JP2015500236A5 - - Google Patents
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- JP2015500236A5 JP2015500236A5 JP2014544901A JP2014544901A JP2015500236A5 JP 2015500236 A5 JP2015500236 A5 JP 2015500236A5 JP 2014544901 A JP2014544901 A JP 2014544901A JP 2014544901 A JP2014544901 A JP 2014544901A JP 2015500236 A5 JP2015500236 A5 JP 2015500236A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- composition according
- weight
- solid form
- 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.)
- Granted
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 25
- 239000007787 solid Substances 0.000 claims 10
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- -1 6- (2-hydroxypropan-2-yl) pyridin-3-yl Chemical group 0.000 claims 5
- HUTNOYOBQPAKIA-UHFFFAOYSA-N 1h-pyrazin-2-one Chemical compound OC1=CN=CC=N1 HUTNOYOBQPAKIA-UHFFFAOYSA-N 0.000 claims 3
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims 3
- 229920003084 Avicel® PH-102 Polymers 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 235000021355 Stearic acid Nutrition 0.000 claims 3
- 239000007884 disintegrant Substances 0.000 claims 3
- 229960001021 lactose monohydrate Drugs 0.000 claims 3
- 235000019359 magnesium stearate Nutrition 0.000 claims 3
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 3
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 3
- 230000037361 pathway Effects 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000008117 stearic acid Substances 0.000 claims 3
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 1
- 241000282412 Homo Species 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims 1
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical group [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 1
- 229960001681 croscarmellose sodium Drugs 0.000 claims 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 239000007888 film coating Substances 0.000 claims 1
- 238000009501 film coating Methods 0.000 claims 1
- 230000001900 immune effect Effects 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000000155 isotopic effect Effects 0.000 claims 1
- 239000002207 metabolite Substances 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 238000001757 thermogravimetry curve Methods 0.000 claims 1
- 230000004580 weight loss Effects 0.000 claims 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161566109P | 2011-12-02 | 2011-12-02 | |
| US61/566,109 | 2011-12-02 | ||
| US201261647288P | 2012-05-15 | 2012-05-15 | |
| US61/647,288 | 2012-05-15 | ||
| US201261653439P | 2012-05-31 | 2012-05-31 | |
| US61/653,439 | 2012-05-31 | ||
| US201261670419P | 2012-07-11 | 2012-07-11 | |
| US61/670,419 | 2012-07-11 | ||
| PCT/US2012/067172 WO2013082344A1 (en) | 2011-12-02 | 2012-11-30 | 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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016215572A Division JP2017048227A (ja) | 2011-12-02 | 2016-11-02 | ７−（６−（２−ヒドロキシプロパン−２−イル）ピリジン−３−イル）−１−（（トランス）−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）−オンの薬剤組成物、その固体形態、およびその使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015500236A JP2015500236A (ja) | 2015-01-05 |
| JP2015500236A5 true JP2015500236A5 (https=) | 2015-12-24 |
| JP6076370B2 JP6076370B2 (ja) | 2017-02-08 |
Family
ID=47324465
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014544901A Active JP6076370B2 (ja) | 2011-12-02 | 2012-11-30 | ７−（６−（２−ヒドロキシプロパン−２−イル）ピリジン−３−イル）−１−（（トランス）−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）−オンの薬剤組成物、その固体形態、およびその使用方法 |
| JP2016215572A Pending JP2017048227A (ja) | 2011-12-02 | 2016-11-02 | ７−（６−（２−ヒドロキシプロパン−２−イル）ピリジン−３−イル）−１−（（トランス）−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）−オンの薬剤組成物、その固体形態、およびその使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016215572A Pending JP2017048227A (ja) | 2011-12-02 | 2016-11-02 | ７−（６−（２−ヒドロキシプロパン−２−イル）ピリジン−３−イル）−１−（（トランス）−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）−オンの薬剤組成物、その固体形態、およびその使用方法 |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US9403829B2 (https=) |
| EP (1) | EP2785325B1 (https=) |
| JP (2) | JP6076370B2 (https=) |
| KR (1) | KR102040997B1 (https=) |
| CN (1) | CN104093398B (https=) |
| AU (1) | AU2012304276B2 (https=) |
| BR (1) | BR112014013332B1 (https=) |
| CA (2) | CA3125862C (https=) |
| CO (1) | CO6990726A2 (https=) |
| EA (1) | EA026390B1 (https=) |
| EC (1) | ECSP14007473A (https=) |
| ES (1) | ES2694413T3 (https=) |
| IL (1) | IL232827B (https=) |
| IN (1) | IN2014CN04037A (https=) |
| MX (1) | MX363034B (https=) |
| MY (1) | MY169749A (https=) |
| NI (1) | NI201400052A (https=) |
| PE (1) | PE20141696A1 (https=) |
| PH (2) | PH12014501230B1 (https=) |
| SG (2) | SG11201402766UA (https=) |
| UA (1) | UA114496C2 (https=) |
| WO (1) | WO2013082344A1 (https=) |
| ZA (1) | ZA201403865B (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101978537B1 (ko) | 2011-10-19 | 2019-05-14 | 시그날 파마소티칼 엘엘씨 | Tor 키나제 억제제를 사용한 암의 치료 |
| 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 |
| EP2945636B1 (en) | 2013-01-16 | 2017-06-28 | Signal Pharmaceuticals, LLC | Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith |
| AU2014254052B2 (en) | 2013-04-17 | 2019-06-06 | Signal Pharmaceuticals, Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| BR112015026292B1 (pt) | 2013-04-17 | 2022-04-12 | Signal Pharmaceuticals, Llc | Uso de 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 e métodos in vitro |
| CN105358177B (zh) | 2013-04-17 | 2018-11-23 | 西格诺药品有限公司 | 包含tor激酶抑制剂和imid化合物的联合疗法用于治疗癌症 |
| TW201521725A (zh) | 2013-04-17 | 2015-06-16 | Signal Pharm Llc | 使用ｔｏｒ激酶抑制劑組合療法以治療癌症之方法 |
| TW201527300A (zh) | 2013-04-17 | 2015-07-16 | Signal Pharm Llc | 關於１－乙基－７－（２－甲基－６－（１Ｈ－１，２，４－三唑－３－基）吡啶－３－基）－３，４－二氫吡并［２，３－ｂ］吡－２（１Ｈ）－酮之醫藥調配物、方法、固態型式及使用方法 |
| BR112015026297B1 (pt) | 2013-04-17 | 2022-08-23 | Signal Pharmaceuticals, Llc | Uso de um inibidor da quinase tor e quinazolinona 5-substituída, composição farmacêutica que os compreende, e kit |
| US9782427B2 (en) | 2013-04-17 | 2017-10-10 | Signal Pharmaceuticals, Llc | Methods for treating cancer using TOR kinase inhibitor combination therapy |
| US9937169B2 (en) * | 2013-04-17 | 2018-04-10 | Signal Pharmaceuticals, Llc | Methods for treating cancer using dihydropyrazino-pyrazine compound combination therapy |
| EP3003313A1 (en) * | 2013-05-29 | 2016-04-13 | Signal Pharmaceuticals, 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 |
| 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 |
| 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 |
| 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 |
| EP3641772B1 (en) * | 2017-06-22 | 2023-08-02 | Celgene Corporation | Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection |
| CN112409399B (zh) * | 2019-08-20 | 2022-06-28 | 德琪(浙江)医药科技有限公司 | 一种药物中间体化合物的制备方法 |
| WO2021067772A1 (en) * | 2019-10-04 | 2021-04-08 | Sumitomo Dainippon Pharma Oncology, Inc. | Axl inhibitor formulations |
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| MY177695A (en) * | 2009-10-26 | 2020-09-23 | Signal Pharm Llc | Methods of synthesis and purification of heteroaryl compounds |
| EP2531194B1 (en) | 2010-02-03 | 2018-04-18 | Signal Pharmaceuticals, LLC | Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors |
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