CN110621662B - 一种盐的结晶性固体形式、制备工艺和使用方法 - Google Patents

一种盐的结晶性固体形式、制备工艺和使用方法 Download PDF

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CN110621662B
CN110621662B CN201880027861.5A CN201880027861A CN110621662B CN 110621662 B CN110621662 B CN 110621662B CN 201880027861 A CN201880027861 A CN 201880027861A CN 110621662 B CN110621662 B CN 110621662B
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cancer
compound
cyclopropane
fluorophenyl
phenyl
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CN110621662A (zh
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K·沙
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Exelixis Inc
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Exelixis Inc
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    • 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
    • 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (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)
  • Quinoline Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
CN201880027861.5A 2017-05-26 2018-05-26 一种盐的结晶性固体形式、制备工艺和使用方法 Active CN110621662B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762511714P 2017-05-26 2017-05-26
US62/511,714 2017-05-26
PCT/US2018/034784 WO2018218233A1 (en) 2017-05-26 2018-05-26 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

Publications (2)

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CN110621662A CN110621662A (zh) 2019-12-27
CN110621662B true CN110621662B (zh) 2023-06-23

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US (3) US11279675B2 (https=)
EP (1) EP3630726B1 (https=)
JP (3) JP7166292B2 (https=)
KR (1) KR102611445B1 (https=)
CN (1) CN110621662B (https=)
AU (1) AU2018272088C1 (https=)
CA (1) CA3060370A1 (https=)
DK (1) DK3630726T3 (https=)
EA (1) EA039654B1 (https=)
ES (1) ES2909390T3 (https=)
HU (1) HUE058196T2 (https=)
IL (1) IL270780B2 (https=)
MA (1) MA48776A (https=)
MX (1) MX2019012505A (https=)
PL (1) PL3630726T3 (https=)
PT (1) PT3630726T (https=)
SG (1) SG11201909161PA (https=)
UA (1) UA127760C2 (https=)
WO (1) WO2018218233A1 (https=)
ZA (1) ZA201906127B (https=)

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KR102354963B1 (ko) * 2014-02-14 2022-01-21 엑셀리시스, 인코포레이티드 N-｛4-[(6,7-다이메톡시퀴놀린-4-일)옥시]페닐｝-n'-(4-플루오로페닐) 사이클로프로판-1,1-다이카복스아마이드의 결정질 고체 형태, 제조 방법 및 사용 방법
AU2018272088C1 (en) * 2017-05-26 2022-09-22 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
UA128476C2 (uk) 2018-01-26 2024-07-24 Екселіксіс, Інк. Сполуки для лікування кіназозалежних розладів
CN113292537B (zh) 2018-06-15 2024-04-05 汉达癌症医药责任有限公司 激酶抑制剂的盐类及其组合物
PL3894012T4 (pl) * 2018-12-13 2026-01-05 Exelixis, Inc. Postacie krystaliczne i postacie soli inhibitora kinazy
CA3139148A1 (en) * 2019-06-03 2020-12-10 Exelixis, Inc. Crystalline salt forms of a kinase inhibitor
CN118974017A (zh) 2022-03-01 2024-11-15 斯索恩有限公司 卡博替尼的l-(+)-酒石酸盐及其固体形式
TW202444365A (zh) 2023-01-31 2024-11-16 漢達生技醫藥股份有限公司 改良之卡博替尼組合物及其使用方法
US11814356B1 (en) 2023-03-29 2023-11-14 Apotex Inc. Salt of cabozantinib

Citations (4)

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WO2005030140A2 (en) * 2003-09-26 2005-04-07 Exelixis, Inc. C-met modulators and methods of use
WO2010083414A1 (en) * 2009-01-16 2010-07-22 Exelixis, Inc. Malate salt of n- (4- { [ 6, 7-bis (methyloxy) quin0lin-4-yl] oxy}phenyl-n' - (4 -fluorophenyl) cyclopropane-1-dicarboxamide, and crystalline forms therof for the treatment of cancer
WO2015177758A1 (en) * 2014-05-23 2015-11-26 Mylan Laboratories Ltd Novel polymorphs of cabozantinib (s)-malate and cabozantinib free base
WO2016150963A1 (en) * 2015-03-25 2016-09-29 Sandoz Ag Cabozantinib salts and their use as anti-cancer agents

