KR20230005190A - 키나제억제제의 제조 공정 - Google Patents
키나제억제제의 제조 공정 Download PDFInfo
- Publication number
- KR20230005190A KR20230005190A KR1020227037607A KR20227037607A KR20230005190A KR 20230005190 A KR20230005190 A KR 20230005190A KR 1020227037607 A KR1020227037607 A KR 1020227037607A KR 20227037607 A KR20227037607 A KR 20227037607A KR 20230005190 A KR20230005190 A KR 20230005190A
- Authority
- KR
- South Korea
- Prior art keywords
- compound
- solvent
- formula
- reaction mixture
- water
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/20—Oxygen atoms
-
- 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
- A61K31/47—Quinolines; Isoquinolines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B43/00—Formation or introduction of functional groups containing nitrogen
- C07B43/06—Formation or introduction of functional groups containing nitrogen of amide groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063017739P | 2020-04-30 | 2020-04-30 | |
| US63/017,739 | 2020-04-30 | ||
| PCT/US2021/030035 WO2021222673A1 (en) | 2020-04-30 | 2021-04-30 | Processes for the preparation of a kinase inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20230005190A true KR20230005190A (ko) | 2023-01-09 |
Family
ID=76076455
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020227037607A Pending KR20230005190A (ko) | 2020-04-30 | 2021-04-30 | 키나제억제제의 제조 공정 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US12497367B2 (https=) |
| EP (1) | EP4143169B1 (https=) |
| JP (2) | JP7728795B2 (https=) |
| KR (1) | KR20230005190A (https=) |
| CN (2) | CN115461328B (https=) |
| AU (1) | AU2021263474A1 (https=) |
| BR (1) | BR112022021712A2 (https=) |
| CA (1) | CA3176042A1 (https=) |
| CL (1) | CL2022003008A1 (https=) |
| CO (1) | CO2022015205A2 (https=) |
| CR (1) | CR20220551A (https=) |
| GE (1) | GEP20267875B (https=) |
| IL (2) | IL297684B1 (https=) |
| MX (1) | MX2022013528A (https=) |
| PE (1) | PE20230110A1 (https=) |
| PH (1) | PH12022552821A1 (https=) |
| TW (1) | TWI887405B (https=) |
| WO (1) | WO2021222673A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN117402114A (zh) * | 2018-01-26 | 2024-01-16 | 埃克塞里艾克西斯公司 | 用于治疗激酶依赖性病症的化合物 |
| TW202334090A (zh) * | 2021-11-03 | 2023-09-01 | 美商艾克塞里克斯公司 | 用於治療激酶依賴性病症之化合物 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1154105A (zh) * | 1994-06-08 | 1997-07-09 | H·隆德贝克有限公司 | 4-芳基-1-(二氢化茚甲基、二氢苯并呋喃甲基或二氢苯并噻吩甲基)哌啶、-四氢吡啶或哌嗪类化合物 |
| ZA954689B (en) | 1994-06-08 | 1996-01-29 | Lundbeck & Co As H | 4-Aryl-1-(indanmethyl dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl) piperidines tetrahydropyridines or piperazines |
| CN101466672B (zh) * | 2006-06-12 | 2012-05-16 | 诺瓦提斯公司 | N-羟基-3-[4-[[[2-(2-甲基-1h-吲哚-3-基)乙基]氨基]甲基]苯基]-2e-2-丙烯酰胺的盐 |
| NZ572547A (en) | 2006-06-12 | 2011-06-30 | Novartis Ag | SALTS OF N-HYDROXY-3-[4-[[[2-(2-METHYL-1H-INDOL-3-yl)ETHYL]AMINO]METHYL]PHENYL]-2E-2-PROPENAMIDE |
| JP5486606B2 (ja) * | 2008-11-13 | 2014-05-07 | エクセリクシス, インク. | キノリン誘導体の調製方法 |
| NZ779754A (en) * | 2009-01-16 | 2023-04-28 | Exelixis Inc | Malate salt of n-(4-{ [6,7-bis(methyloxy)quinolin-4-yl] oxy} phenyl)-n’-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms thereof for the treatment of cancer |
| EA030435B1 (ru) | 2010-07-16 | 2018-08-31 | Экселиксис, Инк. | ТАБЛЕТКА, СОДЕРЖАЩАЯ МОДУЛЯТОР c-MET В ФОРМЕ КРИСТАЛЛИЧЕСКОЙ L-МАЛАТНОЙ СОЛИ (ВАРИАНТЫ), СПОСОБ ЕЕ ПРОИЗВОДСТВА И СПОСОБ ЛЕЧЕНИЯ ОНКОЛОГИЧЕСКОГО ЗАБОЛЕВАНИЯ С ЕЕ ИСПОЛЬЗОВАНИЕМ |
| CN104395284A (zh) | 2011-10-20 | 2015-03-04 | 埃克塞里艾克西斯公司 | 制备喹啉衍生物的方法 |
| EP3174854B1 (en) | 2014-07-31 | 2022-08-24 | Exelixis, Inc. | Method of preparing fluorine-18 labeled cabozantinib and its analogs |
| CR20250117A (es) | 2018-01-26 | 2025-05-09 | Exelixis Inc | COMPUESTOS PARA EL TRATAMIENTO DE TRASTORNOS DEPENDIENTES DE CINASAS (Divisional 2020-0355) |
| CN117402114A (zh) * | 2018-01-26 | 2024-01-16 | 埃克塞里艾克西斯公司 | 用于治疗激酶依赖性病症的化合物 |
