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
NZ779754A (en) 2009-01-16 2023-04-28 Exelixis Inc Malate salt of n-(4-{ [6,7-bis(methyloxy)quinolin-4-yl] oxy} phenyl)-n’-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms thereof for the treatment of cancer
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
EA030435B1 (ru) 2010-07-16 2018-08-31 Экселиксис, Инк. ТАБЛЕТКА, СОДЕРЖАЩАЯ МОДУЛЯТОР c-MET В ФОРМЕ КРИСТАЛЛИЧЕСКОЙ L-МАЛАТНОЙ СОЛИ (ВАРИАНТЫ), СПОСОБ ЕЕ ПРОИЗВОДСТВА И СПОСОБ ЛЕЧЕНИЯ ОНКОЛОГИЧЕСКОГО ЗАБОЛЕВАНИЯ С ЕЕ ИСПОЛЬЗОВАНИЕМ
MX352926B (es) 2010-09-27 2017-12-14 Exelixis Inc Inhibidores dobles de met y factor de crecimiento endotelial vascular (vegf) para el tratamiento de cancer de prostata resistente a la castracion y metastasis osteoblasticas en los huesos.
BR112013020362A2 (pt) 2011-02-10 2018-05-29 Exelixis Inc processos para a preparação de compostos de quinolina, compostos e combinações farmacêuticas que os contem
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
MX2013012695A (es) 2011-05-02 2014-03-27 Exelixis Inc Metodo para el tratamiento del cancer y el dolor por cancer de hueso.
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
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
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
EP3119476A1 (en) 2014-03-17 2017-01-25 Exelixis, Inc. Dosing of cabozantinib formulations
EP3174854B1 (en) 2014-07-31 2022-08-24 Exelixis, Inc. Method of preparing fluorine-18 labeled cabozantinib and its analogs
MX382904B (es) 2014-08-05 2025-03-13 Exelixis Inc Combinaciones de fármacos para tratar mieloma múltiple.
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
EP3476835A4 (en) * 2016-05-16 2020-01-01 GB001, Inc. CRYSTAL OF A CHINOLINID DERIVATIVE
TWI831259B (zh) 2018-06-15 2024-02-01 漢達生技醫藥股份有限公司 包含達沙替尼十二烷基硫酸鹽組合物的膠囊
WO2024163400A1 (en) 2023-01-31 2024-08-08 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
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
CN102510855B (zh) * 2009-07-17 2015-11-25 埃克塞里艾克西斯公司 N-[3-氟-4-({6-(甲基氧基)-7-[(3-吗啉-4-基丙基)氧基]-喹啉-4-基}氧基)苯基]-n′-(4-氟苯基)环丙烷-1，1-二甲酰胺的晶形

Also Published As

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

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