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
-
- 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
- A61K31/4353—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
- 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
- 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
-
- 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)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente invención se refiere a una nueva forma cristalina de tolebrutinib (en lo sucesivo denominada "compuesto I"), un método para su preparación, una composición farmacéutica que contiene la forma cristalina y el uso de la misma en la preparación de un fármaco inhibidor de BTK y un fármaco para el tratamiento de la esclerosis múltiple. La forma cristalina de tolebrutinib proporcionada tiene una o más propiedades mejoradas en comparación con la técnica anterior y tiene gran valor para la optimización y el desarrollo de fármacos en el futuro.
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 (9)
| Country | Link |
|---|---|
| EP (1) | EP4353723A1 (es) |
| KR (1) | KR20240021217A (es) |
| CN (1) | CN117897381A (es) |
| AU (1) | AU2022290946A1 (es) |
| BR (1) | BR112023025841A2 (es) |
| CA (1) | CA3221129A1 (es) |
| CO (1) | CO2024000054A2 (es) |
| IL (1) | IL309263A (es) |
| WO (1) | WO2022257845A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023122072A1 (en) * | 2021-12-21 | 2023-06-29 | Genzyme Corporation | 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 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106459049B (zh) | 2015-06-03 | 2020-11-27 | 普林斯匹亚生物制药公司 | 酪氨酸激酶抑制剂 |
| 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 |
| WO2021150476A1 (en) * | 2020-01-20 | 2021-07-29 | Genzyme Corporation | Therapeutic tyrosine kinase inhibitors for relapsing multiple sclerosis (rms) |
-
2022
- 2022-06-02 IL IL309263A patent/IL309263A/en unknown
- 2022-06-02 CA CA3221129A patent/CA3221129A1/en active Pending
- 2022-06-02 AU AU2022290946A patent/AU2022290946A1/en active Pending
- 2022-06-02 CN CN202280040545.8A patent/CN117897381A/zh active Pending
- 2022-06-02 WO PCT/CN2022/096779 patent/WO2022257845A1/zh active Application Filing
- 2022-06-02 EP EP22819443.7A patent/EP4353723A1/en active Pending
- 2022-06-02 BR BR112023025841A patent/BR112023025841A2/pt unknown
- 2022-06-02 KR KR1020247000650A patent/KR20240021217A/ko unknown
-
2024
- 2024-01-04 CO CONC2024/0000054A patent/CO2024000054A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP4353723A1 (en) | 2024-04-17 |
| KR20240021217A (ko) | 2024-02-16 |
| CA3221129A1 (en) | 2022-12-15 |
| BR112023025841A2 (pt) | 2024-03-05 |
| WO2022257845A1 (zh) | 2022-12-15 |
| IL309263A (en) | 2024-02-01 |
| AU2022290946A1 (en) | 2024-01-25 |
| CN117897381A (zh) | 2024-04-16 |
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