JP2015509939A5 - - Google Patents
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- Publication number
- JP2015509939A5 JP2015509939A5 JP2014557781A JP2014557781A JP2015509939A5 JP 2015509939 A5 JP2015509939 A5 JP 2015509939A5 JP 2014557781 A JP2014557781 A JP 2014557781A JP 2014557781 A JP2014557781 A JP 2014557781A JP 2015509939 A5 JP2015509939 A5 JP 2015509939A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- compound
- group
- alkyl
- organic solvent
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 0 *[C@](COc1cnc(*)nc1*)(C1)[C@@]1C=O Chemical compound *[C@](COc1cnc(*)nc1*)(C1)[C@@]1C=O 0.000 description 1
- HGJBPBRHSNPZSW-UHFFFAOYSA-N O=C1OCC(C2)C12[AlH2] Chemical compound O=C1OCC(C2)C12[AlH2] HGJBPBRHSNPZSW-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261600109P | 2012-02-17 | 2012-02-17 | |
| US61/600,109 | 2012-02-17 | ||
| PCT/US2013/026204 WO2013123240A1 (en) | 2012-02-17 | 2013-02-14 | Methods and compounds useful in the synthesis of orexin-2 receptor antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015509939A JP2015509939A (ja) | 2015-04-02 |
| JP2015509939A5 true JP2015509939A5 (https=) | 2016-03-31 |
| JP6147279B2 JP6147279B2 (ja) | 2017-06-14 |
Family
ID=47755050
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014557781A Active JP6147279B2 (ja) | 2012-02-17 | 2013-02-14 | オレキシン−２受容体アンタゴニストの合成において有用な方法および化合物 |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US9416109B2 (https=) |
| EP (1) | EP2814798B1 (https=) |
| JP (1) | JP6147279B2 (https=) |
| CN (1) | CN104114524B (https=) |
| BR (1) | BR112014019909B1 (https=) |
| CA (1) | CA2861493C (https=) |
| ES (1) | ES2733750T3 (https=) |
| HU (1) | HUE043995T2 (https=) |
| IL (1) | IL232949A (https=) |
| MX (1) | MX352881B (https=) |
| RU (1) | RU2617696C2 (https=) |
| SG (1) | SG11201403216UA (https=) |
| WO (1) | WO2013123240A1 (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2672732T3 (es) | 2012-02-07 | 2018-06-15 | Eolas Therapeutics Inc. | Prolinas/piperidinas sustituidas como antagonistas del receptor de orexina |
| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| JP6147279B2 (ja) * | 2012-02-17 | 2017-06-14 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | オレキシン−２受容体アンタゴニストの合成において有用な方法および化合物 |
| CN107074780B (zh) | 2014-08-06 | 2020-06-12 | 卫材R&D管理有限公司 | 用于生产嘧啶-1-醇化合物及其中间体的方法 |
| JP6663909B2 (ja) | 2014-08-13 | 2020-03-13 | エオラス セラピューティクス， インコーポレイテッド | オレキシンレセプターモジュレーターとしてのジフルオロピロリジン |
| MX2018009656A (es) | 2016-02-12 | 2019-02-20 | Astrazeneca Ab | Piperidinas halo-sustituidas como moduladores de los receptores de orexinas. |
| JP7179049B2 (ja) * | 2017-08-01 | 2022-11-28 | ベルゲン ファーマシューティカル、 エルエルシー | オレキシン受容体拮抗薬の結晶形及びその製造方法並びに用途 |
| GB201807898D0 (en) * | 2018-05-15 | 2018-06-27 | Kancera Ab | New processes and products with increased chiral purity |
| US12098137B2 (en) | 2018-09-07 | 2024-09-24 | Sumitomo Chemical Company, Limited | Method for manufacturing cyclopropane compound |
| TW202432509A (zh) * | 2019-05-15 | 2024-08-16 | 日商衛材R&D企管股份有限公司 | 對於食慾素-2受體拮抗劑之製備有用之方法及化合物、以及雜質少之萊博雷生 |
| WO2020249689A1 (en) | 2019-06-12 | 2020-12-17 | Nouryon Chemicals International B.V. | Process for the production of peroxyesters |
| ES2963382T3 (es) | 2019-06-12 | 2024-03-26 | Nouryon Chemicals Int Bv | Proceso para la producción de peróxidos de diacilo |
| EP3983369B1 (en) | 2019-06-12 | 2023-08-02 | Nouryon Chemicals International B.V. | Process for the production of diacyl peroxides |
| US11976035B2 (en) | 2019-06-12 | 2024-05-07 | Nouryon Chemicals International B.V. | Process for the production of diacyl peroxides |
| WO2020249692A1 (en) * | 2019-06-12 | 2020-12-17 | Nouryon Chemicals International B.V. | Method for isolating carboxylic acid from an aqueous side stream |
| WO2020263253A1 (en) * | 2019-06-26 | 2020-12-30 | Moline Margaret | Lemborexant for treating sleep issues |
| US12534448B2 (en) | 2019-12-11 | 2026-01-27 | Tapi Czech Industries S.R.O | Solid state form of lemborexant |
