JP2016539136A5 - - Google Patents
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- Publication number
- JP2016539136A5 JP2016539136A5 JP2016536109A JP2016536109A JP2016539136A5 JP 2016539136 A5 JP2016539136 A5 JP 2016539136A5 JP 2016536109 A JP2016536109 A JP 2016536109A JP 2016536109 A JP2016536109 A JP 2016536109A JP 2016539136 A5 JP2016539136 A5 JP 2016539136A5
- Authority
- JP
- Japan
- Prior art keywords
- methanone
- triazol
- benzo
- chloro
- methoxy
- 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
- 239000013078 crystal Substances 0.000 claims 19
- -1 ( S)-(2- (6-Chloro-7-methyl-1H-benzo [d] imidazol-2-yl) -2-methylpyrrolidin-1-yl) Chemical group 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
- CZUSBEKFTYZTJS-UHFFFAOYSA-N 5-methoxy-2-(triazol-2-yl)benzaldehyde Chemical compound COC=1C=CC(=C(C=1)C=O)N1N=CC=N1 CZUSBEKFTYZTJS-UHFFFAOYSA-N 0.000 claims 9
- 238000010586 diagram Methods 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 7
- 238000000634 powder X-ray diffraction Methods 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 5
- 208000019901 Anxiety disease Diseases 0.000 claims 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- NBGABHGMJVIVBW-QHCPKHFHSA-N [(2s)-2-(5-chloro-4-methyl-1h-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-[5-methoxy-2-(triazol-2-yl)phenyl]methanone Chemical compound N1([C@](CCC1)(C)C=1NC2=CC=C(Cl)C(C)=C2N=1)C(=O)C1=CC(OC)=CC=C1N1N=CC=N1 NBGABHGMJVIVBW-QHCPKHFHSA-N 0.000 claims 4
- 239000004480 active ingredient Substances 0.000 claims 4
- WSFSSNUMVMOOMR-BJUDXGSMSA-N methanone Chemical compound O=[11CH2] WSFSSNUMVMOOMR-BJUDXGSMSA-N 0.000 claims 4
- 208000019116 sleep disease Diseases 0.000 claims 4
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 208000020685 sleep-wake disease Diseases 0.000 claims 3
- 208000027559 Appetite disease Diseases 0.000 claims 2
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 2
- 208000019022 Mood disease Diseases 0.000 claims 2
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims 2
- 206010022437 insomnia Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 206010003591 Ataxia Diseases 0.000 claims 1
- 208000019888 Circadian rhythm sleep disease Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000014094 Dystonic disease Diseases 0.000 claims 1
- 208000001456 Jet Lag Syndrome Diseases 0.000 claims 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 1
- 206010033664 Panic attack Diseases 0.000 claims 1
- 208000006199 Parasomnias Diseases 0.000 claims 1
- 208000005793 Restless legs syndrome Diseases 0.000 claims 1
- 150000008064 anhydrides Chemical class 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 230000003796 beauty Effects 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 208000010118 dystonia Diseases 0.000 claims 1
- 239000000463 material Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000019906 panic disease Diseases 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 208000028173 post-traumatic stress disease Diseases 0.000 claims 1
