ZA201200389B - Crystalline forms of n-[3-fluoro-4-([6-(methyloxy)-7-[(morpholin-4ylpropyl)oxy}]-quinolin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide - Google Patents

Crystalline forms of n-[3-fluoro-4-([6-(methyloxy)-7-[(morpholin-4ylpropyl)oxy}]-quinolin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide

Info

Publication number
ZA201200389B
ZA201200389B ZA2012/00389A ZA201200389A ZA201200389B ZA 201200389 B ZA201200389 B ZA 201200389B ZA 2012/00389 A ZA2012/00389 A ZA 2012/00389A ZA 201200389 A ZA201200389 A ZA 201200389A ZA 201200389 B ZA201200389 B ZA 201200389B
Authority
ZA
South Africa
Prior art keywords
oxy
4ylpropyl
dicarboxamide
methyloxy
quinolin
Prior art date
Application number
ZA2012/00389A
Other languages
English (en)
Inventor
Hilary Cannon
David Igo
Tri Tran
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 ZA201200389B publication Critical patent/ZA201200389B/en

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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)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
ZA2012/00389A 2009-07-17 2012-01-18 Crystalline forms of n-[3-fluoro-4-([6-(methyloxy)-7-[(morpholin-4ylpropyl)oxy}]-quinolin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide ZA201200389B (en)

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
ZA201200389B true ZA201200389B (en) 2012-09-26

Family

ID=42712017

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA2012/00389A ZA201200389B (en) 2009-07-17 2012-01-18 Crystalline forms of n-[3-fluoro-4-([6-(methyloxy)-7-[(morpholin-4ylpropyl)oxy}]-quinolin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide

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)

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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
AU2010204619B2 (en) 2009-01-16 2016-08-11 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
KR20130038206A (ko) * 2010-03-12 2013-04-17 엑셀리시스, 인코포레이티드 Ｎ-〔3-플루오로-4-(｛6-（메틸옥시）-7-〔（3-모폴린-4-일프로필）옥시〕-퀴놀린-4-일｝옥시）페닐〕-ｎ’-（4-플루오로페닐）사이클로프로판-1,1-디카복사미드의 수화된 결정형 형태
KR20210014770A (ko) 2010-07-16 2021-02-09 엑셀리시스, 인코포레이티드 C-met 조절제 약제학적 조성물
SI2621481T2 (sl) 2010-09-27 2023-02-28 Exelixis, Inc., Dvojni inhibitorji MET in VEGF za zdravljenje proti kastraciji odpornega raka prostate in osteoblastnih kostnih metastaz
DK2673262T3 (da) 2011-02-10 2022-01-24 Exelixis Inc Fremgangsmåder til fremstilling af quinolinforbindelser og farmaceutiske sammensætninger indeholdende sådanne forbindelser
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
KR20140025496A (ko) 2011-05-02 2014-03-04 엑셀리시스, 인코포레이티드 암 및 뼈 암 통증의 치료방법
UA115866C2 (uk) 2011-09-22 2018-01-10 Екселіксіс, Інк. Спосіб лікування остеопорозу
KR102075371B1 (ko) 2011-10-20 2020-02-10 엑셀리시스, 인코포레이티드 퀴놀린 유도체 제조 방법
WO2013166296A1 (en) 2012-05-02 2013-11-07 Exelixis, Inc. A dual met - vegf modulator for treating osteolytic bone metastases
WO2014145715A1 (en) 2013-03-15 2014-09-18 Exelixis, Inc. Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide
KR20150138268A (ko) * 2013-04-04 2015-12-09 엑셀리시스, 인코포레이티드 암을 치료하기 위한 약물 병용요법
US11564915B2 (en) 2013-04-04 2023-01-31 Exelixis, Inc. Cabozantinib dosage form and use in the treatment of cancer
CA3181899A1 (en) 2014-02-14 2015-08-20 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
EA201691850A1 (ru) 2014-03-17 2016-12-30 Экселиксис, Инк. Дозирование составов, содержащих кабозантиниб
CA2956810C (en) 2014-07-31 2022-10-04 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
RU2748549C2 (ru) 2016-04-15 2021-05-26 Экселиксис, Инк. Способ лечения почечно-клеточного рака с использованием n-(4-(6,7-диметоксихинолин-4-илокси)фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, (2s)-гидроксибутандиоата
US20190276405A1 (en) * 2016-05-16 2019-09-12 Pulmagen Therapeutics (Asthma) Limited Crystal of quinoline derivative
KR20210042896A (ko) 2018-06-15 2021-04-20 한다 파마슈티칼스, 인코포레이티드 카이네이스 억제제 염 및 이의 조성물
CA3122576C (en) * 2018-12-20 2025-11-25 Merck Sharp & Dohme Corp Crystalline forms of the nrtti compound 4'-ethynyl-2-fluoro-2'-deoxyadenosine
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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

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CN102282134B (zh) 2008-11-13 2015-04-01 埃克塞里艾克西斯公司 喹啉衍生物制备方法

Also Published As

Publication number Publication date
NZ597695A (en) 2014-05-30
WO2011009095A1 (en) 2011-01-20
JP2012533570A (ja) 2012-12-27
CN102510855A (zh) 2012-06-20
MX2012000809A (es) 2012-03-14
CA2768370A1 (en) 2011-01-20
EP2454238A1 (en) 2012-05-23
US8673912B2 (en) 2014-03-18
CN102510855B (zh) 2015-11-25
WO2011009095A8 (en) 2011-03-24
AU2010274012A1 (en) 2012-02-09
US20120270872A1 (en) 2012-10-25
EA201200144A1 (ru) 2012-08-30
BR112012001118A2 (pt) 2016-02-23
KR20120051702A (ko) 2012-05-22
IL217537A0 (en) 2012-02-29
TW201118072A (en) 2011-06-01

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