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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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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    • 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)
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

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

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EA039654B1 (ru) * 2017-05-26 2022-02-22 Экселиксис, Инк. 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
CA3088200A1 (en) 2018-01-26 2019-08-01 Exelixis, Inc. Compounds for the treatment of kinase-dependent disorders
TWI770624B (zh) 2018-06-15 2022-07-11 漢達生技醫藥股份有限公司 尼洛替尼十二烷基硫酸鹽在製備用於治療慢性骨髓性白血病之劑型的用途
JP7509779B2 (ja) 2018-12-13 2024-07-02 エグゼリクシス， インコーポレイテッド キナーゼ阻害剤の結晶性形態及び塩形態
CA3139148A1 (en) * 2019-06-03 2020-12-10 Exelixis, Inc. Crystalline salt forms of a kinase inhibitor
CA3245315A1 (en) 2022-03-01 2023-09-07 Synthon B.V. L(+) TARTARIC ACID CABOZANTINIB SALT AND ITS SOLID FORMS
AU2024215796A1 (en) 2023-01-31 2025-05-15 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
TWI619495B (zh) 2010-07-16 2018-04-01 艾克塞里克斯公司 Ｃ-ｍｅｔ調節劑醫藥組合物
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EP2621481B2 (en) 2010-09-27 2022-10-19 Exelixis, Inc. Dual inhibitors of met and vegf for the treatment of castration-resistant prostate cancer and osteoblastic bone metastases
CA2826751C (en) * 2011-02-10 2021-05-18 Exelixis, Inc. Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
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KR20140069133A (ko) 2011-09-22 2014-06-09 엑셀리시스, 인코포레이티드 골다공증의 치료방법
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US10980792B2 (en) * 2016-09-12 2021-04-20 Zhuhai Beihai Biotech Co., Ltd. Formulations of Cabozantinib
EP3551612A4 (en) * 2016-12-07 2020-08-12 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) -HYDROXYBUTANYEDIOOR AND ITS POLYDROXYBUTANYMATE
EA039654B1 (ru) * 2017-05-26 2022-02-22 Экселиксис, Инк. 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

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

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