JP2018501266A5 - - Google Patents

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JP2018501266A5
JP2018501266A5 JP2017533569A JP2017533569A JP2018501266A5 JP 2018501266 A5 JP2018501266 A5 JP 2018501266A5 JP 2017533569 A JP2017533569 A JP 2017533569A JP 2017533569 A JP2017533569 A JP 2017533569A JP 2018501266 A5 JP2018501266 A5 JP 2018501266A5
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Priority claimed from PCT/FI2015/050930 external-priority patent/WO2016102776A1/en
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本発明の目的は、式(I)
Figure 2018501266
(式中、R1及びR3は、夫々独立して、H、ハロゲン原子、炭素原子数1乃至3のハロアルキル基、炭素原子数1乃至3のペルハロアルキル基、CN、NO、N(R’)、(CHN(R’)、OR’、(CHOR’からなる群から選択され;
R2は、SOOH、SOR’’、SON(R’)、(CHO)PO(OR’)、COOR’’’、C(O)N(R’)、C(O)(CHN(R’)、C(O)CHNR’C(O)R’、C(O)CHNR’C(O)OR’’及びC(O)R’’’からなる群から選択され;
R4は、H又は炭素原子数1乃至3のアルキル基を表し;
ここで、R’はH又は炭素原子数1乃至6のアルキル基、炭素原子数1乃至3のハロアルキル基、又は炭素原子数1乃至3のペルハロアルキル基を表すか、又はR’がN(R’)の一部である場合、両R’はそれらが結合する窒素原子と一緒になって夫々独立してN及びOから選択される1又は2のヘテロ原子を含む5又は6員の脂肪族の又は芳香族の複素環又は荷電したN(R’) 基(ここでR’は上記で定義された通りである。)を形成し得、
R’’は、炭素原子数1乃至6のアルキル基、炭素原子数1乃至3のハロアルキル基、炭素原子数1乃至3のペルハロアルキル基、又は任意に置換されたフェニル基を表し;
R’’’は、炭素原子数1乃至6のアルキル基;炭素原子数2乃至6のアルケニル基;
−(CH−炭素原子数3乃至6のシクロアルキル基;C(O)R’(ここで、R’は上記で定義した通りである。)によって任意のN原子が所望により置換された、N及びOから夫々独立に選択された1又は2のヘテロ原子を含む5乃至6員の脂肪族の又は芳香族の複素環;又は任意に置換されたフェニル基を表し;
mは、0又は1であり;及び
nは、1又は2であり、
但し、R1がHを表す場合,R2はC(O)Me、C(O)CHNMe、S(O)NH、S(O)NMe、又はS(O)Meを表さない。)で表される新規な化合物により達成し得る。
JP2017533569A 2014-12-23 2015-12-22 17β−HSD1−阻害剤のプロドラッグ Active JP6523461B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FI20146150 2014-12-23
FI20146150 2014-12-23
PCT/FI2015/050930 WO2016102776A1 (en) 2014-12-23 2015-12-22 Prodrugs of 17.beta.-hsd1 -inhibitors

Publications (3)

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JP2018501266A JP2018501266A (ja) 2018-01-18
JP2018501266A5 true JP2018501266A5 (ja) 2019-01-17
JP6523461B2 JP6523461B2 (ja) 2019-06-05

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JP2017533569A Active JP6523461B2 (ja) 2014-12-23 2015-12-22 17β−HSD1−阻害剤のプロドラッグ

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US (1) US10413557B2 (ja)
EP (1) EP3237431B1 (ja)
JP (1) JP6523461B2 (ja)
CN (1) CN107207561B (ja)
WO (1) WO2016102776A1 (ja)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3237430B1 (en) * 2014-12-23 2019-03-20 Forendo Pharma Ltd PRODRUGS OF 17ß -HSD1 -INHIBITORS
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WO2023122075A1 (en) * 2021-12-20 2023-06-29 Ohio State Innovation Foundation Compositions comprising sterol-amino-phosphate compounds and methods of making and use thereof

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