EA039654B1 - Кристаллические твердые формы солей n-{4-[(6,7-диметоксихинолин-4-ил)окси]фенил}-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, способы получения и методы использования - Google Patents

Кристаллические твердые формы солей n-{4-[(6,7-диметоксихинолин-4-ил)окси]фенил}-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, способы получения и методы использования Download PDF

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Publication number
EA039654B1
EA039654B1 EA201992803A EA201992803A EA039654B1 EA 039654 B1 EA039654 B1 EA 039654B1 EA 201992803 A EA201992803 A EA 201992803A EA 201992803 A EA201992803 A EA 201992803A EA 039654 B1 EA039654 B1 EA 039654B1
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EA
Eurasian Patent Office
Prior art keywords
compound
cancer
crystalline solid
peaks
radiograph
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Application number
EA201992803A
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English (en)
Russian (ru)
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EA201992803A1 (ru
Inventor
Халид Шах
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Экселиксис, Инк.
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Publication of EA039654B1 publication Critical patent/EA039654B1/ru

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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)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
EA201992803A 2017-05-26 2018-05-26 Кристаллические твердые формы солей n-{4-[(6,7-диметоксихинолин-4-ил)окси]фенил}-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, способы получения и методы использования EA039654B1 (ru)

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 (2)

Publication Number Publication Date
EA201992803A1 EA201992803A1 (ru) 2020-04-16
EA039654B1 true EA039654B1 (ru) 2022-02-22

Family

ID=62683441

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201992803A EA039654B1 (ru) 2017-05-26 2018-05-26 Кристаллические твердые формы солей n-{4-[(6,7-диметоксихинолин-4-ил)окси]фенил}-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, способы получения и методы использования

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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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
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
TWI831259B (zh) 2018-06-15 2024-02-01 漢達生技醫藥股份有限公司 包含達沙替尼十二烷基硫酸鹽組合物的膠囊
KR102828472B1 (ko) 2018-12-13 2025-07-03 엑셀리시스, 인코포레이티드 키나아제 억제제의 결정질 형태 및 염 형태
MX2021014773A (es) * 2019-06-03 2022-01-18 Exelixis Inc Formas de sales cristalinas de un inhibidor de cinasas.
EP4486725A1 (en) 2022-03-01 2025-01-08 Synthon B.V. Cabozantinib salt with l-(+)-tartaric acid and solid forms thereof
WO2024163400A1 (en) 2023-01-31 2024-08-08 Handa Oncology, Llc Improved cabozantinib compositions and methods of use
US11814356B1 (en) 2023-03-29 2023-11-14 Apotex Inc. Salt of cabozantinib

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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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US20120070368A1 (en) 2010-04-16 2012-03-22 Exelixis, Inc. Methods of Using C-Met Modulators
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
US20140057908A1 (en) 2010-09-27 2014-02-27 Exelixis, Inc. Method of Treating Cancer
MX352926B (es) 2010-09-27 2017-12-14 Exelixis Inc Inhibidores dobles de met y factor de crecimiento endotelial vascular (vegf) para el tratamiento de cancer de prostata resistente a la castracion y metastasis osteoblasticas en los huesos.
BR112013020362A2 (pt) 2011-02-10 2018-05-29 Exelixis Inc processos para a preparação de compostos de quinolina, compostos e combinações farmacêuticas que os contem
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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
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
WO2018104954A1 (en) * 2016-12-07 2018-06-14 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
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

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

Also Published As

Publication number Publication date
JP2024036690A (ja) 2024-03-15
US20210261509A1 (en) 2021-08-26
PL3630726T3 (pl) 2022-05-09
PT3630726T (pt) 2022-03-02
US11279675B2 (en) 2022-03-22
CN110621662B (zh) 2023-06-23
WO2018218233A1 (en) 2018-11-29
JP2020521732A (ja) 2020-07-27
AU2018272088A8 (en) 2019-10-24
AU2018272088B2 (en) 2022-06-16
JP2022145852A (ja) 2022-10-04
US20240010621A1 (en) 2024-01-11
EP3630726A1 (en) 2020-04-08
JP7166292B2 (ja) 2022-11-07
UA127760C2 (uk) 2023-12-27
JP7659097B2 (ja) 2025-04-08
NZ757564A (en) 2025-05-02
US11731941B2 (en) 2023-08-22
KR20200010205A (ko) 2020-01-30
EA201992803A1 (ru) 2020-04-16
US12227481B2 (en) 2025-02-18
AU2018272088A1 (en) 2019-10-17
IL270780B2 (en) 2025-04-01
ZA201906127B (en) 2022-11-30
SG11201909161PA (en) 2019-10-30
CN110621662A (zh) 2019-12-27
DK3630726T3 (da) 2022-03-07
HUE058196T2 (hu) 2022-07-28
KR102611445B1 (ko) 2023-12-06
IL270780B1 (en) 2024-12-01
JP7437460B2 (ja) 2024-02-22
MX2019012505A (es) 2019-12-19
ES2909390T3 (es) 2022-05-06
IL270780A (en) 2020-01-30
EP3630726B1 (en) 2021-12-22
MA48776A (fr) 2020-04-08
US20220162166A1 (en) 2022-05-26
CA3060370A1 (en) 2018-11-29
AU2018272088C1 (en) 2022-09-22

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