JP2017531683A5 - - Google Patents
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- JP2017531683A5 JP2017531683A5 JP2017522213A JP2017522213A JP2017531683A5 JP 2017531683 A5 JP2017531683 A5 JP 2017531683A5 JP 2017522213 A JP2017522213 A JP 2017522213A JP 2017522213 A JP2017522213 A JP 2017522213A JP 2017531683 A5 JP2017531683 A5 JP 2017531683A5
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- JP
- Japan
- Prior art keywords
- effective amount
- therapeutically effective
- once
- formulation
- compound
- 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
- 229940126062 Compound A Drugs 0.000 claims description 113
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims description 113
- 238000009472 formulation Methods 0.000 claims description 100
- 239000000203 mixture Substances 0.000 claims description 100
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims description 52
- 206010022437 insomnia Diseases 0.000 claims description 52
- 238000000034 method Methods 0.000 claims description 31
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 26
- 238000002360 preparation method Methods 0.000 claims 7
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 4
- 238000007922 dissolution test Methods 0.000 claims 4
- 238000004090 dissolution Methods 0.000 claims 3
- -1 (2,4-dimethylpyrimidin-5-yl) oxy Chemical group 0.000 claims 2
- 101000671811 Homo sapiens Ubiquitin carboxyl-terminal hydrolase 37 Proteins 0.000 claims 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 2
- 102100040111 Ubiquitin carboxyl-terminal hydrolase 37 Human genes 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims 2
- 239000008101 lactose Substances 0.000 claims 2
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims 2
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
- AIMMVWOEOZMVMS-UHFFFAOYSA-N cyclopropanecarboxamide Chemical compound NC(=O)C1CC1 AIMMVWOEOZMVMS-UHFFFAOYSA-N 0.000 claims 1
- 238000010828 elution Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims 1
- 229920000053 polysorbate 80 Polymers 0.000 claims 1
- 229940068968 polysorbate 80 Drugs 0.000 claims 1
- 230000036470 plasma concentration Effects 0.000 description 37
- 238000012360 testing method Methods 0.000 description 16
- 206010041349 Somnolence Diseases 0.000 description 8
- 208000032140 Sleepiness Diseases 0.000 description 7
- 230000037321 sleepiness Effects 0.000 description 7
- 230000000694 effects Effects 0.000 description 6
- 239000003814 drug Substances 0.000 description 5
- 229940079593 drug Drugs 0.000 description 5
- 230000008030 elimination Effects 0.000 description 4
- 238000003379 elimination reaction Methods 0.000 description 4
- 230000000007 visual effect Effects 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 230000010365 information processing Effects 0.000 description 2
- 230000035484 reaction time Effects 0.000 description 2
- 230000007958 sleep Effects 0.000 description 2
- 230000004620 sleep latency Effects 0.000 description 2
- 241000282412 Homo Species 0.000 description 1
- 206010039897 Sedation Diseases 0.000 description 1
- 230000006399 behavior Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
- 239000003326 hypnotic agent Substances 0.000 description 1
- 230000000147 hypnotic effect Effects 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 206010029864 nystagmus Diseases 0.000 description 1
- 230000003565 oculomotor Effects 0.000 description 1
- 238000011056 performance test Methods 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 230000036280 sedation Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000002618 waking effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462067443P | 2014-10-23 | 2014-10-23 | |