- 230000003449 preventive effect Effects 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 230000029058 respiratory gaseous exchange Effects 0.000 claims 1
- 238000003756 stirring Methods 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IB2013060596 | 2013-12-03 | ||
| IBPCT/IB2013/060596 | 2013-12-03 | ||
| PCT/IB2014/066508 WO2015083070A1 (en) | 2013-12-03 | 2014-12-02 | Crystalline form of (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1 -yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone and its use as orexin receptor antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016539136A JP2016539136A (ja) | 2016-12-15 |
| JP2016539136A5 true JP2016539136A5 (enExample) | 2018-01-11 |
| JP6496733B2 JP6496733B2 (ja) | 2019-04-03 |
Family
ID=52282786
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016536109A Active JP6496733B2 (ja) | 2013-12-03 | 2014-12-02 | （ｓ）−（２−（６−クロロ−７−メチル−１ｈ−ベンゾ［ｄ］イミダゾール−２−イル）−２−メチルピロリジン−１−イル）（５−メトキシ−２−（２ｈ−１，２，３−トリアゾール−２−イル）フェニル）メタノンの結晶形及びオレキシン受容体アンタゴニストとしてのその使用 |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US9914720B2 (enExample) |
| EP (1) | EP3077389B1 (enExample) |
| JP (1) | JP6496733B2 (enExample) |
| KR (1) | KR102361418B1 (enExample) |
| CN (1) | CN105793257B (enExample) |
| AU (1) | AU2014358742B2 (enExample) |
| CA (1) | CA2929423C (enExample) |
| CL (1) | CL2016001342A1 (enExample) |
| CY (1) | CY1119695T1 (enExample) |
| DK (1) | DK3077389T3 (enExample) |
| EA (1) | EA030137B1 (enExample) |
| ES (1) | ES2651475T3 (enExample) |
| HR (1) | HRP20171773T1 (enExample) |
| HU (1) | HUE035731T2 (enExample) |
| IL (1) | IL245923B (enExample) |
| LT (1) | LT3077389T (enExample) |
| MA (1) | MA39163B1 (enExample) |
| MX (1) | MX364208B (enExample) |
| MY (1) | MY179862A (enExample) |
| NO (1) | NO3077389T3 (enExample) |
| NZ (1) | NZ721438A (enExample) |
| PH (1) | PH12016500988B1 (enExample) |
| PL (1) | PL3077389T3 (enExample) |
| PT (1) | PT3077389T (enExample) |
| SA (1) | SA516371231B1 (enExample) |
| SI (1) | SI3077389T1 (enExample) |
| TW (1) | TWI664177B (enExample) |
| UA (1) | UA119549C2 (enExample) |
| WO (1) | WO2015083070A1 (enExample) |
| ZA (1) | ZA201604499B (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2855453T3 (pl) | 2012-06-04 | 2017-05-31 | Actelion Pharmaceuticals Ltd. | Pochodne benzimidazoloproliny |
| UA119151C2 (uk) | 2013-12-03 | 2019-05-10 | Ідорсія Фармасьютікалз Лтд | КРИСТАЛІЧНА СОЛЬОВА ФОРМА (S)-(2-(6-ХЛОР-7-МЕТИЛ-1H-БЕНЗО[d]ІМІДАЗОЛ-2-ІЛ)-2-МЕТИЛПІРОЛІДИН-1-ІЛ)(5-МЕТОКСИ-2-(2H-1,2,3-ТРИАЗОЛ-2-ІЛ)ФЕНІЛ)МЕТАНОНУ ЯК АНТАГОНІСТ ОРЕКСИНОВОГО РЕЦЕПТОРА |
| EP3077391B1 (en) | 2013-12-04 | 2018-08-15 | Idorsia Pharmaceuticals Ltd | Use of benzimidazole-proline derivatives |
| IL270274B (en) | 2017-05-03 | 2022-08-01 | Idorsia Pharmaceuticals Ltd | Preparation of 2-([1,2,3]triazol-2-yl)-benzoic acid derivatives |
