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)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (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 |
|---|---|---|---|---|
| RS52754B2 (sr) | 2009-01-16 | 2022-08-31 | Exelixis Inc | Malat so n-(4- {[6,7-bis(metiloksi)hinolin-4-il]oksi}fenil-n'- (4-fluorofenil) ciklopropan-1,1-dikarboksamid-a, i njeni kristalni oblici za lečenje karcinoma |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| KR20180056807A (ko) | 2010-07-16 | 2018-05-29 | 엑셀리시스, 인코포레이티드 | C-met 조절제 약제학적 조성물 |
| PL2621481T5 (pl) | 2010-09-27 | 2023-03-13 | Exelixis, Inc. | Podwójne inhibitory MET i VEGF do leczenia opornego na kastrację raka prostaty i osteoblastycznych przerzutów do kości |
| 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 |
| JP2014513129A (ja) | 2011-05-02 | 2014-05-29 | エクセリクシス， インク． | 癌および骨癌疼痛の治療方法 |
| EP2758057B1 (en) | 2011-09-22 | 2017-05-31 | Exelixis, Inc. | Method for treating osteoporosis |
| CN104395284A (zh) | 2011-10-20 | 2015-03-04 | 埃克塞里艾克西斯公司 | 制备喹啉衍生物的方法 |
| 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 |
| 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 |
| WO2015142928A1 (en) | 2014-03-17 | 2015-09-24 | Exelixis, Inc. | Dosing of cabozantinib formulations |
| 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 |
| EA034992B1 (ru) | 2014-08-05 | 2020-04-15 | Экселиксис, Инк. | Комбинации лекарственных средств для лечения множественной миеломы |
| EP3442531A1 (en) | 2016-04-15 | 2019-02-20 | Exelixis, Inc. | Method of treating renal cell carcinoma using n-(4-(6,7-dimethoxyquinolin-4-yloxy) phenyl)-n'-(4-fluoropheny)cyclopropane-1,1-dicarboxamide, (2s)-hydroxybutanedioate |
| JP6906510B2 (ja) | 2016-05-16 | 2021-07-21 | 帝人ファーマ株式会社 | キノリン誘導体の結晶 |
| AU2019285066B2 (en) | 2018-06-15 | 2024-06-13 | Handa Pharmaceuticals, Inc. | Kinase inhibitor salts and compositions thereof |
| EP4658271A1 (en) | 2023-01-31 | 2025-12-10 | Handa Oncology, LLC | Improved cabozantinib compositions and methods of use |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2392565B1 (en) | 2003-09-26 | 2014-03-19 | Exelixis, Inc. | c-Met modulators and methods of use |
| EP2454238A1 (en) * | 2009-07-17 | 2012-05-23 | Exelixis, Inc. | 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 |
-
2011
- 2011-03-11 CN CN2011800137314A patent/CN102933551A/zh active Pending
- 2011-03-11 EA EA201290906A patent/EA201290906A1/ru unknown
- 2011-03-11 AU AU2011224203A patent/AU2011224203A1/en not_active Abandoned
- 2011-03-11 CA CA2792852A patent/CA2792852A1/en not_active Abandoned
- 2011-03-11 US US13/634,275 patent/US20130143881A1/en not_active Abandoned
- 2011-03-11 TW TW100108394A patent/TW201202228A/zh unknown
- 2011-03-11 JP JP2012557269A patent/JP2013522232A/ja active Pending
- 2011-03-11 MX MX2012010506A patent/MX2012010506A/es not_active Application Discontinuation
- 2011-03-11 SG SG2012067732A patent/SG184040A1/en unknown
- 2011-03-11 KR KR1020127025322A patent/KR20130038206A/ko not_active Withdrawn
- 2011-03-11 EP EP11709589A patent/EP2545038A1/en not_active Withdrawn
- 2011-03-11 WO PCT/US2011/028035 patent/WO2011112896A1/en not_active Ceased
- 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 |
|---|---|
| MX2012010506A (es) | 2012-10-15 |
| KR20130038206A (ko) | 2013-04-17 |
| US20130143881A1 (en) | 2013-06-06 |
| EA201290906A1 (ru) | 2013-03-29 |
| EP2545038A1 (en) | 2013-01-16 |
| ZA201206679B (en) | 2013-05-29 |
| TW201202228A (en) | 2012-01-16 |
| WO2011112896A1 (en) | 2011-09-15 |
| AU2011224203A1 (en) | 2012-10-04 |
| CN102933551A (zh) | 2013-02-13 |
| CA2792852A1 (en) | 2011-09-15 |
| JP2013522232A (ja) | 2013-06-13 |
| SG184040A1 (en) | 2012-10-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |