IL303590A - Crystalline form of tolbrotinib, method of preparation and use thereof - Google Patents
Crystalline form of tolbrotinib, method of preparation and use thereofInfo
- Publication number
- IL303590A IL303590A IL303590A IL30359023A IL303590A IL 303590 A IL303590 A IL 303590A IL 303590 A IL303590 A IL 303590A IL 30359023 A IL30359023 A IL 30359023A IL 303590 A IL303590 A IL 303590A
- Authority
- IL
- Israel
- Prior art keywords
- compound
- crystalline form
- present disclosure
- ray powder
- csi
- Prior art date
Links
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
- 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
Landscapes
- 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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 (1)
| Publication Number | Publication Date |
|---|---|
| IL303590A true IL303590A (en) | 2023-08-01 |
Family
ID=81974189
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL303590A IL303590A (en) | 2020-12-10 | 2021-11-22 | Crystalline form of tolbrotinib, method of preparation 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=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112022014058A2 (pt) | 2020-01-20 | 2022-09-13 | Genzyme Corp | Inibidores terapêuticos de tirosina cinase para esclerose múltipla recidivante (rms) |
| AU2021398051A1 (en) | 2020-12-10 | 2023-07-27 | Principia Biopharma Inc. | Crystal form of tolebrutinib, preparation method therefor and use thereof |
| EP4328226A4 (en) | 2021-04-23 | 2025-08-27 | Hangzhou Solipharma Co Ltd | CRYSTALLINE FORM, AMORPHOUS FORM OF TOLEBRUTINIB, PREPARATION PROCESS THEREOF AND USE THEREOF |
| WO2023280132A1 (zh) * | 2021-07-06 | 2023-01-12 | 苏州晶云药物科技股份有限公司 | 氧代二氢咪唑并吡啶类化合物的晶型及其制备方法 |
| 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 |
Family Cites Families (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3760984A (en) | 1971-09-29 | 1973-09-25 | Alza Corp | Osmotically powered agent dispensing device with filling means |
| US3952741A (en) | 1975-01-09 | 1976-04-27 | Bend Research Inc. | Controlled release delivery system by an osmotic bursting mechanism |
| CA2465328C (en) | 2001-11-01 | 2011-06-14 | Michael Francis Gross | Piperidines |
| US20060045822A1 (en) | 2004-09-01 | 2006-03-02 | Board Of Regents, The University Of Texas System | Plasma polymerization for encapsulating particles |
| CN101056877B (zh) | 2004-09-14 | 2010-06-09 | 诺华疫苗和诊断公司 | 咪唑并喹啉化合物 |
| AU2006213746A1 (en) | 2005-02-11 | 2006-08-17 | Coley Pharmaceutical Group, Inc. | Oxime and hydroxylamine substituted imidazo(4,5-c) ring compounds and methods |
| EP2700638A1 (en) | 2006-05-31 | 2014-02-26 | The Regents Of the University of California | Purine analogs |
| DK2526933T3 (en) | 2006-09-22 | 2015-05-18 | Pharmacyclics Inc | Inhibitors of Bruton's tyrosine kinase |
| TW200911803A (en) | 2007-07-16 | 2009-03-16 | Organon Nv | 6-phenyl-1H-imidazo [4,5-c] pyridine-4-carbonitrile derivatives |
| UY32138A (es) | 2008-09-25 | 2010-04-30 | Boehringer Ingelheim Int | Amidas sustituidas del ácido 2-(2,6-dicloro-fenilamino)-6-fluoro-1-metil-1h-bencimidazol-5-carboxílico y sus sales farmacéuticamente aceptables |
| US7718662B1 (en) | 2009-10-12 | 2010-05-18 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase |
| TWI500617B (zh) | 2010-05-31 | 2015-09-21 | Ono Pharmaceutical Co | Purine ketone derivatives |
| PL2710005T3 (pl) | 2011-05-17 | 2017-07-31 | Principia Biopharma Inc. | Inhibitory kinazy tyrozynowej |
| CN103502249A (zh) | 2011-05-17 | 2014-01-08 | 普林斯匹亚生物制药公司 | 作为酪氨酸激酶抑制剂的氮杂吲哚衍生物 |
