ZA201206679B - 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

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Publication number
ZA201206679B
ZA201206679B ZA2012/06679A ZA201206679A ZA201206679B ZA 201206679 B ZA201206679 B ZA 201206679B ZA 2012/06679 A ZA2012/06679 A ZA 2012/06679A ZA 201206679 A ZA201206679 A ZA 201206679A ZA 201206679 B ZA201206679 B ZA 201206679B
Authority
ZA
South Africa
Prior art keywords
oxy
ylpropyl
dicarboxamide
methyloxy
quinolin
Prior art date
Application number
ZA2012/06679A
Other languages
English (en)
Inventor
Hilary Cannon
Feirong Kang
Frederick G Vogt
Original Assignee
Exelixis Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Exelixis Inc filed Critical Exelixis Inc
Publication of ZA201206679B publication Critical patent/ZA201206679B/en

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Classifications

    • 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)
ZA2012/06679A 2010-03-12 2012-09-06 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 ZA201206679B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31319210P 2010-03-12 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 (1)

Publication Number Publication Date
ZA201206679B true ZA201206679B (en) 2013-05-29

Family

ID=43875241

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA2012/06679A ZA201206679B (en) 2010-03-12 2012-09-06 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
TW201920110A (zh) 2009-01-16 2019-06-01 美商艾克塞里克斯公司 包含n-(4-{[6,7-雙(甲氧基)喹啉-4-基]氧基}苯基)-n'-(4-氟苯基)環丙烷-1,1-二甲醯胺之蘋果酸鹽之醫藥組合物及其用途
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
HUE045810T2 (hu) 2010-09-27 2020-01-28 Exelixis Inc MET és VEGF kettõs inhibitorai kasztrációrezisztens prosztatarák és oszteoblasztos csontáttétek kezelésére
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
PL2768796T3 (pl) 2011-10-20 2020-05-18 Exelixis, Inc. Sposób wytwarzania pochodnych chinoliny
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
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
CN106255499A (zh) 2014-03-17 2016-12-21 埃克塞里艾克西斯公司 卡博替尼制剂的给药
EA033834B1 (ru) 2014-07-31 2019-11-29 Exelixis Inc Способ получения кабозантиниба, меченного фтором-18, и его аналогов
MA40457A (fr) 2014-08-05 2017-06-14 Exelixis Inc Combinaison de médicaments pour traiter le myélome multiple
US11141413B2 (en) 2016-04-15 2021-10-12 Exelixis, Inc. Method of treating renal cell carcinoma using N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (2S)-hydroxybutanedioate
US20190276405A1 (en) * 2016-05-16 2019-09-12 Pulmagen Therapeutics (Asthma) Limited Crystal of quinoline derivative
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
KR20250136810A (ko) 2023-01-31 2025-09-16 한다 온콜로지, 엘엘씨 개선된 카보잔티닙 조성물 및 사용 방법

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2210607B1 (en) * 2003-09-26 2011-08-17 Exelixis Inc. N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide for the treatment of cancer
BR112012001118A2 (pt) * 2009-07-17 2016-02-23 Exelixis Inc formas cristalinas de n-[3-flúor-4-({6-(metilóxi)-7-[(3-morfolin-4-ilpropil)óxi]-quinolin-4-il}óxi)fenil]-n'-(4-fluorfenil)ciclopropano-1,1-dicarboxamida, composição farmacêutica com as mesmas, métodos de preparação das mesmas e tratamento de câncer

Also Published As

Publication number Publication date
EA201290906A1 (ru) 2013-03-29
TW201202228A (en) 2012-01-16
AR080584A1 (es) 2012-04-18
EP2545038A1 (en) 2013-01-16
CA2792852A1 (en) 2011-09-15
AU2011224203A1 (en) 2012-10-04
WO2011112896A1 (en) 2011-09-15
KR20130038206A (ko) 2013-04-17
SG184040A1 (en) 2012-10-30
MX2012010506A (es) 2012-10-15
US20130143881A1 (en) 2013-06-06
CN102933551A (zh) 2013-02-13
JP2013522232A (ja) 2013-06-13

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