JP2024521412A - トレブルチニブの結晶形並びにその製造方法及び使用 - Google Patents

トレブルチニブの結晶形並びにその製造方法及び使用 Download PDF

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JP2024521412A
JP2024521412A JP2023575800A JP2023575800A JP2024521412A JP 2024521412 A JP2024521412 A JP 2024521412A JP 2023575800 A JP2023575800 A JP 2023575800A JP 2023575800 A JP2023575800 A JP 2023575800A JP 2024521412 A JP2024521412 A JP 2024521412A
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crystalline form
compound
powder
ray diffraction
diffraction pattern
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Japanese (ja)
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JP2024521412A5 (https=
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ミンフア・チェン
ジャミン・シー
ジン・ジャン
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Genzyme Corp
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Genzyme Corp
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Biophysics (AREA)
  • Psychiatry (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2023575800A 2021-06-11 2022-06-02 トレブルチニブの結晶形並びにその製造方法及び使用 Pending JP2024521412A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN202110652005.2 2021-06-11
CN202110652005 2021-06-11
CN202110690510.6 2021-06-22
CN202110690510 2021-06-22
CN202111326112.2 2021-11-10
CN202111326112 2021-11-10
PCT/CN2022/096779 WO2022257845A1 (zh) 2021-06-11 2022-06-02 Tolebrutinib的晶型及其制备方法和用途

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JP2024521412A true JP2024521412A (ja) 2024-05-31
JP2024521412A5 JP2024521412A5 (https=) 2025-06-10

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JP2023575800A Pending JP2024521412A (ja) 2021-06-11 2022-06-02 トレブルチニブの結晶形並びにその製造方法及び使用

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Country Link
US (1) US20250034130A1 (https=)
EP (1) EP4353723A4 (https=)
JP (1) JP2024521412A (https=)
KR (1) KR20240021217A (https=)
CN (1) CN117897381A (https=)
AU (1) AU2022290946A1 (https=)
BR (1) BR112023025841A2 (https=)
CA (1) CA3221129A1 (https=)
CO (1) CO2024000054A2 (https=)
IL (1) IL309263A (https=)
MX (1) MX2023014722A (https=)
WO (1) WO2022257845A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2021398051A1 (en) 2020-12-10 2023-07-27 Principia Biopharma Inc. Crystal form of tolebrutinib, preparation method therefor and use thereof
US20250145618A1 (en) * 2021-12-21 2025-05-08 Principia Biopharma Inc. Crystalline Forms of (R)-1-(1-Acryloylpiperidin-3-YL)-4-Amino-3-(4-Phenoxyphenyl)-1H-Imidazo[4,5-C]Pyridin-2(3H)-One and salts Thereof
WO2023172663A1 (en) 2022-03-09 2023-09-14 Teva Pharmaceuticals International Gmbh Solid state forms of tolebrutinib and of tolebrutinib salts
AU2023408758A1 (en) * 2022-12-20 2025-07-31 Principia Biopharma Inc. Drug formulations of (r)-1-(1-acryloylpiperidin-3-yl)-4-amino-3-(4- phenoxyphenyl)-1h-imidazo[4,5-c]pyridin-2(3h)-one
WO2026050513A1 (en) 2024-08-30 2026-03-05 Principia Biopharma Inc. Tolebrutinib for multiple sclerosis

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004101551A1 (ja) * 2003-05-14 2004-11-25 Teijin Pharma Limited ベンズイミダゾール誘導体の結晶及びその製造方法
CN105753863A (zh) * 2015-09-11 2016-07-13 东莞市真兴贝特医药技术有限公司 氧代二氢咪唑并吡啶类化合物及其应用
WO2016196840A1 (en) * 2015-06-03 2016-12-08 Principia Biopharma Inc. Tyrosine kinase inhibitors
JP2018518494A (ja) * 2015-06-26 2018-07-12 アクイノックス ファーマシューティカルズ （カナダ） インコーポレイテッド （１Ｓ，３Ｓ，４Ｒ）−４−（（３ａＳ，４Ｒ，５Ｓ，７ａＳ）−４−（アミノメチル）−７ａ−メチル−１−メチレンオクタヒドロ−１Ｈ−インデン−５−イル）−３−（ヒドロキシメチル）−４−メチルシクロヘキサノールの酢酸塩の結晶固体形態

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112022014058A2 (pt) * 2020-01-20 2022-09-13 Genzyme Corp Inibidores terapêuticos de tirosina cinase para esclerose múltipla recidivante (rms)

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004101551A1 (ja) * 2003-05-14 2004-11-25 Teijin Pharma Limited ベンズイミダゾール誘導体の結晶及びその製造方法
WO2016196840A1 (en) * 2015-06-03 2016-12-08 Principia Biopharma Inc. Tyrosine kinase inhibitors
JP2018518494A (ja) * 2015-06-26 2018-07-12 アクイノックス ファーマシューティカルズ （カナダ） インコーポレイテッド （１Ｓ，３Ｓ，４Ｒ）−４−（（３ａＳ，４Ｒ，５Ｓ，７ａＳ）−４−（アミノメチル）−７ａ−メチル−１−メチレンオクタヒドロ−１Ｈ−インデン−５−イル）−３−（ヒドロキシメチル）−４−メチルシクロヘキサノールの酢酸塩の結晶固体形態
CN105753863A (zh) * 2015-09-11 2016-07-13 东莞市真兴贝特医药技术有限公司 氧代二氢咪唑并吡啶类化合物及其应用

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
ASIAN JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 9, JPN6026014912, 2014, pages 163 - 175, ISSN: 0005839198 *
JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 90, no. 11, JPN6026014913, 2001, pages 1878 - 1890, ISSN: 0005839199 *
ORG. PROCESS RES. DEV., vol. 17, JPN6026014911, 2013, pages 457 - 471, ISSN: 0005839197 *
芦澤 一英: "塩・結晶形の最適化と結晶化技術", PHARM TECH JAPAN, vol. 18, no. 10, JPN6013060608, 2002, pages 81 - 96, ISSN: 0005839195 *
高田則幸: "創薬段階における原薬Formスクリーニングと選択", PHARM STAGE, vol. 6, no. 10, JPN6009053755, 15 January 2007 (2007-01-15), pages 20 - 25, ISSN: 0005839196 *

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Publication number Publication date
EP4353723A4 (en) 2025-06-25
BR112023025841A2 (pt) 2024-03-05
EP4353723A1 (en) 2024-04-17
CO2024000054A2 (es) 2024-02-05
WO2022257845A1 (zh) 2022-12-15
CA3221129A1 (en) 2022-12-15
US20250034130A1 (en) 2025-01-30
KR20240021217A (ko) 2024-02-16
CN117897381A (zh) 2024-04-16
MX2023014722A (es) 2024-02-13
AU2022290946A1 (en) 2024-01-25
IL309263A (en) 2024-02-01

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