| MX354412B (es) | 2011-06-10 | 2018-03-05 | Merck Patent Gmbh | Composiciones y metodos para la produccion de compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton. |
| US9199997B2 (en) | 2011-11-29 | 2015-12-01 | Ono Pharmaceutical Co., Ltd. | Purinone derivative hydrochloride |
| US8501724B1 (en) | 2012-01-31 | 2013-08-06 | Pharmacyclics, Inc. | Purinone compounds as kinase inhibitors |
| WO2013191965A1 (en) | 2012-06-18 | 2013-12-27 | Principia Biopharma Inc. | Reversible covalent pyrrolo- or pyrazolopyrimidines useful for the treatment cancer and autoimmune diseases |
| SI2892900T1 (en) | 2012-09-10 | 2018-01-31 | Principia Biopharma Inc. | Pyrazolopyrimidine compounds as kinase inhibitors |
| CN102942567B (zh) * | 2012-11-09 | 2017-02-08 | 诸城市浩天药业有限公司 | 吡咯并喹啉醌的二钠盐结晶 |
| EA201590855A1 (ru) | 2012-11-15 | 2015-11-30 | Фармасайкликс, Инк. | Соединения пирролопиримидина как ингибиторы киназ |
| US20140142099A1 (en) | 2012-11-20 | 2014-05-22 | Principia Biopharma Inc. | Purinone Derivatives as Tyrosine Kinase Inhibitors |
| KR102196882B1 (ko) | 2012-12-20 | 2020-12-30 | 머크 샤프 앤드 돔 코포레이션 | Hdm2 억제제로서의 치환된 이미다조피리딘 |
| MX365640B (es) | 2012-12-21 | 2019-06-10 | Plexxikon Inc | Compuestos y metodos para la modulacion de quinasas y sus indicaciones. |
| WO2015132799A2 (en) | 2014-02-03 | 2015-09-11 | Cadila Healthcare Limited | Novel heterocyclic compounds |
| ES2860648T5 (es) * | 2014-02-07 | 2024-11-27 | Global Blood Therapeutics Inc | Polimorfos cristalinos de la base libre de 2-hidroxi-6-((2-(1-isopropil-1H-pirazol-5-il)piridin-3-il)metoxi)benzaldehído |
| US10253023B2 (en) | 2014-10-06 | 2019-04-09 | Merck Patent Gmbh | Heteroaryl compounds as BTK inhibitors and uses thereof |
| JP2016094368A (ja) * | 2014-11-14 | 2016-05-26 | 大日本住友製薬株式会社 | ベンズイミダゾール化合物の新規結晶、及びその製造方法 |
| WO2016086358A1 (en) | 2014-12-02 | 2016-06-09 | Merck Sharp & Dohme Corp. | Hydroxymethyl piperidine orexin receptor antagonists |
| UA124090C2 (uk) | 2015-06-03 | 2021-07-21 | Прінсіпіа Байофарма Інк. | Інгібітори тирозинкінази |
| 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 |
| EP3414234B1 (en) | 2015-10-14 | 2022-06-29 | Zibo Biopolar Changsheng Pharmaceutical Co. Ltd. | Bruton's tyrosine kinase inhibitors |
| SI3377484T1 (sl) | 2015-11-17 | 2024-02-29 | Merck Patent Gmbh | Postopki za zdravljenje multiple skleroze z uporabo pirimidinskih in piridinskih spojin z btk inhibitorno aktivnostjo |
| WO2019208805A1 (ja) | 2018-04-27 | 2019-10-31 | 小野薬品工業株式会社 | Btk阻害活性を有する化合物を有効成分として含む自己免疫疾患の予防および/または治療剤 |
| BR112022014058A2 (pt) * | 2020-01-20 | 2022-09-13 | Genzyme Corp | Inibidores terapêuticos de tirosina cinase para esclerose múltipla recidivante (rms) |
| US12448363B2 (en) | 2020-06-02 | 2025-10-21 | Vidya Therapeutics, Inc. | Kinase inhibitors |
| WO2022081512A1 (en) | 2020-10-12 | 2022-04-21 | Synubi Pharmaceuticals Llc | Compositions and methods of treatment of neuroinflammatory diseases with bruton's tyrosine kinase inhibitors |
| AU2021398051A1 (en) | 2020-12-10 | 2023-07-27 | Principia Biopharma Inc. | Crystal form of tolebrutinib, preparation method therefor and use thereof |
| US20240051955A1 (en) | 2020-12-23 | 2024-02-15 | Genzyme Corporation | 4-amino-3-(4-phenoxyphenyl)-1,3-dihydro-2h-imidazo[4,5-c]pyridin-2-one derivatives and salts thereof |
| EP4328226A4 (en) | 2021-04-23 | 2025-08-27 | Hangzhou Solipharma Co Ltd | CRYSTALLINE FORM, AMORPHOUS FORM OF TOLEBRUTINIB, PREPARATION PROCESS THEREOF AND USE THEREOF |
| CN117412749A (zh) | 2021-05-21 | 2024-01-16 | 杭州领业医药科技有限公司 | Tolebrutinib盐及其晶型、其制备方法、其药物组合物和用途 |
| WO2022257845A1 (zh) | 2021-06-11 | 2022-12-15 | 苏州科睿思制药有限公司 | Tolebrutinib的晶型及其制备方法和用途 |
