EA201591204A3 - Новые хиральные n-ацил-5,6,7,(8-замещенные)-тетрагидро-[1,2,4]триазоло[4,3-а]пиразины как селективные антагонисты рецептора nk-3, фармацевтическая композиция, способы применения при нарушениях, опосредованных nk-3 рецепторами, и их хиральный синтез - Google Patents
Новые хиральные n-ацил-5,6,7,(8-замещенные)-тетрагидро-[1,2,4]триазоло[4,3-а]пиразины как селективные антагонисты рецептора nk-3, фармацевтическая композиция, способы применения при нарушениях, опосредованных nk-3 рецепторами, и их хиральный синтезInfo
- Publication number
- EA201591204A3 EA201591204A3 EA201591204A EA201591204A EA201591204A3 EA 201591204 A3 EA201591204 A3 EA 201591204A3 EA 201591204 A EA201591204 A EA 201591204A EA 201591204 A EA201591204 A EA 201591204A EA 201591204 A3 EA201591204 A3 EA 201591204A3
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- pharmaceutical composition
- antagonists
- chiral
- triazolo
- tetrahydro
- Prior art date
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Abstract
Данное изобретение относится к новым соединениям формулы Iи их использованию в терапевтических целях. Данное изобретение также относится к новому способу хирального синтеза 5,6,7,(8-замещенных)-тетрагидро[1,2,4]триазоло[4,3-а]пиразинов с использованием N-sp3 защитных групп. Данное изобретение также относится к интермедиатам, использованным для синтеза соединений формулы I.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
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EP11183692 | 2011-10-03 | ||
EP11183681 | 2011-10-03 | ||
EP11183678 | 2011-10-03 | ||
EP11183679 | 2011-10-03 | ||
US201161543611P | 2011-10-05 | 2011-10-05 |
Publications (3)
Publication Number | Publication Date |
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EA201591204A2 EA201591204A2 (ru) | 2016-01-29 |
EA201591204A3 true EA201591204A3 (ru) | 2016-02-29 |
EA030586B1 EA030586B1 (ru) | 2018-08-31 |
Family
ID=48043185
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
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EA201490579A EA029340B1 (ru) | 2011-10-03 | 2012-10-03 | ХИРАЛЬНЫЕ N-АЦИЛ-5,6,7,(8-ЗАМЕЩЕННЫЕ)-ТЕТРАГИДРО[1,2,4]ТРИАЗОЛО[4,3-a]ПИРАЗИНЫ КАК СЕЛЕКТИВНЫЕ АНТАГОНИСТЫ РЕЦЕПТОРА NK-3, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СПОСОБЫ ПРИМЕНЕНИЯ ПРИ НАРУШЕНИЯХ, ОПОСРЕДОВАННЫХ NK-3 РЕЦЕПТОРАМИ, И ИХ ХИРАЛЬНЫЙ СИНТЕЗ |
EA201591204A EA030586B1 (ru) | 2011-10-03 | 2012-10-03 | Интермедиат для получения антагонистов рецептора нейрокинина-3 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
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EA201490579A EA029340B1 (ru) | 2011-10-03 | 2012-10-03 | ХИРАЛЬНЫЕ N-АЦИЛ-5,6,7,(8-ЗАМЕЩЕННЫЕ)-ТЕТРАГИДРО[1,2,4]ТРИАЗОЛО[4,3-a]ПИРАЗИНЫ КАК СЕЛЕКТИВНЫЕ АНТАГОНИСТЫ РЕЦЕПТОРА NK-3, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СПОСОБЫ ПРИМЕНЕНИЯ ПРИ НАРУШЕНИЯХ, ОПОСРЕДОВАННЫХ NK-3 РЕЦЕПТОРАМИ, И ИХ ХИРАЛЬНЫЙ СИНТЕЗ |
Country Status (21)
Country | Link |
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US (4) | US9475814B2 (ru) |
EP (2) | EP2763992B9 (ru) |
JP (2) | JP6023814B2 (ru) |
KR (1) | KR102049534B1 (ru) |
CN (2) | CN103906750B9 (ru) |
AU (1) | AU2012320568C1 (ru) |
BR (1) | BR112014007652B1 (ru) |
CA (1) | CA2849751C (ru) |