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UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
US20120070368A1 (en) 2010-04-16 2012-03-22 Exelixis, Inc. Methods of Using C-Met Modulators
EP2593090B1 (en) 2010-07-16 2021-10-13 Exelixis, Inc. C-met modulator pharmaceutical compositions
EP2621483A1 (en) 2010-09-27 2013-08-07 Exelixis, Inc. Dual inhibitors of met and vegf for the treatment of castration resistant prostate cancer and osteoblastic bone metastases
CA2812750C (en) 2010-09-27 2020-10-06 Exelixis, Inc. Dual inhibitors of met and vegf for the treatment of castration-resistant prostate cancer and osteoblastic bone metastases
JP2014505109A (ja) 2011-02-10 2014-02-27 エクセリクシス， インク． キノリン化合物およびそのような化合物を含有する医薬組成物の調製方法
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
KR20140025496A (ko) 2011-05-02 2014-03-04 엑셀리시스, 인코포레이티드 암 및 뼈 암 통증의 치료방법
GEP201606523B (en) 2011-09-22 2016-08-10 Exelixis Inc Method for treating osteoporosis
US9535315B2 (en) 2011-10-31 2017-01-03 Applied Materials, Inc. Method of fabricating a color filter array using a multilevel structure
JP2014532766A (ja) 2011-11-08 2014-12-08 エクセリクシス， インク． 癌を治療する、ｍｅｔ及びｖｅｇｆの二重阻害剤
EP2775921A1 (en) 2011-11-08 2014-09-17 Exelixis, Inc. Method of quantifying cancer treatment
CN104649969B (zh) 2013-11-22 2019-02-12 广东东阳光药业有限公司 一种替尼类药物的盐及其制备方法
KR102354963B1 (ko) * 2014-02-14 2022-01-21 엑셀리시스, 인코포레이티드 N-｛4-[(6,7-다이메톡시퀴놀린-4-일)옥시]페닐｝-n'-(4-플루오로페닐) 사이클로프로판-1,1-다이카복스아마이드의 결정질 고체 형태, 제조 방법 및 사용 방법
CN104961680B (zh) 2014-11-07 2017-09-12 苏州晶云药物科技有限公司 N‑(4‑{[6,7‑双(甲基氧基)喹啉‑4‑基]氧基}苯基)‑n’‑(4‑氟苯基)环丙烷‑1,1‑二甲酰胺的盐酸盐及其多晶型
CN104961681B (zh) 2014-11-13 2017-06-13 苏州晶云药物科技有限公司 卡博替尼的粘酸盐及其晶型
EP3274332B1 (en) 2015-03-25 2018-12-19 Sandoz AG Crystalline forms of cabozantinib phosphate and cabozantinib hydrochloride
US10980792B2 (en) * 2016-09-12 2021-04-20 Zhuhai Beihai Biotech Co., Ltd. Formulations of Cabozantinib
US11261160B2 (en) * 2016-12-07 2022-03-01 Msn Laboratories Private Limited, R&D Center Process for the preparation of N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N′-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide, (2S)-hydroxybutanedioate and its polymorphs thereof
AU2018272088C1 (en) 2017-05-26 2022-09-22 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

Patent Citations (4)

* 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
WO2010083414A1 (en) * 2009-01-16 2010-07-22 Exelixis, Inc. Malate salt of n- (4- { [ 6, 7-bis (methyloxy) quin0lin-4-yl] oxy}phenyl-n' - (4 -fluorophenyl) cyclopropane-1-dicarboxamide, and crystalline forms therof for the treatment of cancer
WO2015177758A1 (en) * 2014-05-23 2015-11-26 Mylan Laboratories Ltd Novel polymorphs of cabozantinib (s)-malate and cabozantinib free base
WO2016150963A1 (en) * 2015-03-25 2016-09-29 Sandoz Ag Cabozantinib salts and their use as anti-cancer agents

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JP2020521732A (ja) 2020-07-27
JP2024036690A (ja) 2024-03-15
KR102611445B1 (ko) 2023-12-06
JP7437460B2 (ja) 2024-02-22
ZA201906127B (en) 2022-11-30
IL270780B2 (en) 2025-04-01
IL270780A (en) 2020-01-30
MA48776A (fr) 2020-04-08
US11731941B2 (en) 2023-08-22
AU2018272088C1 (en) 2022-09-22
UA127760C2 (uk) 2023-12-27
IL270780B1 (en) 2024-12-01
EA039654B1 (ru) 2022-02-22
HUE058196T2 (hu) 2022-07-28
KR20200010205A (ko) 2020-01-30
EA201992803A1 (ru) 2020-04-16
EP3630726A1 (en) 2020-04-08
PT3630726T (pt) 2022-03-02
JP2022145852A (ja) 2022-10-04
AU2018272088A1 (en) 2019-10-17
WO2018218233A1 (en) 2018-11-29
AU2018272088B2 (en) 2022-06-16
JP7659097B2 (ja) 2025-04-08
US20240010621A1 (en) 2024-01-11
ES2909390T3 (es) 2022-05-06
JP7166292B2 (ja) 2022-11-07
US11279675B2 (en) 2022-03-22
AU2018272088A8 (en) 2019-10-24
CN110621662A (zh) 2019-12-27
SG11201909161PA (en) 2019-10-30
PL3630726T3 (pl) 2022-05-09
EP3630726B1 (en) 2021-12-22
US20220162166A1 (en) 2022-05-26
NZ757564A (en) 2025-05-02
DK3630726T3 (da) 2022-03-07
CA3060370A1 (en) 2018-11-29
MX2019012505A (es) 2019-12-19
US12227481B2 (en) 2025-02-18
US20210261509A1 (en) 2021-08-26

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