JP2015511964A5 - - Google Patents
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- Publication number
- JP2015511964A5 JP2015511964A5 JP2015500599A JP2015500599A JP2015511964A5 JP 2015511964 A5 JP2015511964 A5 JP 2015511964A5 JP 2015500599 A JP2015500599 A JP 2015500599A JP 2015500599 A JP2015500599 A JP 2015500599A JP 2015511964 A5 JP2015511964 A5 JP 2015511964A5
- Authority
- JP
- Japan
- Prior art keywords
- ets
- prostate cancer
- resistant prostate
- dihydropyrazino
- 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
- 206010060862 Prostate cancer Diseases 0.000 claims 20
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 20
- 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
- -1 2-methyl-6- (1H-1,2,4-triazol-3-yl) pyridin-3-yl Chemical group 0.000 claims 8
- 102000005768 DNA-Activated Protein Kinase Human genes 0.000 claims 8
- 108010006124 DNA-Activated Protein Kinase Proteins 0.000 claims 8
- 230000002018 overexpression Effects 0.000 claims 8
- 239000012472 biological sample Substances 0.000 claims 7
- 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
- HUTNOYOBQPAKIA-UHFFFAOYSA-N 1h-pyrazin-2-one Chemical compound OC1=CN=CC=N1 HUTNOYOBQPAKIA-UHFFFAOYSA-N 0.000 claims 5
- 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 4
- 230000005764 inhibitory process Effects 0.000 claims 3
- 230000027405 negative regulation of phosphorylation Effects 0.000 claims 3
- 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 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- NJLOYNGVESEOFW-UHFFFAOYSA-N 5-ethyl-3-[2-methyl-6-(1h-1,2,4-triazol-5-yl)pyridin-3-yl]-7,8-dihydro-6h-pyrazino[2,3-b]pyrazine Chemical compound N1=C2N(CC)CCNC2=NC=C1C(C(=N1)C)=CC=C1C1=NN=CN1 NJLOYNGVESEOFW-UHFFFAOYSA-N 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 238000000691 measurement method Methods 0.000 claims 1
- 238000012544 monitoring process Methods 0.000 claims 1
- 230000026731 phosphorylation Effects 0.000 claims 1
- 238000006366 phosphorylation reaction Methods 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261611428P | 2012-03-15 | 2012-03-15 | |
| US61/611,428 | 2012-03-15 | ||
| US201261715327P | 2012-10-18 | 2012-10-18 | |
| US61/715,327 | 2012-10-18 | ||
| PCT/US2013/031217 WO2013138560A1 (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 |
|---|---|---|---|
| JP2017218388A Division JP6470822B2 (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 |
|---|---|
| JP2015511964A JP2015511964A (ja) | 2015-04-23 |
| JP2015511964A5 true JP2015511964A5 (enExample) | 2016-04-21 |
Family
ID=48045717
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015500599A Pending JP2015511964A (ja) | 2012-03-15 | 2013-03-14 | Ｔｏｒキナーゼ阻害剤を用いた癌の治療 |
| JP2017218388A Active JP6470822B2 (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 |
|---|---|---|---|
| JP2017218388A Active JP6470822B2 (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 (21)
| Country | Link |
|---|---|
| US (1) | US20130245028A1 (enExample) |
| EP (1) | EP2825171B1 (enExample) |
| JP (2) | JP2015511964A (enExample) |
| KR (1) | KR102057357B1 (enExample) |
| CN (2) | CN109846884A (enExample) |
| AU (2) | AU2013202992B2 (enExample) |
| BR (1) | BR112014022700A2 (enExample) |
| CA (1) | CA2867174C (enExample) |
| EA (1) | EA028062B1 (enExample) |
| ES (1) | ES2668279T3 (enExample) |
| IL (1) | IL234639B (enExample) |
| MX (1) | MX359227B (enExample) |
| MY (1) | MY198666A (enExample) |
| NI (1) | NI201400110A (enExample) |
| NZ (1) | NZ628420A (enExample) |
| PH (1) | PH12014502047B1 (enExample) |
| SG (1) | SG11201405686PA (enExample) |
| TW (1) | TWI622395B (enExample) |
| UA (1) | UA114194C2 (enExample) |
| WO (1) | WO2013138560A1 (enExample) |
| ZA (1) | ZA201406708B (enExample) |
Families Citing this family (18)
| 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 |
| SG11201505446WA (en) | 2013-01-16 | 2015-08-28 | Signal Pharm Llc | Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith |
| 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 |
| HK1221168A1 (zh) | 2013-04-17 | 2017-05-26 | 西格诺药品有限公司 | 用於治疗癌症的包括tor激酶抑制剂和n-(3-(5-氟-2-(4-(2-甲氧基乙氧基)苯基氨基)嘧啶-4-基氨基)苯基)丙烯醯胺的组合疗法 |
| WO2014172425A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| MY189663A (en) * | 2013-04-17 | 2022-02-23 | Signal Pharm Llc | Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer |
| JP6382946B2 (ja) | 2013-04-17 | 2018-08-29 | シグナル ファーマシューティカルズ，エルエルシー | ジヒドロピラジノ−ピラジンによる癌治療 |
