JP2015511963A5 - - Google Patents
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- Publication number
- JP2015511963A5 JP2015511963A5 JP2015500593A JP2015500593A JP2015511963A5 JP 2015511963 A5 JP2015511963 A5 JP 2015511963A5 JP 2015500593 A JP2015500593 A JP 2015500593A JP 2015500593 A JP2015500593 A JP 2015500593A JP 2015511963 A5 JP2015511963 A5 JP 2015511963A5
- Authority
- JP
- Japan
- Prior art keywords
- breast cancer
- hormone receptor
- receptor positive
- triple negative
- dihydropyrazino
- 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
- 208000027706 hormone receptor-positive breast cancer Diseases 0.000 claims 20
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims 19
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims 19
- 238000000034 method Methods 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 15
- 102000038030 PI3Ks Human genes 0.000 claims 12
- 108091007960 PI3Ks Proteins 0.000 claims 12
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims 12
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims 12
- 230000037361 pathway Effects 0.000 claims 12
- 102000005768 DNA-Activated Protein Kinase Human genes 0.000 claims 8
- 108010006124 DNA-Activated Protein Kinase Proteins 0.000 claims 8
- 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 7
- 239000012472 biological sample Substances 0.000 claims 7
- -1 2-methyl-6- (1H-1,2,4-triazol-3-yl) pyridin-3-yl Chemical group 0.000 claims 6
- 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
- 102000014160 PTEN Phosphohydrolase Human genes 0.000 claims 6
- 108010011536 PTEN Phosphohydrolase Proteins 0.000 claims 6
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 6
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 6
- 230000035772 mutation Effects 0.000 claims 6
- 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 6
- 230000002018 overexpression Effects 0.000 claims 6
- HUTNOYOBQPAKIA-UHFFFAOYSA-N 1h-pyrazin-2-one Chemical compound OC1=CN=CC=N1 HUTNOYOBQPAKIA-UHFFFAOYSA-N 0.000 claims 5
- 230000005764 inhibitory process Effects 0.000 claims 3
- 230000027405 negative regulation of phosphorylation Effects 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000000523 sample Substances 0.000 claims 2
- 125000001305 1,2,4-triazol-3-yl group Chemical group [H]N1N=C([*])N=C1[H] 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- XVMSFILGAMDHEY-UHFFFAOYSA-N 6-(4-aminophenyl)sulfonylpyridin-3-amine Chemical compound C1=CC(N)=CC=C1S(=O)(=O)C1=CC=C(N)C=N1 XVMSFILGAMDHEY-UHFFFAOYSA-N 0.000 claims 1
- APYXDKYGQKKWDM-UHFFFAOYSA-N 7,8-dihydro-5h-pyrazino[2,3-b]pyrazin-6-one Chemical compound C1=CN=C2NC(=O)CNC2=N1 APYXDKYGQKKWDM-UHFFFAOYSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000001678 irradiating effect Effects 0.000 claims 1
- 238000012544 monitoring process Methods 0.000 claims 1
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 239000011574 phosphorus Substances 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261611374P | 2012-03-15 | 2012-03-15 | |
| US61/611,374 | 2012-03-15 | ||
| US201261715331P | 2012-10-18 | 2012-10-18 | |
| US61/715,331 | 2012-10-18 | ||
| PCT/US2013/031185 WO2013138553A1 (en) | 2012-03-15 | 2013-03-14 | Treatment of cancer with tor kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017218014A Division JP6470820B2 (ja) | 2012-03-15 | 2017-11-13 | Ｔｏｒキナーゼ阻害剤を用いた癌の治療 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015511963A JP2015511963A (ja) | 2015-04-23 |
| JP2015511963A5 true JP2015511963A5 (enExample) | 2016-04-21 |
Family
ID=48014333
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015500593A Pending JP2015511963A (ja) | 2012-03-15 | 2013-03-14 | Ｔｏｒキナーゼ阻害剤を用いた癌の治療 |
| JP2017218014A Active JP6470820B2 (ja) | 2012-03-15 | 2017-11-13 | Ｔｏｒキナーゼ阻害剤を用いた癌の治療 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017218014A Active JP6470820B2 (ja) | 2012-03-15 | 2017-11-13 | Ｔｏｒキナーゼ阻害剤を用いた癌の治療 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US20130245027A1 (enExample) |
| EP (1) | EP2825169B1 (enExample) |
| JP (2) | JP2015511963A (enExample) |
| KR (1) | KR102057359B1 (enExample) |
| CN (1) | CN104271139A (enExample) |
| AU (1) | AU2013202993B2 (enExample) |
| BR (1) | BR112014022707A2 (enExample) |
| CA (1) | CA2867348A1 (enExample) |
| ES (1) | ES2678250T3 (enExample) |
| IL (1) | IL234641B (enExample) |
| MX (1) | MX360880B (enExample) |
| MY (1) | MY178012A (enExample) |
| NI (1) | NI201400112A (enExample) |
