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)
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2210607B1 (en) * | 2003-09-26 | 2011-08-17 | Exelixis Inc. | N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide for the treatment of cancer |
| TW201920110A (zh) | 2009-01-16 | 2019-06-01 | 美商艾克塞里克斯公司 | 包含n-(4-{[6,7-雙(甲氧基)喹啉-4-基]氧基}苯基)-n'-(4-氟苯基)環丙烷-1,1-二甲醯胺之蘋果酸鹽之醫藥組合物及其用途 |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| EA201290906A1 (ru) * | 2010-03-12 | 2013-03-29 | Экселиксис, Инк. | Кристаллогидратные 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 |
| WO2012009722A1 (en) | 2010-07-16 | 2012-01-19 | Exelixis, Inc. | C-met modulator pharmaceutical compositions |
| HUE045810T2 (hu) | 2010-09-27 | 2020-01-28 | Exelixis Inc | MET és VEGF kettõs inhibitorai kasztrációrezisztens prosztatarák és oszteoblasztos csontáttétek kezelésére |
| TW201309650A (zh) | 2011-02-10 | 2013-03-01 | 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 |
| EP2704717A1 (en) | 2011-05-02 | 2014-03-12 | Exelixis, Inc. | Method of treating cancer and bone cancer pain |
| GEP201606523B (en) | 2011-09-22 | 2016-08-10 | Exelixis Inc | Method for treating osteoporosis |
| PL2768796T3 (pl) | 2011-10-20 | 2020-05-18 | Exelixis, Inc. | Sposób wytwarzania pochodnych chinoliny |
| HK1207587A1 (en) | 2012-05-02 | 2016-02-05 | Exelixis, Inc. | A dual met - vegf modulator for treating osteolytic bone metastases |
| 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 |
| EP2983639A1 (en) * | 2013-04-04 | 2016-02-17 | Exelixis, Inc. | Drug combinations to treat cancer |
| ES2927651T3 (es) | 2013-04-04 | 2022-11-10 | Exelixis Inc | Forma de dosificación de cabozantinib y uso en el tratamiento del cáncer |
| EA032757B1 (ru) | 2014-02-14 | 2019-07-31 | Экселиксис, Инк. | Кристаллические твердые формы n-{4-[(6,7-диметоксихинолин-4-ил)окси]фенил}-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, способы получения и способы применения |
| CN106255499A (zh) | 2014-03-17 | 2016-12-21 | 埃克塞里艾克西斯公司 | 卡博替尼制剂的给药 |
| EA033834B1 (ru) | 2014-07-31 | 2019-11-29 | Exelixis Inc | Способ получения кабозантиниба, меченного фтором-18, и его аналогов |
| MA40457A (fr) | 2014-08-05 | 2017-06-14 | Exelixis Inc | Combinaison de médicaments pour traiter le myélome multiple |
| US11141413B2 (en) | 2016-04-15 | 2021-10-12 | Exelixis, Inc. | Method of treating renal cell carcinoma using N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (2S)-hydroxybutanedioate |
| US20190276405A1 (en) * | 2016-05-16 | 2019-09-12 | Pulmagen Therapeutics (Asthma) Limited | Crystal of quinoline derivative |
| TWI787523B (zh) | 2018-06-15 | 2022-12-21 | 漢達生技醫藥股份有限公司 | 達沙替尼十二烷基硫酸鹽之結晶 |
| EP3897660A4 (en) * | 2018-12-20 | 2022-09-07 | Merck Sharp & Dohme Corp. | NEW 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 |
| KR20250136810A (ko) | 2023-01-31 | 2025-09-16 | 한다 온콜로지, 엘엘씨 | 개선된 카보잔티닙 조성물 및 사용 방법 |
Family Cites Families (4)
| 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 |
| EP2210607B1 (en) * | 2003-09-26 | 2011-08-17 | Exelixis Inc. | N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide for the treatment of cancer |
| CA2743416A1 (en) | 2008-11-13 | 2010-05-20 | Exelixis Inc. | Methods of preparing quinoline derivatives |
-
2010
- 2010-07-16 BR BR112012001118A patent/BR112012001118A2/pt not_active IP Right Cessation
- 2010-07-16 CA CA2768370A patent/CA2768370A1/en not_active Abandoned
- 2010-07-16 CN CN201080042037.0A patent/CN102510855B/zh not_active Expired - Fee Related
- 2010-07-16 MX MX2012000809A patent/MX2012000809A/es not_active Application Discontinuation
