KR102828472B1 - 키나아제 억제제의 결정질 형태 및 염 형태 - Google Patents

키나아제 억제제의 결정질 형태 및 염 형태 Download PDF

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KR102828472B1
KR102828472B1 KR1020217021734A KR20217021734A KR102828472B1 KR 102828472 B1 KR102828472 B1 KR 102828472B1 KR 1020217021734 A KR1020217021734 A KR 1020217021734A KR 20217021734 A KR20217021734 A KR 20217021734A KR 102828472 B1 KR102828472 B1 KR 102828472B1
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KR20210102381A (ko
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프레넬 데모린
칼리드 샤
사가 샤키아
페터 옹
커트니 에스. 존슨
멜라니 자넬 베빌
스테판 디 패런트
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엑셀리시스, 인코포레이티드
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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
    • C07D215/48Carbon 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020217021734A 2018-12-13 2019-12-12 키나아제 억제제의 결정질 형태 및 염 형태 Active KR102828472B1 (ko)

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KR1020257021669A KR20250103803A (ko) 2018-12-13 2019-12-12 키나아제 억제제의 결정질 형태 및 염 형태

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862779430P 2018-12-13 2018-12-13
US62/779,430 2018-12-13
US201962856469P 2019-06-03 2019-06-03
US62/856,469 2019-06-03
PCT/US2019/065972 WO2020123800A1 (en) 2018-12-13 2019-12-12 Crystalline forms and salt forms of a kinase inhibitor

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KR1020257021669A Division KR20250103803A (ko) 2018-12-13 2019-12-12 키나아제 억제제의 결정질 형태 및 염 형태

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KR20210102381A KR20210102381A (ko) 2021-08-19
KR102828472B1 true KR102828472B1 (ko) 2025-07-03

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KR1020257021669A Pending KR20250103803A (ko) 2018-12-13 2019-12-12 키나아제 억제제의 결정질 형태 및 염 형태

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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
MX2021014773A (es) * 2019-06-03 2022-01-18 Exelixis Inc Formas de sales cristalinas de un inhibidor de cinasas.
CN115461328B (zh) * 2020-04-30 2025-11-07 埃克塞里艾克西斯公司 用于制备激酶抑制剂的方法
IL300151A (en) * 2020-07-31 2023-03-01 Exelixis Inc Combinations for cancer treatment
JP2023548855A (ja) * 2020-11-05 2023-11-21 エグゼリクシス, インコーポレイテッド キナーゼ阻害剤の医薬組成物
CN112650176B (zh) * 2020-12-22 2022-08-30 天能化工有限公司 一种盐酸解析开停车工序的dcs控制方法
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
US20250368606A1 (en) 2021-12-22 2025-12-04 Exelixis, Inc. Crystalline forms and salt forms of a kinase inhibitor
CN116751161A (zh) * 2023-06-28 2023-09-15 中国人民解放军军事科学院军事医学研究院 喹啉类化合物及其制备方法、药物组合物及医药用途

Citations (3)

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WO2005030140A2 (en) 2003-09-26 2005-04-07 Exelixis, Inc. C-met modulators and methods of use
WO2018218233A1 (en) 2017-05-26 2018-11-29 Exelixis, Inc. Crystalline solid forms of salts of n-{4-[(6,7-dimethoxyquinolin-4-yl) oxy]phenyl}-n'-(4-fluorphenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use
WO2019148044A1 (en) 2018-01-26 2019-08-01 Exelixis, Inc. Compounds for the treatment of kinase-dependent disorders

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CA2604238C (en) 2005-04-15 2015-07-07 Neogenix Oncology, Inc. Recombinant monoclonal antibodies and corresponding antigens for colon and pancreatic cancers
ES2599458T3 (es) 2008-10-14 2017-02-01 Sunshine Lake Pharma Co., Ltd. Compuestos y métodos de uso
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
CN102408411B (zh) 2011-09-19 2014-10-22 北京康辰药业股份有限公司 一种含喹啉基的羟肟酸类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
BR112015007672A2 (pt) 2012-10-04 2017-08-08 Dana Farber Cancer Inst Inc anticorpos anti-pd-l1 monoclonais humanos e métodos de uso
SMT202100065T1 (it) 2013-05-02 2021-03-15 Anaptysbio Inc Anticorpi diretti contro la proteina della morte programmata (pd-1)
BR112016018450A2 (pt) 2014-02-14 2018-09-18 Exelixis Inc formas sólidas cristalinas de n-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-n'-(4-fluorofenil)ciclopropano-1,1-dicarboxamida, processos de preparo e métodos de uso
CN104817497B (zh) 2015-03-20 2017-03-08 南京众睿缘生物科技有限公司 一种炔代喹啉衍生物及其制备方法和用途
MX2021014773A (es) * 2019-06-03 2022-01-18 Exelixis Inc Formas de sales cristalinas de un inhibidor de cinasas.

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005030140A2 (en) 2003-09-26 2005-04-07 Exelixis, Inc. C-met modulators and methods of use
WO2018218233A1 (en) 2017-05-26 2018-11-29 Exelixis, Inc. Crystalline solid forms of salts of n-{4-[(6,7-dimethoxyquinolin-4-yl) oxy]phenyl}-n'-(4-fluorphenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use
WO2019148044A1 (en) 2018-01-26 2019-08-01 Exelixis, Inc. Compounds for the treatment of kinase-dependent disorders

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MD3894012T2 (ro) 2025-11-30
CN113329790A (zh) 2021-08-31
JP2022512399A (ja) 2022-02-03
EP3894012B1 (en) 2025-06-18
CA3122840A1 (en) 2020-06-18
CO2021007613A2 (es) 2021-06-21
SI3894012T1 (sl) 2025-10-30
HUE072868T2 (hu) 2025-12-28
BR112021011333A2 (pt) 2021-08-31
MA54458A (fr) 2021-10-20
EP3894012A1 (en) 2021-10-20
SMT202500346T1 (it) 2025-11-10
ES3052838T3 (en) 2026-01-15
WO2020123800A1 (en) 2020-06-18
JP7509779B2 (ja) 2024-07-02
JP7783870B2 (ja) 2025-12-10
MX2021006951A (es) 2021-07-15
PL3894012T4 (pl) 2026-01-05
HRP20251122T1 (hr) 2025-11-21
AU2025234277A1 (en) 2025-10-16
EP4631505A3 (en) 2025-12-10
IL283860B2 (en) 2025-10-01
KR20250103803A (ko) 2025-07-07
RS67216B1 (sr) 2025-10-31
PT3894012T (pt) 2025-09-25
CR20210375A (es) 2021-08-18
EP4631505A2 (en) 2025-10-15
FI3894012T3 (fi) 2025-09-18
MA54458B1 (fr) 2025-09-30
CL2021001537A1 (es) 2022-02-04
PL3894012T3 (pl) 2026-01-05
IL283860B1 (en) 2025-06-01
US20230029213A1 (en) 2023-01-26
TW202039440A (zh) 2020-11-01
DK3894012T3 (da) 2025-09-15
TWI852963B (zh) 2024-08-21
LT3894012T (lt) 2025-10-10
PH12021551356A1 (en) 2021-12-06
JP2024038167A (ja) 2024-03-19
US12017995B2 (en) 2024-06-25
GEP20247596B (en) 2024-02-26
IL320433A (en) 2025-06-01
IL283860A (en) 2021-07-29
JP2026031599A (ja) 2026-02-24
AU2019395419A1 (en) 2021-07-01
AU2019395419B2 (en) 2025-06-26
SG11202105949RA (en) 2021-07-29
PE20211757A1 (es) 2021-09-07
ZA202103844B (en) 2024-11-27
US20240300897A1 (en) 2024-09-12
KR20210102381A (ko) 2021-08-19
TW202519513A (zh) 2025-05-16

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