JP5268635B2 - １７β−ＨＳＤ１及びＳＴＳインヒビター - Google Patents
１７β−ＨＳＤ１及びＳＴＳインヒビター Download PDFInfo
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- JP5268635B2 JP5268635B2 JP2008512837A JP2008512837A JP5268635B2 JP 5268635 B2 JP5268635 B2 JP 5268635B2 JP 2008512837 A JP2008512837 A JP 2008512837A JP 2008512837 A JP2008512837 A JP 2008512837A JP 5268635 B2 JP5268635 B2 JP 5268635B2
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- Prior art keywords
- alkyl
- group
- optionally substituted
- alkoxy
- aryl
- Prior art date
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- 108010070743 3(or 17)-beta-hydroxysteroid dehydrogenase Proteins 0.000 title description 59
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 109
- 150000002367 halogens Chemical group 0.000 claims description 107
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 106
- 125000004122 cyclic group Chemical group 0.000 claims description 91
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- 125000001072 heteroaryl group Chemical group 0.000 claims description 74
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- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 claims description 52
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- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 43
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 41
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- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims description 17
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- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 8
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- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 6
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- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 claims description 5
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Classifications
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Landscapes
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05104534 | 2005-05-26 | ||
| EP05104534.2 | 2005-05-26 | ||
| PCT/EP2006/062587 WO2006125800A1 (en) | 2005-05-26 | 2006-05-24 | 17β-HSD1 AND STS INHIBITORS |
Publications (3)
| Publication Number | Publication Date |
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| JP2008545678A JP2008545678A (ja) | 2008-12-18 |
| JP2008545678A5 JP2008545678A5 (cg-RX-API-DMAC7.html) | 2009-07-02 |
| JP5268635B2 true JP5268635B2 (ja) | 2013-08-21 |
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| JP2008512837A Expired - Fee Related JP5268635B2 (ja) | 2005-05-26 | 2006-05-24 | １７β−ＨＳＤ１及びＳＴＳインヒビター |
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| US8080540B2 (en) | 2006-09-19 | 2011-12-20 | Abbott Products Gmbh | Therapeutically active triazoles and their use |
| AU2007327653B2 (en) * | 2006-11-30 | 2013-04-18 | Solvay Pharmaceuticals Gmbh | Substituted estratrien derivatives as 17beta HSD inhibitors |
| US8288367B2 (en) | 2006-11-30 | 2012-10-16 | Solvay Pharmaceuticals Gmbh | Substituted estratriene derivatives as 17BETA HSD inhibitors |
| US11072632B2 (en) | 2011-03-25 | 2021-07-27 | UNIVERSITé LAVAL | Inhibitors of 17β-HSD1, 17β-HSD3 and 17β-HSD10 |
| SG195118A1 (en) | 2011-06-01 | 2013-12-30 | Estetra S A | Process for the production of estetrol intermediates |
| PT2714712T (pt) | 2011-06-01 | 2016-11-08 | Estetra Sprl | Processo para a produção de intermediários de estetrol |
| EP2383279A1 (en) | 2011-07-19 | 2011-11-02 | Pantarhei Bioscience B.V. | Process for the preparation of estetrol |
| WO2013078413A1 (en) * | 2011-11-22 | 2013-05-30 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Modulators of lipid storage |
| TW201512215A (zh) | 2013-06-25 | 2015-04-01 | Forendo Pharma Ltd | 治療活性雌三烯噻唑衍生物 |
