CO2024000054A2 - Forma cristalina de tolebrutinib y método de preparación y su uso - Google Patents
Forma cristalina de tolebrutinib y método de preparación y su usoInfo
- Publication number
- CO2024000054A2 CO2024000054A2 CONC2024/0000054A CO2024000054A CO2024000054A2 CO 2024000054 A2 CO2024000054 A2 CO 2024000054A2 CO 2024000054 A CO2024000054 A CO 2024000054A CO 2024000054 A2 CO2024000054 A2 CO 2024000054A2
- Authority
- CO
- Colombia
- Prior art keywords
- crystalline form
- tolebrutinib
- preparation
- drug
- btk
- Prior art date
Links
- KOEUOFPEZFUWRF-LJQANCHMSA-N 4-amino-3-(4-phenoxyphenyl)-1-[(3R)-1-prop-2-enoylpiperidin-3-yl]imidazo[4,5-c]pyridin-2-one Chemical compound C(C=C)(=O)N1C[C@@H](CCC1)N1C(N(C=2C(=NC=CC=21)N)C1=CC=C(C=C1)OC1=CC=CC=C1)=O KOEUOFPEZFUWRF-LJQANCHMSA-N 0.000 title abstract 3
- 238000002360 preparation method Methods 0.000 title abstract 3
- 229940073613 tolebrutinib Drugs 0.000 title abstract 3
- 239000003814 drug Substances 0.000 abstract 3
- 229940079593 drug Drugs 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 201000006417 multiple sclerosis Diseases 0.000 abstract 1
- 238000005457 optimization Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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)
- 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)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202110652005 | 2021-06-11 | ||
| CN202110690510 | 2021-06-22 | ||
| 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 |
|---|---|
| CO2024000054A2 true CO2024000054A2 (es) | 2024-02-05 |
Family
ID=84425691
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2024/0000054A CO2024000054A2 (es) | 2021-06-11 | 2024-01-04 | Forma cristalina de tolebrutinib y método de preparación y su uso |
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=) |
Families Citing this family (5)
| 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 |
Family Cites Families (5)
| 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) |
-
2022
- 2022-06-02 WO PCT/CN2022/096779 patent/WO2022257845A1/zh not_active Ceased
- 2022-06-02 AU AU2022290946A patent/AU2022290946A1/en active Pending
- 2022-06-02 MX MX2023014722A patent/MX2023014722A/es unknown
- 2022-06-02 CN CN202280040545.8A patent/CN117897381A/zh active Pending
- 2022-06-02 EP EP22819443.7A patent/EP4353723A4/en active Pending
- 2022-06-02 CA CA3221129A patent/CA3221129A1/en active Pending
- 2022-06-02 BR BR112023025841A patent/BR112023025841A2/pt unknown
- 2022-06-02 JP JP2023575800A patent/JP2024521412A/ja active Pending
- 2022-06-02 IL IL309263A patent/IL309263A/en unknown
- 2022-06-02 KR KR1020247000650A patent/KR20240021217A/ko active Pending
- 2022-06-02 US US18/568,484 patent/US20250034130A1/en active Pending
-
2024
- 2024-01-04 CO CONC2024/0000054A patent/CO2024000054A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP4353723A4 (en) | 2025-06-25 |
| BR112023025841A2 (pt) | 2024-03-05 |
| EP4353723A1 (en) | 2024-04-17 |
| 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 |
| JP2024521412A (ja) | 2024-05-31 |
| IL309263A (en) | 2024-02-01 |
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