JP2015516375A5 - - Google Patents
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- Publication number
- JP2015516375A5 JP2015516375A5 JP2015500595A JP2015500595A JP2015516375A5 JP 2015516375 A5 JP2015516375 A5 JP 2015516375A5 JP 2015500595 A JP2015500595 A JP 2015500595A JP 2015500595 A JP2015500595 A JP 2015500595A JP 2015516375 A5 JP2015516375 A5 JP 2015516375A5
- Authority
- JP
- Japan
- Prior art keywords
- ets
- dihydropyrazino
- ethyl
- methyl
- triazol
- 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
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 18
- 238000000034 method Methods 0.000 claims 17
- 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
- 239000012472 biological sample Substances 0.000 claims 7
- 230000002018 overexpression Effects 0.000 claims 7
- 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 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
- 102100022466 Eukaryotic translation initiation factor 4E-binding protein 1 Human genes 0.000 claims 5
- 108050000946 Eukaryotic translation initiation factor 4E-binding protein 1 Proteins 0.000 claims 5
- 230000005764 inhibitory process Effects 0.000 claims 3
- 230000027405 negative regulation of phosphorylation Effects 0.000 claims 3
- HUTNOYOBQPAKIA-UHFFFAOYSA-N 1h-pyrazin-2-one Chemical compound OC1=CN=CC=N1 HUTNOYOBQPAKIA-UHFFFAOYSA-N 0.000 claims 2
- 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 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
- 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
- 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
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000012544 monitoring process Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 239000011574 phosphorus Substances 0.000 claims 1
- 230000026731 phosphorylation Effects 0.000 claims 1
- 238000006366 phosphorylation reaction Methods 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261611370P | 2012-03-15 | 2012-03-15 | |
| US61/611,370 | 2012-03-15 | ||
| US201261715329P | 2012-10-18 | 2012-10-18 | |
| US61/715,329 | 2012-10-18 | ||
| PCT/US2013/031202 WO2013138556A1 (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 |
|---|---|---|---|
| JP2017218364A Division JP6470821B2 (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 |
|---|---|
| JP2015516375A JP2015516375A (ja) | 2015-06-11 |
| JP2015516375A5 true JP2015516375A5 (enExample) | 2016-04-21 |
Family
ID=47998542
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015500595A Pending JP2015516375A (ja) | 2012-03-15 | 2013-03-14 | Ｔｏｒキナーゼ阻害剤を用いた癌の治療 |
| JP2017218364A Active JP6470821B2 (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 |
|---|---|---|---|
| JP2017218364A Active JP6470821B2 (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 (20)
| Country | Link |
|---|---|
| US (1) | US20130245029A1 (enExample) |
| EP (1) | EP2825168B1 (enExample) |
| JP (2) | JP2015516375A (enExample) |
| KR (3) | KR20190058673A (enExample) |
| CN (2) | CN107137402A (enExample) |
| AU (1) | AU2013203156C1 (enExample) |
| BR (1) | BR112014022697A2 (enExample) |
| CA (1) | CA2867349A1 (enExample) |
| EA (1) | EA028434B1 (enExample) |
| ES (1) | ES2677908T3 (enExample) |
| IL (2) | IL234640B (enExample) |
| MX (1) | MX360877B (enExample) |
| MY (1) | MY182650A (enExample) |
| NI (1) | NI201400109A (enExample) |
| NZ (1) | NZ628421A (enExample) |
| PH (2) | PH12014502048B1 (enExample) |
| SG (1) | SG11201405706TA (enExample) |
| TW (2) | TWI600428B (enExample) |
| WO (1) | WO2013138556A1 (enExample) |
| ZA (1) | ZA201406709B (enExample) |
Families Citing this family (21)
| 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 |
| MX2015009209A (es) | 2013-01-16 | 2016-03-17 | Signal Pharm Llc | Compuestos sustituidos de pirrolopirimidina, composiciones de los mismos, y metodos de tratamiento con los mismos. |
| 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 |
| 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. |
| CA2908353C (en) | 2013-04-17 | 2021-11-02 | Signal Pharmaceuticals, Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| AU2014254059B2 (en) | 2013-04-17 | 2019-06-06 | Signal Pharmaceuticals, Llc | Combination therapy comprising a TOR kinase inhibitor and a cytidine analog for treating cancer |
| CA2908957C (en) | 2013-04-17 | 2021-05-18 | Signal Pharmaceuticals, Llc | Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer |
