JP2017521469A5 - - Google Patents
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- Publication number
- JP2017521469A5 JP2017521469A5 JP2017504062A JP2017504062A JP2017521469A5 JP 2017521469 A5 JP2017521469 A5 JP 2017521469A5 JP 2017504062 A JP2017504062 A JP 2017504062A JP 2017504062 A JP2017504062 A JP 2017504062A JP 2017521469 A5 JP2017521469 A5 JP 2017521469A5
- Authority
- JP
- Japan
- Prior art keywords
- weight
- quinolin
- imidazo
- ylmethyl
- fluoro
- 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.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 claims 23
- LIOLIMKSCNQPLV-UHFFFAOYSA-N 2-fluoro-n-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide Chemical compound C1=C(F)C(C(=O)NC)=CC=C1C1=NN2C(CC=3C=C4C=CC=NC4=CC=3)=CN=C2N=C1 LIOLIMKSCNQPLV-UHFFFAOYSA-N 0.000 claims 13
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 12
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 11
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 11
- 239000008108 microcrystalline cellulose Substances 0.000 claims 11
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 11
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims 10
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 claims 10
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims 10
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 8
- -1 quinolin-6-ylmethyl Chemical group 0.000 claims 7
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 6
- 229930195725 Mannitol Natural products 0.000 claims 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 6
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims 6
- 239000012458 free base Substances 0.000 claims 6
- 235000019359 magnesium stearate Nutrition 0.000 claims 6
- 239000000594 mannitol Substances 0.000 claims 6
- 235000010355 mannitol Nutrition 0.000 claims 6
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 6
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 6
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 239000008187 granular material Substances 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 239000000314 lubricant Substances 0.000 claims 3
- 238000002156 mixing Methods 0.000 claims 3
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 239000007884 disintegrant Substances 0.000 claims 2
- 239000000945 filler Substances 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 238000007873 sieving Methods 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- ZTNPHABKLIJXTL-UHFFFAOYSA-N 2-fluoro-n-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide;dihydrochloride Chemical class Cl.Cl.C1=C(F)C(C(=O)NC)=CC=C1C1=NN2C(CC=3C=C4C=CC=NC4=CC=3)=CN=C2N=C1 ZTNPHABKLIJXTL-UHFFFAOYSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000001894 Nasopharyngeal Neoplasms Diseases 0.000 claims 1
- 206010061306 Nasopharyngeal cancer Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 238000001035 drying Methods 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 1
