IL270780B2 - Crystalline solid forms of salts of N–{4–[(7,6–dimethoxyquinolin–4–yl)oxy]phenyl}–N'–(4–fluorophenyl)cyclopropane–1,1–dicarboxamide, processes for preparation and methods of use - Google Patents

Crystalline solid forms of salts of N–{4–[(7,6–dimethoxyquinolin–4–yl)oxy]phenyl}–N'–(4–fluorophenyl)cyclopropane–1,1–dicarboxamide, processes for preparation and methods of use

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Publication number
IL270780B2
IL270780B2 IL270780A IL27078019A IL270780B2 IL 270780 B2 IL270780 B2 IL 270780B2 IL 270780 A IL270780 A IL 270780A IL 27078019 A IL27078019 A IL 27078019A IL 270780 B2 IL270780 B2 IL 270780B2
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compound
cancer
crystalline solid
weight
forms
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IL270780A
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English (en)
Hebrew (he)
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IL270780A (en
IL270780B1 (en
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Exelixis Inc
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Application filed by Exelixis Inc filed Critical Exelixis Inc
Publication of IL270780A publication Critical patent/IL270780A/en
Publication of IL270780B1 publication Critical patent/IL270780B1/en
Publication of IL270780B2 publication Critical patent/IL270780B2/en

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    • 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
    • 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
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • 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)
  • 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)
IL270780A 2017-05-26 2018-05-26 Crystalline solid forms of salts of N–{4–[(7,6–dimethoxyquinolin–4–yl)oxy]phenyl}–N'–(4–fluorophenyl)cyclopropane–1,1–dicarboxamide, processes for preparation and methods of use IL270780B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762511714P 2017-05-26 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 (3)

Publication Number Publication Date
IL270780A IL270780A (en) 2020-01-30
IL270780B1 IL270780B1 (en) 2024-12-01
IL270780B2 true IL270780B2 (en) 2025-04-01

Family

ID=62683441

Family Applications (1)

Application Number Title Priority Date Filing Date
IL270780A IL270780B2 (en) 2017-05-26 2018-05-26 Crystalline solid forms of salts of N–{4–[(7,6–dimethoxyquinolin–4–yl)oxy]phenyl}–N'–(4–fluorophenyl)cyclopropane–1,1–dicarboxamide, processes for preparation and methods of use

Country Status (20)

Country Link
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

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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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PT2213661E (pt) 2003-09-26 2011-12-15 Exelixis Inc Moduladores de c-met e métodos de uso
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Also Published As

Publication number Publication date
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
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
CN110621662B (zh) 2023-06-23
MX2019012505A (es) 2019-12-19
US12227481B2 (en) 2025-02-18
US20210261509A1 (en) 2021-08-26

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