| US9505764B2 (en) | 2013-04-17 | 2016-11-29 | Signal Pharmaceuticals, Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| EA030726B1 (ru) | 2013-04-17 | 2018-09-28 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | ФАРМАЦЕВТИЧЕСКИЕ СОСТАВЫ, СПОСОБЫ, ТВЕРДЫЕ ФОРМЫ И СПОСОБЫ ПРИМЕНЕНИЯ, ОТНОСЯЩИЕСЯ К 1-ЭТИЛ-7-(2-МЕТИЛ-6-(1H-1,2,4-ТРИАЗОЛ-3-ИЛ)ПИРИДИН-3-ИЛ)-3,4-ДИГИДРОПИРАЗИНО[2,3-b]ПИРАЗИН-2(1H)-ОНУ |
| HK1223286A1 (zh) | 2013-05-29 | 2017-07-28 | 西格诺药品有限公司 | 7-(6-(2-羟基丙-2-基)吡啶-3-基)-1-((反式)-4-甲氧基环己基)-3，4-二氢吡嗪并[2，3-b]吡嗪-2(1h)-酮的药物组合物、其固体形式及它们的使用方法 |
| JP2017511367A (ja) | 2014-04-16 | 2017-04-20 | シグナル ファーマシューティカルズ，エルエルシー | １−エチル−７−（２−メチル−６−（１Ｈ−１，２，４−トリアゾール−３−イル）ピリジン−３−イル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オン及び共形成物を含む固体形態、その組成物及び使用方法 |
| 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 |
| EP3131552B1 (en) | 2014-04-16 | 2020-07-15 | Signal Pharmaceuticals, LLC | Methods for treating cancer using tor kinase inhibitor combination therapy |
| EA201790189A1 (ru) | 2014-07-14 | 2017-11-30 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Способы лечения злокачественного новообразования с использованием замещенных пирролопиримидиновых соединений, композиции на их основе |
| 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 |
| PE20191474A1 (es) | 2016-12-20 | 2019-10-16 | Astrazeneca Ab | Compuestos de amino-triazolopiridina y su uso en el tratamiento del cancer |
| ES2959860T3 (es) | 2017-06-22 | 2024-02-28 | Celgene Corp | Tratamiento del carcinoma hepatocelular caracterizado por la infección por el virus de la hepatitis B |
| EP3759545B1 (en) * | 2018-03-01 | 2023-12-20 | Essilor International | Lens element |
| BR202019004173Y1 (pt) | 2018-03-01 | 2024-02-20 | Essilor International | Dispositivo óptico |
| CN113493471B (zh) * | 2020-04-03 | 2024-06-11 | 山东轩竹医药科技有限公司 | 杂芳环类激酶抑制剂 |
Family Cites Families (5)
| 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 |
| US7981893B2 (en) * | 2006-10-19 | 2011-07-19 | Signal Pharmaceuticals, Llc | Heteroaryl compounds, compositions thereof, and methods of treatment therewith |
| 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 |
| NZ618135A (en) | 2009-10-26 | 2015-05-29 | Signal Pharm Llc | Methods of synthesis and purification of heteroaryl compounds |
| WO2011133668A2 (en) * | 2010-04-20 | 2011-10-27 | President And Fellows Of Harvard College | Methods and compositions for the treatment of cancer |
-
2013
- 2013-03-14 CN CN201710422322.9A patent/CN107137402A/zh active Pending
- 2013-03-14 SG SG11201405706TA patent/SG11201405706TA/en unknown
- 2013-03-14 NZ NZ628421A patent/NZ628421A/en not_active IP Right Cessation
- 2013-03-14 US US13/803,323 patent/US20130245029A1/en not_active Abandoned
- 2013-03-14 JP JP2015500595A patent/JP2015516375A/ja active Pending
- 2013-03-14 MX MX2014011117A patent/MX360877B/es active IP Right Grant
- 2013-03-14 TW TW102109153A patent/TWI600428B/zh active
- 2013-03-14 EP EP13712647.0A patent/EP2825168B1/en active Active
- 2013-03-14 TW TW106122809A patent/TWI664968B/zh active
- 2013-03-14 CA CA2867349A patent/CA2867349A1/en not_active Abandoned
- 2013-03-14 BR BR112014022697-0A patent/BR112014022697A2/pt not_active Application Discontinuation
- 2013-03-14 KR KR1020197014135A patent/KR20190058673A/ko not_active Ceased
- 2013-03-14 MY MYPI2014702606A patent/MY182650A/en unknown
- 2013-03-14 ES ES13712647.0T patent/ES2677908T3/es active Active
- 2013-03-14 AU AU2013203156A patent/AU2013203156C1/en not_active Ceased
- 2013-03-14 CN CN201380025102.2A patent/CN104302295B/zh active Active
- 2013-03-14 KR KR1020147028710A patent/KR102057358B1/ko active Active
- 2013-03-14 KR KR1020207008188A patent/KR20200034818A/ko not_active Ceased
- 2013-03-14 EA EA201491694A patent/EA028434B1/ru not_active IP Right Cessation
- 2013-03-14 WO PCT/US2013/031202 patent/WO2013138556A1/en not_active Ceased
-
2014
- 2014-09-12 NI NI201400109A patent/NI201400109A/es unknown
- 2014-09-12 ZA ZA2014/06709A patent/ZA201406709B/en unknown
- 2014-09-14 IL IL234640A patent/IL234640B/en active IP Right Grant
- 2014-09-15 PH PH12014502048A patent/PH12014502048B1/en unknown
-
2017
- 2017-11-13 JP JP2017218364A patent/JP6470821B2/ja active Active
-
2018
- 2018-10-18 PH PH12018502234A patent/PH12018502234B1/en unknown
-
2020
- 2020-04-28 IL IL274318A patent/IL274318A/en unknown
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