AU2022290946A1 - 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
AU2022290946A1
AU2022290946A1 AU2022290946A AU2022290946A AU2022290946A1 AU 2022290946 A1 AU2022290946 A1 AU 2022290946A1 AU 2022290946 A AU2022290946 A AU 2022290946A AU 2022290946 A AU2022290946 A AU 2022290946A AU 2022290946 A1 AU2022290946 A1 AU 2022290946A1
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Prior art keywords
crystalline form
compound
ray powder
diffraction pattern
powder diffraction
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Pending
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AU2022290946A
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English (en)
Inventor
Minhua Chen
Jiaming Shi
Jing Zhang
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Principia Biopharma Inc
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Principia Biopharma Inc
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Publication of AU2022290946A1 publication Critical patent/AU2022290946A1/en
Assigned to PRINCIPIA BIOPHARMA INC. reassignment PRINCIPIA BIOPHARMA INC. Request for Assignment Assignors: GENZYME CORPORATION
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

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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)
AU2022290946A 2021-06-11 2022-06-02 Crystal form of tolebrutinib, preparation method therefor and use thereof Pending AU2022290946A1 (en)

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

Publications (1)

Publication Number Publication Date
AU2022290946A1 true AU2022290946A1 (en) 2024-01-25

Family

ID=84425691

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2022290946A Pending AU2022290946A1 (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 (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=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12049463B2 (en) 2020-12-10 2024-07-30 Genzyme Corporation Crystalline form of Tolebrutinib

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

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
UA124090C2 (uk) * 2015-06-03 2021-07-21 Прінсіпіа Байофарма Інк. Інгібітори тирозинкінази
CA2986790A1 (en) * 2015-06-26 2016-12-29 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
BR112022014058A2 (pt) * 2020-01-20 2022-09-13 Genzyme Corp Inibidores terapêuticos de tirosina cinase para esclerose múltipla recidivante (rms)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12049463B2 (en) 2020-12-10 2024-07-30 Genzyme Corporation Crystalline form of Tolebrutinib

Also Published As

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
JP2024521412A (ja) 2024-05-31
IL309263A (en) 2024-02-01

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Owner name: PRINCIPIA BIOPHARMA INC.

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