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

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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
ES2909390T3 (es) * 2017-05-26 2022-05-06 Exelixis Inc Formas sólidas cristalinas de sales de N-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-N'-(4-fluorofenil)ciclopropano-1,1-dicarboxamida, procedimientos de fabricación y procedimientos de uso
CN117624045A (zh) 2018-01-26 2024-03-01 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
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
RS67216B1 (sr) * 2018-12-13 2025-10-31 Exelixis Inc Kristalni oblici i oblici soli inhibitora kinaze
AU2019449809A1 (en) * 2019-06-03 2021-12-16 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

Citations (3)

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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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CA2744997A1 (en) 2003-09-26 2005-04-07 Exelixis, Inc. C-met modulators and method of use
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
SG10201609324UA (en) 2010-07-16 2017-01-27 Exelixis Inc C-met modulator pharmaceutical compositions
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
US20140057908A1 (en) 2010-09-27 2014-02-27 Exelixis, Inc. Method of Treating Cancer
GEP20247677B (en) * 2011-02-10 2024-10-10 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
JP2014513129A (ja) 2011-05-02 2014-05-29 エクセリクシス， インク． 癌および骨癌疼痛の治療方法
AU2012312364B2 (en) 2011-09-22 2017-11-09 Exelixis, Inc. Method for treating osteoporosis
WO2013066296A1 (en) 2011-10-31 2013-05-10 Hewlett-Packard Development Company, L.P. Method of fabricating a color filter array using a multilevel structure
BR112014011009A2 (pt) 2011-11-08 2017-06-06 Exelixis Inc inibidor duplo de met e vegf para tratar câncer
KR20140094597A (ko) 2011-11-08 2014-07-30 엑셀리시스, 인코포레이티드 암 치료를 정량하는 방법
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
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
CN109922790B (zh) * 2016-09-12 2022-06-14 珠海贝海生物技术有限公司 卡博替尼制剂
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
ES2909390T3 (es) * 2017-05-26 2022-05-06 Exelixis Inc Formas sólidas cristalinas de sales de N-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-N'-(4-fluorofenil)ciclopropano-1,1-dicarboxamida, procedimientos de fabricación y procedimientos de uso

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
CN110621662B (zh) 2023-06-23
EP3630726B1 (en) 2021-12-22
IL270780A (en) 2020-01-30
IL270780B1 (en) 2024-12-01
AU2018272088A8 (en) 2019-10-24
AU2018272088A1 (en) 2019-10-17
WO2018218233A1 (en) 2018-11-29
MA48776A (fr) 2020-04-08
MX2019012505A (es) 2019-12-19
UA127760C2 (uk) 2023-12-27
US20210261509A1 (en) 2021-08-26
EP3630726A1 (en) 2020-04-08
US20240010621A1 (en) 2024-01-11
JP7166292B2 (ja) 2022-11-07
US11279675B2 (en) 2022-03-22
EA039654B1 (ru) 2022-02-22
NZ757564A (en) 2025-05-02
JP2022145852A (ja) 2022-10-04
JP2020521732A (ja) 2020-07-27
PL3630726T3 (pl) 2022-05-09
JP2024036690A (ja) 2024-03-15
DK3630726T3 (da) 2022-03-07
CA3060370A1 (en) 2018-11-29
CN110621662A (zh) 2019-12-27
AU2018272088C1 (en) 2022-09-22
PT3630726T (pt) 2022-03-02
US12227481B2 (en) 2025-02-18
SG11201909161PA (en) 2019-10-30
US11731941B2 (en) 2023-08-22
JP7659097B2 (ja) 2025-04-08
US20220162166A1 (en) 2022-05-26
KR102611445B1 (ko) 2023-12-06
ES2909390T3 (es) 2022-05-06
HUE058196T2 (hu) 2022-07-28
JP7437460B2 (ja) 2024-02-22
AU2018272088B2 (en) 2022-06-16
EA201992803A1 (ru) 2020-04-16
ZA201906127B (en) 2022-11-30
KR20200010205A (ko) 2020-01-30

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