CY (1) | CY1117773T1 (ru) |
DK (1) | DK2763992T3 (ru) |
EA (2) | EA029340B1 (ru) |
ES (1) | ES2572604T3 (ru) |
HK (1) | HK1197676A1 (ru) |
HR (1) | HRP20160396T1 (ru) |
HU (1) | HUE028858T2 (ru) |
MX (1) | MX367774B (ru) |
PL (1) | PL2763992T3 (ru) |
RS (1) | RS54833B1 (ru) |
SI (1) | SI2763992T1 (ru) |
SM (1) | SMT201600164B (ru) |
WO (1) | WO2013050424A1 (ru) |
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BR112012025101B1 (pt) | 2010-04-02 | 2021-08-31 | Ogeda S.A. | Compostos antagonistas seletivos de receptor nk-3, composição farmacêutica e medicamento compreendendo os mesmos |
US10065960B2 (en) | 2010-04-02 | 2018-09-04 | Ogeda Sa | NK-3 receptor selective antagonist compounds, pharmaceutical composition and methods for use in NK-3 receptors mediated disorders |
EP2763992B9 (en) | 2011-10-03 | 2016-08-24 | Euroscreen S.A. | Novel chiral n-acyl-5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective nk-3 receptor antagonists, pharmaceutical composition, and methods for use in nk-3 receptor mediated disorders |
LT2948455T (lt) | 2013-03-29 | 2017-11-27 | Ogeda S.A. | N-acil-(3-pakeisto)-(8-pakeisto)-5,6-dihidro- [1,2,4]triazol[4,3-a]pirazinai, kaip selektyvūs nk-3 receptorių antagonistai, farmacinė kompozicija, būdai, skirti naudoti nk-3 receptoriaus sąlygotų sutrikimų gydymui |
WO2014154897A1 (en) | 2013-03-29 | 2014-10-02 | Euroscreen Sa | NOVEL N-ACYL-(3-SUBSTITUTED)-(8-METHYL)-5,6-DIHYDRO-[1,2,4]TRIAZOLO[4,3-a]PYRAZINES AS SELECTIVE NK-3 RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITION, METHODS FOR USE IN NK-3 RECEPTOR-MEDIATED DISORDERS |
US9969738B2 (en) | 2013-03-29 | 2018-05-15 | Ogeda Sa | N-acyl-(3-substituted)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor-mediated disorders |
US10183948B2 (en) | 2013-03-29 | 2019-01-22 | Ogeda Sa | N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists |
GB201315846D0 (en) | 2013-09-05 | 2013-10-23 | Imp Innovations Ltd | Method for treating or preventing hot flushes |
WO2016046398A1 (en) * | 2014-09-25 | 2016-03-31 | Euroscreen Sa | Novel chiral synthesis of n-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines |
BR112017019829A2 (pt) * | 2015-03-16 | 2018-05-29 | Ogeda Sa | antagonista do receptor nk-3, para o tratamento terapêutico ou cosmético de gordura corporal em excesso |
JP2021014404A (ja) * | 2017-10-13 | 2021-02-12 | アステラス製薬株式会社 | トリアゾロピラジン誘導体の塩及び結晶 |
CN113767094A (zh) * | 2018-12-21 | 2021-12-07 | 奥格达股份有限公司 | 3-甲基-1,2,4-噻二唑-5-碳酰肼及其甲基-d3氘代形式的合成 |
CN111499640A (zh) * | 2019-01-31 | 2020-08-07 | 上海医药工业研究院 | 哌嗪并三唑类衍生物的手性拆分方法 |
CN112272670B (zh) * | 2019-04-16 | 2023-12-12 | 上海翰森生物医药科技有限公司 | 含二并环类衍生物抑制剂、其制备方法和应用 |
AU2020358948A1 (en) * | 2019-09-30 | 2022-05-26 | Janssen Pharmaceutica Nv | Radiolabelled MGL PET ligands |
CN113527307A (zh) * | 2020-04-20 | 2021-10-22 | 上海翰森生物医药科技有限公司 | 含三唑基的并环类衍生物抑制剂、其制备方法和应用 |
CN113549074A (zh) * | 2020-04-26 | 2021-10-26 | 上海翰森生物医药科技有限公司 | 含三唑基的并环类衍生物抑制剂、其制备方法和应用 |
WO2022022680A1 (zh) * | 2020-07-30 | 2022-02-03 | 上海翰森生物医药科技有限公司 | 含氮并环类衍生物抑制剂、其制备方法和应用 |
KR20230146639A (ko) * | 2021-04-21 | 2023-10-19 | 장춘 진사이언스 파마슈티컬 씨오., 엘티디. | 이미다졸 함유 축합고리계 유도체, 이의 제조방법 및 이의 의약적 용도 |
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