- 2010-07-16 AU AU2010274012A patent/AU2010274012A1/en not_active Abandoned
- 2010-07-16 EA EA201200144A patent/EA201200144A1/ru unknown
- 2010-07-16 US US13/384,451 patent/US8673912B2/en active Active
- 2010-07-16 NZ NZ597695A patent/NZ597695A/en not_active IP Right Cessation
- 2010-07-16 JP JP2012520827A patent/JP2012533570A/ja active Pending
- 2010-07-16 WO PCT/US2010/042353 patent/WO2011009095A1/en not_active Ceased
- 2010-07-16 KR KR1020127004144A patent/KR20120051702A/ko not_active Withdrawn
- 2010-07-16 EP EP10737177A patent/EP2454238A1/en not_active Withdrawn
- 2010-07-16 TW TW099123569A patent/TW201118072A/zh unknown
-
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 |
| ZA201200389B (en) | 2012-09-26 |
| AU2010274012A1 (en) | 2012-02-09 |
| NZ597695A (en) | 2014-05-30 |
| CA2768370A1 (en) | 2011-01-20 |
| JP2012533570A (ja) | 2012-12-27 |
| CN102510855B (zh) | 2015-11-25 |
| IL217537A0 (en) | 2012-02-29 |
| EP2454238A1 (en) | 2012-05-23 |
| US20120270872A1 (en) | 2012-10-25 |
| CN102510855A (zh) | 2012-06-20 |
| MX2012000809A (es) | 2012-03-14 |
| WO2011009095A8 (en) | 2011-03-24 |
| WO2011009095A1 (en) | 2011-01-20 |
| KR20120051702A (ko) | 2012-05-22 |
| BR112012001118A2 (pt) | 2016-02-23 |
| TW201118072A (en) | 2011-06-01 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EA201290906A1 (ru) | Кристаллогидратные 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 | |
| MX2012000809A (es) | Formas cristalinas de n-[3-fluoro-4-({6-(metiloxi)-7-[(3-morfolin- 4-ilpropil)oxi]-quinolin-4-il}oxi)fenil]-n'-(4-fluorofenil)ciclop ropan-1,1-dicarboxamida. | |
| EA201400110A1 (ru) | Малатная соль n-(4-{[6,7-бис-(метилокси)хинолин-4-ил]окси}фенил-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида и ее кристаллические формы для лечения рака | |
| EA201690752A1 (ru) | Ингибиторы g12c kras | |
| MX2019013954A (es) | Inhibidores covalentes de kras. | |
| EA201490696A1 (ru) | 3-пиримидин-4-ил-оксазолидин-2-оны в качестве ингибиторов мутантной idh | |
| MX2013012588A (es) | Inhibidores de cinasa. | |
| EA201792214A1 (ru) | Соединения замещенного хиназолина | |
| EA201891091A1 (ru) | Соединения ингибитора jak киназы для лечения респираторного заболевания | |
| RU2013156378A (ru) | 4-амино-5-фтор-3-[6-(4-метилпиперазин-1-ил)-1н-бензимидазол-2-ил]-1н-хинолин-2-он для применения при лечении аденокистозной карциномы | |
| EA201291348A1 (ru) | Активаторы растворимой гуанилатциклазы | |
| EA201390766A1 (ru) | БЕНЗОКСАЗЕПИНЫ КАК ИНГИБИТОРЫ PI3K/mTOR И СПОСОБЫ ИХ ИСПОЛЬЗОВАНИЯ И ПОЛУЧЕНИЯ | |
| EA201500266A1 (ru) | Ингибиторы репликации вирусов гриппа | |
| EA201200472A1 (ru) | Сульфонамиды в качестве ингибиторов белков семейства bcl-2, предназначенные для лечения рака | |
| EA201500293A1 (ru) | Антихолинэргическая нейропротективная композиция и способы | |
| EA201400963A1 (ru) | Фармацевтический препарат, содержащий производное дигидрохиназолина с противовирусной активностью | |
| EA201600337A1 (ru) | 2,6-замещенные пуриновые производные и их применение в лечении пролиферативных заболеваний | |
| BR112012033117A2 (pt) | pirazolo[1,5-a]pirimidinas como agentes antivirais | |
| BR112014011981A2 (pt) | formulações farmacêuticas | |
| EA201590074A1 (ru) | Производное бензодиоксола, способ его получения и его применение | |
| JOP20200079A1 (ar) | مثبطات مستقبل عامل نمو البشرة | |
| MX2014014066A (es) | Compuestos de cromano. | |
| NZ702835A (en) | 3-o-heteroaryl-ingenol | |
| IN2014KN01113A (cg-RX-API-DMAC10.html) | ||
| EA201401238A1 (ru) | Фторзамещенные (3r,4r,5s)-5-гуанидино-4-ациламино-3-(пентан-3-илокси)циклогексен-1-карбоновые кислоты, их эфиры и способ применения |