WO2026040323A1 - Monododécyl sulfate d'ibrutinib, son procédé de préparation et son utilisation - Google Patents

Monododécyl sulfate d'ibrutinib, son procédé de préparation et son utilisation

Info

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
Application number
PCT/CN2025/074163
Other languages
English (en)
Chinese (zh)
Inventor
叶勇
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Chengdu Talent Bio Pharmaceutical Technology Co Ltd
Original Assignee
Chengdu Talent Bio Pharmaceutical Technology Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Chengdu Talent Bio Pharmaceutical Technology Co Ltd filed Critical Chengdu Talent Bio Pharmaceutical Technology Co Ltd
Publication of WO2026040323A1 publication Critical patent/WO2026040323A1/fr
Pending legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/42Separation; Purification; Stabilisation; Use of additives
    • C07C303/44Separation; Purification
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C305/00Esters of sulfuric acids
    • C07C305/02Esters of sulfuric acids having oxygen atoms of sulfate groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C305/04Esters of sulfuric acids having oxygen atoms of sulfate groups bound to acyclic carbon atoms of a carbon skeleton being acyclic and saturated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-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.
PCT/CN2025/074163 2024-08-23 2025-01-23 Monododécyl sulfate d'ibrutinib, son procédé de préparation et son utilisation Pending WO2026040323A1 (fr)

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)

* Cited by examiner, † Cited by third party
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
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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