| CA3088198A1 (en) | 2018-01-26 | 2019-08-01 | Exelixis, Inc. | Compounds for the treatment of kinase-dependent disorders |
| KR102828472B1 (ko) * | 2018-12-13 | 2025-07-03 | 엑셀리시스, 인코포레이티드 | 키나아제 억제제의 결정질 형태 및 염 형태 |
| CN109761899B (zh) | 2019-02-14 | 2022-11-15 | 广州六顺生物科技股份有限公司 | 喹啉衍生物、其药学上可接受的盐或其溶剂合物、其应用、药物及药物组合物 |
-
2021
- 2021-04-30 CN CN202180031136.7A patent/CN115461328B/zh active Active
- 2021-04-30 MX MX2022013528A patent/MX2022013528A/es unknown
- 2021-04-30 KR KR1020227037607A patent/KR20230005190A/ko active Pending
- 2021-04-30 EP EP21727657.5A patent/EP4143169B1/en active Active
- 2021-04-30 CN CN202511511945.4A patent/CN121591655A/zh active Pending
- 2021-04-30 CA CA3176042A patent/CA3176042A1/en active Pending
- 2021-04-30 JP JP2022566135A patent/JP7728795B2/ja active Active
- 2021-04-30 AU AU2021263474A patent/AU2021263474A1/en active Pending
- 2021-04-30 US US17/922,208 patent/US12497367B2/en active Active
- 2021-04-30 PH PH1/2022/552821A patent/PH12022552821A1/en unknown
- 2021-04-30 CR CR20220551A patent/CR20220551A/es unknown
- 2021-04-30 PE PE2022002513A patent/PE20230110A1/es unknown
- 2021-04-30 WO PCT/US2021/030035 patent/WO2021222673A1/en not_active Ceased
- 2021-04-30 TW TW110115786A patent/TWI887405B/zh active
- 2021-04-30 GE GEAP202516101A patent/GEP20267875B/en unknown
- 2021-04-30 BR BR112022021712A patent/BR112022021712A2/pt unknown
-
2022
- 2022-10-26 IL IL297684A patent/IL297684B1/en unknown
- 2022-10-26 CO CONC2022/0015205A patent/CO2022015205A2/es unknown
- 2022-10-28 CL CL2022003008A patent/CL2022003008A1/es unknown
-
2025
- 2025-06-20 JP JP2025104881A patent/JP2025128388A/ja active Pending
- 2025-10-21 IL IL324105A patent/IL324105A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN115461328A (zh) | 2022-12-09 |
| GEP20267875B (en) | 2026-03-25 |
| EP4143169B1 (en) | 2026-04-15 |
| JP2025128388A (ja) | 2025-09-02 |
| CL2022003008A1 (es) | 2023-06-23 |
| TW202208335A (zh) | 2022-03-01 |
| MX2022013528A (es) | 2022-11-16 |
| PH12022552821A1 (en) | 2024-02-12 |
| CR20220551A (es) | 2022-12-07 |
| CN121591655A (zh) | 2026-03-03 |
| US20230192619A1 (en) | 2023-06-22 |
| IL297684B1 (en) | 2026-03-01 |
| EP4143169A1 (en) | 2023-03-08 |
| CN115461328B (zh) | 2025-11-07 |
| CO2022015205A2 (es) | 2022-10-31 |
| PE20230110A1 (es) | 2023-01-25 |
| IL297684A (en) | 2022-12-01 |
| BR112022021712A2 (pt) | 2022-12-06 |
| IL324105A (en) | 2025-12-01 |
| AU2021263474A1 (en) | 2022-11-17 |
| US12497367B2 (en) | 2025-12-16 |
| JP2023524692A (ja) | 2023-06-13 |
| WO2021222673A1 (en) | 2021-11-04 |
| JP7728795B2 (ja) | 2025-08-25 |
| TWI887405B (zh) | 2025-06-21 |
| CA3176042A1 (en) | 2021-11-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
St.27 status event code: A-0-1-A10-A15-nap-PA0105 |
|
| PG1501 | Laying open of application |
St.27 status event code: A-1-1-Q10-Q12-nap-PG1501 |
|
| A201 | Request for examination | ||
| E13-X000 | Pre-grant limitation requested |
St.27 status event code: A-2-3-E10-E13-lim-X000 |
|
| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |
|
| P13-X000 | Application amended |
St.27 status event code: A-2-2-P10-P13-nap-X000 |
|
| PA0201 | Request for examination |
St.27 status event code: A-1-2-D10-D11-exm-PA0201 |
|
| D21 | Rejection of application intended |
Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D21-EXM-PE0902 (AS PROVIDED BY THE NATIONAL OFFICE) |
|
| PE0902 | Notice of grounds for rejection |
St.27 status event code: A-1-2-D10-D21-exm-PE0902 |
|
| E13 | Pre-grant limitation requested |
Free format text: ST27 STATUS EVENT CODE: A-2-3-E10-E13-LIM-X000 (AS PROVIDED BY THE NATIONAL OFFICE) |
|
| E13-X000 | Pre-grant limitation requested |
St.27 status event code: A-2-3-E10-E13-lim-X000 |
|
| P11 | Amendment of application requested |
Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-NAP-X000 (AS PROVIDED BY THE NATIONAL OFFICE) |
|
| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |