JP5925809B2 - 三環系ピロロ誘導体、その調製方法およびそのキナーゼ阻害剤としての使用 - Google Patents

三環系ピロロ誘導体、その調製方法およびそのキナーゼ阻害剤としての使用 Download PDF

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JP5925809B2
JP5925809B2 JP2013550833A JP2013550833A JP5925809B2 JP 5925809 B2 JP5925809 B2 JP 5925809B2 JP 2013550833 A JP2013550833 A JP 2013550833A JP 2013550833 A JP2013550833 A JP 2013550833A JP 5925809 B2 JP5925809 B2 JP 5925809B2
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formula
compound
methyl
pyrrolo
quinazoline
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JP2014503567A (ja
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カルダレツリ,マリーナ
アンジヨリニ,マウロ
ベリア,イタロ
ブラスカ,マリア・ガブリエツラ
カスシエツリ,フランチエスコ
ダレツシオ,ロベルト
ロンバルデイ・ボルジア,アンドレア
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ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ
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JP2013550833A 2011-01-26 2012-01-19 三環系ピロロ誘導体、その調製方法およびそのキナーゼ阻害剤としての使用 Active JP5925809B2 (ja)

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EP11152190.2 2011-01-26
EP11152190 2011-01-26
PCT/EP2012/050773 WO2012101032A1 (en) 2011-01-26 2012-01-19 Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors

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JP2015203440A Division JP6118383B2 (ja) 2011-01-26 2015-10-15 三環系ピロロ誘導体、その調製方法およびそのキナーゼ阻害剤としての使用

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JP2014503567A JP2014503567A (ja) 2014-02-13
JP2014503567A5 JP2014503567A5 (enExample) 2015-03-05
JP5925809B2 true JP5925809B2 (ja) 2016-05-25

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JP2015203440A Active JP6118383B2 (ja) 2011-01-26 2015-10-15 三環系ピロロ誘導体、その調製方法およびそのキナーゼ阻害剤としての使用

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US (2) US8975267B2 (enExample)
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BR (1) BR112013018515B1 (enExample)
ES (1) ES2602791T3 (enExample)
RU (1) RU2591191C2 (enExample)
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WO2012101032A1 (en) 2012-08-02
US9309253B2 (en) 2016-04-12
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RU2591191C2 (ru) 2016-07-10
BR112013018515A2 (pt) 2016-10-18
US8975267B2 (en) 2015-03-10
JP6118383B2 (ja) 2017-04-19
BR112013018515B1 (pt) 2021-06-29
US20150141408A1 (en) 2015-05-21
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