EA201790540A1 - НОВЫЙ СПОСОБ ХИРАЛЬНОГО СИНТЕЗА N-АЦИЛ-(3-ЗАМЕЩЕННЫХ)-(8-ЗАМЕЩЕННЫХ)-5,6-ДИГИДРО[1,2,4]ТРИАЗОЛО[4,3-a]ПИРАЗИНОВ - Google Patents
НОВЫЙ СПОСОБ ХИРАЛЬНОГО СИНТЕЗА N-АЦИЛ-(3-ЗАМЕЩЕННЫХ)-(8-ЗАМЕЩЕННЫХ)-5,6-ДИГИДРО[1,2,4]ТРИАЗОЛО[4,3-a]ПИРАЗИНОВInfo
- Publication number
- EA201790540A1 EA201790540A1 EA201790540A EA201790540A EA201790540A1 EA 201790540 A1 EA201790540 A1 EA 201790540A1 EA 201790540 A EA201790540 A EA 201790540A EA 201790540 A EA201790540 A EA 201790540A EA 201790540 A1 EA201790540 A1 EA 201790540A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- substituted
- pyrazines
- triazolo
- dihydro
- acyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
- C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Abstract
Данное изобретение относится к новому способу хирального синтеза N-ацил-(3-замещенных)-(8-замещенных)-5,6-дигидро[1,2,4]триазоло[4,3-а]пиразинов формулы I, без использования стадий установки и удаления защитных групп.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP14186447 | 2014-09-25 | ||
PCT/EP2015/072167 WO2016046398A1 (en) | 2014-09-25 | 2015-09-25 | Novel chiral synthesis of n-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201790540A1 true EA201790540A1 (ru) | 2017-07-31 |
EA032052B1 EA032052B1 (ru) | 2019-03-29 |
Family
ID=51730305
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201790540A EA032052B1 (ru) | 2014-09-25 | 2015-09-25 | СПОСОБ ХИРАЛЬНОГО СИНТЕЗА N-АЦИЛ-(3-ЗАМЕЩЕННЫХ)-(8-ЗАМЕЩЕННЫХ)-5,6-ДИГИДРО-[1,2,4]ТРИАЗОЛО[4,3-a]ПИРАЗИНОВ |
Country Status (18)
Country | Link |
---|---|
US (2) | US20170298070A1 (ru) |
EP (1) | EP3197876B1 (ru) |
JP (1) | JP6469214B2 (ru) |
KR (1) | KR102558711B1 (ru) |
CN (1) | CN107001289B (ru) |
AU (1) | AU2015323702B2 (ru) |
CA (1) | CA2961984C (ru) |
EA (1) | EA032052B1 (ru) |
ES (1) | ES2711095T3 (ru) |
IL (1) | IL251304B (ru) |
MX (1) | MX367633B (ru) |
NZ (1) | NZ730295A (ru) |
PL (1) | PL3197876T3 (ru) |
PT (1) | PT3197876T (ru) |
SG (2) | SG11201702368PA (ru) |
TR (1) | TR201902080T4 (ru) |
WO (1) | WO2016046398A1 (ru) |
ZA (1) | ZA201701949B (ru) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RS54833B1 (sr) | 2011-10-03 | 2016-10-31 | Euroscreen Sa | Novi hiralni n-acil-5,6,7, (8-supstituisan)-tetrahidro-[1,2,4]triazolo [4,3-a]pirazini kao selektivni antagonisti nk-3 receptora, farmaceutsko jedinjenje, i postupci za upotrebu u nk-3 receptorom posredovanim poremećajima |
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 |
JP6316932B2 (ja) | 2013-03-29 | 2018-04-25 | オゲダ エス.エー. | 選択的NK−3受容体拮抗薬としての新規なN−アシル−(3位置換)−(8位置換)−5,6−ジヒドロ−[1,2,4]トリアゾロ[4,3−a]ピラジン、医薬組成物、NK−3受容体媒介性障害における使用方法 |
SG11201707521QA (en) | 2015-03-16 | 2017-10-30 | Ogeda Sa | Nk-3 receptor antagonists for therapeutic or cosmetic treatment of excess body fat |
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 |
WO2022031773A1 (en) | 2020-08-04 | 2022-02-10 | Teva Pharmaceuticals International Gmbh | Solid state forms of fezolinetant and salts thereof |
Family Cites Families (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP3252483B2 (ja) | 1992-10-20 | 2002-02-04 | 東レ株式会社 | 3環性トリアゾロ誘導体の製造方法 |
SK13532001A3 (sk) | 1999-04-01 | 2003-02-04 | Pfizer Products Inc. | Aminopiridíny ako inhibítory sorbitoldehydrogenázy |
DE60316416T2 (de) | 2002-03-25 | 2008-06-26 | Merck & Co., Inc. | Heterocyclische beta-aminoverbindungen als inhibitoren der dipeptidylpeptidase zur behandlung bzw. prävention von diabetes |
ATE335744T1 (de) | 2002-08-07 | 2006-09-15 | Novartis Pharma Gmbh | Organische verbindungen als mittel zur behandlung von aldosteronbedingten zuständen |
MY139563A (en) | 2002-09-04 | 2009-10-30 | Bristol Myers Squibb Co | Heterocyclic aromatic compounds useful as growth hormone secretagogues |
AR043443A1 (es) | 2003-03-07 | 2005-07-27 | Merck & Co Inc | Procedimiento de preparacion de tetrahidrotriazolopirazinas y productos intermedios |
