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
Inventor
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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    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • 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
    • 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
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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

Country Status (14)

Country Link
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)

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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

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EA038195B1 (ru) 2009-01-16 2021-07-22 Экселиксис, Инк. Малатная соль n-(4-{[6,7-бис-(метилокси)хинолин-4-ил]окси}фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида и ее применение для лечения рака почек и печени
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
WO2012009722A1 (en) 2010-07-16 2012-01-19 Exelixis, Inc. C-met modulator pharmaceutical compositions
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
GEP201606523B (en) 2011-09-22 2016-08-10 Exelixis Inc Method for treating osteoporosis
EP2768796B1 (en) 2011-10-20 2019-11-20 Exelixis, Inc. Process for preparing quinoline derivatives
WO2013166296A1 (en) 2012-05-02 2013-11-07 Exelixis, Inc. A dual met - vegf modulator for treating osteolytic bone metastases
CA2907334C (en) 2013-03-15 2021-12-07 Exelixis, Inc. Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
US11564915B2 (en) 2013-04-04 2023-01-31 Exelixis, Inc. Cabozantinib dosage form and use in the treatment of cancer
AU2015218236B2 (en) 2014-02-14 2019-06-13 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
US10159666B2 (en) 2014-03-17 2018-12-25 Exelixis, Inc. Dosing of cabozantinib formulations
CN106715397B (zh) 2014-07-31 2021-07-23 埃克塞里艾克西斯公司 制备氟-18标记的卡博替尼及其类似物的方法
BR112017002318A2 (pt) 2014-08-05 2018-07-17 Exelixis, Inc. combinações de fármacos para tratar mieloma múltiplo.
CN109069499A (zh) 2016-04-15 2018-12-21 埃克塞里艾克西斯公司 使用 n-(4-(6,7-二甲氧基喹啉-4-基氧基)苯基)-n’-(4-氟苯基)环丙烷-1,1-二甲酰胺,(2s)-羟基丁二酸盐治疗肾细胞癌的方法
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
AU2024215796A1 (en) 2023-01-31 2025-05-15 Handa Oncology, Llc Improved cabozantinib compositions and methods of use

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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

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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

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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

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

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