JP2013522232A - N−[3−フルオロ−4−({6−(メチロキシ)−7−[(3−モルホリン−4−イルプロピル)オキシ]−キノリン−4−イル}オキシ)フェニル]−n’−(4−フルオロフェニル)シクロプロパン−1,1−ジカルボサミドの水和結晶性形状 - Google Patents

N−[3−フルオロ−4−({6−(メチロキシ)−7−[(3−モルホリン−4−イルプロピル)オキシ]−キノリン−4−イル}オキシ)フェニル]−n’−(4−フルオロフェニル)シクロプロパン−1,1−ジカルボサミドの水和結晶性形状 Download PDF

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JP2013522232A
JP2013522232A JP2012557269A JP2012557269A JP2013522232A JP 2013522232 A JP2013522232 A JP 2013522232A JP 2012557269 A JP2012557269 A JP 2012557269A JP 2012557269 A JP2012557269 A JP 2012557269A JP 2013522232 A JP2013522232 A JP 2013522232A
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oxy
cancer
methyloxy
morpholin
fluorophenyl
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JP2013522232A5 (enExample
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ヒラリー キャノン,
フェイロン カン,
フレデリック ジー. フォグト,
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エグゼリクシス, インコーポレイテッド
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
JP2012557269A 2010-03-12 2011-03-11 N−[3−フルオロ−4−({6−(メチロキシ)−7−[(3−モルホリン−4−イルプロピル)オキシ]−キノリン−4−イル}オキシ)フェニル]−n’−(4−フルオロフェニル)シクロプロパン−1,1−ジカルボサミドの水和結晶性形状 Pending JP2013522232A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US31319210P 2010-03-12 2010-03-12
US61/313,192 2010-03-12
PCT/US2011/028035 WO2011112896A1 (en) 2010-03-12 2011-03-11 Hydrated crystalline forms of n-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]-quinolin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

Publications (2)

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JP2013522232A true JP2013522232A (ja) 2013-06-13
JP2013522232A5 JP2013522232A5 (enExample) 2014-04-24

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JP2012557269A Pending JP2013522232A (ja) 2010-03-12 2011-03-11 N−[3−フルオロ−4−({6−(メチロキシ)−7−[(3−モルホリン−4−イルプロピル)オキシ]−キノリン−4−イル}オキシ)フェニル]−n’−(4−フルオロフェニル)シクロプロパン−1,1−ジカルボサミドの水和結晶性形状

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US (1) US20130143881A1 (enExample)
EP (1) EP2545038A1 (enExample)
JP (1) JP2013522232A (enExample)
KR (1) KR20130038206A (enExample)
CN (1) CN102933551A (enExample)
AR (1) AR080584A1 (enExample)
AU (1) AU2011224203A1 (enExample)
CA (1) CA2792852A1 (enExample)
EA (1) EA201290906A1 (enExample)
MX (1) MX2012010506A (enExample)
SG (1) SG184040A1 (enExample)
TW (1) TW201202228A (enExample)
WO (1) WO2011112896A1 (enExample)
ZA (1) ZA201206679B (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017199903A1 (ja) * 2016-05-16 2017-11-23 帝人ファーマ株式会社 キノリン誘導体の結晶

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS52754B2 (sr) 2009-01-16 2022-08-31 Exelixis Inc Malat so n-(4- {[6,7-bis(metiloksi)hinolin-4-il]oksi}fenil-n'- (4-fluorofenil) ciklopropan-1,1-dikarboksamid-a, i njeni kristalni oblici za lečenje karcinoma
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
KR20180056807A (ko) 2010-07-16 2018-05-29 엑셀리시스, 인코포레이티드 C-met 조절제 약제학적 조성물
PL2621481T5 (pl) 2010-09-27 2023-03-13 Exelixis, Inc. Podwójne inhibitory MET i VEGF do leczenia opornego na kastrację raka prostaty i osteoblastycznych przerzutów do kości
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
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
EP2758057B1 (en) 2011-09-22 2017-05-31 Exelixis, Inc. Method for treating osteoporosis
CN104395284A (zh) 2011-10-20 2015-03-04 埃克塞里艾克西斯公司 制备喹啉衍生物的方法
HK1207587A1 (en) 2012-05-02 2016-02-05 Exelixis, Inc. A dual met - vegf modulator for treating osteolytic bone metastases
GEP20196995B (en) 2013-03-15 2019-07-25 Inc Exelixis Metabolites of n-(4-{[6,7-bis (methyloxy)quinolin-4-yl] oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide
ES2927651T3 (es) 2013-04-04 2022-11-10 Exelixis Inc Forma de dosificación de cabozantinib y uso en el tratamiento del cáncer
EP3738952A1 (en) 2014-02-14 2020-11-18 Exelixis, Inc. Crystalline solid forms of n-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use
WO2015142928A1 (en) 2014-03-17 2015-09-24 Exelixis, Inc. Dosing of cabozantinib formulations
MA40386A (fr) 2014-07-31 2016-02-04 Exelixis Inc Procédé de préparation de cabozantinib marqué au fluor-18 et d'analogues de celui-ci
EA034992B1 (ru) 2014-08-05 2020-04-15 Экселиксис, Инк. Комбинации лекарственных средств для лечения множественной миеломы
EP3442531A1 (en) 2016-04-15 2019-02-20 Exelixis, Inc. Method of treating renal cell carcinoma using n-(4-(6,7-dimethoxyquinolin-4-yloxy) phenyl)-n'-(4-fluoropheny)cyclopropane-1,1-dicarboxamide, (2s)-hydroxybutanedioate
AU2019285066B2 (en) 2018-06-15 2024-06-13 Handa Pharmaceuticals, Inc. Kinase inhibitor salts and compositions thereof
EP4658271A1 (en) 2023-01-31 2025-12-10 Handa Oncology, LLC Improved cabozantinib compositions and methods of use

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007506777A (ja) * 2003-09-26 2007-03-22 エグゼリクシス, インコーポレイテッド c−Metモジュレーターおよびその使用

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2454238A1 (en) * 2009-07-17 2012-05-23 Exelixis, Inc. Crystalline forms of n-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]-quinolin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007506777A (ja) * 2003-09-26 2007-03-22 エグゼリクシス, インコーポレイテッド c−Metモジュレーターおよびその使用

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
有機化合物結晶作製ハンドブック −原理とノウハウ−, JPN6011053065, 25 July 2008 (2008-07-25), pages 57 - 84, ISSN: 0002998939 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017199903A1 (ja) * 2016-05-16 2017-11-23 帝人ファーマ株式会社 キノリン誘導体の結晶
JPWO2017199903A1 (ja) * 2016-05-16 2019-02-28 帝人ファーマ株式会社 キノリン誘導体の結晶
US10626089B2 (en) 2016-05-16 2020-04-21 GBOO1, Inc. Quinoline derivative in crystal form

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MX2012010506A (es) 2012-10-15
KR20130038206A (ko) 2013-04-17
AR080584A1 (es) 2012-04-18
US20130143881A1 (en) 2013-06-06
EA201290906A1 (ru) 2013-03-29
EP2545038A1 (en) 2013-01-16
ZA201206679B (en) 2013-05-29
TW201202228A (en) 2012-01-16
WO2011112896A1 (en) 2011-09-15
AU2011224203A1 (en) 2012-10-04
CN102933551A (zh) 2013-02-13
CA2792852A1 (en) 2011-09-15
SG184040A1 (en) 2012-10-30

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