AR080584A1 - Formas cristalinas hidratadas de n-(3-fluoro-4-({6-(metiloxi)-7-[(3-morfolin-4-ilpropil)oxi]-quinolin-4-il}oxi) fenil]-n'- (4-fluorofenil) ciclopropano-1,1-dicarboxiamida - Google Patents
Formas cristalinas hidratadas de n-(3-fluoro-4-({6-(metiloxi)-7-[(3-morfolin-4-ilpropil)oxi]-quinolin-4-il}oxi) fenil]-n'- (4-fluorofenil) ciclopropano-1,1-dicarboxiamidaInfo
- Publication number
- AR080584A1 AR080584A1 ARP110100801A ARP110100801A AR080584A1 AR 080584 A1 AR080584 A1 AR 080584A1 AR P110100801 A ARP110100801 A AR P110100801A AR P110100801 A ARP110100801 A AR P110100801A AR 080584 A1 AR080584 A1 AR 080584A1
- Authority
- AR
- Argentina
- Prior art keywords
- oxy
- quinolin
- fluorophenyl
- fluoro
- phenyl
- Prior art date
Links
- -1 4-FLUOROPHENYL Chemical class 0.000 title 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 title 1
- 239000013078 crystal Substances 0.000 title 1
- 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 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000007787 solid Substances 0.000 abstract 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 238000001237 Raman spectrum Methods 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 238000001460 carbon-13 nuclear magnetic resonance spectrum Methods 0.000 abstract 1
- 238000000806 fluorine-19 nuclear magnetic resonance spectrum Methods 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 230000036571 hydration Effects 0.000 abstract 1
- 238000006703 hydration reaction Methods 0.000 abstract 1
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 125000004549 quinolin-4-yl group Chemical group N1=CC=C(C2=CC=CC=C12)* 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07D215/22—Oxygen atoms attached in position 2 or 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Quinoline Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31319210P | 2010-03-12 | 2010-03-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080584A1 true AR080584A1 (es) | 2012-04-18 |
Family
ID=43875241
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100801A AR080584A1 (es) | 2010-03-12 | 2011-03-14 | Formas cristalinas hidratadas de n-(3-fluoro-4-({6-(metiloxi)-7-[(3-morfolin-4-ilpropil)oxi]-quinolin-4-il}oxi) fenil]-n'- (4-fluorofenil) ciclopropano-1,1-dicarboxiamida |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20130143881A1 (enExample) |
| EP (1) | EP2545038A1 (enExample) |
| JP (1) | JP2013522232A (enExample) |
| KR (1) | KR20130038206A (enExample) |
| CN (1) | CN102933551A (enExample) |
| AR (1) | AR080584A1 (enExample) |
| AU (1) | AU2011224203A1 (enExample) |
| CA (1) | CA2792852A1 (enExample) |
| EA (1) | EA201290906A1 (enExample) |
| MX (1) | MX2012010506A (enExample) |
| SG (1) | SG184040A1 (enExample) |
| TW (1) | TW201202228A (enExample) |
| WO (1) | WO2011112896A1 (enExample) |
| ZA (1) | ZA201206679B (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 | |
| 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 |
| 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 |
| KR20250136810A (ko) | 2023-01-31 | 2025-09-16 | 한다 온콜로지, 엘엘씨 | 개선된 카보잔티닙 조성물 및 사용 방법 |
Family Cites Families (2)
| 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 |
| BR112012001118A2 (pt) * | 2009-07-17 | 2016-02-23 | Exelixis Inc | 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 |
-
2011
- 2011-03-11 EA EA201290906A patent/EA201290906A1/ru unknown
- 2011-03-11 WO PCT/US2011/028035 patent/WO2011112896A1/en not_active Ceased
- 2011-03-11 CN CN2011800137314A patent/CN102933551A/zh active Pending
- 2011-03-11 AU AU2011224203A patent/AU2011224203A1/en not_active Abandoned
- 2011-03-11 KR KR1020127025322A patent/KR20130038206A/ko not_active Withdrawn
- 2011-03-11 JP JP2012557269A patent/JP2013522232A/ja active Pending
- 2011-03-11 US US13/634,275 patent/US20130143881A1/en not_active Abandoned
- 2011-03-11 MX MX2012010506A patent/MX2012010506A/es not_active Application Discontinuation
- 2011-03-11 EP EP11709589A patent/EP2545038A1/en not_active Withdrawn
- 2011-03-11 SG SG2012067732A patent/SG184040A1/en unknown
- 2011-03-11 TW TW100108394A patent/TW201202228A/zh unknown
- 2011-03-11 CA CA2792852A patent/CA2792852A1/en not_active Abandoned
- 2011-03-14 AR ARP110100801A patent/AR080584A1/es unknown
-
2012
- 2012-09-06 ZA ZA2012/06679A patent/ZA201206679B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EA201290906A1 (ru) | 2013-03-29 |
| TW201202228A (en) | 2012-01-16 |
| EP2545038A1 (en) | 2013-01-16 |
| CA2792852A1 (en) | 2011-09-15 |
| AU2011224203A1 (en) | 2012-10-04 |
| WO2011112896A1 (en) | 2011-09-15 |
| KR20130038206A (ko) | 2013-04-17 |
| SG184040A1 (en) | 2012-10-30 |
| MX2012010506A (es) | 2012-10-15 |
| ZA201206679B (en) | 2013-05-29 |
| US20130143881A1 (en) | 2013-06-06 |
| CN102933551A (zh) | 2013-02-13 |
| JP2013522232A (ja) | 2013-06-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |