CN113939503B - 激酶抑制剂的结晶盐形式 - Google Patents

激酶抑制剂的结晶盐形式 Download PDF

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Publication number
CN113939503B
CN113939503B CN201980097028.2A CN201980097028A CN113939503B CN 113939503 B CN113939503 B CN 113939503B CN 201980097028 A CN201980097028 A CN 201980097028A CN 113939503 B CN113939503 B CN 113939503B
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compound
peaks
xrpd pattern
scale
salt form
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CN201980097028.2A
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English (en)
Chinese (zh)
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CN113939503A (zh
Inventor
F·德莫林
K·沙阿
S·释迦
P·黄
C·S·约翰逊
M·J·比维尔
S·D·帕伦特
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Exelixis Inc
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Exelixis Inc
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    • 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
    • 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
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201980097028.2A 2019-06-03 2019-12-12 激酶抑制剂的结晶盐形式 Active CN113939503B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962856404P 2019-06-03 2019-06-03
US62/856,404 2019-06-03
PCT/US2019/065980 WO2020247019A1 (en) 2019-06-03 2019-12-12 Crystalline salt forms of a kinase inhibitor

Publications (2)

Publication Number Publication Date
CN113939503A CN113939503A (zh) 2022-01-14
CN113939503B true CN113939503B (zh) 2024-05-07

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CN201980097028.2A Active CN113939503B (zh) 2019-06-03 2019-12-12 激酶抑制剂的结晶盐形式

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US (1) US20230052703A1 (enExample)
EP (1) EP3976587B1 (enExample)
JP (1) JP7579281B2 (enExample)
KR (1) KR102826380B1 (enExample)
CN (1) CN113939503B (enExample)
AU (1) AU2019449809B2 (enExample)
BR (1) BR112021024300A2 (enExample)
CA (1) CA3139148A1 (enExample)
CL (1) CL2021003205A1 (enExample)
CO (1) CO2021017343A2 (enExample)
CR (1) CR20210616A (enExample)
DO (1) DOP2021000236A (enExample)
ES (1) ES3008963T3 (enExample)
GE (2) GEP20247655B (enExample)
IL (1) IL288484A (enExample)
MA (1) MA56001A (enExample)
MX (1) MX2021014773A (enExample)
PE (1) PE20220962A1 (enExample)
PH (1) PH12021553020A1 (enExample)
SG (1) SG11202111978VA (enExample)
WO (1) WO2020247019A1 (enExample)
ZA (1) ZA202108034B (enExample)

Families Citing this family (5)

* 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
KR102828472B1 (ko) * 2018-12-13 2025-07-03 엑셀리시스, 인코포레이티드 키나아제 억제제의 결정질 형태 및 염 형태
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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109761899A (zh) * 2019-02-14 2019-05-17 陆瑞燕 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

Family Cites Families (9)

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EP2210607B1 (en) * 2003-09-26 2011-08-17 Exelixis Inc. N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide for the treatment of cancer
CA2604238C (en) 2005-04-15 2015-07-07 Neogenix Oncology, Inc. Recombinant monoclonal antibodies and corresponding antigens for colon and pancreatic cancers
ES2598530T3 (es) * 2010-07-14 2017-01-27 Betta Pharmaceuticals Co., Ltd. Nuevos derivados heterocíclicos condensados útiles como inhibidores de la tirosina quinasa c-Met
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)
US20180009758A1 (en) * 2015-06-29 2018-01-11 Ontogenesis, Llc Multi-Tyrosine Kinase Inhibitors Derivatives and Methods of Use
MA48776A (fr) * 2017-05-26 2020-04-08 Exelixis Inc Formes solides cristallines de sels de n-{4-[(6,7-diméthoxyquinolin-4-yl) oxy]phényl}-n'-(4-fluorphényl) cyclopropane-1,1-dicarboxamide, procédés de préparation et d'utilisation
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
KR102828472B1 (ko) * 2018-12-13 2025-07-03 엑셀리시스, 인코포레이티드 키나아제 억제제의 결정질 형태 및 염 형태

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109761899A (zh) * 2019-02-14 2019-05-17 陆瑞燕 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

Also Published As

Publication number Publication date
PH12021553020A1 (en) 2023-08-23
JP7579281B2 (ja) 2024-11-07
ES3008963T3 (en) 2025-03-25
EP3976587A1 (en) 2022-04-06
EP3976587B1 (en) 2024-12-04
BR112021024300A2 (pt) 2022-01-11
AU2019449809B2 (en) 2026-02-05
SG11202111978VA (en) 2021-11-29
CN113939503A (zh) 2022-01-14
IL288484A (en) 2022-01-01
KR102826380B1 (ko) 2025-06-26
AU2019449809A1 (en) 2021-12-16
DOP2021000236A (es) 2022-04-18
CA3139148A1 (en) 2020-12-10
GEAP202415849A (en) 2024-03-11
KR20220016117A (ko) 2022-02-08
PE20220962A1 (es) 2022-06-10
US20230052703A1 (en) 2023-02-16
EP3976587C0 (en) 2024-12-04
JP2022535072A (ja) 2022-08-04
MA56001A (fr) 2022-04-06
WO2020247019A1 (en) 2020-12-10
CO2021017343A2 (es) 2022-01-17
GEP20247655B (en) 2024-08-26
ZA202108034B (en) 2025-02-26
CR20210616A (es) 2022-03-22
CL2021003205A1 (es) 2022-09-30
MX2021014773A (es) 2022-01-18

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