TWI883107B - 用於復發型多發性硬化症的治療性酪胺酸激酶抑制劑 - Google Patents
用於復發型多發性硬化症的治療性酪胺酸激酶抑制劑 Download PDFInfo
- Publication number
- TWI883107B TWI883107B TW110101887A TW110101887A TWI883107B TW I883107 B TWI883107 B TW I883107B TW 110101887 A TW110101887 A TW 110101887A TW 110101887 A TW110101887 A TW 110101887A TW I883107 B TWI883107 B TW I883107B
- Authority
- TW
- Taiwan
- Prior art keywords
- btk inhibitor
- pyridin
- phenoxyphenyl
- imidazo
- acryloylpiperidin
- Prior art date
Links
Classifications
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202062963238P | 2020-01-20 | 2020-01-20 | |
| US62/963,238 | 2020-01-20 | ||
| US202062970502P | 2020-02-05 | 2020-02-05 | |
| US62/970,502 | 2020-02-05 | ||
| US202063013895P | 2020-04-22 | 2020-04-22 | |
| US63/013,895 | 2020-04-22 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202140002A TW202140002A (zh) | 2021-11-01 |
| TWI883107B true TWI883107B (zh) | 2025-05-11 |
Family
ID=74626161
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW110101887A TWI883107B (zh) | 2020-01-20 | 2021-01-19 | 用於復發型多發性硬化症的治療性酪胺酸激酶抑制劑 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US11969418B2 (https=) |
| EP (1) | EP4093397A1 (https=) |
| JP (2) | JP2023510604A (https=) |
| KR (1) | KR20220130179A (https=) |
| CN (1) | CN115348862A (https=) |
| AU (1) | AU2021209608A1 (https=) |
| BR (1) | BR112022014058A2 (https=) |
| CA (1) | CA3168146A1 (https=) |
| IL (1) | IL294560A (https=) |
| MX (1) | MX2022008875A (https=) |
| TW (1) | TWI883107B (https=) |
| WO (1) | WO2021150476A1 (https=) |
Families Citing this family (11)
| 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 |
| 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 |
| 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 |
| CA3260159A1 (en) * | 2022-06-30 | 2024-01-04 | Principia Biopharma Inc. | Therapeutic Tyrosine Kinase Inhibitors for the Treatment of Multiple Sclerosis and Myasthenia Gravis |
| EP4601647A1 (en) * | 2022-10-11 | 2025-08-20 | Principia Biopharma Inc. | Therapeutic tyrosine kinase inhibitors for multiple sclerosis |
| 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 |
| JP2026505764A (ja) | 2023-02-01 | 2026-02-18 | プリンシピア バイオファーマ インコーポレイテッド | 多発性硬化症を診断及び治療する方法 |
| WO2025264860A2 (en) | 2024-06-18 | 2025-12-26 | Yale University | Methods of treating post-covid airway disease |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2809918A (en) | 1955-10-17 | 1957-10-15 | Victor M Hermelin | Sustained release pharmaceutical preparations |
| DE2010416B2 (de) | 1970-03-05 | 1979-03-29 | Hoechst Ag, 6000 Frankfurt | Oral anwendbare Arzneiform mit Retardwirkung |
| US3760984A (en) | 1971-09-29 | 1973-09-25 | Alza Corp | Osmotically powered agent dispensing device with filling means |
| US4107288A (en) | 1974-09-18 | 1978-08-15 | Pharmaceutical Society Of Victoria | Injectable compositions, nanoparticles useful therein, and process of manufacturing same |
| US3952741A (en) | 1975-01-09 | 1976-04-27 | Bend Research Inc. | Controlled release delivery system by an osmotic bursting mechanism |
| US4728512A (en) | 1985-05-06 | 1988-03-01 | American Home Products Corporation | Formulations providing three distinct releases |
| US4794001A (en) | 1986-03-04 | 1988-12-27 | American Home Products Corporation | Formulations providing three distinct releases |
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| 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 |
| 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 |
| PL2710005T3 (pl) | 2011-05-17 | 2017-07-31 | Principia Biopharma Inc. | Inhibitory kinazy tyrozynowej |
| 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 |
| 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 |
| US10253023B2 (en) | 2014-10-06 | 2019-04-09 | Merck Patent Gmbh | Heteroaryl compounds as BTK inhibitors and uses thereof |
| 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 |
| BR112022014058A2 (pt) | 2020-01-20 | 2022-09-13 | Genzyme Corp | Inibidores terapêuticos de tirosina cinase para esclerose múltipla recidivante (rms) |
| 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 |
| EP4328226A4 (en) | 2021-04-23 | 2025-08-27 | Hangzhou Solipharma Co Ltd | CRYSTALLINE FORM, AMORPHOUS FORM OF TOLEBRUTINIB, PREPARATION PROCESS THEREOF AND USE THEREOF |
-
2021
- 2021-01-19 BR BR112022014058A patent/BR112022014058A2/pt unknown
- 2021-01-19 CN CN202180009557.XA patent/CN115348862A/zh active Pending
- 2021-01-19 US US17/151,954 patent/US11969418B2/en active Active
- 2021-01-19 EP EP21705735.5A patent/EP4093397A1/en active Pending
- 2021-01-19 IL IL294560A patent/IL294560A/en unknown
- 2021-01-19 KR KR1020227028409A patent/KR20220130179A/ko active Pending
- 2021-01-19 MX MX2022008875A patent/MX2022008875A/es unknown
- 2021-01-19 TW TW110101887A patent/TWI883107B/zh active
- 2021-01-19 AU AU2021209608A patent/AU2021209608A1/en active Pending
- 2021-01-19 WO PCT/US2021/013883 patent/WO2021150476A1/en not_active Ceased
- 2021-01-19 CA CA3168146A patent/CA3168146A1/en active Pending
- 2021-01-19 JP JP2022543411A patent/JP2023510604A/ja active Pending
-
2024
- 2024-03-22 US US18/613,641 patent/US20240366585A1/en active Pending
-
2025
- 2025-09-19 JP JP2025155610A patent/JP2026001038A/ja active Pending
Non-Patent Citations (1)
| Title |
|---|
| 網路文獻 Principia Biopharma Inc Principia Biopharma Presents Phase 1 Clinical Data from CNS Penetrating BTK Inhibitor Candidate PRN2246/SAR442168 at ACTRIMS 2019 2019/03/01 https://www.nasdaq.com/press-release/principia-biopharma-presents-phase-1-clinical-data-cns-penetrating-btk-inhibitor |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2021150476A1 (en) | 2021-07-29 |
| TW202140002A (zh) | 2021-11-01 |
| EP4093397A1 (en) | 2022-11-30 |
| MX2022008875A (es) | 2022-08-11 |
| CA3168146A1 (en) | 2021-07-29 |
| US20240366585A1 (en) | 2024-11-07 |
| US20210244720A1 (en) | 2021-08-12 |
| CN115348862A (zh) | 2022-11-15 |
| US11969418B2 (en) | 2024-04-30 |
| JP2023510604A (ja) | 2023-03-14 |
| KR20220130179A (ko) | 2022-09-26 |
| BR112022014058A2 (pt) | 2022-09-13 |
| IL294560A (en) | 2022-09-01 |
| AU2021209608A1 (en) | 2022-09-15 |
| JP2026001038A (ja) | 2026-01-06 |
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