KR20120051702A - N-〔3-플루오로-4-({6-(메틸옥시)-7-〔(3-모르폴린-4-일프로필)옥시〕퀴놀린-4-일}옥시)페닐〕-n''-(4-플루오로페닐)시클로프로판-1,1-디카르복사미드의 결정형 - Google Patents

N-〔3-플루오로-4-({6-(메틸옥시)-7-〔(3-모르폴린-4-일프로필)옥시〕퀴놀린-4-일}옥시)페닐〕-n''-(4-플루오로페닐)시클로프로판-1,1-디카르복사미드의 결정형 Download PDF

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Publication number
KR20120051702A
KR20120051702A KR1020127004144A KR20127004144A KR20120051702A KR 20120051702 A KR20120051702 A KR 20120051702A KR 1020127004144 A KR1020127004144 A KR 1020127004144A KR 20127004144 A KR20127004144 A KR 20127004144A KR 20120051702 A KR20120051702 A KR 20120051702A
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South Korea
Prior art keywords
oxy
cyclopropane
fluorophenyl
fluoro
phenyl
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KR1020127004144A
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English (en)
Korean (ko)
Inventor
힐러리 캐논
데이비드 이고
트리 트란
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엑셀리시스, 인코포레이티드
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Publication of KR20120051702A publication Critical patent/KR20120051702A/ko
Withdrawn legal-status Critical Current

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    • 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
    • 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
    • A61K31/535Heterocyclic 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
KR1020127004144A 2009-07-17 2010-07-16 N-〔3-플루오로-4-({6-(메틸옥시)-7-〔(3-모르폴린-4-일프로필)옥시〕퀴놀린-4-일}옥시)페닐〕-n''-(4-플루오로페닐)시클로프로판-1,1-디카르복사미드의 결정형 Withdrawn KR20120051702A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22650909P 2009-07-17 2009-07-17
US61/226,509 2009-07-17

Publications (1)

Publication Number Publication Date
KR20120051702A true KR20120051702A (ko) 2012-05-22

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Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020127004144A Withdrawn KR20120051702A (ko) 2009-07-17 2010-07-16 N-〔3-플루오로-4-({6-(메틸옥시)-7-〔(3-모르폴린-4-일프로필)옥시〕퀴놀린-4-일}옥시)페닐〕-n''-(4-플루오로페닐)시클로프로판-1,1-디카르복사미드의 결정형

Country Status (15)

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

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WO2005030140A2 (en) 2003-09-26 2005-04-07 Exelixis, Inc. C-met modulators and methods of use
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
MX2012010506A (es) * 2010-03-12 2012-10-15 Exelixis Inc Formas cristalinas hidratadas del n-[3-fluoro-4-({6-(metiloxi)-7-[ (3-morfolin-4-ilpropil)oxi]-quinolin-4-il}oxi)fenil]-n'-(4-fluoro fenil)ciclopropano-1,1-dicarboxamida.
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
AU2014248001A1 (en) * 2013-04-04 2015-11-19 Exelixis, Inc. Drug combinations to treat cancer
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
US12227536B2 (en) 2018-12-20 2025-02-18 Merck Sharp & Dohme Llc Crystalline forms of an NRTTI compound
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
EP4658271A1 (en) 2023-01-31 2025-12-10 Handa Oncology, LLC Improved cabozantinib compositions and methods of use

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100883731B1 (ko) 2001-06-22 2009-02-12 기린 파마 가부시끼가이샤 간세포 증식 인자 수용체 자기 인산화를 저해하는 퀴놀린유도체 및 퀴나졸린 유도체 및 이들을 함유하는 의약 조성물
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
WO2005030140A2 (en) * 2003-09-26 2005-04-07 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
EA201200144A1 (ru) 2012-08-30
CN102510855B (zh) 2015-11-25
WO2011009095A8 (en) 2011-03-24
MX2012000809A (es) 2012-03-14
AU2010274012A1 (en) 2012-02-09
ZA201200389B (en) 2012-09-26
US20120270872A1 (en) 2012-10-25
US8673912B2 (en) 2014-03-18
JP2012533570A (ja) 2012-12-27
BR112012001118A2 (pt) 2016-02-23
IL217537A0 (en) 2012-02-29
TW201118072A (en) 2011-06-01
CA2768370A1 (en) 2011-01-20
CN102510855A (zh) 2012-06-20
WO2011009095A1 (en) 2011-01-20
NZ597695A (en) 2014-05-30
EP2454238A1 (en) 2012-05-23

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PA0105 International application

Patent event date: 20120216

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PC1203 Withdrawal of no request for examination
WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid