JP2021102637A5 - - Google Patents
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- Publication number
- JP2021102637A5 JP2021102637A5 JP2021050188A JP2021050188A JP2021102637A5 JP 2021102637 A5 JP2021102637 A5 JP 2021102637A5 JP 2021050188 A JP2021050188 A JP 2021050188A JP 2021050188 A JP2021050188 A JP 2021050188A JP 2021102637 A5 JP2021102637 A5 JP 2021102637A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- day
- dihydropyrazino
- pyrazine
- ethyl
- 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
- 239000008194 pharmaceutical composition Substances 0.000 claims 34
- 150000003839 salts Chemical class 0.000 claims 13
- HUTNOYOBQPAKIA-UHFFFAOYSA-N 1h-pyrazin-2-one Chemical compound OC1=CN=CC=N1 HUTNOYOBQPAKIA-UHFFFAOYSA-N 0.000 claims 11
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 9
- 239000012472 biological sample Substances 0.000 claims 9
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims 9
- 102000005768 DNA-Activated Protein Kinase Human genes 0.000 claims 8
- 108010006124 DNA-Activated Protein Kinase Proteins 0.000 claims 8
- 238000000034 method Methods 0.000 claims 8
- 102100022466 Eukaryotic translation initiation factor 4E-binding protein 1 Human genes 0.000 claims 6
- 108050000946 Eukaryotic translation initiation factor 4E-binding protein 1 Proteins 0.000 claims 6
- -1 pyridine-3-yl Chemical group 0.000 claims 6
- 230000026731 phosphorylation Effects 0.000 claims 3
- 238000006366 phosphorylation reaction Methods 0.000 claims 3
- 239000000523 sample Substances 0.000 claims 3
- GMYLVKUGJMYTFB-UHFFFAOYSA-N 5-ethyl-3-[2-methyl-6-(1h-1,2,4-triazol-5-yl)pyridin-3-yl]-7,8-dihydropyrazino[2,3-b]pyrazin-6-one Chemical compound N1=C2N(CC)C(=O)CNC2=NC=C1C(C(=N1)C)=CC=C1C1=NN=CN1 GMYLVKUGJMYTFB-UHFFFAOYSA-N 0.000 claims 2
- 102000038030 PI3Ks Human genes 0.000 claims 2
- 108091007960 PI3Ks Proteins 0.000 claims 2
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims 2
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims 2
- 230000001143 conditioned effect Effects 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 230000037361 pathway Effects 0.000 claims 2
- FROWTTVEPOUWQS-UHFFFAOYSA-N 2-methyl-6-(1h-1,2,4-triazol-5-yl)pyridine Chemical compound CC1=CC=CC(C2=NNC=N2)=N1 FROWTTVEPOUWQS-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 102000014160 PTEN Phosphohydrolase Human genes 0.000 claims 1
- 108010011536 PTEN Phosphohydrolase Proteins 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 1
- 238000011156 evaluation Methods 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 1
- 230000002018 overexpression Effects 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261611361P | 2012-03-15 | 2012-03-15 | |
| US61/611,361 | 2012-03-15 | ||
| US201261715323P | 2012-10-18 | 2012-10-18 | |
| US61/715,323 | 2012-10-18 | ||
| JP2019038434A JP2019108368A (ja) | 2012-03-15 | 2019-03-04 | Ｔｏｒキナーゼ阻害剤を用いた癌の治療 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019038434A Division JP2019108368A (ja) | 2012-03-15 | 2019-03-04 | Ｔｏｒキナーゼ阻害剤を用いた癌の治療 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2021102637A JP2021102637A (ja) | 2021-07-15 |
| JP2021102637A5 true JP2021102637A5 (https=) | 2021-08-26 |
Family
ID=48014336
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015500596A Pending JP2015510891A (ja) | 2012-03-15 | 2013-03-14 | Ｔｏｒキナーゼ阻害剤を用いた癌の治療 |
