EA201200144A1 - Кристаллические формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида - Google Patents
Кристаллические формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамидаInfo
- Publication number
- EA201200144A1 EA201200144A1 EA201200144A EA201200144A EA201200144A1 EA 201200144 A1 EA201200144 A1 EA 201200144A1 EA 201200144 A EA201200144 A EA 201200144A EA 201200144 A EA201200144 A EA 201200144A EA 201200144 A1 EA201200144 A1 EA 201200144A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- fluoro
- crystalline forms
- photorphenyl
- oxirinyl
- diparboxamide
- Prior art date
Links
- -1 methyloxyl Chemical group 0.000 title 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 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 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Reproductive Health (AREA)
- Gastroenterology & Hepatology (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Oncology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Quinoline Compounds (AREA)
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 |
|---|---|
| EA201200144A1 true EA201200144A1 (ru) | 2012-08-30 |
Family
ID=42712017
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201200144A EA201200144A1 (ru) | 2009-07-17 | 2010-07-16 | Кристаллические формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида |
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) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2651730T3 (es) * | 2003-09-26 | 2018-01-29 | Exelixis, Inc. | Moduladores c-Met y métodos de uso |
| CA2758030C (en) | 2009-01-16 | 2019-01-08 | Exelixis, Inc. | Malate salt of n-(4-{[6,7-bis(methyloxy)quin0lin-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 | |
| 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. |
| TWI619495B (zh) | 2010-07-16 | 2018-04-01 | 艾克塞里克斯公司 | Ｃ-ｍｅｔ調節劑醫藥組合物 |
| EP2621481B2 (en) | 2010-09-27 | 2022-10-19 | Exelixis, Inc. | Dual inhibitors of met and vegf for the treatment of castration-resistant prostate cancer and osteoblastic bone metastases |
| CA2826751C (en) | 2011-02-10 | 2021-05-18 | Exelixis, Inc. | Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds |
| US20120252840A1 (en) | 2011-04-04 | 2012-10-04 | Exelixis, Inc. | Method of Treating Cancer |
| MX2013012695A (es) | 2011-05-02 | 2014-03-27 | Exelixis Inc | Metodo para el tratamiento del cancer y el dolor por cancer de hueso. |
| KR20140069133A (ko) | 2011-09-22 | 2014-06-09 | 엑셀리시스, 인코포레이티드 | 골다공증의 치료방법 |
| 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 |
| BR112015023109A2 (pt) | 2013-03-15 | 2018-05-15 | Exelixis Inc | Metabolitos de n-(4-{[6,7-bis(metiloxi)quinoloin-4-il] oxi}fenil)-n -(4-fluorofenil)ciclopropano-1, 1- dicarboxamida |
| JP2016515628A (ja) * | 2013-04-04 | 2016-05-30 | エグゼリクシス， インコーポレイテッド | 癌を治療するための複合薬 |
| WO2014165786A1 (en) | 2013-04-04 | 2014-10-09 | Exelixis, Inc. | Cabozantinib dosage form and use in the treatment of cancer |
| CA2939546C (en) | 2014-02-14 | 2023-01-17 | 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 |
| MA40386A (fr) | 2014-07-31 | 2016-02-04 | Exelixis Inc | Procédé de préparation de cabozantinib marqué au fluor-18 et d'analogues de celui-ci |
| 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 |
| MX2018013764A (es) | 2016-05-16 | 2019-08-05 | Gb001 Inc | Cristal de derivado de quinolina. |
| TWI770624B (zh) | 2018-06-15 | 2022-07-11 | 漢達生技醫藥股份有限公司 | 尼洛替尼十二烷基硫酸鹽在製備用於治療慢性骨髓性白血病之劑型的用途 |
| 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 |
| AU2024215796A1 (en) | 2023-01-31 | 2025-05-15 | Handa Oncology, Llc | Improved cabozantinib compositions and methods of use |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003000660A1 (fr) | 2001-06-22 | 2003-01-03 | Kirin Beer Kabushiki Kaisha | Derive de quinoleine et derive de quinoleine permettant d'inhiber l'auto-phosphorylation du recepteur des proliferateurs des hepatocytes, ainsi que des compositions medicinales contenant ce derive |
| 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 |
| ES2651730T3 (es) * | 2003-09-26 | 2018-01-29 | Exelixis, Inc. | Moduladores c-Met y métodos de uso |
| EP2350011A1 (en) | 2008-11-13 | 2011-08-03 | Exelixis, Inc. | Methods of preparing quinoline derivatives |
-
2010
- 2010-07-16 WO PCT/US2010/042353 patent/WO2011009095A1/en not_active Ceased
- 2010-07-16 US US13/384,451 patent/US8673912B2/en active Active
- 2010-07-16 KR KR1020127004144A patent/KR20120051702A/ko not_active Withdrawn
- 2010-07-16 EA EA201200144A patent/EA201200144A1/ru unknown
- 2010-07-16 AU AU2010274012A patent/AU2010274012A1/en not_active Abandoned
- 2010-07-16 JP JP2012520827A patent/JP2012533570A/ja active Pending
- 2010-07-16 CA CA2768370A patent/CA2768370A1/en not_active Abandoned
- 2010-07-16 EP EP10737177A patent/EP2454238A1/en not_active Withdrawn
- 2010-07-16 BR BR112012001118A patent/BR112012001118A2/pt not_active IP Right Cessation
- 2010-07-16 TW TW099123569A patent/TW201118072A/zh unknown
- 2010-07-16 MX MX2012000809A patent/MX2012000809A/es not_active Application Discontinuation
- 2010-07-16 CN CN201080042037.0A patent/CN102510855B/zh not_active Expired - Fee Related
- 2010-07-16 NZ NZ597695A patent/NZ597695A/en not_active IP Right Cessation
-
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 |
|---|---|
| US8673912B2 (en) | 2014-03-18 |
| WO2011009095A1 (en) | 2011-01-20 |
| EP2454238A1 (en) | 2012-05-23 |
| CN102510855A (zh) | 2012-06-20 |
| TW201118072A (en) | 2011-06-01 |
| NZ597695A (en) | 2014-05-30 |
| BR112012001118A2 (pt) | 2016-02-23 |
| MX2012000809A (es) | 2012-03-14 |
| WO2011009095A8 (en) | 2011-03-24 |
| IL217537A0 (en) | 2012-02-29 |
| CN102510855B (zh) | 2015-11-25 |
| KR20120051702A (ko) | 2012-05-22 |
| JP2012533570A (ja) | 2012-12-27 |
| CA2768370A1 (en) | 2011-01-20 |
| ZA201200389B (en) | 2012-09-26 |
| US20120270872A1 (en) | 2012-10-25 |
| AU2010274012A1 (en) | 2012-02-09 |
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