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 (https=) |
| EP (1) | EP2545038A1 (https=) |
| JP (1) | JP2013522232A (https=) |
| KR (1) | KR20130038206A (https=) |
| CN (1) | CN102933551A (https=) |
| AR (1) | AR080584A1 (https=) |
| AU (1) | AU2011224203A1 (https=) |
| CA (1) | CA2792852A1 (https=) |
| EA (1) | EA201290906A1 (https=) |
| MX (1) | MX2012010506A (https=) |
| SG (1) | SG184040A1 (https=) |
| TW (1) | TW201202228A (https=) |
| WO (1) | WO2011112896A1 (https=) |
| ZA (1) | ZA201206679B (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG173014A1 (en) | 2009-01-16 | 2011-08-29 | 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 therof 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 | |
| EP2593090B1 (en) | 2010-07-16 | 2021-10-13 | Exelixis, Inc. | C-met modulator pharmaceutical compositions |
| CA2812750C (en) | 2010-09-27 | 2020-10-06 | Exelixis, Inc. | Dual inhibitors of met and vegf for the treatment of castration-resistant prostate cancer and osteoblastic bone metastases |
| JP2014505109A (ja) | 2011-02-10 | 2014-02-27 | エクセリクシス， インク． | キノリン化合物およびそのような化合物を含有する医薬組成物の調製方法 |
| US20120252840A1 (en) | 2011-04-04 | 2012-10-04 | Exelixis, Inc. | Method of Treating Cancer |
| KR20140025496A (ko) | 2011-05-02 | 2014-03-04 | 엑셀리시스, 인코포레이티드 | 암 및 뼈 암 통증의 치료방법 |
| GEP201606523B (en) | 2011-09-22 | 2016-08-10 | Exelixis Inc | Method for treating osteoporosis |
| DK2768796T3 (da) | 2011-10-20 | 2020-02-24 | Exelixis Inc | Fremgangsmåde til fremstilling af quinolin-derivater |
| JP2015515988A (ja) | 2012-05-02 | 2015-06-04 | エクセリクシス， インク． | 溶骨性骨転移を治療するためのｍｅｔ−ｖｅｇｆ二重調節剤 |
| AU2014232714B2 (en) | 2013-03-15 | 2018-07-19 | Exelixis, Inc. | Metabolites of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide |
| EP2981263B1 (en) | 2013-04-04 | 2022-06-29 | Exelixis, Inc. | Cabozantinib dosage form and use in the treatment of cancer |
| KR102354963B1 (ko) | 2014-02-14 | 2022-01-21 | 엑셀리시스, 인코포레이티드 | N-｛4-[(6,7-다이메톡시퀴놀린-4-일)옥시]페닐｝-n'-(4-플루오로페닐) 사이클로프로판-1,1-다이카복스아마이드의 결정질 고체 형태, 제조 방법 및 사용 방법 |
| EA201691850A1 (ru) | 2014-03-17 | 2016-12-30 | Экселиксис, Инк. | Дозирование составов, содержащих кабозантиниб |
| ES2929888T3 (es) | 2014-07-31 | 2022-12-02 | Exelixis Inc | Procedimiento para preparar cabozantinib marcado con flúor 18 y sus análogos |
| BR112017002318A2 (pt) | 2014-08-05 | 2018-07-17 | Exelixis, Inc. | combinações de fármacos para tratar mieloma múltiplo. |
| RU2748549C2 (ru) | 2016-04-15 | 2021-05-26 | Экселиксис, Инк. | Способ лечения почечно-клеточного рака с использованием n-(4-(6,7-диметоксихинолин-4-илокси)фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, (2s)-гидроксибутандиоата |
| CA3025049A1 (en) | 2016-05-16 | 2017-11-23 | Pulmagen Therapeutics (Asthma) Limited | Crystal of quinoline derivative |
| CN113292537B (zh) | 2018-06-15 | 2024-04-05 | 汉达癌症医药责任有限公司 | 激酶抑制剂的盐类及其组合物 |
| TW202444365A (zh) | 2023-01-31 | 2024-11-16 | 漢達生技醫藥股份有限公司 | 改良之卡博替尼組合物及其使用方法 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2213661E (pt) * | 2003-09-26 | 2011-12-15 | Exelixis Inc | Moduladores de c-met e métodos de uso |
| JP2012533570A (ja) * | 2009-07-17 | 2012-12-27 | エグゼリクシス， インコーポレイテッド | Ｎ−［３−フルオロ−４−（｛６−（メチルオキシ）−７−［（３−モルホリン−４−イルプロピル）オキシ］−キノリン−４−イル｝オキシ）フェニル］−ｎ’−（４−フルオロフェニル）シクロプロパン−１，１−ジカルボキサミドの結晶形 |
-
2011
- 2011-03-11 CA CA2792852A patent/CA2792852A1/en not_active Abandoned
- 2011-03-11 AU AU2011224203A patent/AU2011224203A1/en not_active Abandoned
- 2011-03-11 MX MX2012010506A patent/MX2012010506A/es not_active Application Discontinuation
- 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 EP EP11709589A patent/EP2545038A1/en not_active Withdrawn
- 2011-03-11 CN CN2011800137314A patent/CN102933551A/zh active Pending
- 2011-03-11 SG SG2012067732A patent/SG184040A1/en unknown
- 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 TW TW100108394A patent/TW201202228A/zh unknown
- 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 |
|---|---|
| KR20130038206A (ko) | 2013-04-17 |
| JP2013522232A (ja) | 2013-06-13 |
| CN102933551A (zh) | 2013-02-13 |
| ZA201206679B (en) | 2013-05-29 |
| US20130143881A1 (en) | 2013-06-06 |
| EA201290906A1 (ru) | 2013-03-29 |
| WO2011112896A1 (en) | 2011-09-15 |
| SG184040A1 (en) | 2012-10-30 |
| TW201202228A (en) | 2012-01-16 |
| MX2012010506A (es) | 2012-10-15 |
| CA2792852A1 (en) | 2011-09-15 |
| AU2011224203A1 (en) | 2012-10-04 |
| EP2545038A1 (en) | 2013-01-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |