CA3221129A1 - Crystal form of tolebrutinib, preparation method therefor and use thereof - Google Patents

Crystal form of tolebrutinib, preparation method therefor and use thereof Download PDF

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Publication number
CA3221129A1
CA3221129A1 CA3221129A CA3221129A CA3221129A1 CA 3221129 A1 CA3221129 A1 CA 3221129A1 CA 3221129 A CA3221129 A CA 3221129A CA 3221129 A CA3221129 A CA 3221129A CA 3221129 A1 CA3221129 A1 CA 3221129A1
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Canada
Prior art keywords
crystal form
compound
ray powder
preparation
crystal
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Pending
Application number
CA3221129A
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English (en)
French (fr)
Inventor
Minhua Chen
Jiaming Shi
Jing Zhang
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.)
Genzyme Corp
Original Assignee
Genzyme Corp
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Application filed by Genzyme Corp filed Critical Genzyme Corp
Publication of CA3221129A1 publication Critical patent/CA3221129A1/en
Pending legal-status Critical Current

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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

Landscapes

  • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Inorganic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CA3221129A 2021-06-11 2022-06-02 Crystal form of tolebrutinib, preparation method therefor and use thereof Pending CA3221129A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN202110652005.2 2021-06-11
CN202110652005 2021-06-11
CN202110690510 2021-06-22
CN202110690510.6 2021-06-22
CN202111326112 2021-11-10
CN202111326112.2 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

Publications (1)

Publication Number Publication Date
CA3221129A1 true CA3221129A1 (en) 2022-12-15

Family

ID=84425691

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3221129A Pending CA3221129A1 (en) 2021-06-11 2022-06-02 Crystal form of tolebrutinib, preparation method therefor and use thereof

Country Status (12)

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

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3168146A1 (en) 2020-01-20 2021-07-29 Genzyme Corporation Therapeutic tyrosine kinase inhibitors for relapsing multiple sclerosis (rms)
CA3201936A1 (en) 2020-12-10 2022-06-16 Minhua Chen Crystal form of tolebrutinib and preparation method thereof
IL303834A (en) 2020-12-23 2023-08-01 Genzyme Corp 4-amino-3-(4-phenoxyphenyl)-1,3-dihydro-2H-imidazo[4,5-C]pyridin-2-one derivatives and their salts
CA3241687A1 (en) * 2021-12-21 2023-06-29 Tim Owens 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
US20250188076A1 (en) 2022-03-09 2025-06-12 Teva Pharmaceutical International Gmbh Solid state forms of tolebrutinib and of tolebrutinib salts
US20240238267A1 (en) * 2022-12-20 2024-07-18 Genzyme Corporation 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

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CL2004001034A1 (es) * 2003-05-14 2005-03-28 Teijin Pharma Ltd Formas cristalinas de acido 4-(1-((,etilbenzotiofen-3-il)me til)benzimidazol-2-iltio)butanoico; procedimiento de preparacion de las formas cristalinas; composicion farmaceutica; y su uso para el tratamiento de enfermedades inflamatorias, alergicas, r
EP3912979B1 (en) * 2015-06-03 2026-03-25 Principia Biopharma Inc. Tyrosine kinase inhibitors
EP3313811A1 (en) * 2015-06-26 2018-05-02 Aquinox Pharmaceuticals (Canada) Inc. Crystalline solid forms of the acetate salt of (1s,3s,4r)-4-((3as,4r,5s,7as)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1h-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexanol
CN105753863B (zh) * 2015-09-11 2018-07-31 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
CA3168146A1 (en) * 2020-01-20 2021-07-29 Genzyme Corporation Therapeutic tyrosine kinase inhibitors for relapsing multiple sclerosis (rms)

Also Published As

Publication number Publication date
IL309263A (en) 2024-02-01
KR20240021217A (ko) 2024-02-16
AU2022290946A1 (en) 2024-01-25
CO2024000054A2 (es) 2024-02-05
JP2024521412A (ja) 2024-05-31
US20250034130A1 (en) 2025-01-30
WO2022257845A1 (zh) 2022-12-15
MX2023014722A (es) 2024-02-13
BR112023025841A2 (pt) 2024-03-05
CN117897381A (zh) 2024-04-16
EP4353723A1 (en) 2024-04-17
EP4353723A4 (en) 2025-06-25

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