AU2021398051A1 - 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
AU2021398051A1
AU2021398051A1 AU2021398051A AU2021398051A AU2021398051A1 AU 2021398051 A1 AU2021398051 A1 AU 2021398051A1 AU 2021398051 A AU2021398051 A AU 2021398051A AU 2021398051 A AU2021398051 A AU 2021398051A AU 2021398051 A1 AU2021398051 A1 AU 2021398051A1
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compound
amorphous
present disclosure
crystalline form
csi
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AU2021398051A
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AU2021398051A9 (en
Inventor
Minhua Chen
Jiaming Shi
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Principia Biopharma Inc
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Principia Biopharma Inc
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Publication of AU2021398051A1 publication Critical patent/AU2021398051A1/en
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Publication of AU2021398051A9 publication Critical patent/AU2021398051A9/en
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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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Crystals, And After-Treatments Of Crystals (AREA)
  • Inorganic Compounds Of Heavy Metals (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2021398051A 2020-12-10 2021-11-22 Crystal form of tolebrutinib, preparation method therefor and use thereof Pending AU2021398051A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN202011455573.5 2020-12-10
CN202011455573 2020-12-10
PCT/CN2021/132028 WO2022121670A1 (zh) 2020-12-10 2021-11-22 Tolebrutinib的晶型及其制备方法和用途

Publications (2)

Publication Number Publication Date
AU2021398051A1 true AU2021398051A1 (en) 2023-07-27
AU2021398051A9 AU2021398051A9 (en) 2024-10-17

Family

ID=81974189

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2021398051A Pending AU2021398051A1 (en) 2020-12-10 2021-11-22 Crystal form of tolebrutinib, preparation method therefor and use thereof

Country Status (11)

Country Link
US (2) US12049463B2 (https=)
EP (1) EP4261212A4 (https=)
JP (2) JP2023553930A (https=)
KR (1) KR102872880B1 (https=)
CN (1) CN118434732A (https=)
AU (1) AU2021398051A1 (https=)
CA (1) CA3201936A1 (https=)
CO (1) CO2023008949A2 (https=)
IL (1) IL303590A (https=)
MX (1) MX2023006854A (https=)
WO (1) WO2022121670A1 (https=)

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EP4328226A4 (en) 2021-04-23 2025-08-27 Hangzhou Solipharma Co Ltd CRYSTALLINE FORM, AMORPHOUS FORM OF TOLEBRUTINIB, PREPARATION PROCESS THEREOF AND USE THEREOF
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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
WO2026050513A1 (en) 2024-08-30 2026-03-05 Principia Biopharma Inc. Tolebrutinib for multiple sclerosis

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Also Published As

Publication number Publication date
WO2022121670A1 (zh) 2022-06-16
CN118434732A (zh) 2024-08-02
US12049463B2 (en) 2024-07-30
US20220389011A1 (en) 2022-12-08
KR102872880B1 (ko) 2025-10-20
EP4261212A4 (en) 2024-11-27
JP2023553930A (ja) 2023-12-26
KR20230118154A (ko) 2023-08-10
AU2021398051A9 (en) 2024-10-17
JP2026041905A (ja) 2026-03-10
CO2023008949A2 (es) 2023-09-29
IL303590A (en) 2023-08-01
CA3201936A1 (en) 2022-06-16
MX2023006854A (es) 2023-07-20
EP4261212A1 (en) 2023-10-18
US20240391915A1 (en) 2024-11-28

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Owner name: PRINCIPIA BIOPHARMA INC.

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SREP Specification republished