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 |
|---|---|---|---|---|
| TW202112751A (zh) | 2009-01-16 | 2021-04-01 | 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 | |
| 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 |
| EA027476B1 (ru) | 2010-09-27 | 2017-07-31 | Экселиксис, Инк. | Применение n-(4-{[6,7-бис-(метилокси)хинолин-4-ил]окси}фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида для лечения кастрационно-резистентного рака простаты и остеобластических метастазов в кости |
| HUE057574T2 (hu) | 2011-02-10 | 2022-05-28 | Exelixis Inc | Eljárás kinolin-származékok és ilyen vegyületeket tartalmazó gyógyászati készítmények elõállítására |
| US20120252840A1 (en) | 2011-04-04 | 2012-10-04 | Exelixis, Inc. | Method of Treating Cancer |
| CN103717221A (zh) | 2011-05-02 | 2014-04-09 | 埃克塞里艾克西斯公司 | 治疗癌症和骨癌疼痛的方法 |
| CA2848512A1 (en) | 2011-09-22 | 2013-03-28 | Exelixis, Inc. | Method for treating osteoporosis |
| BR112014009302B1 (pt) | 2011-10-20 | 2020-04-28 | Exelis Inc Us/Us | processo para preparar derivados de quinolina |
| HK1207587A1 (en) | 2012-05-02 | 2016-02-05 | Exelixis, Inc. | A dual met - vegf modulator for treating osteolytic bone metastases |
| NZ712330A (en) | 2013-03-15 | 2020-04-24 | 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 |
| 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 |
| EP3119476A1 (en) | 2014-03-17 | 2017-01-25 | Exelixis, Inc. | Dosing of cabozantinib formulations |
| CN106715397B (zh) | 2014-07-31 | 2021-07-23 | 埃克塞里艾克西斯公司 | 制备氟-18标记的卡博替尼及其类似物的方法 |
| 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 |
| 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 |
| CN115192540A (zh) | 2018-06-15 | 2022-10-18 | 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 |
| AU2024215796A1 (en) | 2023-01-31 | 2025-05-15 | 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 |
| WO2011009095A1 (en) * | 2009-07-17 | 2011-01-20 | Exelixis, Inc. | 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 |
-
2011
- 2011-03-11 KR KR1020127025322A patent/KR20130038206A/ko not_active Withdrawn
- 2011-03-11 AU AU2011224203A patent/AU2011224203A1/en not_active Abandoned
- 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 WO PCT/US2011/028035 patent/WO2011112896A1/en not_active Ceased
- 2011-03-11 SG SG2012067732A patent/SG184040A1/en unknown
- 2011-03-11 EA EA201290906A patent/EA201290906A1/ru unknown
- 2011-03-11 TW TW100108394A patent/TW201202228A/zh unknown
- 2011-03-11 MX MX2012010506A patent/MX2012010506A/es not_active Application Discontinuation
- 2011-03-11 CN CN2011800137314A patent/CN102933551A/zh active Pending
- 2011-03-11 JP JP2012557269A patent/JP2013522232A/ja active Pending
- 2011-03-11 EP EP11709589A patent/EP2545038A1/en 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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