK4 inhibition or/and degradation effects, have potential value in clinical application, and are expected to be capable of improving the prognosis of patients and reducing the possibility of drug resistance; in addition, said crystal forms have good solubility, physical and chemical stability and mechanical stability.[French]
L'invention concerne des formes cristallines d'un composé ayant des cycles à cinq et six chaînons fusionnés, leur procédé de préparation et leur utilisation. L'invention concerne en particulier une forme cristalline A, une forme cristalline B, une forme cristalline C, une forme cristalline D, une forme cristalline F, une forme cristalline G, une forme cristalline H, une forme cristalline I ou une forme cristalline J dudit composé représenté par la formule X. Le motif de diffraction de rayons X sur poudre de la forme cristalline A utilisant un rayonnement Cu-Kα et représenté par 2θ présente des pics de diffraction à 6,9 ± 0,2 °, 11,2 ± 0,2 °, 12,2 ± 0,2 °, 13,7 ± 0,2 °, 17,3 ± 0,2 °, 18,2 ± 0,2 ° et 24,3 ± 0,2 °. Les formes cristallines dudit composé ont des effets d'inhibition et/ou de dégradation de IRAK4, ont une valeur potentielle dans l'application clinique, et sont censées être capables d'améliorer le pronostic de patients et de réduire la possibilité de résistance aux médicaments ; en outre, lesdites formes cristallines présentent une bonne solubilité, une bonne stabilité physique et chimique et une stabilité mécanique.[Chinese]
提供一种五元并六元化合物的晶型、其制备方法及应用,具体提供一种如式X所示的五元并六元化合物的晶型A、晶型B、晶型C、晶型D、晶型F、晶型G、晶型H、晶型I或晶型J。所述的晶型A使用Cu-Kα辐射、以2θ角表示的X-射线粉末衍射图在6.9±0.2°,11.2±0.2°,12.2±0.2°,13.7±0.2°,17.3±0.2°,18.2±0.2°和24.3±0.2°处有衍射峰,所提供的五元并六元化合物的晶型对IRAK4具有抑制或/和降解效果,具有潜在的临床应用价值,预期可提高患者预后并降低耐药可能性,且具有较好的溶解度、物理化学稳定性和机械稳定性。