BR112012001118A2 - formas cristalinas de n-[3-flúor-4-({6-(metilóxi)-7-[(3-morfolin-4-ilpropil)óxi]-quinolin-4-il}óxi)fenil]-n'-(4-fluorfenil)ciclopropano-1,1-dicarboxamida, composição farmacêutica com as mesmas, métodos de preparação das mesmas e tratamento de câncer - Google Patents

formas cristalinas de n-[3-flúor-4-({6-(metilóxi)-7-[(3-morfolin-4-ilpropil)óxi]-quinolin-4-il}óxi)fenil]-n'-(4-fluorfenil)ciclopropano-1,1-dicarboxamida, composição farmacêutica com as mesmas, métodos de preparação das mesmas e tratamento de câncer

Info

Publication number
BR112012001118A2
BR112012001118A2 BR112012001118A BR112012001118A BR112012001118A2 BR 112012001118 A2 BR112012001118 A2 BR 112012001118A2 BR 112012001118 A BR112012001118 A BR 112012001118A BR 112012001118 A BR112012001118 A BR 112012001118A BR 112012001118 A2 BR112012001118 A2 BR 112012001118A2
Authority
BR
Brazil
Prior art keywords
oxy
fluorphenyl
ylpropyl
dicarboxamide
methyloxy
Prior art date
Application number
BR112012001118A
Other languages
English (en)
Portuguese (pt)
Inventor
Cannon Hilary
Igo David
Tran Tri
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 BR112012001118A2 publication Critical patent/BR112012001118A2/pt

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Classifications

    • 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
BR112012001118A 2009-07-17 2010-07-16 formas cristalinas de n-[3-flúor-4-({6-(metilóxi)-7-[(3-morfolin-4-ilpropil)óxi]-quinolin-4-il}óxi)fenil]-n'-(4-fluorfenil)ciclopropano-1,1-dicarboxamida, composição farmacêutica com as mesmas, métodos de preparação das mesmas e tratamento de câncer BR112012001118A2 (pt)

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
BR112012001118A2 true BR112012001118A2 (pt) 2016-02-23

Family

ID=42712017

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012001118A BR112012001118A2 (pt) 2009-07-17 2010-07-16 formas cristalinas de n-[3-flúor-4-({6-(metilóxi)-7-[(3-morfolin-4-ilpropil)óxi]-quinolin-4-il}óxi)fenil]-n'-(4-fluorfenil)ciclopropano-1,1-dicarboxamida, composição farmacêutica com as mesmas, métodos de preparação das mesmas e tratamento de câncer

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
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
CN102933551A (zh) * 2010-03-12 2013-02-13 埃克塞里艾克西斯公司 N-[3-氟-4-({6-(甲氧基)-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-1,1-二甲酰胺的水合结晶形式
EP2593090B1 (en) 2010-07-16 2021-10-13 Exelixis, Inc. C-met modulator pharmaceutical compositions
FI2621481T4 (fi) 2010-09-27 2023-01-13 Met- ja vegf-kaksoisestäjiä kastraatioresistentin eturauhassyövän ja osteoblastisten luun etäispesäkkeiden hoitamiseen
EA033513B1 (ru) 2011-02-10 2019-10-31 Exelixis Inc Способы получения хинолиновых соединений и фармацевтических композиций, содержащих такие соединения
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
BR212013028314U2 (pt) 2011-05-02 2015-11-03 Exelixis Inc método para tratar câncer e dor de câncer de osso
EP2758057B1 (en) 2011-09-22 2017-05-31 Exelixis, Inc. Method for treating osteoporosis
PT2768796T (pt) 2011-10-20 2020-02-21 Exelixis Inc Processo para a preparação de derivados de quinolina
EP2844254A1 (en) 2012-05-02 2015-03-11 Exelixis, Inc. A dual met - vegf modulator for treating osteolytic bone metastases
JP6389238B2 (ja) 2013-03-15 2018-09-12 エグゼリクシス， インコーポレイテッド Ｎ−（４−｛［６，７−ビス（メンチルオキシ）キノリン−４−イル］オキシ｝フェニル）−ｎ’−（４−フルオロフェニル）サイクロプロペイン−１，１−ジカルボキシアミドのメタボライト
US11564915B2 (en) 2013-04-04 2023-01-31 Exelixis, Inc. Cabozantinib dosage form and use in the treatment of cancer
BR112015025408A8 (pt) * 2013-04-04 2018-07-10 Exelixis Inc combinações de drogas para tratar câncer
MX384828B (es) 2014-02-14 2025-03-14 Exelixis Inc Formas solidas cristalinas de n-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-n'-(4-fluorofenil)ciclopropan-1,1-dicarboxamida, procesos para elaboracion y metodos de uso.
WO2015142928A1 (en) 2014-03-17 2015-09-24 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
MA40457A (fr) 2014-08-05 2017-06-14 Exelixis Inc Combinaison de médicaments pour traiter le myélome multiple
CA3020749A1 (en) 2016-04-15 2017-10-19 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
CN113292537B (zh) 2018-06-15 2024-04-05 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
AU2019403024A1 (en) * 2018-12-20 2021-07-15 Merck Sharp & Dohme Llc Novel 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
CN120417903A (zh) 2023-01-31 2025-08-01 汉达癌症医药责任有限公司 改良的卡博替尼组合物及其使用方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CA2744997A1 (en) * 2003-09-26 2005-04-07 Exelixis, Inc. C-met modulators and method of use
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
WO2011009095A1 (en) 2011-01-20
MX2012000809A (es) 2012-03-14
ZA201200389B (en) 2012-09-26
US8673912B2 (en) 2014-03-18
JP2012533570A (ja) 2012-12-27
CA2768370A1 (en) 2011-01-20
IL217537A0 (en) 2012-02-29
KR20120051702A (ko) 2012-05-22
AU2010274012A1 (en) 2012-02-09
EA201200144A1 (ru) 2012-08-30
EP2454238A1 (en) 2012-05-23
CN102510855A (zh) 2012-06-20
US20120270872A1 (en) 2012-10-25
WO2011009095A8 (en) 2011-03-24
NZ597695A (en) 2014-05-30
TW201118072A (en) 2011-06-01
CN102510855B (zh) 2015-11-25

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