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) | EP3848376A1 (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) | EA039220B1 (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) | TW202200148A (enExample) |
| WO (1) | WO2016012963A1 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2868202C (en) | 2012-04-03 | 2021-08-10 | Novartis Ag | Combination products with tyrosine kinase inhibitors and their use |
| DK3172209T3 (da) | 2014-07-25 | 2021-02-22 | Novartis Ag | Tabletformulering med 2-fluor-n-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamid |
| TWI736660B (zh) | 2016-08-10 | 2021-08-21 | 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 |
| US11407735B2 (en) | 2019-05-16 | 2022-08-09 | Novartis Ag | Crystalline forms of N-[4-(Chlorodifluoromethoxy)phenyl]-6-[(3R)-3-hydroxypyrrolidin-1-yl]-5-(1H-pyrazol-5-yl)pyridine-3-carboxamide |
| JP7675071B2 (ja) * | 2019-10-24 | 2025-05-12 | ハンミ ファーマシューティカル カンパニー リミテッド | がん細胞の成長を阻害するアミド誘導体を含む医薬調製物およびそれを含有する医薬品 |
| 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 |
| CN114853762A (zh) * | 2021-02-03 | 2022-08-05 | 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 |
| AU2023324893A1 (en) * | 2022-08-19 | 2025-03-13 | Mirati Therapeutics, Inc. | Adagrasib solid pharmaceutical compositions |
| WO2024206858A1 (en) | 2023-03-30 | 2024-10-03 | 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 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| 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 |
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 |
| EP1909777A2 (en) * | 2005-07-22 | 2008-04-16 | 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 |
| PL2497470T3 (pl) | 2006-11-22 | 2016-04-29 | Incyte Holdings Corp | Imidazotriazyny i imidazopirymidyny jako inhibitory kinazy |
| JP6022158B2 (ja) | 2008-05-21 | 2016-11-09 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | 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］ベンズアミドの塩及びそれを調製することに関する方法 |
| PT4066821T (pt) * | 2009-11-09 | 2025-06-03 | Wyeth Llc | Formulações de comprimidos de maleato de neratinib |
| JP5846647B2 (ja) | 2010-02-25 | 2016-01-20 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | アピキサバン製剤 |
| NZ603686A (en) * | 2010-05-21 | 2014-11-28 | Incyte Corp | Topical formulation for a jak inhibitor |
| WO2012006298A2 (en) | 2010-07-06 | 2012-01-12 | Janssen Pharmaceutica Nv | Formulation for co-therapy treatment of diabetes |
| RU2705095C2 (ru) | 2012-08-16 | 2019-11-05 | Новартис Аг | Комбинация ингибитора pik3 и ингибитора с-мет |
| DK3172209T3 (da) | 2014-07-25 | 2021-02-22 | Novartis Ag | Tabletformulering med 2-fluor-n-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamid |
-
2015
- 2015-07-22 DK DK15744702.0T patent/DK3172209T3/da active
- 2015-07-22 SI SI201531507T patent/SI3172209T1/sl unknown
- 2015-07-22 KR KR1020237031767A patent/KR20230136693A/ko not_active Ceased
- 2015-07-22 PL PL15744702T patent/PL3172209T3/pl unknown
- 2015-07-22 AU AU2015293539A patent/AU2015293539A1/en not_active Abandoned
- 2015-07-22 CN CN202210949714.1A patent/CN115364061A/zh active Pending
- 2015-07-22 EP EP20210458.4A patent/EP3848376A1/en not_active Withdrawn
- 2015-07-22 ES ES15744702T patent/ES2857523T3/es active Active
- 2015-07-22 PE PE2017000097A patent/PE20170523A1/es unknown
- 2015-07-22 CA CA2954840A patent/CA2954840A1/en active Pending
- 2015-07-22 SG SG11201700147SA patent/SG11201700147SA/en unknown
- 2015-07-22 EA EA201790259A patent/EA039220B1/ru unknown
- 2015-07-22 EA EA202191301A patent/EA202191301A1/ru 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 PT PT157447020T patent/PT3172209T/pt unknown
- 2015-07-22 MY MYPI2017700061A patent/MY187276A/en unknown
- 2015-07-22 CN CN201580052264.4A patent/CN106714784A/zh active Pending
- 2015-07-22 KR KR1020177004939A patent/KR102581121B1/ko active Active
- 2015-07-22 HU HUE15744702A patent/HUE053346T2/hu unknown
- 2015-07-22 EP EP15744702.0A patent/EP3172209B1/en active Active
- 2015-07-22 US US15/328,661 patent/US10085993B2/en active Active
- 2015-07-22 SG SG10201900648SA patent/SG10201900648SA/en unknown
- 2015-07-22 JP JP2017504062A patent/JP6770946B2/ja active 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
- 2015-07-23 JO JOP/2015/0174A patent/JO3618B1/ar 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 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 NL NL301208C patent/NL301208I2/nl unknown
- 2022-12-16 NO NO2022058C patent/NO2022058I1/no 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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