| JP6456373B2 (ja) * | 2013-06-25 | 2019-01-23 | フォレンド ファーマ リミテッド | １７β−ヒドロキシステロイドデヒドロゲナーゼ タイプ１の阻害剤として治療活性のあるエストラトリエンチアゾール誘導体 |
| JP6556125B2 (ja) * | 2013-06-25 | 2019-08-07 | フォレンド ファーマ リミテッド | １７β−ヒドロキシステロイドデヒドロゲナーゼの阻害剤としての治療的に活性な１７−窒素置換エストラトリエンチアゾール誘導体 |
| JP6545266B2 (ja) | 2014-12-23 | 2019-07-17 | フォレンド ファーマ リミテッド | １７β‐ＨＳＤ１抑制剤のプロドラッグ |
| CN107207561B (zh) * | 2014-12-23 | 2020-03-31 | 佛恩多制药有限公司 | 17β-HSD1–抑制剂的前药 |
| LT3310346T (lt) | 2015-06-18 | 2021-06-10 | Estetra Sprl | Burnoje disperguojama tabletė, turinti estetrolio |
| LT3310345T (lt) | 2015-06-18 | 2021-06-25 | Estetra Sprl | Burnoje disperguojama tabletė, turinti estetrolio |
| DK3701944T3 (da) | 2015-06-18 | 2022-03-14 | Estetra Srl | Oro-dispergerbar doseringsenhed indeholdende en estetrolkomponent |
| CR20180042A (es) | 2015-06-18 | 2018-05-03 | Mithra Pharmaceuticals S A | Unidad de dosificación orodispersable que contiene un componente estetrol. |
| CN105963301B (zh) * | 2016-04-26 | 2018-12-28 | 兰州大学 | 以人fkbp51蛋白为靶点的先导化合物及筛选方法与应用 |
| CZ307437B6 (cs) | 2016-06-07 | 2018-08-22 | Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v.v.i. | 15β-substituované deriváty estronu jako selektivní inhibitory 17β-hydroxysteoiddehydrogenáz |
| KR102712911B1 (ko) | 2016-08-05 | 2024-10-04 | 에스테트라, 소시에떼 아 레스폰서빌리떼 리미떼 | 월경통 및 생리통의 관리방법 |
| HRP20240679T1 (hr) * | 2017-06-08 | 2024-08-16 | Organon R&D Finland Ltd | 17-oksimi 15.beta.-[3-propanamido]-supstituiranih etera-1,3,5(10)-trien-17-ona za uporabu u inhibiciji 17.beta.-hidroksisteroid dehidrogenaza |
| TWI801561B (zh) | 2018-04-19 | 2023-05-11 | 比利時商依思特拉私人有限責任公司 | 化合物及其用於緩解絕經相關症狀的用途 |
| CN111989105B (zh) | 2018-04-19 | 2024-07-19 | 埃斯特拉私人有限责任公司 | 化合物以及它们在缓解绝经相关症状中的用途 |
| JP7417608B2 (ja) | 2018-12-05 | 2024-01-18 | フォレンド ファーマ リミテッド | １７－ｈｓｄ１阻害剤としての１６（１７）位でピラゾール環と縮合しているエストラ－１，３，５（１０）－トリエン化合物 |
| TWI893101B (zh) | 2020-04-16 | 2025-08-11 | 比利時商埃斯特拉有限責任公司 | 具有降低之副作用之避孕組成物 |
| US20240082208A1 (en) * | 2021-01-08 | 2024-03-14 | Industry-Academic Cooperation Foundation, Yonsei University | Antiviral pharmaceutical composition comprising steroid sulfatase inhibitor |
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| HU208150B (en) * | 1988-10-31 | 1993-08-30 | Endorecherche Inc | Process for producing new estrogen derivatives having steroid hormone inhibitor activity and pharmaceutical compositions comprising such derivatives |
| US7015211B2 (en) * | 2003-03-21 | 2006-03-21 | Yale University | 15α-substituted estradiol carboxylic acid esters as locally active estrogens |
| GB0306718D0 (en) * | 2003-03-24 | 2003-04-30 | Sterix Ltd | Compound |
| TWI331154B (en) * | 2003-11-12 | 2010-10-01 | Solvay Pharm Gmbh | Novel 17-hydroxysteroid dehydrogenase type i inhibitors |
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|---|---|
| BRPI0611623A2 (pt) | 2010-09-21 |
| EP1888615B1 (en) | 2012-05-16 |
| ZA200709854B (en) | 2009-03-25 |
| CA2609726A1 (en) | 2006-11-30 |
| RU2007147416A (ru) | 2009-07-10 |
| KR20080012960A (ko) | 2008-02-12 |
| CA2609726C (en) | 2013-10-01 |
| ES2388297T3 (es) | 2012-10-11 |
| AU2006251154A1 (en) | 2006-11-30 |
| IL187620A0 (en) | 2008-03-20 |
| AU2006251154B2 (en) | 2012-06-28 |
| IL187620A (en) | 2014-03-31 |
| MX2007014736A (es) | 2008-02-15 |
| CN102796160A (zh) | 2012-11-28 |
| HK1117538A1 (en) | 2009-01-16 |
| JP2008545678A (ja) | 2008-12-18 |
| CN101189251A (zh) | 2008-05-28 |
| WO2006125800A1 (en) | 2006-11-30 |
| RU2412196C2 (ru) | 2011-02-20 |
| KR101364412B1 (ko) | 2014-02-21 |
| NO20076616L (no) | 2008-02-01 |
| CN101189251B (zh) | 2012-09-12 |
| EP1888615A1 (en) | 2008-02-20 |
| UA92348C2 (en) | 2010-10-25 |
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