| MX2022007304A (es) | 2019-12-20 | 2022-08-22 | Eisai R&D Man Co Ltd | Uso de lemborexant para tratamiento del insomnio. |
| US20230103250A1 (en) | 2020-01-16 | 2023-03-30 | Eisai R&D Management Co., Ltd. | Drug substance of lemborexant and medicinal composition comprising same |
| ES2933074B2 (es) * | 2021-07-26 | 2023-09-29 | Moehs Iberica Sl | Procedimiento de sintesis de 2,4-dimetilpirimidin-5-ol, nuevos intermedios de dicho procedimiento y uso del producto en la sintesis de lemborexant |
| WO2023178702A1 (zh) * | 2022-03-25 | 2023-09-28 | 浙江华海药业股份有限公司 | 莱博雷生及其中间体化合物的制备方法 |
| CN118871427A (zh) * | 2022-03-25 | 2024-10-29 | 浙江华海药业股份有限公司 | 一种莱博雷生及其中间体的制备方法 |
| CN114778745B (zh) * | 2022-06-21 | 2022-09-16 | 南京威凯尔生物医药科技有限公司 | 一种高效液相色谱法检测仑布雷生中间体及其对映体杂质的方法 |
| CN121045084A (zh) * | 2024-06-01 | 2025-12-02 | 常州市第四制药厂有限公司 | 一种莱博雷生关键中间体及其合成方法 |
| CN119930526B (zh) * | 2025-04-07 | 2025-07-08 | 东北制药集团股份有限公司 | 一种莱博雷生中间体的制备方法 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2302994A1 (fr) * | 1975-03-06 | 1976-10-01 | Fabre Sa Pierre | Procede de preparation d'acides aryl-1, hydroxy methyl-2 cyclopropanes carboxyliques et de leurs lactones utiles comme intermediaires de synthese dans l'industrie pharmaceutique |
| US5849954A (en) * | 1996-01-18 | 1998-12-15 | Research Corporation Technologies, Inc. | Method of peptide synthesis |
| WO2004037212A2 (en) | 2002-10-24 | 2004-05-06 | Sepracor, Inc. | Compositions comprising zopiclone derivatives and methods of making and using the same |
| US8138377B2 (en) * | 2006-11-07 | 2012-03-20 | Dov Pharmaceutical, Inc. | Arylbicyclo[3.1.0]hexylamines and methods and compositions for their preparation and use |
| WO2008150364A1 (en) * | 2007-05-23 | 2008-12-11 | Merck & Co., Inc. | Cyclopropyl pyrrolidine orexin receptor antagonists |
| JP4881476B2 (ja) * | 2007-05-23 | 2012-02-22 | メルク・シャープ・エンド・ドーム・コーポレイション | ピリジルピペリジン・オレキシン受容体アンタゴニスト |
| CN102159548A (zh) | 2008-09-18 | 2011-08-17 | 辉瑞有限公司 | 在治疗中有用的酰胺化合物 |
| AR074426A1 (es) | 2008-12-02 | 2011-01-19 | Glaxo Group Ltd | Compuesto de n-(((1s,4s,6s)-3-(2-piridinilcarbonil)3-azabiciclo (4,1.0)hept-4-il) metil)-2-heteroarilamina, su uso para la prepracion de un medicamento para el tratamiento de una enfermedad que requiere un antagonista de un receptor de orexina humana y composicion farmaceutica que lo comprende |
| FR2941454B1 (fr) * | 2009-01-29 | 2011-04-01 | Pf Medicament | Proced de synthese du (1s,2r)-milnacipran |
| US8101643B2 (en) | 2009-02-27 | 2012-01-24 | Enanta Pharmaceuticals, Inc. | Benzimidazole derivatives |
| EP2406362A1 (en) | 2009-03-09 | 2012-01-18 | Novozymes A/S | Enzymatic removal of steryl glycosides in fatty acid alkyl esters |
| WO2012039371A1 (ja) * | 2010-09-22 | 2012-03-29 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | シクロプロパン化合物 |
| JP6147279B2 (ja) * | 2012-02-17 | 2017-06-14 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | オレキシン−２受容体アンタゴニストの合成において有用な方法および化合物 |
-
2013
- 2013-02-14 JP JP2014557781A patent/JP6147279B2/ja active Active
- 2013-02-14 WO PCT/US2013/026204 patent/WO2013123240A1/en not_active Ceased
- 2013-02-14 HU HUE13706874A patent/HUE043995T2/hu unknown
- 2013-02-14 SG SG11201403216UA patent/SG11201403216UA/en unknown
- 2013-02-14 MX MX2014009917A patent/MX352881B/es active IP Right Grant
- 2013-02-14 BR BR112014019909A patent/BR112014019909B1/pt active IP Right Grant
- 2013-02-14 EP EP13706874.8A patent/EP2814798B1/en active Active
- 2013-02-14 RU RU2014137470A patent/RU2617696C2/ru active
- 2013-02-14 US US14/379,063 patent/US9416109B2/en active Active
- 2013-02-14 ES ES13706874T patent/ES2733750T3/es active Active
- 2013-02-14 CN CN201380009575.3A patent/CN104114524B/zh active Active
- 2013-02-14 CA CA2861493A patent/CA2861493C/en active Active
-
2014
- 2014-06-02 IL IL232949A patent/IL232949A/en active IP Right Grant
-
2016
- 2016-05-19 US US15/158,687 patent/US9828336B2/en active Active
-
2017
- 2017-10-24 US US15/791,814 patent/US20180044285A1/en not_active Abandoned
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