JP2013522232A5 - - Google Patents
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- Publication number
- JP2013522232A5 JP2013522232A5 JP2012557269A JP2012557269A JP2013522232A5 JP 2013522232 A5 JP2013522232 A5 JP 2013522232A5 JP 2012557269 A JP2012557269 A JP 2012557269A JP 2012557269 A JP2012557269 A JP 2012557269A JP 2013522232 A5 JP2013522232 A5 JP 2013522232A5
- Authority
- JP
- Japan
- Prior art keywords
- oxy
- cancer
- methyloxy
- morpholin
- fluorophenyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 30
- 206010028980 Neoplasm Diseases 0.000 claims description 18
- 201000011510 cancer Diseases 0.000 claims description 18
- 238000000034 method Methods 0.000 claims description 16
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 8
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 8
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims description 8
- 239000007787 solid Substances 0.000 claims description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 8
- -1 3-morpholin-4-ylpropyl Chemical group 0.000 claims description 6
- 230000036571 hydration Effects 0.000 claims description 6
- 238000006703 hydration reaction Methods 0.000 claims description 6
- 206010041823 squamous cell carcinoma Diseases 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 4
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 206010009944 Colon cancer Diseases 0.000 claims description 4
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 4
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 206010063916 Metastatic gastric cancer Diseases 0.000 claims description 4
- 206010060862 Prostate cancer Diseases 0.000 claims description 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 4
- 238000001237 Raman spectrum Methods 0.000 claims description 4
- 206010038389 Renal cancer Diseases 0.000 claims description 4
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 4
- 238000001460 carbon-13 nuclear magnetic resonance spectrum Methods 0.000 claims description 4
- 238000000806 fluorine-19 nuclear magnetic resonance spectrum Methods 0.000 claims description 4
- 125000001207 fluorophenyl group Chemical group 0.000 claims description 4
- 206010017758 gastric cancer Diseases 0.000 claims description 4
- 201000010536 head and neck cancer Diseases 0.000 claims description 4
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 4
- 201000011066 hemangioma Diseases 0.000 claims description 4
- 201000010982 kidney cancer Diseases 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- 208000025113 myeloid leukemia Diseases 0.000 claims description 4
- 239000000843 powder Substances 0.000 claims description 4
- 201000011549 stomach cancer Diseases 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 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 claims description 2
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 2
- 239000007864 aqueous solution Substances 0.000 claims description 2
- 239000003125 aqueous solvent Substances 0.000 claims description 2
- 201000010279 papillary renal cell carcinoma Diseases 0.000 claims description 2
- 201000010941 papillary squamous carcinoma Diseases 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 14
- 238000004519 manufacturing process Methods 0.000 description 2
- 125000004549 quinolin-4-yl group Chemical group N1=CC=C(C2=CC=CC=C12)* 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31319210P | 2010-03-12 | 2010-03-12 | |
| US61/313,192 | 2010-03-12 | ||
| PCT/US2011/028035 WO2011112896A1 (en) | 2010-03-12 | 2011-03-11 | Hydrated 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013522232A JP2013522232A (ja) | 2013-06-13 |
| JP2013522232A5 true JP2013522232A5 (enExample) | 2014-04-24 |
Family
ID=43875241