| JP2019038434A Pending JP2019108368A (ja) | 2012-03-15 | 2019-03-04 | Ｔｏｒキナーゼ阻害剤を用いた癌の治療 |
| JP2021050188A Pending JP2021102637A (ja) | 2012-03-15 | 2021-03-24 | Ｔｏｒキナーゼ阻害剤を用いた癌の治療 |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015500596A Pending JP2015510891A (ja) | 2012-03-15 | 2013-03-14 | Ｔｏｒキナーゼ阻害剤を用いた癌の治療 |
| JP2019038434A Pending JP2019108368A (ja) | 2012-03-15 | 2019-03-04 | Ｔｏｒキナーゼ阻害剤を用いた癌の治療 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US20130245026A1 (https=) |
| EP (1) | EP2825170B1 (https=) |
| JP (3) | JP2015510891A (https=) |
| KR (3) | KR20200070416A (https=) |
| CN (2) | CN104519885A (https=) |
| AU (1) | AU2013203153B2 (https=) |
| BR (1) | BR112014022703A2 (https=) |
| CA (1) | CA2866872A1 (https=) |
| EA (1) | EA028414B1 (https=) |
| ES (1) | ES2677874T3 (https=) |
| IL (1) | IL234602B (https=) |
| MX (1) | MX360878B (https=) |
| MY (1) | MY174022A (https=) |
| NI (1) | NI201400111A (https=) |
| NZ (1) | NZ628416A (https=) |
| PH (1) | PH12014502029B1 (https=) |
| SG (1) | SG11201405707XA (https=) |
| TW (1) | TWI583385B (https=) |
| UA (1) | UA114315C2 (https=) |
| WO (1) | WO2013138557A1 (https=) |
| ZA (1) | ZA201406706B (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112014022703A2 (pt) * | 2012-03-15 | 2021-05-04 | Signal Pharmaceuticals, Llc | método para o tratamento de carcinoma de células escamosas de cabeça e de pescoço, método para melhorar os critérios de avaliação, método para inibição da fosforilação, método para inibição de dna, método para a medição da inibição da fosforilação, kit |
| AU2013203714B2 (en) | 2012-10-18 | 2015-12-03 | Signal Pharmaceuticals, Llc | Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity |
| PE20151995A1 (es) | 2013-01-16 | 2016-01-13 | Signal Pharm Llc | Compuestos sustituidos de pirrolopirimidina, composiciones de los mismos, y metodos de tratamiento con los mismos |
| US9630966B2 (en) | 2013-04-17 | 2017-04-25 | Signal Pharmaceuticals, Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| CN105377299B (zh) | 2013-04-17 | 2018-06-12 | 西格诺药品有限公司 | 用于治疗前列腺癌的包含二氢吡嗪并-吡嗪化合物和雄激素受体拮抗剂的组合疗法 |
| CA2908742C (en) * | 2013-04-17 | 2021-06-01 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer |
| WO2014172436A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer |
| TW201526894A (zh) * | 2013-04-17 | 2015-07-16 | Signal Pharm Llc | 藉二氫吡并吡治療癌症 |
| US9505764B2 (en) | 2013-04-17 | 2016-11-29 | Signal Pharmaceuticals, Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| CA2909579A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer |
| CA2909629C (en) | 2013-04-17 | 2022-12-13 | Signal Pharmaceuticals, Llc | Pharmaceutical formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one |
| NZ629486A (en) | 2013-05-29 | 2017-11-24 | Signal Pharm Llc | Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use |
| US9512129B2 (en) | 2014-04-16 | 2016-12-06 | Signal Pharmaceuticals, Llc | Solid forms comprising 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and a coformer |
| NZ714742A (en) | 2014-04-16 | 2017-04-28 | Signal Pharm Llc | Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use |
| ES2823756T3 (es) | 2014-04-16 | 2021-05-10 | Signal Pharm Llc | Métodos para tratar el cáncer usando terapia de combinación de inhibidores de quinasa TOR |
| WO2016010886A1 (en) | 2014-07-14 | 2016-01-21 | Signal Pharmaceuticals, Llc | Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof |
