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 |
| ES2638179T3 (es) | 2013-01-16 | 2017-10-19 | Signal Pharmaceuticals, Llc | Compuestos de pirrolopirimidina sustituidos, composiciones de los mismos, y métodos de tratamiento con los mismos |
| WO2014172431A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer |
| KR102459285B1 (ko) | 2013-04-17 | 2022-10-27 | 시그날 파마소티칼 엘엘씨 | 1-에틸-7-(2-메틸-6-(1H-1,2,4-트리아졸-3-일)피리딘-3-일)-3,4-디하이드로피라지노[2,3-b]피라진-2(1H)-온에 관한 약학 제제, 제조방법, 고체 형태 및 사용 방법 |
| TWI654979B (zh) | 2013-04-17 | 2019-04-01 | 美商標誌製藥公司 | 使用ｔｏｒ激酶抑制劑組合療法以治療癌症之方法 |
| JP6382945B2 (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 |
| WO2014172432A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer |
| KR102221029B1 (ko) | 2013-04-17 | 2021-02-26 | 시그날 파마소티칼 엘엘씨 | 디하이드로피라지노-피라진을 사용한 암의 치료 |
| 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 |
| CN113831345A (zh) | 2013-05-29 | 2021-12-24 | 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 |
| EP3131551A4 (en) | 2014-04-16 | 2017-09-20 | 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 |
| 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 |
| WO2015160868A1 (en) | 2014-04-16 | 2015-10-22 | Signal Pharmaceuticals, Llc | Methods for treating cancer using tor kinase inhibitor combination therapy |
| JP2017520603A (ja) | 2014-07-14 | 2017-07-27 | シグナル ファーマシューティカルズ，エルエルシー | 置換ピロロピリミジン化合物を使用するがんの治療方法及びその組成物 |
| 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 |
| JP2018519308A (ja) * | 2015-06-24 | 2018-07-19 | セルジーン コーポレイション | Ｄｎａｐｋ阻害剤でのがんの治療 |
| 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 |
| SG11201912403SA (en) | 2017-06-22 | 2020-01-30 | Celgene Corp | Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20140104060A (ko) | 2006-10-19 | 2014-08-27 | 시그날 파마소티칼 엘엘씨 | 헤테로아릴 화합물, 이들의 조성물 그리고 단백질 키나아제 억제제로서의 이들의 용도 |
| ZA200902384B (en) | 2006-10-19 | 2010-07-28 | Signal Pharm Llc | Heteroaryl compounds, compositions thereof, and use thereof as protein kinase inhibitors |
| US8236428B2 (en) * | 2008-07-10 | 2012-08-07 | Jx Nippon Mining & Metals Corporation | Hybrid silicon wafer and method for manufacturing same |
| 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 |
| 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 |
| WO2010058572A1 (en) * | 2008-11-20 | 2010-05-27 | Oncotherapy Science, Inc. | Methods for diagnosing or treating prostate cancer |
| MX2011012037A (es) * | 2009-05-13 | 2012-02-28 | Amgen Inc | Compuestos de heteroarilo como inhibidores de pikk. |
| MY177695A (en) | 2009-10-26 | 2020-09-23 | 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 EA EA201491701A patent/EA028062B1/ru not_active IP Right Cessation
- 2013-03-14 CN CN201910158858.3A patent/CN109846884A/zh active Pending
- 2013-03-14 CA CA2867174A patent/CA2867174C/en active Active
- 2013-03-14 EP EP13714092.7A patent/EP2825171B1/en active Active
- 2013-03-14 WO PCT/US2013/031217 patent/WO2013138560A1/en not_active Ceased
- 2013-03-14 JP JP2015500599A patent/JP2015511964A/ja active Pending
- 2013-03-14 CN CN201380024216.5A patent/CN104271138A/zh active Pending
- 2013-03-14 MY MYPI2014702599A patent/MY198666A/en unknown
- 2013-03-14 TW TW102109152A patent/TWI622395B/zh active
- 2013-03-14 KR KR1020147028708A patent/KR102057357B1/ko active Active
- 2013-03-14 UA UAA201411214A patent/UA114194C2/uk unknown
- 2013-03-14 NZ NZ628420A patent/NZ628420A/en unknown
- 2013-03-14 BR BR112014022700-4A patent/BR112014022700A2/pt not_active Application Discontinuation
- 2013-03-14 MX MX2014011116A patent/MX359227B/es active IP Right Grant
- 2013-03-14 ES ES13714092.7T patent/ES2668279T3/es active Active
- 2013-03-14 AU AU2013202992A patent/AU2013202992B2/en active Active
- 2013-03-14 SG SG11201405686PA patent/SG11201405686PA/en unknown
- 2013-03-14 US US13/803,317 patent/US20130245028A1/en not_active Abandoned
-
2014
- 2014-09-12 NI NI201400110A patent/NI201400110A/es unknown
- 2014-09-12 ZA ZA2014/06708A patent/ZA201406708B/en 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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