| JP7564347B2 (ja) | 2021-09-03 | 2024-10-08 | ノバルティス アーゲー | 多発性硬化症を治療するためのlou064 |
| 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 |
| US20260027100A1 (en) | 2022-05-13 | 2026-01-29 | Principia Biopharma Inc. | Therapeutic tyrosine kinase inhibitors for myelin oligodendrocyte glycoprotein antibody disease (mogad) |
| CA3259743A1 (en) | 2022-06-22 | 2023-12-28 | Principia Biopharma Inc. | METHODS FOR MANUFACTURING MODIFIED BTK INHIBITORS |
| CA3260159A1 (en) | 2022-06-30 | 2024-01-04 | Principia Biopharma Inc. | Therapeutic Tyrosine Kinase Inhibitors for the Treatment of Multiple Sclerosis and Myasthenia Gravis |
-
2021
- 2021-11-22 AU AU2021398051A patent/AU2021398051A1/en active Pending
- 2021-11-22 IL IL303590A patent/IL303590A/en unknown
- 2021-11-22 MX MX2023006854A patent/MX2023006854A/es unknown
- 2021-11-22 CN CN202180083380.8A patent/CN118434732A/zh active Pending
- 2021-11-22 KR KR1020237023108A patent/KR102872880B1/ko active Active
- 2021-11-22 WO PCT/CN2021/132028 patent/WO2022121670A1/zh not_active Ceased
- 2021-11-22 CA CA3201936A patent/CA3201936A1/en active Pending
- 2021-11-22 EP EP21902377.7A patent/EP4261212A4/en active Pending
- 2021-11-22 JP JP2023535327A patent/JP2023553930A/ja active Pending
-
2022
- 2022-08-10 US US17/818,846 patent/US12049463B2/en active Active
-
2023
- 2023-07-05 CO CONC2023/0008949A patent/CO2023008949A2/es unknown
-
2024
- 2024-05-28 US US18/676,250 patent/US20240391915A1/en active Pending
-
2025
- 2025-12-05 JP JP2025234453A patent/JP2026041905A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| WO2022121670A1 (zh) | 2022-06-16 |
| CN118434732A (zh) | 2024-08-02 |
| US12049463B2 (en) | 2024-07-30 |
| AU2021398051A1 (en) | 2023-07-27 |
| 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 |
| CA3201936A1 (en) | 2022-06-16 |
| MX2023006854A (es) | 2023-07-20 |
| EP4261212A1 (en) | 2023-10-18 |
| US20240391915A1 (en) | 2024-11-28 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| IL303590A (en) | Crystalline form of tolbrotinib, method of preparation and use thereof | |
| EP4353723A1 (en) | Crystal form of tolebrutinib, preparation method therefor and use thereof | |
| AU2017373239B2 (en) | Crystalline forms of a bromodomain and extraterminal protein inhibitor drug, processes for preparation thereof, and use thereof | |
| CN110577533B (zh) | 苯甲酰氨基吡啶衍生物的盐及其在药物中的应用 | |
| EP3456722B1 (en) | Crystal forms of crisaborole in free form and preparation method and use thereof | |
| EP4180435A1 (en) | Crystal form of upadacitinib, preparation method therefor, and use thereof | |
| CN110577534A (zh) | 苯甲酰氨基吡啶衍生物的盐及其在药物中的应用 | |
| CN110577536A (zh) | 苯甲酰氨基吡啶衍生物的盐及其在药物中的应用 | |
| CN113549067A (zh) | 二氢萘啶类化合物的晶型及其用途 | |
| HK40094757A (en) | Crystal form of tolebrutinib, preparation method therefor and use thereof | |
| IL184781A (en) | CRYSTALLINE 1H-IMIDAZO[4,5-b]PYRIDIN-5-AMINE, 7-[5-[(CYCLOHEXYLMETHYLAMINO)-METHYL]-1H-INDOL-2-YL]-2-METHYL, SULFATE (1:1), TRIHYDRATE AND ITS PHARMACEUTICAL USES | |
| HK40111001A (en) | Crystal form of tolebrutinib, preparation method therefor and use thereof | |
| EP4631937A1 (en) | Crystalline form or amorphous form of oxoisoindole-5-formamide compound or salt and solvate thereof | |
| KR20260027280A (ko) | 박스드로스타트의 결정 형태, 및 이의 제조 방법 및 용도 | |
| TW202506661A (zh) | 一種酪氨酸激酶抑制劑的可藥用鹽、結晶形式及其製備方法 | |
| CN118401513A (zh) | 他伐帕敦的晶型及其制备方法和用途 | |
| KR20250144411A (ko) | 벤조 질소 헤테로 방향족 고리 유도체의 염, 결정형 및 이의 의약적 응용 | |
| HK40064722A (en) | Polymorph of cdk9 inhibitor and preparation method for polymorph and use thereof | |
| HK40025351A (en) | Crystal form of oxopicolinamide derivative and preparation method therefor |