TW201118072A - 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 - Google Patents
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 Download PDFInfo
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- TW201118072A TW201118072A TW099123569A TW99123569A TW201118072A TW 201118072 A TW201118072 A TW 201118072A TW 099123569 A TW099123569 A TW 099123569A TW 99123569 A TW99123569 A TW 99123569A TW 201118072 A TW201118072 A TW 201118072A
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- CXQHYVUVSFXTMY-UHFFFAOYSA-N N1'-[3-fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide Chemical compound C1=CN=C2C=C(OCCCN3CCOCC3)C(OC)=CC2=C1OC(C(=C1)F)=CC=C1NC(=O)C1(C(=O)NC=2C=CC(F)=CC=2)CC1 CXQHYVUVSFXTMY-UHFFFAOYSA-N 0.000 title abstract description 3
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- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 16
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- 206010055031 vascular neoplasm Diseases 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
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)
- 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)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22650909P | 2009-07-17 | 2009-07-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW201118072A true TW201118072A (en) | 2011-06-01 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| TW099123569A TW201118072A (en) | 2009-07-17 | 2010-07-16 | 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 |
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)
| 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 |
| 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 |
| 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 |
Family Cites Families (4)
| 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 |
| WO2005030140A2 (en) * | 2003-09-26 | 2005-04-07 | Exelixis, Inc. | C-met modulators and methods of use |
| WO2010056960A1 (en) | 2008-11-13 | 2010-05-20 | Exelixis Inc. | Methods of preparing quinoline derivatives |
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2010
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- 2010-07-16 AU AU2010274012A patent/AU2010274012A1/en not_active Abandoned
- 2010-07-16 BR BR112012001118A patent/BR112012001118A2/pt not_active IP Right Cessation
- 2010-07-16 US US13/384,451 patent/US8673912B2/en active Active
- 2010-07-16 TW TW099123569A patent/TW201118072A/zh unknown
- 2010-07-16 CN CN201080042037.0A patent/CN102510855B/zh not_active Expired - Fee Related
- 2010-07-16 CA CA2768370A patent/CA2768370A1/en not_active Abandoned
- 2010-07-16 MX MX2012000809A patent/MX2012000809A/es not_active Application Discontinuation
- 2010-07-16 KR KR1020127004144A patent/KR20120051702A/ko not_active Withdrawn
- 2010-07-16 EA EA201200144A patent/EA201200144A1/ru unknown
- 2010-07-16 NZ NZ597695A patent/NZ597695A/en not_active IP Right Cessation
- 2010-07-16 WO PCT/US2010/042353 patent/WO2011009095A1/en not_active Ceased
- 2010-07-16 EP EP10737177A patent/EP2454238A1/en not_active Withdrawn
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2012
- 2012-01-15 IL IL217537A patent/IL217537A0/en unknown
- 2012-01-18 ZA ZA2012/00389A patent/ZA201200389B/en unknown
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 |
| JP2012533570A (ja) | 2012-12-27 |
| BR112012001118A2 (pt) | 2016-02-23 |
| IL217537A0 (en) | 2012-02-29 |
| KR20120051702A (ko) | 2012-05-22 |
| 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 |
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