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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    • 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

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)

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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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IL270780B2 (en) * 2017-05-26 2025-04-01 Exelixis Inc 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
GEAP202415420A (en) 2018-01-26 2024-12-25 Exelixis Inc Compounds for the treatment of kinase-dependent disorders
CN120305263A (zh) 2018-06-15 2025-07-15 汉达癌症医药责任有限公司 卡博替尼的盐类于制备治疗癌症的剂型的用途
EP4631505A3 (en) * 2018-12-13 2025-12-10 Exelixis, Inc. Crystalline forms and salt forms of a kinase inhibitor
SG11202111978VA (en) * 2019-06-03 2021-11-29 Exelixis Inc Crystalline salt forms of a kinase inhibitor
WO2023165948A1 (en) 2022-03-01 2023-09-07 Synthon B.V. Cabozantinib salt with l-(+)-tartaric acid and solid forms thereof
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
WO2012009722A1 (en) 2010-07-16 2012-01-19 Exelixis, Inc. C-met modulator pharmaceutical compositions
CN103391773A (zh) 2010-09-27 2013-11-13 埃克塞里艾克西斯公司 用于治疗去势抵抗性前列腺癌和成骨性骨转移的met和vegf的双重抑制剂
DK2621481T4 (da) 2010-09-27 2023-01-09 Exelixis Inc Dobbelte inhibitorer af MET og VEGF til behandling af kastrationsresistent prostatacancer og osteoblastiske knoglemetastaser
TWI640509B (zh) 2011-02-10 2018-11-11 艾克塞里克斯公司 製造喹啉化合物之方法及包含該化合物之醫藥組合物
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
TWI610918B (zh) 2011-05-02 2018-01-11 艾克塞里克斯公司 治療癌症及骨癌疼痛之方法
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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
WO2016150966A1 (en) 2015-03-25 2016-09-29 Sandoz Ag Crystalline forms of cabozantinib phosphate and cabozantinib hydrochloride
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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
IL270780B2 (en) * 2017-05-26 2025-04-01 Exelixis Inc 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

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

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