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)
  • Medicinal Preparation (AREA)
  • Quinoline Compounds (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)

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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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EA032757B1 (ru) * 2014-02-14 2019-07-31 Экселиксис, Инк. Кристаллические твердые формы n-{4-[(6,7-диметоксихинолин-4-ил)окси]фенил}-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, способы получения и способы применения
MX2019012505A (es) * 2017-05-26 2019-12-19 Exelixis Inc Formas solidas cristalinas de sales de ciclopropano-1,1-dicarboxam ida de n-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-n'-(4-fluorofen il), procesos para realizarlas y metodos de uso.
HRP20251184T1 (hr) 2018-01-26 2025-12-05 Exelixis, Inc. Spojevi za liječenje poremećaja ovisnih o kinazi
TWI787523B (zh) 2018-06-15 2022-12-21 漢達生技醫藥股份有限公司 達沙替尼十二烷基硫酸鹽之結晶
PL3894012T4 (pl) 2018-12-13 2026-01-05 Exelixis, Inc. Postacie krystaliczne i postacie soli inhibitora kinazy
KR102826380B1 (ko) * 2019-06-03 2025-06-26 엑셀리시스, 인코포레이티드 카이네이스 저해제의 결정질 염 형태
CA3202761A1 (en) 2020-11-25 2022-06-02 Nanocopoeia, Llc Amorphous cabozantinib particles and uses thereof
US20250171403A1 (en) 2022-03-01 2025-05-29 Synthon B.V. Cabozantinib salt with l-(+)-tartaric acid and solid forms thereof
KR20250136810A (ko) 2023-01-31 2025-09-16 한다 온콜로지, 엘엘씨 개선된 카보잔티닙 조성물 및 사용 방법
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
HUE045810T2 (hu) 2010-09-27 2020-01-28 Exelixis Inc MET és VEGF kettõs inhibitorai kasztrációrezisztens prosztatarák és oszteoblasztos csontáttétek kezelésére
WO2012044577A1 (en) 2010-09-27 2012-04-05 Exelixis, Inc. Dual inhibitors of met and vegf for the treatment of castration resistant prostate cancer and osteoblastic bone metastases
TW201309650A (zh) 2011-02-10 2013-03-01 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
EP2704717A1 (en) 2011-05-02 2014-03-12 Exelixis, Inc. Method of treating cancer and bone cancer pain
GEP201606523B (en) 2011-09-22 2016-08-10 Exelixis Inc Method for treating osteoporosis
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EA032757B1 (ru) * 2014-02-14 2019-07-31 Экселиксис, Инк. Кристаллические твердые формы n-{4-[(6,7-диметоксихинолин-4-ил)окси]фенил}-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, способы получения и способы применения
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
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US10053427B2 (en) 2015-03-25 2018-08-21 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
MX2019012505A (es) * 2017-05-26 2019-12-19 Exelixis Inc Formas solidas cristalinas de sales de ciclopropano-1,1-dicarboxam ida de n-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-n'-(4-fluorofen il), procesos para realizarlas y metodos de uso.

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

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