- 229960002584 gefitinib Drugs 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims 1
- 235000002639 sodium chloride Nutrition 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 229920002554 vinyl polymer Polymers 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462028865P | 2014-07-25 | 2014-07-25 | |
| US62/028,865 | 2014-07-25 | ||
| PCT/IB2015/055561 WO2016012963A1 (en) | 2014-07-25 | 2015-07-22 | Tablet formulation of 2-fluoro-n-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020058164A Division JP7002587B2 (ja) | 2014-07-25 | 2020-03-27 | ２－フルオロ－ｎ－メチル－４－［７－（キノリン－６－イルメチル）イミダゾ［１，２－ｂ］［１，２，４］トリアジン－２－イル］ベンズアミドの錠剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017521469A JP2017521469A (ja) | 2017-08-03 |
| JP2017521469A5 true JP2017521469A5 (https=) | 2018-08-30 |
| JP6770946B2 JP6770946B2 (ja) | 2020-10-21 |
Family
ID=53762251
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017504062A Active JP6770946B2 (ja) | 2014-07-25 | 2015-07-22 | ２−フルオロ−ｎ−メチル−４−［７−（キノリン−６−イルメチル）イミダゾ［１，２−ｂ］［１，２，４］トリアジン−２−イル］ベンズアミドの錠剤 |
| JP2020058164A Active JP7002587B2 (ja) | 2014-07-25 | 2020-03-27 | ２－フルオロ－ｎ－メチル－４－［７－（キノリン－６－イルメチル）イミダゾ［１，２－ｂ］［１，２，４］トリアジン－２－イル］ベンズアミドの錠剤 |
| JP2021211526A Pending JP2022046659A (ja) | 2014-07-25 | 2021-12-24 | ２－フルオロ－ｎ－メチル－４－［７－（キノリン－６－イルメチル）イミダゾ［１，２－ｂ］［１，２，４］トリアジン－２－イル］ベンズアミドの錠剤 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020058164A Active JP7002587B2 (ja) | 2014-07-25 | 2020-03-27 | ２－フルオロ－ｎ－メチル－４－［７－（キノリン－６－イルメチル）イミダゾ［１，２－ｂ］［１，２，４］トリアジン－２－イル］ベンズアミドの錠剤 |
| JP2021211526A Pending JP2022046659A (ja) | 2014-07-25 | 2021-12-24 | ２－フルオロ－ｎ－メチル－４－［７－（キノリン－６－イルメチル）イミダゾ［１，２－ｂ］［１，２，４］トリアジン－２－イル］ベンズアミドの錠剤 |
Country Status (31)
| Country | Link |
|---|---|
| US (5) | US10085993B2 (https=) |
| EP (2) | EP3172209B1 (https=) |
| JP (3) | JP6770946B2 (https=) |
| KR (2) | KR102581121B1 (https=) |
| CN (2) | CN106714784A (https=) |
| AR (1) | AR101286A1 (https=) |
| AU (4) | AU2015293539A1 (https=) |
| CA (1) | CA2954840A1 (https=) |
| CL (1) | CL2017000180A1 (https=) |
| CO (1) | CO2017000586A2 (https=) |
| DK (1) | DK3172209T3 (https=) |
| EA (2) | EA202191301A1 (https=) |
| EC (1) | ECSP17011672A (https=) |
| ES (1) | ES2857523T3 (https=) |
| FR (1) | FR22C1058I2 (https=) |
| GT (1) | GT201700007A (https=) |
| HU (2) | HUE053346T2 (https=) |
| IL (1) | IL250166B (https=) |
| JO (1) | JO3618B1 (https=) |
| MX (2) | MX379279B (https=) |
| MY (1) | MY187276A (https=) |
| NL (1) | NL301208I2 (https=) |
| NO (1) | NO2022058I1 (https=) |
| PE (1) | PE20170523A1 (https=) |
| PH (1) | PH12017500121A1 (https=) |
| PL (1) | PL3172209T3 (https=) |
| PT (1) | PT3172209T (https=) |
| SG (2) | SG11201700147SA (https=) |
| SI (1) | SI3172209T1 (https=) |
| TW (2) | TW202200148A (https=) |
| WO (1) | WO2016012963A1 (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015512425A (ja) | 2012-04-03 | 2015-04-27 | ノバルティス アーゲー | チロシンキナーゼ阻害剤との組合せ製品及びそれらの使用 |
| US10085993B2 (en) | 2014-07-25 | 2018-10-02 | Novartis Ag | Tablet formulation of 2-fluoro-N-methyl-4-[ 7-( quinolin-6-ylmethyl) imidazo [1,2-B] [1,2,4] triazin-2-yl] benzamide |
