TW201202228A - 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 - Google Patents

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 Download PDF

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Publication number
TW201202228A
TW201202228A TW100108394A TW100108394A TW201202228A TW 201202228 A TW201202228 A TW 201202228A TW 100108394 A TW100108394 A TW 100108394A TW 100108394 A TW100108394 A TW 100108394A TW 201202228 A TW201202228 A TW 201202228A
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Taiwan
Prior art keywords
oxy
cancer
ylpropyl
phenyl
hydrate
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TW100108394A
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English (en)
Chinese (zh)
Inventor
Hilary Cannon
Fei-Rong Kang
Frederick G Vogt
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Exelixis Inc
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Publication date
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Publication of TW201202228A publication Critical patent/TW201202228A/zh

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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)
TW100108394A 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 TW201202228A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US31319210P 2010-03-12 2010-03-12

Publications (1)

Publication Number Publication Date
TW201202228A true TW201202228A (en) 2012-01-16

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Application Number Title Priority Date Filing Date
TW100108394A TW201202228A (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

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)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2387563T4 (da) 2009-01-16 2022-07-18 Exelixis Inc Malatsalt af n-(4-{ [ 6, 7-bis(methyloxy)quinolin-4-yl]oxy}phenyl-n'-(4-fluorphenyl)cyclopropan-1,1-dicarboxamid, og krystallinske former deraf til behandling af cancer
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
SG187060A1 (en) 2010-07-16 2013-02-28 Exelixis Inc C-met modulator pharmaceutical compositions
US20140057943A1 (en) 2010-09-27 2014-02-27 Exelixix, Inc. Method of Treating Cancer
KR20230158644A (ko) 2011-02-10 2023-11-20 엑셀리시스, 인코포레이티드 퀴놀린 화합물들의 제조 방법들 및 상기 화합물들을 함유하는 약학 조성물들
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
WO2012151326A1 (en) 2011-05-02 2012-11-08 Exelixis, Inc. Method of treating cancer and bone cancer pain
CA2848512A1 (en) 2011-09-22 2013-03-28 Exelixis, Inc. Method for treating osteoporosis
BR112014009302B1 (pt) 2011-10-20 2020-04-28 Exelis Inc Us/Us processo para preparar derivados de quinolina
US9861624B2 (en) 2012-05-02 2018-01-09 Exelixis, Inc. Method of treating cancer
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
JP6666849B2 (ja) 2014-03-17 2020-03-18 エグゼリクシス, インコーポレイテッド カボザンチニブ製剤の投与
EP3174854B1 (en) 2014-07-31 2022-08-24 Exelixis, Inc. Method of preparing fluorine-18 labeled cabozantinib and its analogs
CN106573042A (zh) 2014-08-05 2017-04-19 埃克塞里艾克西斯公司 治疗多发性骨髓瘤的药物组合
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
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
EP3806858A4 (en) 2018-06-15 2022-03-09 Handa Pharmaceuticals, Inc. KINA INHIBITOR SALTS AND COMPOSITIONS THEREOF
EP4658271A1 (en) 2023-01-31 2025-12-10 Handa Oncology, LLC Improved cabozantinib compositions and methods of use

Family Cites Families (2)

* 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
JP2012533570A (ja) * 2009-07-17 2012-12-27 エグゼリクシス, インコーポレイテッド N−[3−フルオロ−4−({6−(メチルオキシ)−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−ジカルボキサミドの結晶形

Also Published As

Publication number Publication date
KR20130038206A (ko) 2013-04-17
JP2013522232A (ja) 2013-06-13
SG184040A1 (en) 2012-10-30
EA201290906A1 (ru) 2013-03-29
CN102933551A (zh) 2013-02-13
ZA201206679B (en) 2013-05-29
MX2012010506A (es) 2012-10-15
AR080584A1 (es) 2012-04-18
EP2545038A1 (en) 2013-01-16
CA2792852A1 (en) 2011-09-15
AU2011224203A1 (en) 2012-10-04
US20130143881A1 (en) 2013-06-06
WO2011112896A1 (en) 2011-09-15

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