| US62/067,443 | 2014-10-23 | ||
| PCT/JP2015/080304 WO2016063995A1 (en) | 2014-10-23 | 2015-10-21 | Compositions and methods for treating insomnia |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017531683A JP2017531683A (ja) | 2017-10-26 |
| JP2017531683A5 true JP2017531683A5 (enExample) | 2019-11-21 |
| JP6659681B2 JP6659681B2 (ja) | 2020-03-04 |
Family
ID=55761025
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017522213A Active JP6659681B2 (ja) | 2014-10-23 | 2015-10-21 | 不眠症を治療するための組成物および方法 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US10188652B2 (enExample) |
| EP (1) | EP3209298B1 (enExample) |
| JP (1) | JP6659681B2 (enExample) |
| KR (1) | KR102444608B1 (enExample) |
| CN (1) | CN107810006B (enExample) |
| AU (1) | AU2015336463B2 (enExample) |
| BR (1) | BR112017007063A2 (enExample) |
| CA (1) | CA2964504C (enExample) |
| ES (1) | ES2843952T3 (enExample) |
| IL (1) | IL251759B (enExample) |
| MX (1) | MX376164B (enExample) |
| RU (1) | RU2703297C2 (enExample) |
| SG (2) | SG11201703064WA (enExample) |
| WO (1) | WO2016063995A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6659681B2 (ja) | 2014-10-23 | 2020-03-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 不眠症を治療するための組成物および方法 |
| RU2763493C2 (ru) * | 2016-05-12 | 2021-12-29 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Способы лечения расстройств циркадного ритма сна |
| CN109789141B (zh) * | 2016-08-10 | 2022-08-26 | 豪夫迈·罗氏有限公司 | 包含Akt蛋白激酶抑制剂的药物组合物 |
| 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 |
| KR20210124188A (ko) | 2018-11-21 | 2021-10-14 | 트루모 파마슈티칼스, 인크. | 정제된 형태의 로페콕시브, 제조 및 사용 방법 |
| MX2021016090A (es) * | 2019-06-26 | 2022-02-03 | Eisai R&D Man Co Ltd | Lemborexant para el tratamiento de problemas del sueño. |
| WO2020263253A1 (en) * | 2019-06-26 | 2020-12-30 | Moline Margaret | Lemborexant for treating sleep issues |
| JP2022538170A (ja) * | 2019-06-26 | 2022-08-31 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 睡眠問題の治療のためのレンボレキサント |
| KR20220061950A (ko) | 2019-09-13 | 2022-05-13 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 불면증을 치료하기 위한 약제학적 조성물 |
| WO2021048822A1 (en) * | 2019-09-13 | 2021-03-18 | Takeda Pharmaceutical Company Limited | Tak-925 for use in treating narcolepsy |
| EP4076463A1 (en) * | 2019-12-20 | 2022-10-26 | Eisai R&D Management Co., Ltd. | Use of lemborexant for treating insomnia |
| IL328515A (en) | 2020-01-16 | 2026-07-01 | Eisai R&D Man Co Ltd | Lamborxant drug substance and medical preparation containing it |
| MX2022011179A (es) | 2020-04-19 | 2022-10-07 | Idorsia Pharmaceuticals Ltd | Uso medico de daridorexant. |
| CN111450076A (zh) * | 2020-05-25 | 2020-07-28 | 安徽省逸欣铭医药科技有限公司 | 一种Lemborexant软胶囊组合物及其制备方法 |
| CN120076808A (zh) | 2022-09-23 | 2025-05-30 | 卫材R&D管理有限公司 | 减少与神经退行性疾病相关的神经退行性变的方法 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH06328057A (ja) | 1993-05-26 | 1994-11-29 | Sanyo Electric Co Ltd | 厨芥処理装置 |
| EP0828751A4 (en) | 1995-05-05 | 1999-01-20 | Human Genome Sciences Inc | HUMAN NEUROPEPTIDE RECEPTOR |
| US6001963A (en) | 1996-12-17 | 1999-12-14 | Smithkline Beecham Corporation | Ligands of the neuropeptide receptor HFGAN72 |
| US6309854B1 (en) | 1996-12-17 | 2001-10-30 | Smithkline Beecham Corporation | Polynucleotides encoding ligands of the neuropeptide receptor HFGAN72 |
| US6020157A (en) | 1997-04-30 | 2000-02-01 | Smithkline Beecham Corporation | Polynucleotides encoding HFGAN72X receptor |
| US5935814A (en) | 1997-04-30 | 1999-08-10 | Smithkline Beecham Corporation | Polynucleotides encoding HFGAN72Y receptor |