| PH12022552763A1 (en) * | 2020-04-19 | 2024-03-25 | Idorsia Pharmaceuticals Ltd | Medical use of daridorexant |
| CN116783182B (zh) * | 2021-02-02 | 2025-08-29 | 南京明德新药研发有限公司 | 四氢吡咯并环化合物及其应用 |
| CN115925699B (zh) * | 2022-02-25 | 2023-10-03 | 南京知和医药科技有限公司 | 具有镇痛活性的稠环化合物及其制备方法与用途 |
| ES3038762A1 (es) | 2024-04-12 | 2025-10-14 | Moehs Iberica Sl | Procedimiento de síntesis de ácido 5-metoxi-2-(2H-1,2,3-triazol-2yl)benzoico, sal sódica de dicho ácido como intermedio de síntesis y uso del ácido o de su sal en la preparación de daridorexant y ciertos intermedios en la síntesis del mismo |
Family Cites Families (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3282927A (en) | 1964-05-21 | 1966-11-01 | Bristol Myers Co | 5-phenyl-4-thiazolylpenicillins |
| AU2001272476A1 (en) | 2000-06-16 | 2001-12-24 | Smithkline Beecham Plc | Piperidines for use as orexin receptor antagonists |
| JP2004510765A (ja) | 2000-10-06 | 2004-04-08 | ニューロジェン・コーポレーション | Ｃｒｆ受容体調節物質としてのベンズイミダゾールおよびインドール誘導体類 |
| ATE286897T1 (de) | 2000-11-28 | 2005-01-15 | Smithkline Beecham Plc | Morpholinderivate als antagonisten an orexinrezeptoren |
| AU2002341123A1 (en) | 2001-05-05 | 2002-11-18 | Smithkline Beecham P.L.C. | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
| ES2299567T3 (es) | 2001-05-05 | 2008-06-01 | Smithkline Beecham Plc | N-aroilaminas ciclicas. |
| GB0115862D0 (en) | 2001-06-28 | 2001-08-22 | Smithkline Beecham Plc | Compounds |
| EP1705179A1 (en) * | 2001-06-28 | 2006-09-27 | Smithkline Beecham Plc | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
| GB0124463D0 (en) | 2001-10-11 | 2001-12-05 | Smithkline Beecham Plc | Compounds |
| GB0127145D0 (en) | 2001-11-10 | 2002-01-02 | Smithkline Beecham | Compounds |
| GB0130335D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| GB0130393D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| ATE344261T1 (de) | 2002-09-18 | 2006-11-15 | Glaxo Group Ltd | Cyclische n-aroylamine als orexinrezeptorantagonisten |
| GB0225884D0 (en) | 2002-11-06 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
| GB0225938D0 (en) | 2002-11-06 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
| GB0225944D0 (en) | 2002-11-06 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
| BRPI0508263B8 (pt) | 2004-03-01 | 2021-05-25 | Idorsia Pharmaceuticals Ltd | derivados de 1, 2, 3, 4-tetra-hidro-isoquinolina, composição farmacêutica, e, uso de derivado de 1, 2, 3, 4-tetra-hidro-isoquinolina |
| CN101400348A (zh) | 2006-03-15 | 2009-04-01 | 埃科特莱茵药品有限公司 | 用于提高记忆功能的四氢异喹啉衍生物 |
| WO2007135527A2 (en) * | 2006-05-23 | 2007-11-29 | Pfizer Products Inc. | Benzimidazolyl compounds |
| ATE500250T1 (de) | 2006-08-15 | 2011-03-15 | Actelion Pharmaceuticals Ltd | Azetidinverbindungen als orexin-rezeptor- antagonisten |
| 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. |
| WO2008087611A2 (en) | 2007-01-19 | 2008-07-24 | Actelion Pharmaceuticals Ltd | Pyrrolidine- and piperidine- bis-amide derivatives |
