JP6787791B2 - 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)−オンの固体形態、その組成物、及びそれらの使用方法 - Google Patents

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)−オンの固体形態、その組成物、及びそれらの使用方法 Download PDF

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JP6787791B2
JP6787791B2 JP2016562778A JP2016562778A JP6787791B2 JP 6787791 B2 JP6787791 B2 JP 6787791B2 JP 2016562778 A JP2016562778 A JP 2016562778A JP 2016562778 A JP2016562778 A JP 2016562778A JP 6787791 B2 JP6787791 B2 JP 6787791B2
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JP2017511361A (ja
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エクケルト ジェフレイ
エクケルト ジェフレイ
メノン アニル
メノン アニル
ケイ.パリクフ ダルシャン
ケイ.パリクフ ダルシャン
ボエルセン ナサン
ボエルセン ナサン
レエ トーマス
レエ トーマス
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シグナル ファーマシューティカルズ,エルエルシー
シグナル ファーマシューティカルズ,エルエルシー
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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JP2016562778A 2014-04-16 2015-04-15 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)−オンの固体形態、その組成物、及びそれらの使用方法 Active JP6787791B2 (ja)

Applications Claiming Priority (5)

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US201461980108P 2014-04-16 2014-04-16
US61/980,108 2014-04-16
US201462003173P 2014-05-27 2014-05-27
US62/003,173 2014-05-27
PCT/US2015/025850 WO2015160875A1 (en) 2014-04-16 2015-04-15 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

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JP2019039173A Division JP2019116491A (ja) 2014-04-16 2019-03-05 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)−オンの固体形態、その組成物、及びそれらの使用方法

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JP2017511361A JP2017511361A (ja) 2017-04-20
JP2017511361A5 JP2017511361A5 (enExample) 2018-05-17
JP6787791B2 true JP6787791B2 (ja) 2020-11-18

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JP2016562778A Active JP6787791B2 (ja) 2014-04-16 2015-04-15 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)−オンの固体形態、その組成物、及びそれらの使用方法
JP2019039173A Withdrawn JP2019116491A (ja) 2014-04-16 2019-03-05 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)−オンの固体形態、その組成物、及びそれらの使用方法
JP2020208893A Pending JP2021054844A (ja) 2014-04-16 2020-12-17 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)−オンの固体形態、その組成物、及びそれらの使用方法

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JP2020208893A Pending JP2021054844A (ja) 2014-04-16 2020-12-17 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)−オンの固体形態、その組成物、及びそれらの使用方法

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US (2) US9416134B2 (enExample)
EP (1) EP3131553B1 (enExample)
JP (3) JP6787791B2 (enExample)
CA (2) CA3164682A1 (enExample)
ES (1) ES2913071T3 (enExample)
MX (2) MX370786B (enExample)
NZ (1) NZ714742A (enExample)
WO (1) WO2015160875A1 (enExample)

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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
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

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