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EA201290906A1 - Кристаллогидратные формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида - Google Patents

Кристаллогидратные формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида

Info

Publication number
EA201290906A1
EA201290906A1 EA201290906A EA201290906A EA201290906A1 EA 201290906 A1 EA201290906 A1 EA 201290906A1 EA 201290906 A EA201290906 A EA 201290906A EA 201290906 A EA201290906 A EA 201290906A EA 201290906 A1 EA201290906 A1 EA 201290906A1
Authority
EA
Eurasian Patent Office
Prior art keywords
oxy
phenyl
photorphenyl
diparboxamide
cyclopropan
Prior art date
Application number
EA201290906A
Other languages
English (en)
Inventor
Хилари Кэннон
Фэйжун Кан
Фредерик Г. Вогт
Original Assignee
Экселиксис, Инк.
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 Экселиксис, Инк. filed Critical Экселиксис, Инк.
Publication of EA201290906A1 publication Critical patent/EA201290906A1/ru

Links

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)

Abstract

Изобретение относится к кристаллогидрату N-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-N'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, соединение (I). Изобретение представляет способы лечения рака путем применения модуляции протеинкиназной активности. Изобретение также представляет фармацевтические композиции, содержащие кристаллогидрат соединения (I) и фармацевтически приемлемый эксципиент.
EA201290906A 2010-03-12 2011-03-11 Кристаллогидратные формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида EA201290906A1 (ru)

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
EA201290906A1 true EA201290906A1 (ru) 2013-03-29

Family

ID=43875241

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201290906A EA201290906A1 (ru) 2010-03-12 2011-03-11 Кристаллогидратные формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида

Country Status (14)

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

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI447108B (zh) 2009-01-16 2014-08-01 Exelixis Inc 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及其結晶型
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
KR20200029633A (ko) 2010-07-16 2020-03-18 엑셀리시스, 인코포레이티드 C-met 조절제 약제학적 조성물
HUE045810T2 (hu) 2010-09-27 2020-01-28 Exelixis Inc MET és VEGF kettõs inhibitorai kasztrációrezisztens prosztatarák és oszteoblasztos csontáttétek kezelésére
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
GEP201706678B (en) 2011-05-02 2017-06-12 Exelixis Inc Method of treating cancer and bone cancer
CA2848512A1 (en) 2011-09-22 2013-03-28 Exelixis, Inc. Method for treating osteoporosis
TWI642650B (zh) 2011-10-20 2018-12-01 艾克塞里克斯公司 用於製備喹啉衍生物之方法
WO2013166296A1 (en) 2012-05-02 2013-11-07 Exelixis, Inc. A dual met - vegf modulator for treating osteolytic bone metastases
ES2729626T3 (es) 2013-03-15 2019-11-05 Exelixis Inc Metabolitos de N-(4-{[6,7-bis(metiloxi)quinolin-4-il]oxi}fenil)-N'-(4-fuorofenil)ciclopropano-1,1-dicarboxamida
ES2927651T3 (es) 2013-04-04 2022-11-10 Exelixis Inc Forma de dosificación de cabozantinib y uso en el tratamiento del cáncer
MX2021001583A (es) 2014-02-14 2023-02-08 Exelixis Inc Formas sólidas cristalinas de n-{4-[(6,7-dimetoxiquinolin-4-il)oxi ] fenil}-n'-(4-fluorofenil)ciclopropan-1,1-dicarboxamida, procesos para elaboración y métodos de uso.
WO2015142928A1 (en) 2014-03-17 2015-09-24 Exelixis, Inc. Dosing of cabozantinib formulations
EA033834B1 (ru) 2014-07-31 2019-11-29 Exelixis Inc Способ получения кабозантиниба, меченного фтором-18, и его аналогов
EA034992B1 (ru) 2014-08-05 2020-04-15 Экселиксис, Инк. Комбинации лекарственных средств для лечения множественной миеломы
CA3020749A1 (en) 2016-04-15 2017-10-19 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
AU2017267768A1 (en) * 2016-05-16 2019-01-03 Gb001, Inc. Crystal of quinoline derivative
CN113321647B (zh) 2018-06-15 2024-08-27 汉达癌症医药责任有限公司 激酶抑制剂的盐类及其组合物

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2392565T3 (pl) * 2003-09-26 2014-08-29 Exelixis Inc Modulatory c-Met i sposoby stosowania
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

Also Published As

Publication number Publication date
SG184040A1 (en) 2012-10-30
TW201202228A (en) 2012-01-16
CN102933551A (zh) 2013-02-13
AU2011224203A1 (en) 2012-10-04
KR20130038206A (ko) 2013-04-17
EP2545038A1 (en) 2013-01-16
JP2013522232A (ja) 2013-06-13
MX2012010506A (es) 2012-10-15
US20130143881A1 (en) 2013-06-06
WO2011112896A1 (en) 2011-09-15
CA2792852A1 (en) 2011-09-15
ZA201206679B (en) 2013-05-29
AR080584A1 (es) 2012-04-18

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