| CL2008000836A1 (es) | 2007-03-26 | 2008-11-07 | Actelion Pharmaceuticals Ltd | Compuestos derivados de tiazolidina, antagonistas del receptor de orexina; composicion farmaceutica que los comprende; y su uso en el tratamiento de neurosis emocional, depresion grave, trastornos psicoticos, alzheimer, parkinson, dolor, entre otras. |
| DE602008002934D1 (de) | 2007-05-14 | 2010-11-18 | Actelion Pharmaceuticals Ltd | 2-cyclopropylthiazolderivate |
| CA2687230A1 (en) | 2007-05-23 | 2008-12-11 | Merck & Co., Inc. | Cyclopropyl pyrrolidine orexin receptor antagonists |
| CA2691638A1 (en) | 2007-07-03 | 2009-01-08 | Glaxo Group Limited | Piperidine derivatives useful as orexin receptor antagonists |
| WO2009004584A1 (en) | 2007-07-03 | 2009-01-08 | Actelion Pharmaceuticals Ltd | 3-aza-bicyclo[3.3.0]octane compounds |
| GB0712888D0 (en) | 2007-07-03 | 2007-08-15 | Glaxo Group Ltd | Novel compounds |
| RU2478099C2 (ru) | 2007-07-27 | 2013-03-27 | Актелион Фармасьютиклз Лтд | Производные 2-аза-бицикло[3.3.0]октана |
| CN101790515A (zh) | 2007-07-27 | 2010-07-28 | 埃科特莱茵药品有限公司 | 反式-3-氮杂-双环[3.1.0]己烷衍生物 |
| WO2009040730A2 (en) | 2007-09-24 | 2009-04-02 | Actelion Pharmaceuticals Ltd | Pyrrolidines and piperidines as orexin receptor antagonists |
| PE20091010A1 (es) | 2007-10-10 | 2009-08-08 | Actelion Pharmaceuticals Ltd | Derivados de tetrahidroquinolina |
| US8236801B2 (en) | 2008-02-21 | 2012-08-07 | Actelion Pharmaceuticals Ltd. | 2-aza-bicyclo[2.2.1]heptane derivatives |
| GB0806536D0 (en) | 2008-04-10 | 2008-05-14 | Glaxo Group Ltd | Novel compounds |
| US20110105491A1 (en) | 2008-07-07 | 2011-05-05 | Hamed Aissaoui | Thiazolidine compounds as orexin receptor antagonists |
| WO2010038200A1 (en) | 2008-10-01 | 2010-04-08 | Actelion Pharmaceuticals Ltd | Oxazolidine compounds as orexin receptor antagonists |
| EP2358711A1 (en) | 2008-11-26 | 2011-08-24 | Glaxo Group Limited | Piperidine derivatives useful as orexin receptor antagonists |
| JP2012509911A (ja) | 2008-11-26 | 2012-04-26 | グラクソ グループ リミテッド | 新規の化合物 |
| JP2012509912A (ja) | 2008-11-26 | 2012-04-26 | グラクソ グループ リミテッド | 新規の化合物 |
| 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 |
| UY32277A (es) | 2008-12-02 | 2010-05-31 | Glaxo Group Ltd | Derivados de n-{[1r,4s,6r)-3-(2-piridinilcarbonil)-3-azabiciclo[4.1.0-il}metil}-2heteroarilamina y uso de los mismos |
| GB0823467D0 (en) * | 2008-12-23 | 2009-01-28 | Glaxo Group Ltd | Novel Compounds |
| WO2010122151A1 (en) | 2009-04-24 | 2010-10-28 | Glaxo Group Limited | 3 -azabicyclo [4.1.0] heptanes used as orexin antagonists |
| US8895606B2 (en) | 2010-08-24 | 2014-11-25 | Actelion Pharmaceuticals Ltd. | Proline sulfonamide derivatives as orexin receptor antagonists |
| CA2815179A1 (en) | 2010-11-10 | 2012-05-18 | Actelion Pharmaceuticals Ltd | Lactam derivatives useful as orexin receptor antagonists |
| JP5987005B2 (ja) | 2011-02-18 | 2016-09-06 | アクテリオン ファーマシューティカルズ リミテッドＡｃｔｅｌｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ | オレキシン拮抗薬として有用な新規なピラゾール及びイミダゾール誘導体 |
