TWI887405B - 製備激酶抑制劑之方法 - Google Patents

製備激酶抑制劑之方法 Download PDF

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Publication number
TWI887405B
TWI887405B TW110115786A TW110115786A TWI887405B TW I887405 B TWI887405 B TW I887405B TW 110115786 A TW110115786 A TW 110115786A TW 110115786 A TW110115786 A TW 110115786A TW I887405 B TWI887405 B TW I887405B
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TW
Taiwan
Prior art keywords
compound
solvent
formula
group
reaction mixture
Prior art date
Application number
TW110115786A
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English (en)
Chinese (zh)
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TW202208335A (zh
Inventor
菲倫爾 德摩林
卡利德 沙赫
莎格 薩卡
王勇
許維
Original Assignee
美商艾克塞里克斯公司
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Publication of TW202208335A publication Critical patent/TW202208335A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/20Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B43/00Formation or introduction of functional groups containing nitrogen
    • C07B43/06Formation or introduction of functional groups containing nitrogen of amide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines

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  • 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)
TW110115786A 2020-04-30 2021-04-30 製備激酶抑制劑之方法 TWI887405B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202063017739P 2020-04-30 2020-04-30
US63/017,739 2020-04-30

Publications (2)

Publication Number Publication Date
TW202208335A TW202208335A (zh) 2022-03-01
TWI887405B true TWI887405B (zh) 2025-06-21

Family

ID=76076455

Family Applications (1)

Application Number Title Priority Date Filing Date
TW110115786A TWI887405B (zh) 2020-04-30 2021-04-30 製備激酶抑制劑之方法

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)

* Cited by examiner, † Cited by third party
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019148044A1 (en) * 2018-01-26 2019-08-01 Exelixis, Inc. Compounds for the treatment of kinase-dependent disorders

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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)
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019148044A1 (en) * 2018-01-26 2019-08-01 Exelixis, Inc. Compounds for the treatment of kinase-dependent disorders

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
CA3176042A1 (en) 2021-11-04
KR20230005190A (ko) 2023-01-09

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