| US6166193A (en) | 1997-07-25 | 2000-12-26 | Board Of Regents, University Of Texas System | Polynucleotides encoding MY1 receptor |
| RU2378257C2 (ru) | 2004-03-01 | 2010-01-10 | Актелион Фармасьютиклз Лтд | Замещенные производные 1,2,3,4-тетрагидроизохинолина |
| WO2006033005A2 (en) | 2004-09-23 | 2006-03-30 | Pfizer Products Inc. | Thrombopoietin receptor agonists |
| JP2006328057A (ja) | 2005-04-25 | 2006-12-07 | Eisai R & D Management Co Ltd | 抗不安薬及びそのスクリーニング方法 |
| EA015256B1 (ru) | 2006-03-15 | 2011-06-30 | Актелион Фармасьютикалз Лтд. | Производные тетрагидроизохинолина для повышения функции памяти |
| WO2007129188A1 (en) | 2006-05-10 | 2007-11-15 | Pfizer Japan Inc. | Cyclopropanecarboxamide compound |
| CA2662538A1 (en) | 2006-09-11 | 2008-03-20 | Glaxo Group Limited | Azabicyclic compounds as inhibitors of monoamines reuptake |
| CL2007002809A1 (es) | 2006-09-29 | 2008-04-18 | Actelion Pharmaceuticals Ltd | Compuestos derivados de 3-aza biciclo [3.1.0]hexano; y su uso en el tratamiento de enfermedades tales como desordenes psicoticos y de ansiedad, desordenes del sueno, uso y abuso de sustancias psicoactivas, demencia y deterioro de funciones cognitivas |
| PE20081229A1 (es) | 2006-12-01 | 2008-08-28 | Merck & Co Inc | Antagonistas de receptor de orexina de diazepam sustituido |
| AR064561A1 (es) | 2006-12-28 | 2009-04-08 | Actelion Pharmaceuticals Ltd | Derivados de 2-aza-biciclo[3.1.0]hexano y su uso en la preparacion de un medicamento para el tratamiento de enfermedades relacionadas con disfunciones generales del sistema de la orexina. |
| MX2010002419A (es) | 2007-09-21 | 2010-03-30 | Sanofi Aventis | (ciclopropilfenil) feniloxamidas, metodo para su produccion y uso como un medicamento. |
| PE20091010A1 (es) | 2007-10-10 | 2009-08-08 | Actelion Pharmaceuticals Ltd | Derivados de tetrahidroquinolina |
| CN102742210B (zh) * | 2010-02-15 | 2015-11-25 | 皇家飞利浦电子股份有限公司 | 用于减轻控制信道干扰的装置和方法 |
| RU2571414C2 (ru) * | 2010-09-22 | 2015-12-20 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Циклопропановые соединения |
| US20120165339A1 (en) | 2010-12-22 | 2012-06-28 | Eisai R&D Management Co., Ltd. | Cyclopropane derivatives |
| JP6659681B2 (ja) | 2014-10-23 | 2020-03-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 不眠症を治療するための組成物および方法 |
-
2015
- 2015-10-21 JP JP2017522213A patent/JP6659681B2/ja active Active
- 2015-10-21 KR KR1020177009858A patent/KR102444608B1/ko active Active
- 2015-10-21 CA CA2964504A patent/CA2964504C/en active Active
- 2015-10-21 SG SG11201703064WA patent/SG11201703064WA/en unknown
- 2015-10-21 ES ES15851934T patent/ES2843952T3/es active Active
- 2015-10-21 EP EP15851934.8A patent/EP3209298B1/en active Active
- 2015-10-21 CN CN201580055472.XA patent/CN107810006B/zh active Active
- 2015-10-21 MX MX2017004950A patent/MX376164B/es active IP Right Grant
- 2015-10-21 WO PCT/JP2015/080304 patent/WO2016063995A1/en not_active Ceased
- 2015-10-21 US US15/519,676 patent/US10188652B2/en active Active
- 2015-10-21 BR BR112017007063-4A patent/BR112017007063A2/pt not_active Application Discontinuation
- 2015-10-21 RU RU2017112308A patent/RU2703297C2/ru active
- 2015-10-21 AU AU2015336463A patent/AU2015336463B2/en active Active
- 2015-10-21 SG SG10202007759RA patent/SG10202007759RA/en unknown
-
2017
- 2017-04-18 IL IL251759A patent/IL251759B/en active IP Right Grant
-
2019
- 2019-01-23 US US16/255,116 patent/US10702529B2/en active Active
-
2020
- 2020-03-16 US US16/819,341 patent/US11026944B2/en active Active
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