DE602005008558D1 (de) | 2004-02-18 | 2008-09-11 | Astrazeneca Ab | Kondensierte heterocyclische verbindungen und deren verwendung als antagonisten des metabotropen reznkungen |
TWI378091B (en) | 2006-03-09 | 2012-12-01 | Eisai R&D Man Co Ltd | Multi-cyclic cinnamide derivatives |
JP5635910B2 (ja) | 2008-01-09 | 2014-12-03 | アレイ バイオファーマ、インコーポレイテッド | AKTタンパク質キナーゼ阻害剤としての5H−シクロペンタ[d]ピリミジン |
WO2009090055A1 (en) | 2008-01-17 | 2009-07-23 | Grünenthal GmbH | Substituted sulfonamide derivatives |
JP5654001B2 (ja) * | 2009-04-29 | 2015-01-14 | グラクソ グループ リミテッドGlaxo Group Limited | P2X7調節因子としての5,6,7,8−テトラヒドロ[1,2,4]トリアゾロ[4,3−a]ピラジン誘導体 |
WO2011007756A1 (ja) | 2009-07-13 | 2011-01-20 | 武田薬品工業株式会社 | 複素環化合物及びその用途 |
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 |
RS54833B1 (sr) | 2011-10-03 | 2016-10-31 | Euroscreen Sa | Novi hiralni n-acil-5,6,7, (8-supstituisan)-tetrahidro-[1,2,4]triazolo [4,3-a]pirazini kao selektivni antagonisti nk-3 receptora, farmaceutsko jedinjenje, i postupci za upotrebu u nk-3 receptorom posredovanim poremećajima |
CA2907813C (en) | 2013-03-29 | 2021-09-07 | Euroscreen Sa | Novel 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 |
JP6316932B2 (ja) | 2013-03-29 | 2018-04-25 | オゲダ エス.エー. | 選択的NK−3受容体拮抗薬としての新規なN−アシル−(3位置換)−(8位置換)−5,6−ジヒドロ−[1,2,4]トリアゾロ[4,3−a]ピラジン、医薬組成物、NK−3受容体媒介性障害における使用方法 |
EP2989103B1 (en) | 2013-03-29 | 2019-02-20 | Ogeda Sa | 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 |
-
2015
- 2015-09-25 PL PL15767559T patent/PL3197876T3/pl unknown
- 2015-09-25 SG SG11201702368PA patent/SG11201702368PA/en unknown
- 2015-09-25 WO PCT/EP2015/072167 patent/WO2016046398A1/en active Application Filing
- 2015-09-25 CA CA2961984A patent/CA2961984C/en active Active
- 2015-09-25 PT PT15767559T patent/PT3197876T/pt unknown
- 2015-09-25 ES ES15767559T patent/ES2711095T3/es active Active
- 2015-09-25 SG SG10201800162RA patent/SG10201800162RA/en unknown
- 2015-09-25 US US15/512,919 patent/US20170298070A1/en not_active Abandoned
- 2015-09-25 TR TR2019/02080T patent/TR201902080T4/tr unknown
- 2015-09-25 JP JP2017516089A patent/JP6469214B2/ja active Active
- 2015-09-25 KR KR1020177011099A patent/KR102558711B1/ko active IP Right Grant
- 2015-09-25 EA EA201790540A patent/EA032052B1/ru not_active IP Right Cessation
- 2015-09-25 NZ NZ730295A patent/NZ730295A/en unknown
- 2015-09-25 EP EP15767559.6A patent/EP3197876B1/en active Active
- 2015-09-25 CN CN201580063383.XA patent/CN107001289B/zh active Active
- 2015-09-25 AU AU2015323702A patent/AU2015323702B2/en active Active
- 2015-09-25 MX MX2017003980A patent/MX367633B/es active IP Right Grant
-
2017
- 2017-03-20 ZA ZA2017/01949A patent/ZA201701949B/en unknown
- 2017-03-21 IL IL251304A patent/IL251304B/en active IP Right Grant
-
2019
- 2019-03-22 US US16/361,737 patent/US10787458B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
US10787458B2 (en) | 2020-09-29 |
PT3197876T (pt) | 2019-02-21 |
MX2017003980A (es) | 2017-05-08 |
US20190218225A1 (en) | 2019-07-18 |
SG11201702368PA (en) | 2017-04-27 |
CA2961984A1 (en) | 2016-03-31 |
ES2711095T3 (es) | 2019-04-30 |
BR112017005880A2 (pt) | 2018-02-06 |
ZA201701949B (en) | 2021-06-30 |
TR201902080T4 (tr) | 2019-03-21 |
US20170298070A1 (en) | 2017-10-19 |
CA2961984C (en) | 2023-01-24 |
CN107001289A (zh) | 2017-08-01 |
MX367633B (es) | 2019-08-29 |
WO2016046398A1 (en) | 2016-03-31 |
SG10201800162RA (en) | 2018-02-27 |
EA032052B1 (ru) | 2019-03-29 |
JP6469214B2 (ja) | 2019-02-13 |
AU2015323702B2 (en) | 2020-03-12 |
AU2015323702A1 (en) | 2017-04-13 |
JP2017529370A (ja) | 2017-10-05 |
EP3197876B1 (en) | 2018-11-28 |
IL251304A0 (en) | 2017-05-29 |
EP3197876A1 (en) | 2017-08-02 |
IL251304B (en) | 2019-07-31 |
NZ730295A (en) | 2023-05-26 |
PL3197876T3 (pl) | 2019-05-31 |
CN107001289B (zh) | 2019-12-31 |
KR102558711B1 (ko) | 2023-07-21 |
KR20170072898A (ko) | 2017-06-27 |
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MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
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