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

Landscapes

  • 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)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (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)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2744997A1 (en) * 2003-09-26 2005-04-07 Exelixis, Inc. C-met modulators and method of use
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
EP2545038A1 (en) * 2010-03-12 2013-01-16 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
WO2012009722A1 (en) 2010-07-16 2012-01-19 Exelixis, Inc. C-met modulator pharmaceutical compositions
DK2621481T4 (da) 2010-09-27 2023-01-09 Exelixis Inc Dobbelte inhibitorer af MET og VEGF til behandling af kastrationsresistent prostatacancer og osteoblastiske knoglemetastaser
TWI640509B (zh) 2011-02-10 2018-11-11 艾克塞里克斯公司 製造喹啉化合物之方法及包含該化合物之醫藥組合物
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
GEP201606523B (en) 2011-09-22 2016-08-10 Exelixis Inc Method for treating osteoporosis
EP2768796B1 (en) 2011-10-20 2019-11-20 Exelixis, Inc. Process for preparing quinoline derivatives
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
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
AU2015218236B2 (en) 2014-02-14 2019-06-13 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
US10159666B2 (en) 2014-03-17 2018-12-25 Exelixis, Inc. Dosing of cabozantinib formulations
CN106715397B (zh) 2014-07-31 2021-07-23 埃克塞里艾克西斯公司 制备氟-18标记的卡博替尼及其类似物的方法
BR112017002318A2 (pt) 2014-08-05 2018-07-17 Exelixis, Inc. combinações de fármacos para tratar mieloma múltiplo.
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
CN109415323A (zh) * 2016-05-16 2019-03-01 普尔玛根治疗(哮喘)有限公司 喹啉衍生物的结晶
CN120305263A (zh) 2018-06-15 2025-07-15 汉达癌症医药责任有限公司 卡博替尼的盐类于制备治疗癌症的剂型的用途
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
AU2024215796A1 (en) 2023-01-31 2025-05-15 Handa Oncology, Llc Improved cabozantinib compositions and methods of use

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2454538A1 (en) 2001-06-22 2003-01-03 Kirin Beer Kabushiki Kaisha Quinoline derivatives and quinazoline derivatives capable of inhibiting autophosphorylation of hepatocyte growth factor receptors, and pharmaceutical composition comprising 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
CA2744997A1 (en) 2003-09-26 2005-04-07 Exelixis, Inc. C-met modulators and method of use
CA2743416A1 (en) 2008-11-13 2010-05-20 Exelixis Inc. Methods of preparing quinoline derivatives

Also Published As

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

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