| UA112317C2 (uk) | 2011-11-08 | 2016-08-25 | Актеліон Фармасьютікалз Лтд | Похідні 2-(1,2,3-триазол-2-іл)бензаміду та 3-(1,2,3-триазол-2-іл)піколінаміду як антагоністи рецептора орексину |
| PL2855453T3 (pl) * | 2012-06-04 | 2017-05-31 | Actelion Pharmaceuticals Ltd. | Pochodne benzimidazoloproliny |
| CN104703980B (zh) | 2012-10-10 | 2017-09-22 | 埃科特莱茵药品有限公司 | 属于[邻双(杂)芳基]‑[2‑(间双(杂)芳基)吡咯烷‑1‑基]甲酮衍生物的食欲素受体拮抗剂 |
| WO2014141065A1 (en) | 2013-03-12 | 2014-09-18 | Actelion Pharmaceuticals Ltd | Azetidine amide derivatives as orexin receptor antagonists |
| UA119151C2 (uk) | 2013-12-03 | 2019-05-10 | Ідорсія Фармасьютікалз Лтд | КРИСТАЛІЧНА СОЛЬОВА ФОРМА (S)-(2-(6-ХЛОР-7-МЕТИЛ-1H-БЕНЗО[d]ІМІДАЗОЛ-2-ІЛ)-2-МЕТИЛПІРОЛІДИН-1-ІЛ)(5-МЕТОКСИ-2-(2H-1,2,3-ТРИАЗОЛ-2-ІЛ)ФЕНІЛ)МЕТАНОНУ ЯК АНТАГОНІСТ ОРЕКСИНОВОГО РЕЦЕПТОРА |
| EP3077391B1 (en) | 2013-12-04 | 2018-08-15 | Idorsia Pharmaceuticals Ltd | Use of benzimidazole-proline derivatives |
-
2014
- 2014-12-02 LT LTEP14824107.8T patent/LT3077389T/lt unknown
- 2014-12-02 AU AU2014358742A patent/AU2014358742B2/en active Active
- 2014-12-02 CA CA2929423A patent/CA2929423C/en active Active
- 2014-12-02 JP JP2016536109A patent/JP6496733B2/ja active Active
- 2014-12-02 MA MA39163A patent/MA39163B1/fr unknown
- 2014-12-02 MY MYPI2016701997A patent/MY179862A/en unknown
- 2014-12-02 ES ES14824107.8T patent/ES2651475T3/es active Active
- 2014-12-02 HU HUE14824107A patent/HUE035731T2/hu unknown
- 2014-12-02 CN CN201480065274.7A patent/CN105793257B/zh active Active
- 2014-12-02 NZ NZ721438A patent/NZ721438A/en unknown
- 2014-12-02 HR HRP20171773TT patent/HRP20171773T1/hr unknown
- 2014-12-02 MX MX2016007215A patent/MX364208B/es active IP Right Grant
- 2014-12-02 PL PL14824107T patent/PL3077389T3/pl unknown
- 2014-12-02 SI SI201430489T patent/SI3077389T1/en unknown
- 2014-12-02 PT PT148241078T patent/PT3077389T/pt unknown
- 2014-12-02 KR KR1020167017644A patent/KR102361418B1/ko active Active
- 2014-12-02 WO PCT/IB2014/066508 patent/WO2015083070A1/en not_active Ceased
- 2014-12-02 EP EP14824107.8A patent/EP3077389B1/en active Active
- 2014-12-02 TW TW103141828A patent/TWI664177B/zh active
- 2014-12-02 UA UAA201607114A patent/UA119549C2/uk unknown
- 2014-12-02 DK DK14824107.8T patent/DK3077389T3/da active
- 2014-12-02 EA EA201600435A patent/EA030137B1/ru not_active IP Right Cessation
- 2014-12-02 NO NO14824107A patent/NO3077389T3/no unknown
- 2014-12-02 US US15/101,768 patent/US9914720B2/en active Active
-
2016
- 2016-05-26 PH PH12016500988A patent/PH12016500988B1/en unknown
- 2016-05-30 IL IL245923A patent/IL245923B/en active IP Right Grant
- 2016-05-30 SA SA516371231A patent/SA516371231B1/ar unknown
- 2016-06-02 CL CL2016001342A patent/CL2016001342A1/es unknown
- 2016-07-01 ZA ZA2016/04499A patent/ZA201604499B/en unknown
-
2017
- 2017-12-12 CY CY20171101301T patent/CY1119695T1/el unknown
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