JP2018502098A5 - - Google Patents

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JP2018502098A5
JP2018502098A5 JP2017534308A JP2017534308A JP2018502098A5 JP 2018502098 A5 JP2018502098 A5 JP 2018502098A5 JP 2017534308 A JP2017534308 A JP 2017534308A JP 2017534308 A JP2017534308 A JP 2017534308A JP 2018502098 A5 JP2018502098 A5 JP 2018502098A5
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optionally substituted
alkyl
pharmaceutically acceptable
acceptable salt
solvate
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JP2018502098A (ja
JP6854762B2 (ja
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Priority claimed from PCT/US2015/000297 external-priority patent/WO2016105528A2/en
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JP2017534308A 2014-12-23 2015-12-23 サイクリン依存性キナーゼ7(cdk7)の阻害剤 Active JP6854762B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462096040P 2014-12-23 2014-12-23
US62/096,040 2014-12-23
PCT/US2015/000297 WO2016105528A2 (en) 2014-12-23 2015-12-23 Inhibitors of cyclin-dependent kinase 7 (cdk7)

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JP2018502098A JP2018502098A (ja) 2018-01-25
JP2018502098A5 true JP2018502098A5 (enExample) 2020-07-09
JP6854762B2 JP6854762B2 (ja) 2021-04-07

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US (2) US10870651B2 (enExample)
EP (1) EP3236959B1 (enExample)
JP (1) JP6854762B2 (enExample)
AU (1) AU2015371251B2 (enExample)
WO (1) WO2016105528A2 (enExample)

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