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

Info

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
Authority
KR
South Korea
Prior art keywords
oxy
cyclopropane
fluorophenyl
fluoro
phenyl
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
KR1020127004144A
Other languages
English (en)
Korean (ko)
Inventor
힐러리 캐논
데이비드 이고
트리 트란
Original Assignee
엑셀리시스, 인코포레이티드
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 엑셀리시스, 인코포레이티드 filed Critical 엑셀리시스, 인코포레이티드
Publication of KR20120051702A publication Critical patent/KR20120051702A/ko
Withdrawn legal-status Critical Current

Links

Images

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (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

Family

ID=42712017

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

Families Citing this family (25)

* 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
EA038195B1 (ru) 2009-01-16 2021-07-22 Экселиксис, Инк. Малатная соль n-(4-{[6,7-бис-(метилокси)хинолин-4-ил]окси}фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида и ее применение для лечения рака почек и печени
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
KR20180056807A (ko) 2010-07-16 2018-05-29 엑셀리시스, 인코포레이티드 C-met 조절제 약제학적 조성물
DK2621481T4 (da) 2010-09-27 2023-01-09 Exelixis Inc Dobbelte inhibitorer af MET og VEGF til behandling af kastrationsresistent prostatacancer og osteoblastiske knoglemetastaser
HUE057574T2 (hu) 2011-02-10 2022-05-28 Exelixis Inc Eljárás kinolin-származékok és ilyen vegyületeket tartalmazó gyógyászati készítmények elõállítására
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
TWI610918B (zh) 2011-05-02 2018-01-11 艾克塞里克斯公司 治療癌症及骨癌疼痛之方法
WO2013043840A1 (en) 2011-09-22 2013-03-28 Exelixis, Inc. Method for treating osteoporosis
CN110511158A (zh) 2011-10-20 2019-11-29 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
CN105121412B (zh) 2013-03-15 2019-07-12 埃克塞里艾克西斯公司 N-(4-{[6,7-双(甲基氧基)喹啉-4-基]氧基}苯基)-n′-(4-氟苯基)环丙烷-1,1-二甲酰胺的代谢物
WO2014165786A1 (en) 2013-04-04 2014-10-09 Exelixis, Inc. Cabozantinib dosage form and use in the treatment of cancer
CA2908815A1 (en) * 2013-04-04 2014-10-09 Exelixis, Inc. Drug combinations to treat cancer
US10501418B2 (en) 2014-02-14 2019-12-10 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
MA39735A (fr) 2014-03-17 2017-01-25 Exelixis Inc Dosage de préparations de cabozantinib
ES2929888T3 (es) 2014-07-31 2022-12-02 Exelixis Inc Procedimiento para preparar cabozantinib marcado con flúor 18 y sus análogos
EP3177311B1 (en) 2014-08-05 2024-10-30 Exelixis, Inc. Drug combinations of cabozantinib with proteasome inhibitor to treat multiple myeloma
MA44672A (fr) 2016-04-15 2019-02-20 Exelixis Inc Procédé de traitement du cancer à cellules rénales à l'aide de n-(4-(6,7-diméthoxyquinolin-4-yloxy) phényl)-n'-(4-fluorophény)cyclopropane-1,1-dicarboxamide, (2s)-hydroxybutanedioate
US20190276405A1 (en) 2016-05-16 2019-09-12 Pulmagen Therapeutics (Asthma) Limited 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
KR20210105931A (ko) 2018-12-20 2021-08-27 머크 샤프 앤드 돔 코포레이션 Nrtti 화합물의 신규 결정질 형태
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
TW202444365A (zh) 2023-01-31 2024-11-16 漢達生技醫藥股份有限公司 改良之卡博替尼組合物及其使用方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2002313249B2 (en) 2001-06-22 2008-08-21 Kirin Pharma Kabushiki Kaisha Quinoline derivative and quinazoline derivate inhibiting self-phosphorylation of hepatocytus proliferator receptor, and medicinal composition containing the same
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
PL2392565T3 (pl) * 2003-09-26 2014-08-29 Exelixis Inc Modulatory c-Met i sposoby stosowania
JP5486606B2 (ja) 2008-11-13 2014-05-07 エクセリクシス, インク. キノリン誘導体の調製方法

Also Published As

Publication number Publication date
TW201118072A (en) 2011-06-01
EP2454238A1 (en) 2012-05-23
ZA201200389B (en) 2012-09-26
US20120270872A1 (en) 2012-10-25
AU2010274012A1 (en) 2012-02-09
US8673912B2 (en) 2014-03-18
WO2011009095A1 (en) 2011-01-20
EA201200144A1 (ru) 2012-08-30
NZ597695A (en) 2014-05-30
BR112012001118A2 (pt) 2016-02-23
CN102510855B (zh) 2015-11-25
IL217537A0 (en) 2012-02-29
JP2012533570A (ja) 2012-12-27
WO2011009095A8 (en) 2011-03-24
CA2768370A1 (en) 2011-01-20
MX2012000809A (es) 2012-03-14
CN102510855A (zh) 2012-06-20

Similar Documents

Publication Publication Date Title
KR20120051702A (ko) 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
US11123338B2 (en) C-met modulator pharmaceutical compositions
CN106083714B (zh) N-(4-{[6,7-双(甲基氧基)喹啉-4-基]氧基}苯基)-n′-(4-氟苯基)环丙烷-1,1-二甲酰胺苹果酸盐及其结晶型
JP2013522232A (ja) N−[3−フルオロ−4−({6−(メチロキシ)−7−[(3−モルホリン−4−イルプロピル)オキシ]−キノリン−4−イル}オキシ)フェニル]−n’−(4−フルオロフェニル)シクロプロパン−1,1−ジカルボサミドの水和結晶性形状
HK40074566A (en) C-met modulator pharmaceutical compositions
HK1231054B (zh) N-(4-{[6,7-雙(甲基氧基)喹啉-4-基]氧基}苯基)-n'-(4-氟苯基)環丙烷-1,1-二甲酰胺蘋果酸鹽及其結晶型
HK1185553B (en) C-met modulator pharmaceutical compositions

Legal Events

Date Code Title Description
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