JP2012533570A - N−[3−フルオロ−4−({6−(メチルオキシ)−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−ジカルボキサミドの結晶形 - Google Patents

N−[3−フルオロ−4−({6−(メチルオキシ)−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−ジカルボキサミドの結晶形 Download PDF

Info

Publication number
JP2012533570A
JP2012533570A JP2012520827A JP2012520827A JP2012533570A JP 2012533570 A JP2012533570 A JP 2012533570A JP 2012520827 A JP2012520827 A JP 2012520827A JP 2012520827 A JP2012520827 A JP 2012520827A JP 2012533570 A JP2012533570 A JP 2012533570A
Authority
JP
Japan
Prior art keywords
oxy
methyloxy
fluoro
ylpropyl
cyclopropane
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.)
Pending
Application number
JP2012520827A
Other languages
English (en)
Japanese (ja)
Other versions
JP2012533570A5 (OSRAM
Inventor
ヒラリー キャノン,
デイビッド イゴ,
トリ トラン,
Original Assignee
エグゼリクシス, インコーポレイテッド
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 エグゼリクシス, インコーポレイテッド filed Critical エグゼリクシス, インコーポレイテッド
Publication of JP2012533570A publication Critical patent/JP2012533570A/ja
Publication of JP2012533570A5 publication Critical patent/JP2012533570A5/ja
Pending legal-status Critical Current

Links

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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (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)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
JP2012520827A 2009-07-17 2010-07-16 N−[3−フルオロ−4−({6−(メチルオキシ)−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−ジカルボキサミドの結晶形 Pending JP2012533570A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22650909P 2009-07-17 2009-07-17
US61/226,509 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
JP2012533570A true JP2012533570A (ja) 2012-12-27
JP2012533570A5 JP2012533570A5 (OSRAM) 2013-08-29

Family

ID=42712017

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012520827A Pending JP2012533570A (ja) 2009-07-17 2010-07-16 N−[3−フルオロ−4−({6−(メチルオキシ)−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−ジカルボキサミドの結晶形

Country Status (15)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017199903A1 (ja) * 2016-05-16 2017-11-23 帝人ファーマ株式会社 キノリン誘導体の結晶

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005030140A2 (en) 2003-09-26 2005-04-07 Exelixis, Inc. C-met modulators and methods 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
MX2012010506A (es) * 2010-03-12 2012-10-15 Exelixis Inc Formas cristalinas hidratadas del n-[3-fluoro-4-({6-(metiloxi)-7-[ (3-morfolin-4-ilpropil)oxi]-quinolin-4-il}oxi)fenil]-n'-(4-fluoro fenil)ciclopropano-1,1-dicarboxamida.
SG187060A1 (en) 2010-07-16 2013-02-28 Exelixis Inc C-met modulator pharmaceutical compositions
US20140057943A1 (en) 2010-09-27 2014-02-27 Exelixix, Inc. Method of Treating Cancer
KR20230158644A (ko) 2011-02-10 2023-11-20 엑셀리시스, 인코포레이티드 퀴놀린 화합물들의 제조 방법들 및 상기 화합물들을 함유하는 약학 조성물들
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
WO2012151326A1 (en) 2011-05-02 2012-11-08 Exelixis, Inc. Method of treating cancer and bone cancer pain
CA2848512A1 (en) 2011-09-22 2013-03-28 Exelixis, Inc. Method for treating osteoporosis
BR112014009302B1 (pt) 2011-10-20 2020-04-28 Exelis Inc Us/Us processo para preparar derivados de quinolina
US9861624B2 (en) 2012-05-02 2018-01-09 Exelixis, Inc. Method of treating cancer
GEP20196995B (en) 2013-03-15 2019-07-25 Inc Exelixis Metabolites of n-(4-{[6,7-bis (methyloxy)quinolin-4-yl] oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide
ES2927651T3 (es) 2013-04-04 2022-11-10 Exelixis Inc Forma de dosificación de cabozantinib y uso en el tratamiento del cáncer
AU2014248001A1 (en) * 2013-04-04 2015-11-19 Exelixis, Inc. Drug combinations to treat cancer
EP3738952A1 (en) 2014-02-14 2020-11-18 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
JP6666849B2 (ja) 2014-03-17 2020-03-18 エグゼリクシス, インコーポレイテッド カボザンチニブ製剤の投与
EP3174854B1 (en) 2014-07-31 2022-08-24 Exelixis, Inc. Method of preparing fluorine-18 labeled cabozantinib and its analogs
CN106573042A (zh) 2014-08-05 2017-04-19 埃克塞里艾克西斯公司 治疗多发性骨髓瘤的药物组合
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
EP3806858A4 (en) 2018-06-15 2022-03-09 Handa Pharmaceuticals, Inc. KINA INHIBITOR SALTS AND COMPOSITIONS THEREOF
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
EP4658271A1 (en) 2023-01-31 2025-12-10 Handa Oncology, LLC Improved cabozantinib compositions and methods of use

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007506777A (ja) * 2003-09-26 2007-03-22 エグゼリクシス, インコーポレイテッド c−Metモジュレーターおよびその使用

Family Cites Families (3)

* 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
WO2010056960A1 (en) 2008-11-13 2010-05-20 Exelixis Inc. Methods of preparing quinoline derivatives

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007506777A (ja) * 2003-09-26 2007-03-22 エグゼリクシス, インコーポレイテッド c−Metモジュレーターおよびその使用

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017199903A1 (ja) * 2016-05-16 2017-11-23 帝人ファーマ株式会社 キノリン誘導体の結晶
JPWO2017199903A1 (ja) * 2016-05-16 2019-02-28 帝人ファーマ株式会社 キノリン誘導体の結晶
US10626089B2 (en) 2016-05-16 2020-04-21 GBOO1, Inc. Quinoline derivative in crystal form

Also Published As

Publication number Publication date
EA201200144A1 (ru) 2012-08-30
CN102510855B (zh) 2015-11-25
WO2011009095A8 (en) 2011-03-24
MX2012000809A (es) 2012-03-14
AU2010274012A1 (en) 2012-02-09
ZA201200389B (en) 2012-09-26
US20120270872A1 (en) 2012-10-25
US8673912B2 (en) 2014-03-18
BR112012001118A2 (pt) 2016-02-23
IL217537A0 (en) 2012-02-29
KR20120051702A (ko) 2012-05-22
TW201118072A (en) 2011-06-01
CA2768370A1 (en) 2011-01-20
CN102510855A (zh) 2012-06-20
WO2011009095A1 (en) 2011-01-20
NZ597695A (en) 2014-05-30
EP2454238A1 (en) 2012-05-23

Similar Documents

Publication Publication Date Title
JP2012533570A (ja) N−[3−フルオロ−4−({6−(メチルオキシ)−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−ジカルボキサミドの結晶形
JP6756617B2 (ja) N−{4−[(6,7−ジメトキシキノリン−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−ジカルボキサミドの結晶性固体形態、製造プロセス、及び使用方法
JP6931372B2 (ja) N−(4−{[6,7−ビス(メチルオキシ)キノリン−4−イル]オキシ}フェニル)−n’−(4−フルオロフェニル)シクロプロパン−1,1−ジカルボキサミドのリンゴ酸塩およびその結晶質形態
JP2017505796A5 (OSRAM)
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
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

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130712

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20130712

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20140725

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20150114