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
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- JP
- Japan
- Prior art keywords
- pharmaceutical composition
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- 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.)
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- 239000008194 pharmaceutical composition Substances 0.000 claims 25
- 239000007787 solid Substances 0.000 claims 10
- -1 6- (2-hydroxypropan-2-yl) pyridin-3-yl Chemical group 0.000 claims 7
- QIQXTHQIDYTFRH-UHFFFAOYSA-N Stearic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 6
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 6
- WSVLPVUVIUVCRA-RJMJUYIDSA-N (2R,3R,4S,5R,6S)-2-(hydroxymethyl)-6-[(2R,3S,4R,5R)-4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol;hydrate 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)OC(O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-RJMJUYIDSA-N 0.000 claims 3
- HUTNOYOBQPAKIA-UHFFFAOYSA-N 1H-pyrazin-2-one Chemical compound OC1=CN=CC=N1 HUTNOYOBQPAKIA-UHFFFAOYSA-N 0.000 claims 3
- 229920003084 Avicel® PH-102 Polymers 0.000 claims 3
- 229960001021 Lactose Monohydrate Drugs 0.000 claims 3
- 235000021355 Stearic acid Nutrition 0.000 claims 3
- 239000007884 disintegrant Substances 0.000 claims 3
- 235000019359 magnesium stearate Nutrition 0.000 claims 3
- 230000037361 pathway Effects 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000011780 sodium chloride Substances 0.000 claims 3
- 239000008117 stearic acid Substances 0.000 claims 3
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 2
- 102000030951 Phosphotransferases Human genes 0.000 claims 2
- 108091000081 Phosphotransferases 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
- 208000008787 Cardiovascular Disease Diseases 0.000 claims 1
- 229960001681 Croscarmellose Sodium Drugs 0.000 claims 1
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 1
- 206010012601 Diabetes mellitus Diseases 0.000 claims 1
- 241000282412 Homo Species 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010053643 Neurodegenerative disease Diseases 0.000 claims 1
- 206010029331 Neuropathy peripheral Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 1
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 1
- 201000010099 disease 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
- 201000010915 glioblastoma multiforme Diseases 0.000 claims 1
- 230000001900 immune effect Effects 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000000155 isotopic Effects 0.000 claims 1
- 239000002207 metabolite Substances 0.000 claims 1
- 201000009251 multiple myeloma Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 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
Claims (32)
- 有効量の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)−オンまたはその薬剤的に許容される塩、同位体族、代謝産物、もしくは固体形態、ステアリン酸、およびラクトース一水和物を含む薬剤組成物。
- 約0.1〜5重量%のステアリン酸を含む請求項1に記載の薬剤組成物。
- 約0.4重量%のステアリン酸を含む請求項2に記載の薬剤組成物。
- 約40〜60重量%のラクトース一水和物を含む請求項1に記載の薬剤組成物。
- 約49.2重量%のラクトース一水和物を含む請求項4に記載の薬剤組成物。
- 微晶質セルロースをさらに含む請求項1に記載の薬剤組成物。
- 上記微晶質セルロースはAVICEL PH 102 (登録商標)である請求項6に記載の薬剤組成物。
- 約20〜40重量%のAVICEL PH 102 (登録商標)を含む請求項7に記載の薬剤組成物。
- 約31重量%のAVICEL PH 102 (登録商標)を含む請求項8に記載の薬剤組成物。
- 崩壊剤をさらに含む請求項1に記載の薬剤組成物。
- 上記崩壊剤はクロスカルメロースナトリウムである請求項10に記載の薬剤組成物。
- 上記崩壊剤はAC−DI−SOL(登録商標)である請求項10に記載の薬剤組成物。
- 約1〜5重量%からのAC−DI−SOL(登録商標)を含む請求項12の薬剤組成物。
- 約40〜60重量%の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)−オンまたはその薬剤的に許容される塩、同位体族、もしくは固体形態を含む請求項1に記載の薬剤組成物。
- 約15重量%の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)−オンまたはその薬剤的に許容される塩、同位体族、もしくは固体形態を含む請求項14に記載の薬剤組成物。