| TWI777658B (zh) | 2016-08-10 | 2022-09-11 | 瑞士商赫孚孟拉羅股份公司 | 包含Akt蛋白質激酶抑制劑之醫藥組合物 |
| TWI853027B (zh) | 2019-05-16 | 2024-08-21 | 瑞士商諾華公司 | N-[4-(氯二氟甲氧基)苯基]-6-[(3r)-3-羥基吡咯啶-1-基]-5-(1h-吡唑-5-基)吡啶-3-甲醯胺之結晶形狀 |
| CN114502144A (zh) * | 2019-10-24 | 2022-05-13 | 韩美药品株式会社 | 包含抑制癌细胞生长的酰胺衍生物的药物制剂以及包含其的药物产品 |
| WO2022007752A1 (zh) * | 2020-07-06 | 2022-01-13 | 苏州晶云药物科技股份有限公司 | 苯甲酰胺类化合物及其二盐酸盐的新晶型及其制备方法 |
| CN114853762B (zh) * | 2021-02-03 | 2026-03-06 | 四川科伦药物研究院有限公司 | 一种咪唑并三嗪类化合物的固体形式及其制备方法和用途 |
| CN118251220A (zh) * | 2022-01-19 | 2024-06-25 | 江苏奥赛康药业有限公司 | 一种包含嘧啶基团的三并环类化合物的组合物及其制备方法和应用 |
| WO2023249994A1 (en) * | 2022-06-22 | 2023-12-28 | Mayo Foundation For Medical Education And Research | Methods and materials for treating cancer |
| PE20251110A1 (es) * | 2022-08-19 | 2025-04-22 | Mirati Therapeutics Inc | Composiciones farmaceuticas solidas de adagrasib |
| EP4687905A1 (en) | 2023-03-30 | 2026-02-11 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6762778B1 (en) | 1999-06-10 | 2004-07-13 | Dassault Systemes | Three dimensional graphical manipulator |
| CA2465565A1 (en) * | 2003-06-12 | 2004-12-12 | Warner-Lambert Company Llc | Pharmaceutical compositions of atorvastatin |
| KR20080039876A (ko) | 2005-07-22 | 2008-05-07 | 미리어드 제네틱스, 인크. | 높은 약물 충진 제형 및 투여형 |
| PT1928409E (pt) | 2005-09-12 | 2012-11-27 | Actelion Pharmaceuticals Ltd | Composição farmacêutica estável que compreende uma pirimidina-sulfamida |
| CA2563690C (en) | 2006-10-12 | 2014-10-07 | Pharmascience Inc. | Pharmaceutical compositions comprising intra- and extra- granular fractions |
| ME02372B (me) * | 2006-11-22 | 2016-06-20 | Incyte Holdings Corp | Imidazotriazini i imidazopiramidini kao inhibitori kinaze |
| WO2009143211A2 (en) * | 2008-05-21 | 2009-11-26 | Incyte Corporation | Salts of 2-fluoro-n-methyl-4-[7-(quinolin-6-yl-methyl)- imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide and processes related to preparing the same |
| AU2010316683B2 (en) * | 2009-11-09 | 2015-10-08 | Wyeth Llc | Tablet formulations of neratinib maleate |
| IN2012DN06587A (https=) | 2010-02-25 | 2015-10-23 | Bristol Myers Squibb Co | |
| RS54824B1 (sr) * | 2010-05-21 | 2016-10-31 | Incyte Holdings Corp | Topikalna formulacija za inhibiciju jak-a |
| EP2590631B1 (en) * | 2010-07-06 | 2016-10-26 | Janssen Pharmaceutica NV | Formulation for co-therapy treatment of diabetes |
| HK1211476A1 (en) | 2012-08-16 | 2016-05-27 | Novartis Ag | Combination of pi3k inhibitor and c-met inhibitor |
| US10085993B2 (en) | 2014-07-25 | 2018-10-02 | Novartis Ag | Tablet formulation of 2-fluoro-N-methyl-4-[ 7-( quinolin-6-ylmethyl) imidazo [1,2-B] [1,2,4] triazin-2-yl] benzamide |
-
2015
- 2015-07-22 US US15/328,661 patent/US10085993B2/en active Active
- 2015-07-22 EA EA202191301A patent/EA202191301A1/ru unknown
- 2015-07-22 EP EP15744702.0A patent/EP3172209B1/en active Active
- 2015-07-22 CA CA2954840A patent/CA2954840A1/en active Pending