| NZ (1) | NZ628407A (enExample) |
| PH (1) | PH12014502046B1 (enExample) |
| SG (1) | SG11201405724RA (enExample) |
| TW (1) | TWI635862B (enExample) |
| WO (1) | WO2013138553A1 (enExample) |
| ZA (1) | ZA201406701B (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| KR102242505B1 (ko) * | 2013-04-17 | 2021-04-20 | 시그날 파마소티칼 엘엘씨 | 암 치료용 tor 키나제 억제제 및 시티딘 유사체를 포함하는 병용 요법 |
| SG11201508527VA (en) | 2013-04-17 | 2015-11-27 | Signal Pharm 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 |
| ES2944478T3 (es) | 2013-04-17 | 2023-06-21 | Signal Pharm Llc | 1-etil-7-(2-metil-6-(1H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-ona para tratar el glioblastoma multiforme |
| NZ629411A (en) | 2013-04-17 | 2017-06-30 | Signal Pharm Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| MX368286B (es) | 2013-04-17 | 2019-09-27 | Signal Pharm Llc | Terapia de combinacion que comprende un inhibidor de tor cinasa y un compuesto de quinazolinona 5-sustituida para tratar cancer. |
| AU2014254057A1 (en) | 2013-04-17 | 2015-11-05 | 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 |
| BR112015026257B1 (pt) | 2013-04-17 | 2022-12-20 | Signal Pharmaceuticals, Llc | Uso de um composto dihidropirazino-pirazina e enzalutamida, composição farmacêutica que os compreende, e kit |
| JP6401250B2 (ja) | 2013-05-29 | 2018-10-10 | シグナル ファーマシューティカルズ，エルエルシー | ７−（６−（２−ヒドロキシプロパン−２−イル）ピリジン−３−イル）−１−（（ｔｒａｎｓ）−４−メトキシシクロヘキシル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オン、その固体形態の医薬組成物、及びその使用方法 |
| US9737535B2 (en) | 2014-04-16 | 2017-08-22 | Signal Pharmaceuticals, Llc | Methods for treating cancer using TOR kinase inhibitor combination therapy comprising administering substituted pyrazino[2,3-b]pyrazines |
| 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 |
| US9718824B2 (en) | 2014-04-16 | 2017-08-01 | Signal Pharmaceuticals, Llc | Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, and a coformer, compositions and methods of use thereof |
| 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 |
| EP3641772B1 (en) | 2017-06-22 | 2023-08-02 | Celgene Corporation | Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection |
| CN112933088B (zh) * | 2021-02-03 | 2022-02-22 | 南华大学附属第一医院 | Y041-5921在制备抗肿瘤药物中的应用 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2383370T3 (es) | 2006-10-19 | 2012-06-20 | Signal Pharmaceuticals Llc | Compuestos de heteroarilo, sus composiciones y uso de los mismos como inhibidores de proteína quinasa |
| EP2457913B1 (en) * | 2006-10-19 | 2017-04-19 | Signal Pharmaceuticals, LLC | Heteroaryl compounds, compositions thereof, and methods of treatment therewith |
| EP2285392A4 (en) * | 2008-04-11 | 2012-06-06 | Bionovo Inc | PROCEDURE AGAINST CANCER WITH EXTRACTS FROM GLEDITSIA SINENSIS LAM |
| 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 |
| JP2013508456A (ja) | 2009-10-26 | 2013-03-07 | シグナル ファーマシューティカルズ， エルエルシー | ヘテロアリール化合物の合成方法および精製方法 |
-
2013
- 2013-03-14 MY MYPI2014702602A patent/MY178012A/en unknown
- 2013-03-14 KR KR1020147028898A patent/KR102057359B1/ko active Active
- 2013-03-14 ES ES13713003.5T patent/ES2678250T3/es active Active
- 2013-03-14 EP EP13713003.5A patent/EP2825169B1/en active Active
- 2013-03-14 WO PCT/US2013/031185 patent/WO2013138553A1/en not_active Ceased
- 2013-03-14 MX MX2014011118A patent/MX360880B/es active IP Right Grant
- 2013-03-14 CA CA2867348A patent/CA2867348A1/en not_active Abandoned
- 2013-03-14 TW TW102109151A patent/TWI635862B/zh active
- 2013-03-14 JP JP2015500593A patent/JP2015511963A/ja active Pending
- 2013-03-14 CN CN201380024241.3A patent/CN104271139A/zh active Pending
- 2013-03-14 NZ NZ628407A patent/NZ628407A/en not_active IP Right Cessation
- 2013-03-14 US US13/803,305 patent/US20130245027A1/en not_active Abandoned
- 2013-03-14 BR BR112014022707-1A patent/BR112014022707A2/pt not_active IP Right Cessation
- 2013-03-14 SG SG11201405724RA patent/SG11201405724RA/en unknown
- 2013-03-14 AU AU2013202993A patent/AU2013202993B2/en not_active Ceased
-
2014
- 2014-09-12 ZA ZA2014/06701A patent/ZA201406701B/en unknown
- 2014-09-12 NI NI201400112A patent/NI201400112A/es unknown
- 2014-09-14 IL IL234641A patent/IL234641B/en active IP Right Grant
- 2014-09-15 PH PH12014502046A patent/PH12014502046B1/en unknown
-
2017
- 2017-11-13 JP JP2017218014A patent/JP6470820B2/ja active Active
-
2022
- 2022-10-28 US US17/976,471 patent/US20230338370A1/en not_active Abandoned
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