| NZ629796A (en) | 2014-07-14 | 2015-12-24 | Signal Pharm Llc | Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use |
| TWI787284B (zh) | 2017-06-22 | 2022-12-21 | 美商西建公司 | 以b型肝炎病毒感染表徵之肝細胞癌之治療 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2666624C (en) | 2006-10-19 | 2015-12-29 | Signal Pharmaceuticals, Llc | Heteroaryl compounds, compositions thereof, and use thereof as protein kinase inhibitors |
| MX337906B (es) * | 2006-10-19 | 2016-03-28 | Signal Pharm Llc | Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas. |
| US20110200556A1 (en) * | 2008-08-20 | 2011-08-18 | The United States Of America, As Represented By Th E Secretary, Department Of Health And Human Servi | Chemoprevention of head and neck squamous cell carcinomas |
| US8110578B2 (en) * | 2008-10-27 | 2012-02-07 | Signal Pharmaceuticals, Llc | Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway |
| SG10201500511TA (en) | 2009-10-26 | 2015-03-30 | Signal Pharm Llc | Methods Of Synthesis And Purification Of Heteroaryl Compounds |
| US20120028972A1 (en) * | 2010-07-30 | 2012-02-02 | Lilly Wong | Biomarker assays for detecting or measuring inhibition of tor kinase activity |
| BR112014022703A2 (pt) * | 2012-03-15 | 2021-05-04 | Signal Pharmaceuticals, Llc | método para o tratamento de carcinoma de células escamosas de cabeça e de pescoço, método para melhorar os critérios de avaliação, método para inibição da fosforilação, método para inibição de dna, método para a medição da inibição da fosforilação, kit |
-
2013
- 2013-03-14 BR BR112014022703-9A patent/BR112014022703A2/pt not_active IP Right Cessation
- 2013-03-14 WO PCT/US2013/031206 patent/WO2013138557A1/en not_active Ceased
- 2013-03-14 AU AU2013203153A patent/AU2013203153B2/en not_active Ceased
- 2013-03-14 NZ NZ628416A patent/NZ628416A/en not_active IP Right Cessation
- 2013-03-14 SG SG11201405707XA patent/SG11201405707XA/en unknown
- 2013-03-14 KR KR1020207016306A patent/KR20200070416A/ko not_active Ceased
- 2013-03-14 EP EP13713006.8A patent/EP2825170B1/en active Active
- 2013-03-14 CN CN201380024859.XA patent/CN104519885A/zh active Pending
- 2013-03-14 EA EA201491699A patent/EA028414B1/ru not_active IP Right Cessation
- 2013-03-14 TW TW102109160A patent/TWI583385B/zh active
- 2013-03-14 KR KR1020217017407A patent/KR20210071101A/ko not_active Ceased
- 2013-03-14 CA CA2866872A patent/CA2866872A1/en not_active Abandoned
- 2013-03-14 US US13/803,061 patent/US20130245026A1/en not_active Abandoned
- 2013-03-14 KR KR1020147028707A patent/KR102122617B1/ko active Active
- 2013-03-14 ES ES13713006.8T patent/ES2677874T3/es active Active
- 2013-03-14 MY MYPI2014702568A patent/MY174022A/en unknown
- 2013-03-14 UA UAA201411218A patent/UA114315C2/uk unknown
- 2013-03-14 JP JP2015500596A patent/JP2015510891A/ja active Pending
- 2013-03-14 MX MX2014011077A patent/MX360878B/es active IP Right Grant
- 2013-03-14 CN CN201811057528.7A patent/CN108992446A/zh active Pending
-
2014
- 2014-09-11 IL IL234602A patent/IL234602B/en active IP Right Grant
- 2014-09-12 ZA ZA2014/06706A patent/ZA201406706B/en unknown
- 2014-09-12 PH PH12014502029A patent/PH12014502029B1/en unknown
- 2014-09-12 NI NI201400111A patent/NI201400111A/es unknown
-
2019
- 2019-03-04 JP JP2019038434A patent/JP2019108368A/ja active Pending
-
2021
- 2021-03-24 JP JP2021050188A patent/JP2021102637A/ja active Pending
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