CN102510855B - 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 - Google Patents

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 Download PDF

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Publication number
CN102510855B
CN102510855B CN201080042037.0A CN201080042037A CN102510855B CN 102510855 B CN102510855 B CN 102510855B CN 201080042037 A CN201080042037 A CN 201080042037A CN 102510855 B CN102510855 B CN 102510855B
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oxy
compound
cancer
fluoro
fluorophenyl
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Expired - Fee Related
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Chinese (zh)
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CN102510855A (zh
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H·肯农
D·伊戈
T·特兰
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Exelixis Inc
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Exelixis Inc
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (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)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
CN201080042037.0A 2009-07-17 2010-07-16 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 Expired - Fee Related CN102510855B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22650909P 2009-07-17 2009-07-17
US61/226509 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 (2)

Publication Number Publication Date
CN102510855A CN102510855A (zh) 2012-06-20
CN102510855B true CN102510855B (zh) 2015-11-25

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CN201080042037.0A Expired - Fee Related CN102510855B (zh) 2009-07-17 2010-07-16 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

Country Status (15)

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

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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
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
AU2011224203A1 (en) * 2010-03-12 2012-10-04 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
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
WO2014165779A1 (en) * 2013-04-04 2014-10-09 Exelixis, Inc. Drug combinations to treat 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
CA3122576C (en) 2018-12-20 2025-11-25 Merck Sharp & Dohme Llc CRYSTALLINE FORMS OF THE NRTTI COMPOUND OF 4'-ETHYNYL-2-FLUORO-2'-DESOXYADENOSINE
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
WO2024163400A1 (en) 2023-01-31 2024-08-08 Handa Oncology, Llc Improved cabozantinib compositions and methods of use

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WO2005030140A2 (en) * 2003-09-26 2005-04-07 Exelixis, Inc. C-met modulators and methods of use
CN1780627A (zh) * 2003-04-29 2006-05-31 贝林格尔.英格海姆国际有限公司 用于治疗涉及细胞增殖、骨髓瘤细胞迁移或凋亡或者血管增殖疾病的联用药物

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Also Published As

Publication number Publication date
BR112012001118A2 (pt) 2016-02-23
TW201118072A (en) 2011-06-01
KR20120051702A (ko) 2012-05-22
WO2011009095A1 (en) 2011-01-20
EA201200144A1 (ru) 2012-08-30
MX2012000809A (es) 2012-03-14
US20120270872A1 (en) 2012-10-25
AU2010274012A1 (en) 2012-02-09
ZA201200389B (en) 2012-09-26
WO2011009095A8 (en) 2011-03-24
CA2768370A1 (en) 2011-01-20
EP2454238A1 (en) 2012-05-23
US8673912B2 (en) 2014-03-18
NZ597695A (en) 2014-05-30
JP2012533570A (ja) 2012-12-27
IL217537A0 (en) 2012-02-29
CN102510855A (zh) 2012-06-20

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