BR112012001118A2 - 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 - Google Patents

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

Info

Publication number
BR112012001118A2
BR112012001118A2 BR112012001118A BR112012001118A BR112012001118A2 BR 112012001118 A2 BR112012001118 A2 BR 112012001118A2 BR 112012001118 A BR112012001118 A BR 112012001118A BR 112012001118 A BR112012001118 A BR 112012001118A BR 112012001118 A2 BR112012001118 A2 BR 112012001118A2
Authority
BR
Brazil
Prior art keywords
oxy
fluorphenyl
ylpropyl
dicarboxamide
methyloxy
Prior art date
Application number
BR112012001118A
Other languages
English (en)
Inventor
Cannon Hilary
Igo David
Tran Tri
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 BR112012001118A2 publication Critical patent/BR112012001118A2/pt

Links

Classifications

    • 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
    • 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
    • A61K31/535—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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
BR112012001118A 2009-07-17 2010-07-16 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 BR112012001118A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22650909P 2009-07-17 2009-07-17
PCT/US2010/042353 WO2011009095A1 (en) 2009-07-17 2010-07-16 Crystalline forms of n-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]-quin0lin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide

Publications (1)

Publication Number Publication Date
BR112012001118A2 true BR112012001118A2 (pt) 2016-02-23

Family

ID=42712017

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012001118A BR112012001118A2 (pt) 2009-07-17 2010-07-16 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

Country Status (15)

Country Link
US (1) US8673912B2 (pt)
EP (1) EP2454238A1 (pt)
JP (1) JP2012533570A (pt)
KR (1) KR20120051702A (pt)
CN (1) CN102510855B (pt)
AU (1) AU2010274012A1 (pt)
BR (1) BR112012001118A2 (pt)
CA (1) CA2768370A1 (pt)
EA (1) EA201200144A1 (pt)
IL (1) IL217537A0 (pt)
MX (1) MX2012000809A (pt)
NZ (1) NZ597695A (pt)
TW (1) TW201118072A (pt)
WO (1) WO2011009095A1 (pt)
ZA (1) ZA201200389B (pt)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2004275842B2 (en) * 2003-09-26 2010-09-02 Exelixis Inc. c-MET modulators and methods of use
KR102187034B1 (ko) 2009-01-16 2020-12-04 엑셀리시스, 인코포레이티드 암 치료용 ｎ-（４-｛〔６，７-비스（메틸옥시）퀴놀린-4-일〕옥시｝페닐）-ｎ＇-（４-플루오로페닐）사이클로프로판-1,1-디카르복사미드의 말산염 및 그 결정형
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
SG184040A1 (en) * 2010-03-12 2012-10-30 Exelixis Inc 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
SG10201609324UA (en) 2010-07-16 2017-01-27 Exelixis Inc C-met modulator pharmaceutical compositions
KR101882328B1 (ko) 2010-09-27 2018-07-27 엑셀리시스, 인코포레이티드 거세-저항성 전립선 암 및 골형성성 뼈전이의 치료용 met 및 vegf 이중 억제제들
PL2673262T3 (pl) 2011-02-10 2022-04-11 Exelixis, Inc. Sposoby wytwarzania związków chinolinowych i kompozycje farmaceutyczne zawierające takie związki
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.
KR20140069133A (ko) 2011-09-22 2014-06-09 엑셀리시스, 인코포레이티드 골다공증의 치료방법
HUE048023T2 (hu) 2011-10-20 2020-05-28 Exelixis Inc Eljárás kinolin-származékok elõállítására
JP2015515988A (ja) 2012-05-02 2015-06-04 エクセリクシス， インク． 溶骨性骨転移を治療するためのｍｅｔ−ｖｅｇｆ二重調節剤
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
ES2927651T3 (es) 2013-04-04 2022-11-10 Exelixis Inc Forma de dosificación de cabozantinib y uso en el tratamiento del cáncer
BR112015025408A8 (pt) * 2013-04-04 2018-07-10 Exelixis Inc combinações de drogas para tratar câncer
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
WO2015142928A1 (en) 2014-03-17 2015-09-24 Exelixis, Inc. Dosing of cabozantinib formulations
US11124481B2 (en) 2014-07-31 2021-09-21 Exelixis, Inc. Method of preparing fluorine-18 labeled Cabozantinib and its analogs
WO2016022697A1 (en) 2014-08-05 2016-02-11 Exelixis, Inc. Drug combinations to treat multiple myeloma
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
CA3025049A1 (en) * 2016-05-16 2017-11-23 Pulmagen Therapeutics (Asthma) Limited Crystal of quinoline derivative
CN113194959A (zh) * 2018-12-20 2021-07-30 默沙东公司 Nrtti化合物的新型结晶形式
CN110357814A (zh) * 2019-07-12 2019-10-22 上海翔锦生物科技有限公司 对甲苯磺酸盐新晶型及其应用

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100415720C (zh) 2001-06-22 2008-09-03 麒麟医药株式会社 喹啉衍生物和喹唑啉衍生物以及含有这些化合物的药物组合物
US20050043233A1 (en) * 2003-04-29 2005-02-24 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
AU2004275842B2 (en) * 2003-09-26 2010-09-02 Exelixis Inc. c-MET modulators and methods of use
WO2010056960A1 (en) 2008-11-13 2010-05-20 Exelixis Inc. Methods of preparing quinoline derivatives

Also Published As

Publication number Publication date
IL217537A0 (en) 2012-02-29
JP2012533570A (ja) 2012-12-27
CA2768370A1 (en) 2011-01-20
KR20120051702A (ko) 2012-05-22
TW201118072A (en) 2011-06-01
WO2011009095A8 (en) 2011-03-24
EA201200144A1 (ru) 2012-08-30
AU2010274012A1 (en) 2012-02-09
WO2011009095A1 (en) 2011-01-20
NZ597695A (en) 2014-05-30
CN102510855A (zh) 2012-06-20
ZA201200389B (en) 2012-09-26
US8673912B2 (en) 2014-03-18
US20120270872A1 (en) 2012-10-25
EP2454238A1 (en) 2012-05-23
CN102510855B (zh) 2015-11-25
MX2012000809A (es) 2012-03-14

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B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

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