WO2026040323A1 - Monododécyl sulfate d'ibrutinib, son procédé de préparation et son utilisation - Google Patents
Monododécyl sulfate d'ibrutinib, son procédé de préparation et son utilisationInfo
- Publication number
- WO2026040323A1 WO2026040323A1 PCT/CN2025/074163 CN2025074163W WO2026040323A1 WO 2026040323 A1 WO2026040323 A1 WO 2026040323A1 CN 2025074163 W CN2025074163 W CN 2025074163W WO 2026040323 A1 WO2026040323 A1 WO 2026040323A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- ibrutinib
- sulfate
- monolaurate
- preparation
- good solvent
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
- C07C303/42—Separation; Purification; Stabilisation; Use of additives
- C07C303/44—Separation; Purification
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C305/00—Esters of sulfuric acids
- C07C305/02—Esters of sulfuric acids having oxygen atoms of sulfate groups bound to acyclic carbon atoms of a carbon skeleton
- C07C305/04—Esters of sulfuric acids having oxygen atoms of sulfate groups bound to acyclic carbon atoms of a carbon skeleton being acyclic and saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La présente invention concerne un composé cristallin de monododécyle sulfate d'ibrutinib, son procédé de préparation et son utilisation. La formule développée du composé cristallin est telle que représentée par la formule II. Le monododécyle sulfate d'ibrutinib est un composé cristallin ou un composé amorphe, et le composé cristallin est présent sous une forme anhydre et sans solvant. Le composé cristallin assure une bonne pharmacopotentialité de l'ibrutinib et améliore également de manière significative sa biodisponibilité pendant l'absorption orale ; de plus, le composé cristallin est également favorable à la réduction de la différence de l'effet de l'ibrutinib avant et après les repas, ce qui permet de réduire les réactions gastro-intestinales et la toxicité potentielle et les effets secondaires.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202411167700.X | 2024-08-23 | ||
| CN202411167700.XA CN121591740A (zh) | 2024-08-23 | 2024-08-23 | 一种依鲁替尼单月桂醇硫酸盐、制备方法、应用 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2026040323A1 true WO2026040323A1 (fr) | 2026-02-26 |
Family
ID=98864281
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/CN2025/074163 Pending WO2026040323A1 (fr) | 2024-08-23 | 2025-01-23 | Monododécyl sulfate d'ibrutinib, son procédé de préparation et son utilisation |
Country Status (2)
| Country | Link |
|---|---|
| CN (1) | CN121591740A (fr) |
| WO (1) | WO2026040323A1 (fr) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013184572A1 (fr) * | 2012-06-04 | 2013-12-12 | Pharmacyclics, Inc. | Formes cristallines d'un inhibiteur de tyrosine kinase de bruton |
| CN112423757A (zh) * | 2018-06-15 | 2021-02-26 | 汉达生技医药责任有限公司 | 激酶抑制剂的盐类及其组合物 |
-
2024
- 2024-08-23 CN CN202411167700.XA patent/CN121591740A/zh active Pending
-
2025
- 2025-01-23 WO PCT/CN2025/074163 patent/WO2026040323A1/fr active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013184572A1 (fr) * | 2012-06-04 | 2013-12-12 | Pharmacyclics, Inc. | Formes cristallines d'un inhibiteur de tyrosine kinase de bruton |
| CN112423757A (zh) * | 2018-06-15 | 2021-02-26 | 汉达生技医药责任有限公司 | 激酶抑制剂的盐类及其组合物 |
Also Published As
| Publication number | Publication date |
|---|---|
| CN121591740A (zh) | 2026-03-03 |
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| Date | Code | Title | Description |
|---|---|---|---|
| 121 | Ep: the epo has been informed by wipo that ep was designated in this application |
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