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 (enExample) | 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 (enExample) |
| EP (2) | EP3172209B1 (enExample) |
| JP (3) | JP6770946B2 (enExample) |
| KR (2) | KR20230136693A (enExample) |
| CN (2) | CN115364061A (enExample) |
| AR (1) | AR101286A1 (enExample) |
| AU (4) | AU2015293539A1 (enExample) |
| CA (1) | CA2954840A1 (enExample) |
| CL (1) | CL2017000180A1 (enExample) |
| CO (1) | CO2017000586A2 (enExample) |
| DK (1) | DK3172209T3 (enExample) |
| EA (2) | EA202191301A1 (enExample) |
| EC (1) | ECSP17011672A (enExample) |
| ES (1) | ES2857523T3 (enExample) |
| FR (1) | FR22C1058I2 (enExample) |
| GT (1) | GT201700007A (enExample) |
| HU (2) | HUE053346T2 (enExample) |
| IL (1) | IL250166B (enExample) |
| JO (1) | JO3618B1 (enExample) |
| MX (2) | MX379279B (enExample) |
| MY (1) | MY187276A (enExample) |
| NL (1) | NL301208I2 (enExample) |
| NO (1) | NO2022058I1 (enExample) |
| PE (1) | PE20170523A1 (enExample) |
| PH (1) | PH12017500121A1 (enExample) |
| PL (1) | PL3172209T3 (enExample) |
| PT (1) | PT3172209T (enExample) |
| SG (2) | SG11201700147SA (enExample) |
| SI (1) | SI3172209T1 (enExample) |
| TW (2) | TWI724993B (enExample) |
| WO (1) | WO2016012963A1 (enExample) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2013243097A1 (en) | 2012-04-03 | 2014-10-09 | Novartis Ag | Combination products with tyrosine kinase inhibitors and their use |
| CA2954840A1 (en) | 2014-07-25 | 2016-01-28 | 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 |
| BR112019002007B1 (pt) | 2016-08-10 | 2024-01-16 | F. Hoffmann-La Roche Ag | Composição farmacêutica e uso de uma composição farmacêutica |
| TW202444706A (zh) | 2019-05-16 | 2024-11-16 | 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 |
| BR112022007744A2 (pt) * | 2019-10-24 | 2022-07-19 | Hanmi Pharm Ind Co Ltd | Preparação farmacêutica compreendendo um derivado de amida inibidor do crescimento de células câncer e produto farmacêutico que a contem |
| 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 |
| CN120112284A (zh) | 2022-08-19 | 2025-06-06 | 米拉蒂治疗股份有限公司 | 阿达格拉西布固体药物组合物 |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (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 |
| 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 |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| 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 |
| CA2615063A1 (en) | 2005-07-22 | 2007-02-01 | Myriad Genetics, Inc. | High drug load formulations and dosage forms |
| WO2007031933A2 (en) | 2005-09-12 | 2007-03-22 | Actelion Pharmaceuticals Ltd | Stable pharmaceutical composition comprising a pyrimidine-sulfamide |
| CA2563690C (en) | 2006-10-12 | 2014-10-07 | Pharmascience Inc. | Pharmaceutical compositions comprising intra- and extra- granular fractions |
| RS54510B1 (sr) | 2006-11-22 | 2016-06-30 | Incyte Holdings Corporation | Imidazotriazini i imidazopirimidini kao inhibitori kinaze |
| TWI472529B (zh) | 2008-05-21 | 2015-02-11 | Incyte Corp | ２－氟－Ｎ－甲基－４－〔７－（喹啉－６－基－甲基）－咪唑并〔１，２－ｂ〕〔１，２，４〕三－２－基〕苯甲醯胺之鹽類及其相關製備方法 |
| AU2010316683B2 (en) * | 2009-11-09 | 2015-10-08 | Wyeth Llc | Tablet formulations of neratinib maleate |
| SI2538925T1 (sl) | 2010-02-25 | 2016-04-29 | Bristol-Myers Squibb Company | Apiksaban formulacije |
| PE20130216A1 (es) * | 2010-05-21 | 2013-02-27 | Incyte Corp | Formulacion topica para un inhibidor de jak |
| EP2590631B1 (en) * | 2010-07-06 | 2016-10-26 | Janssen Pharmaceutica NV | Formulation for co-therapy treatment of diabetes |
| WO2014028566A1 (en) | 2012-08-16 | 2014-02-20 | Novartis Ag | Combination of pi3k inhibitor and c-met inhibitor |
| CA2954840A1 (en) | 2014-07-25 | 2016-01-28 | 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 CA CA2954840A patent/CA2954840A1/en active Pending
- 2015-07-22 CN CN202210949714.1A patent/CN115364061A/zh active Pending
- 2015-07-22 EA EA202191301A patent/EA202191301A1/ru unknown
- 2015-07-22 US US15/328,661 patent/US10085993B2/en active Active
- 2015-07-22 MY MYPI2017700061A patent/MY187276A/en unknown
- 2015-07-22 PE PE2017000097A patent/PE20170523A1/es unknown
- 2015-07-22 ES ES15744702T patent/ES2857523T3/es active Active
- 2015-07-22 CN CN201580052264.4A patent/CN106714784A/zh active Pending
- 2015-07-22 JP JP2017504062A patent/JP6770946B2/ja active Active
- 2015-07-22 SI SI201531507T patent/SI3172209T1/sl unknown
- 2015-07-22 KR KR1020237031767A patent/KR20230136693A/ko not_active Ceased
- 2015-07-22 DK DK15744702.0T patent/DK3172209T3/da active
- 2015-07-22 KR KR1020177004939A patent/KR102581121B1/ko active Active
- 2015-07-22 PL PL15744702T patent/PL3172209T3/pl unknown
- 2015-07-22 SG SG11201700147SA patent/SG11201700147SA/en unknown
- 2015-07-22 EA EA201790259A patent/EA039220B1/ru unknown
- 2015-07-22 EP EP15744702.0A patent/EP3172209B1/en active Active
- 2015-07-22 SG SG10201900648SA patent/SG10201900648SA/en unknown
- 2015-07-22 PT PT157447020T patent/PT3172209T/pt unknown
- 2015-07-22 AU AU2015293539A patent/AU2015293539A1/en not_active Abandoned
- 2015-07-22 HU HUE15744702A patent/HUE053346T2/hu unknown
- 2015-07-22 MX MX2017001177A patent/MX379279B/es unknown
- 2015-07-22 WO PCT/IB2015/055561 patent/WO2016012963A1/en not_active Ceased
- 2015-07-22 EP EP20210458.4A patent/EP3848376A1/en not_active Withdrawn
- 2015-07-23 TW TW104123937A patent/TWI724993B/zh active
- 2015-07-23 JO JOP/2015/0174A patent/JO3618B1/ar active
- 2015-07-23 TW TW110109338A patent/TW202200148A/zh unknown
- 2015-07-23 AR ARP150102336A patent/AR101286A1/es unknown
-
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 CO CONC2017/0000586A patent/CO2017000586A2/es unknown
- 2017-01-24 CL CL2017000180A patent/CL2017000180A1/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
-
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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