| EP3549940A1 (en) | 2013-04-17 | 2019-10-09 | Signal Pharmaceuticals, LLC | Pharmaceutical formulations, 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 |
| 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 |
| CN107474051B (zh) | 2013-05-29 | 2020-10-30 | 西格诺药品有限公司 | 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途 |
| 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 |
| WO2015160880A1 (en) | 2014-04-16 | 2015-10-22 | 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, COMPOSITIONS AND METHODS OF USE THEREOF |
| EP3131552B1 (en) | 2014-04-16 | 2020-07-15 | Signal Pharmaceuticals, LLC | Methods for treating cancer using tor kinase inhibitor combination therapy |
| 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 |
| WO2016010886A1 (en) | 2014-07-14 | 2016-01-21 | Signal Pharmaceuticals, Llc | Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof |
| US20180369241A1 (en) * | 2015-06-24 | 2018-12-27 | Celgene Corporation | Treatment of cancer with dnapk inhibitors |
| WO2017132235A1 (en) * | 2016-01-26 | 2017-08-03 | Dana-Farber Cancer Institute, Inc. | METHODS FOR TREATING BRAIN METASTASES USING COMBINATIONS OF ANTI-P13K AND ANTI-mTOR AGENTS |
| IL271491B2 (en) | 2017-06-22 | 2023-09-01 | Celgene Corp | Treatment of carcinoma of the liver characterized by hepatitis b virus infection |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2627352T3 (es) | 2006-10-19 | 2017-07-27 | Signal Pharmaceuticals, Llc | Compuestos heteroarilo, sus composiciones y su uso como inhibidores de proteínas quinasas |
| RU2474582C2 (ru) | 2006-10-19 | 2013-02-10 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Гетероарильные соединения, их композиции и их применение в качестве ингибиторов протеинкиназы |
| JP5279828B2 (ja) * | 2008-07-10 | 2013-09-04 | Ｊｘ日鉱日石金属株式会社 | ハイブリッドシリコンウエハ及びその製造方法 |
| WO2010022243A1 (en) * | 2008-08-20 | 2010-02-25 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Chemoprevention of head and neck squamous cell carcinomas |
| WO2010044893A1 (en) * | 2008-10-17 | 2010-04-22 | Merck & Co. | Combination therapy |
| 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 |
| EP2367939A4 (en) * | 2008-11-20 | 2012-07-04 | Oncotherapy Science Inc | METHOD FOR DIAGNOSIS OR TREATMENT OF PROSTATE CANCER |
| CA2760778A1 (en) * | 2009-05-13 | 2010-11-18 | Amgen Inc. | Heteroaryl compounds as pikk inhibitors |
| NZ599549A (en) | 2009-10-26 | 2013-11-29 | Signal Pharm Llc | Methods of synthesis and purification of heteroaryl compounds |
| AR078793A1 (es) * | 2009-10-27 | 2011-12-07 | Orion Corp | Derivados de carboxamidas no esteroidales y acil hidrazona moduladores de receptores androgenicos de tejido selectivo (sarm), composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer de prostata entre otros |
-
2013
- 2013-03-14 ES ES13714092.7T patent/ES2668279T3/es active Active
- 2013-03-14 US US13/803,317 patent/US20130245028A1/en not_active Abandoned
- 2013-03-14 EA EA201491701A patent/EA028062B1/ru not_active IP Right Cessation
- 2013-03-14 AU AU2013202992A patent/AU2013202992B2/en active Active
- 2013-03-14 CN CN201910158858.3A patent/CN109846884A/zh active Pending
- 2013-03-14 WO PCT/US2013/031217 patent/WO2013138560A1/en not_active Ceased
- 2013-03-14 MX MX2014011116A patent/MX359227B/es active IP Right Grant
- 2013-03-14 KR KR1020147028708A patent/KR102057357B1/ko active Active
- 2013-03-14 SG SG11201405686PA patent/SG11201405686PA/en unknown
- 2013-03-14 TW TW102109152A patent/TWI622395B/zh active
- 2013-03-14 BR BR112014022700-4A patent/BR112014022700A2/pt not_active Application Discontinuation
- 2013-03-14 CN CN201380024216.5A patent/CN104271138A/zh active Pending
- 2013-03-14 JP JP2015500599A patent/JP2015511964A/ja active Pending
- 2013-03-14 NZ NZ628420A patent/NZ628420A/en unknown
- 2013-03-14 UA UAA201411214A patent/UA114194C2/uk unknown
- 2013-03-14 CA CA2867174A patent/CA2867174C/en active Active
- 2013-03-14 EP EP13714092.7A patent/EP2825171B1/en active Active
- 2013-03-14 MY MYPI2014702599A patent/MY198666A/en unknown
-
2014
- 2014-09-12 ZA ZA2014/06708A patent/ZA201406708B/en unknown
- 2014-09-12 NI NI201400110A patent/NI201400110A/es unknown
- 2014-09-14 IL IL234639A patent/IL234639B/en active IP Right Grant
- 2014-09-15 PH PH12014502047A patent/PH12014502047B1/en unknown
-
2015
- 2015-08-13 AU AU2015213353A patent/AU2015213353B2/en active Active
-
2017
- 2017-11-13 JP JP2017218388A patent/JP6470822B2/ja active Active
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