- 2015-07-22 EP EP20210458.4A patent/EP3848376A1/en not_active Withdrawn
- 2015-07-22 JP JP2017504062A patent/JP6770946B2/ja active Active
- 2015-07-22 MX MX2017001177A patent/MX379279B/es unknown
- 2015-07-22 KR KR1020177004939A patent/KR102581121B1/ko active Active
- 2015-07-22 SG SG11201700147SA patent/SG11201700147SA/en unknown
- 2015-07-22 PL PL15744702T patent/PL3172209T3/pl unknown
- 2015-07-22 CN CN201580052264.4A patent/CN106714784A/zh active Pending
- 2015-07-22 CN CN202210949714.1A patent/CN115364061A/zh active Pending
- 2015-07-22 MY MYPI2017700061A patent/MY187276A/en unknown
- 2015-07-22 DK DK15744702.0T patent/DK3172209T3/da active
- 2015-07-22 EA EA201790259A patent/EA039220B1/ru unknown
- 2015-07-22 ES ES15744702T patent/ES2857523T3/es active Active
- 2015-07-22 PE PE2017000097A patent/PE20170523A1/es unknown
- 2015-07-22 PT PT157447020T patent/PT3172209T/pt unknown
- 2015-07-22 AU AU2015293539A patent/AU2015293539A1/en not_active Abandoned
- 2015-07-22 WO PCT/IB2015/055561 patent/WO2016012963A1/en not_active Ceased
- 2015-07-22 HU HUE15744702A patent/HUE053346T2/hu unknown
- 2015-07-22 SG SG10201900648SA patent/SG10201900648SA/en unknown
- 2015-07-22 KR KR1020237031767A patent/KR20230136693A/ko not_active Ceased
- 2015-07-22 SI SI201531507T patent/SI3172209T1/sl unknown
- 2015-07-23 JO JOP/2015/0174A patent/JO3618B1/ar active
- 2015-07-23 AR ARP150102336A patent/AR101286A1/es unknown
- 2015-07-23 TW TW110109338A patent/TW202200148A/zh unknown
- 2015-07-23 TW TW104123937A patent/TWI724993B/zh active
-
2017
- 2017-01-17 IL IL250166A patent/IL250166B/en active IP Right Grant
- 2017-01-20 PH PH12017500121A patent/PH12017500121A1/en unknown
- 2017-01-24 CL CL2017000180A patent/CL2017000180A1/es unknown
- 2017-01-24 CO CONC2017/0000586A patent/CO2017000586A2/es unknown
- 2017-01-25 GT GT201700007A patent/GT201700007A/es unknown
- 2017-01-25 MX MX2021000595A patent/MX2021000595A/es unknown
- 2017-02-24 EC ECIEPI201711672A patent/ECSP17011672A/es unknown
-
2018
- 2018-07-23 AU AU2018207947A patent/AU2018207947A1/en not_active Abandoned
- 2018-09-18 US US16/134,162 patent/US10596178B2/en active Active
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2020
- 2020-02-07 AU AU2020200912A patent/AU2020200912B2/en active Active
- 2020-02-13 US US16/789,655 patent/US20210113569A1/en not_active Abandoned
- 2020-03-27 JP JP2020058164A patent/JP7002587B2/ja active Active
-
2021
- 2021-04-23 AU AU2021202500A patent/AU2021202500A1/en not_active Abandoned
- 2021-12-15 US US17/644,473 patent/US12208101B2/en active Active
- 2021-12-24 JP JP2021211526A patent/JP2022046659A/ja active Pending
-
2022
- 2022-12-06 FR FR22C1058C patent/FR22C1058I2/fr active Active
- 2022-12-16 NO NO2022058C patent/NO2022058I1/no unknown
- 2022-12-16 NL NL301208C patent/NL301208I2/nl unknown
- 2022-12-19 HU HUS2200054C patent/HUS2200054I1/hu unknown
-
2024
- 2024-12-16 US US18/982,128 patent/US20250339440A1/en active Pending
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