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012557269A Pending JP2013522232A (ja) | 2010-03-12 | 2011-03-11 | Ｎ−［３−フルオロ−４−（｛６−（メチロキシ）−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−ジカルボサミドの水和結晶性形状 |
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 |
|---|---|---|---|---|
| NZ779754A (en) | 2009-01-16 | 2023-04-28 | Exelixis Inc | Malate salt of n-(4-{ [6,7-bis(methyloxy)quinolin-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 | |
| EA030435B1 (ru) | 2010-07-16 | 2018-08-31 | Экселиксис, Инк. | ТАБЛЕТКА, СОДЕРЖАЩАЯ МОДУЛЯТОР c-MET В ФОРМЕ КРИСТАЛЛИЧЕСКОЙ L-МАЛАТНОЙ СОЛИ (ВАРИАНТЫ), СПОСОБ ЕЕ ПРОИЗВОДСТВА И СПОСОБ ЛЕЧЕНИЯ ОНКОЛОГИЧЕСКОГО ЗАБОЛЕВАНИЯ С ЕЕ ИСПОЛЬЗОВАНИЕМ |
| MX352926B (es) | 2010-09-27 | 2017-12-14 | Exelixis Inc | Inhibidores dobles de met y factor de crecimiento endotelial vascular (vegf) para el tratamiento de cancer de prostata resistente a la castracion y metastasis osteoblasticas en los huesos. |
| BR112013020362A2 (pt) | 2011-02-10 | 2018-05-29 | Exelixis Inc | processos para a preparação de compostos de quinolina, compostos e combinações farmacêuticas que os contem |
| 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. |
| 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 |
| WO2013166296A1 (en) | 2012-05-02 | 2013-11-07 | Exelixis, Inc. | A dual met - vegf modulator for treating osteolytic bone metastases |
| CA2907334C (en) | 2013-03-15 | 2021-12-07 | Exelixis, Inc. | Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
| US11564915B2 (en) | 2013-04-04 | 2023-01-31 | Exelixis, Inc. | Cabozantinib dosage form and use in the treatment of cancer |
| BR112016018450A2 (pt) | 2014-02-14 | 2018-09-18 | Exelixis Inc | formas sólidas cristalinas de n-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-n'-(4-fluorofenil)ciclopropano-1,1-dicarboxamida, processos de preparo e métodos de uso |
| EP3119476A1 (en) | 2014-03-17 | 2017-01-25 | Exelixis, Inc. | Dosing of cabozantinib formulations |
| EP3174854B1 (en) | 2014-07-31 | 2022-08-24 | Exelixis, Inc. | Method of preparing fluorine-18 labeled cabozantinib and its analogs |
| MX382904B (es) | 2014-08-05 | 2025-03-13 | Exelixis Inc | Combinaciones de fármacos para tratar mieloma múltiple. |
| 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 |
| EP3476835A4 (en) * | 2016-05-16 | 2020-01-01 | GB001, Inc. | CRYSTAL OF A CHINOLINID DERIVATIVE |
| TWI831259B (zh) | 2018-06-15 | 2024-02-01 | 漢達生技醫藥股份有限公司 | 包含達沙替尼十二烷基硫酸鹽組合物的膠囊 |
| WO2024163400A1 (en) | 2023-01-31 | 2024-08-08 | Handa Oncology, Llc | Improved cabozantinib compositions and methods of use |
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 |
| CN102510855B (zh) * | 2009-07-17 | 2015-11-25 | 埃克塞里艾克西斯公司 | N-[3-氟-4-({6-(甲基氧基)-7-[(3-吗啉-4-基丙基)氧基]-喹啉-4-基}氧基)苯基]-n′-(4-氟苯基)环丙烷-1，1-二甲酰胺的晶形 |
-
2011
- 2011-03-11 AU AU2011224203A patent/AU2011224203A1/en not_active Abandoned
- 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 CA CA2792852A patent/CA2792852A1/en not_active Abandoned
- 2011-03-11 EP EP11709589A patent/EP2545038A1/en not_active Withdrawn
- 2011-03-11 WO PCT/US2011/028035 patent/WO2011112896A1/en not_active Ceased
- 2011-03-11 CN CN2011800137314A patent/CN102933551A/zh active Pending
- 2011-03-11 EA EA201290906A patent/EA201290906A1/ru unknown
- 2011-03-11 MX MX2012010506A patent/MX2012010506A/es not_active Application Discontinuation
- 2011-03-11 TW TW100108394A patent/TW201202228A/zh unknown
- 2011-03-11 SG SG2012067732A patent/SG184040A1/en unknown
- 2011-03-11 KR KR1020127025322A patent/KR20130038206A/ko not_active Withdrawn
- 2011-03-14 AR ARP110100801A patent/AR080584A1/es unknown
-
2012
- 2012-09-06 ZA ZA2012/06679A patent/ZA201206679B/en unknown
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