- 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)−オンの形態Aを含む請求項15に記載の薬剤組成物。
- ステアリン酸マグネシウムをさらに含む請求項1に記載の薬剤組成物。
- 約0.5〜3重量%からのステアリン酸マグネシウムを含む請求項17に記載の薬剤組成物。
- 約1重量%からのステアリン酸マグネシウムを含む請求項18に記載の薬剤組成物。
- 錠剤として製剤化されている請求項1に記載の薬剤組成物。
- 上記錠剤はフィルムコーティングされている請求項20に記載の薬剤組成物。
- 上記フィルムコーティングは上記錠剤の重量の約4%である請求項21に記載の薬剤組成物。
- 癌、炎症状態、免疫学的状態、神経変性疾患、糖尿病、肥満、神経障害、加齢関連疾患、心血管疾患、またはキナーゼ経路の阻害によって治療または予防可能な状態を治療または予防する方法であって、請求項1に記載の有効量の薬剤組成物を、それを必要とする患者(ヒトを除く)に投与する工程を含む方法。
- 上記キナーゼ経路はTORキナーゼ経路である請求項23に記載の方法。
- 患者(ヒトを除く)における完全奏効、部分奏効、または安定の固形癌効果評価基準(RECIST1.1)を達成するための方法であって、請求項1に記載の有効量の薬剤組成物を、固形腫瘍を有する患者(ヒトを除く)に投与する工程を有する方法。
- NHLのための国際ワークショップ基準(IWC)、多発性骨髄腫のための国際統一効果基準(IURC)、東部共同腫瘍学グループパフォーマンスステータス(ECOG)、またはGBMのための神経腫瘍学(RANO)ワーキンググループのための効果評価を改善する方法であって、請求項1に記載の有効量の薬剤組成物を、それを必要とする患者(ヒトを除く)に投与する工程を有する方法。
- 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)−オンの固体形態A。
- 2−θにおいておよそ8.3、13.2、18.2または21.7度で表される1つ以上のピークを有するX線粉末回折パターンを有する請求項27に記載の固体形態A。
- 約199℃のピーク温度で吸熱を有するDSCサーモグラムを有する請求項28に記載の固体形態A。
- 熱重量サーモグラムにおいて約25℃〜約100℃の間で約0.1%の重量損失を有する請求項29に記載の固体形態A。
- 無水である請求項30に記載の固体形態A。
- 実質的に純粋である請求項31に記載の固体形態A。
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 (ja) | 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 (24)
Country | Link |
---|---|
US (1) | US9403829B2 (ja) |
EP (1) | EP2785325B1 (ja) |
JP (2) | JP6076370B2 (ja) |
KR (1) | KR102040997B1 (ja) |
CN (1) | CN104093398B (ja) |
AU (1) | AU2012304276B2 (ja) |
BR (1) | BR112014013332B1 (ja) |
CA (2) | CA3125862A1 (ja) |
CO (1) | CO6990726A2 (ja) |
EA (1) | EA026390B1 (ja) |
EC (1) | ECSP14007473A (ja) |
ES (1) | ES2694413T3 (ja) |
HK (1) | HK1202052A1 (ja) |
IL (1) | IL232827B (ja) |
IN (1) | IN2014CN04037A (ja) |
MX (1) | MX363034B (ja) |
MY (1) | MY169749A (ja) |
NI (1) | NI201400052A (ja) |
PE (1) | PE20141696A1 (ja) |
PH (2) | PH12014501230B1 (ja) |
SG (2) | SG10201604558SA (ja) |
UA (1) | UA114496C2 (ja) |
WO (1) | WO2013082344A1 (ja) |
ZA (1) | ZA201403865B (ja) |
Cited By (1)
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JP7282045B2 (ja) | 2017-06-22 | 2023-05-26 | セルジーン コーポレイション | B型肝炎ウイルス感染を特徴とする肝細胞癌の治療 |
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AU2014254058B2 (en) * | 2013-04-17 | 2019-06-06 | Signal Pharmaceuticals, Llc | Combination therapy comprising a Dihydropyrazino-Pyrazine Compound and an androgen receptor antagonist for treating prostate cancer |
MX2015014455A (es) | 2013-04-17 | 2016-07-21 | Signal Pharm Llc | Terapia de combinacion que comprende un inhibidor de tor cinasa y n-(3-(5-fluoro-2-(4-(2-metoxietoxi)fenilamino)pirimidin-4-ilamino )fenil)acrilamida para tratar cancer. |
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KR102223060B1 (ko) | 2013-04-17 | 2021-03-05 | 시그날 파마소티칼 엘엘씨 | 암 치료를 위한 TOR 키나제 억제제 및 IMiD 화합물을 포함하는 조합요법 |
CA3143529A1 (en) * | 2013-05-29 | 2014-12-04 | Signal Pharmaceuticals, Llc | Pharmaceutical compositions 0f 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 |
ES2823756T3 (es) | 2014-04-16 | 2021-05-10 | Signal Pharm Llc | Métodos para tratar el cáncer usando terapia de combinación de inhibidores de quinasa TOR |
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 |
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EA201790189A1 (ru) | 2014-07-14 | 2017-11-30 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Способы лечения злокачественного новообразования с использованием замещенных пирролопиримидиновых соединений, композиции на их основе |
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
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JP7282045B2 (ja) | 2017-06-22 | 2023-05-26 | セルジーン コーポレイション | B型肝炎ウイルス感染を特徴とする肝細胞癌の治療 |
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