JP2017518981A5 - - Google Patents

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JP2017518981A5
JP2017518981A5 JP2016567819A JP2016567819A JP2017518981A5 JP 2017518981 A5 JP2017518981 A5 JP 2017518981A5 JP 2016567819 A JP2016567819 A JP 2016567819A JP 2016567819 A JP2016567819 A JP 2016567819A JP 2017518981 A5 JP2017518981 A5 JP 2017518981A5
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trka
composition
pain
cancer
compound
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JP6499672B2 (ja
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JP2016567819A 2014-05-15 2015-05-14 TrkAキナーゼ阻害剤としての1−((3S,4R)−4−(3−フルオロフェニル)−1−(2−メトキシエチル)ピロリジン−3−イル)−3−(4−メチル−3−(2−メチルピリミジン−5−イル)−1−フェニル−1H−ピラゾール−5−イル)尿素 Active JP6499672B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461993426P 2014-05-15 2014-05-15
US61/993,426 2014-05-15
PCT/US2015/030795 WO2015175788A1 (en) 2014-05-15 2015-05-14 1-((3s,4r)-4-(3-fluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(4-methyl-3-(2-methylpyrimidin-5-yl)-1-phenyl-1h-pyrazol-5-yl)urea as a trka kinase inhibitor

Related Child Applications (1)

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JP2019048124A Division JP2019085427A (ja) 2014-05-15 2019-03-15 TrkAキナーゼ阻害剤としての1−((3S,4R)−4−(3−フルオロフェニル)−1−(2−メトキシエチル)ピロリジン−3−イル)−3−(4−メチル−3−(2−メチルピリミジン−5−イル)−1−フェニル−1H−ピラゾール−5−イル)尿素

Publications (3)

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JP2017518981A JP2017518981A (ja) 2017-07-13
JP2017518981A5 true JP2017518981A5 (enExample) 2018-10-25
JP6499672B2 JP6499672B2 (ja) 2019-04-10

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JP2016567819A Active JP6499672B2 (ja) 2014-05-15 2015-05-14 TrkAキナーゼ阻害剤としての1−((3S,4R)−4−(3−フルオロフェニル)−1−(2−メトキシエチル)ピロリジン−3−イル)−3−(4−メチル−3−(2−メチルピリミジン−5−イル)−1−フェニル−1H−ピラゾール−5−イル)尿素
JP2019048124A Pending JP2019085427A (ja) 2014-05-15 2019-03-15 TrkAキナーゼ阻害剤としての1−((3S,4R)−4−(3−フルオロフェニル)−1−(2−メトキシエチル)ピロリジン−3−イル)−3−(4−メチル−3−(2−メチルピリミジン−5−イル)−1−フェニル−1H−ピラゾール−5−イル)尿素

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JP2019048124A Pending JP2019085427A (ja) 2014-05-15 2019-03-15 TrkAキナーゼ阻害剤としての1−((3S,4R)−4−(3−フルオロフェニル)−1−(2−メトキシエチル)ピロリジン−3−イル)−3−(4−メチル−3−(2−メチルピリミジン−5−イル)−1−フェニル−1H−ピラゾール−5−イル)尿素

Country Status (30)

Country Link
US (1) US10835533B2 (enExample)
EP (2) EP3154959B1 (enExample)
JP (2) JP6499672B2 (enExample)
KR (2) KR102321883B1 (enExample)
CN (2) CN109970614B (enExample)
AU (2) AU2015259075B2 (enExample)
CA (1) CA2949160C (enExample)
CL (1) CL2016002900A1 (enExample)
CR (1) CR20160583A (enExample)
CY (1) CY1122075T1 (enExample)
DK (1) DK3154959T3 (enExample)
ES (1) ES2746530T3 (enExample)
HR (1) HRP20191593T1 (enExample)
HU (1) HUE045340T2 (enExample)
IL (1) IL248924B (enExample)
LT (1) LT3154959T (enExample)
MA (1) MA40434B1 (enExample)
MX (2) MX2016014945A (enExample)
MY (1) MY191956A (enExample)
NZ (1) NZ727418A (enExample)
PH (2) PH12016502242B1 (enExample)
PL (1) PL3154959T3 (enExample)
PT (1) PT3154959T (enExample)
RS (1) RS59286B1 (enExample)
RU (1) RU2719489C2 (enExample)
SG (2) SG11201609550PA (enExample)
SI (1) SI3154959T1 (enExample)
SM (1) SMT201900522T1 (enExample)
UA (1) UA122126C2 (enExample)
WO (1) WO2015175788A1 (enExample)

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