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 |
|---|---|---|---|
| IBPCT/IB2013/060596 | 2013-12-03 | ||
| IB2013060596 | 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 (https=) | 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 (31)
| Country | Link |
|---|---|
| US (1) | US9914720B2 (https=) |
| EP (1) | EP3077389B1 (https=) |
| JP (1) | JP6496733B2 (https=) |
| KR (1) | KR102361418B1 (https=) |
| CN (1) | CN105793257B (https=) |
| AU (1) | AU2014358742B2 (https=) |
| CA (1) | CA2929423C (https=) |
| CL (1) | CL2016001342A1 (https=) |
| CY (1) | CY1119695T1 (https=) |
| DK (1) | DK3077389T3 (https=) |
| EA (1) | EA030137B1 (https=) |
| ES (1) | ES2651475T3 (https=) |
| HK (1) | HK1225731B (https=) |
| HR (1) | HRP20171773T1 (https=) |
| HU (1) | HUE035731T2 (https=) |
| IL (1) | IL245923B (https=) |
| LT (1) | LT3077389T (https=) |
| MA (1) | MA39163B1 (https=) |
| MX (1) | MX364208B (https=) |
| MY (1) | MY179862A (https=) |
| NO (1) | NO3077389T3 (https=) |
| NZ (1) | NZ721438A (https=) |
| PH (1) | PH12016500988A1 (https=) |
| PL (1) | PL3077389T3 (https=) |
| PT (1) | PT3077389T (https=) |
| SA (1) | SA516371231B1 (https=) |
| SI (1) | SI3077389T1 (https=) |
| TW (1) | TWI664177B (https=) |
| UA (1) | UA119549C2 (https=) |
| WO (1) | WO2015083070A1 (https=) |
| ZA (1) | ZA201604499B (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101689093B1 (ko) * | 2012-06-04 | 2016-12-22 | 액테리온 파마슈티칼 리미티드 | 벤즈이미다졸-프롤린 유도체 |
| 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 |
| HRP20181710T1 (hr) | 2013-12-04 | 2018-12-28 | Idorsia Pharmaceuticals Ltd | Uporaba derivata benzimidazol-prolina |
| HRP20211304T1 (hr) * | 2017-05-03 | 2021-11-12 | Idorsia Pharmaceuticals Ltd | Pripravljanje derivata 2-([1,2,3]triazol-2-il)-benzojeve kiseline |
| US20230134935A1 (en) * | 2020-04-19 | 2023-05-04 | Idorsia Pharmaceuticals Ltd | Medical use of daridorexant |
| JP7681113B2 (ja) * | 2021-02-02 | 2025-05-21 | メッドシャイン ディスカバリー インコーポレイテッド | テトラヒドロピロロ環化合物及びその使用 |
| WO2023160004A1 (zh) * | 2022-02-25 | 2023-08-31 | 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 |
| US6677354B2 (en) | 2000-06-16 | 2004-01-13 | Smithkline Beecham P.L.C. | Piperdines for use as orexin receptor antagonists |
| KR20030060904A (ko) | 2000-10-06 | 2003-07-16 | 뉴로젠 코포레이션 | Ｃｒｆ 수용체 조절자로서 벤즈이미다졸 및 인돌 유도체 |
| JP4246490B2 (ja) | 2000-11-28 | 2009-04-02 | スミスクライン ビーチャム ピー エル シー | オレキシン受容体のアンタゴニストとしてのモルホリン誘導体 |
| US20040192673A1 (en) | 2001-05-05 | 2004-09-30 | Pascale Gaillard | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
| IL158463A0 (en) | 2001-05-05 | 2004-05-12 | Smithkline Beecham Plc | N-aroyl cyclic amines |
| BR0210609A (pt) * | 2001-06-28 | 2004-07-20 | Smithkline Beecham Plc | Derivados de amina cìclica n-aroila como antagonistas do receptor da orexina |
| GB0115862D0 (en) | 2001-06-28 | 2001-08-22 | Smithkline Beecham Plc | Compounds |
| 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 |
| US20060040937A1 (en) | 2002-09-18 | 2006-02-23 | Glaxo Group Limited | N-aroyl cyclic amines as orexin receptor antagonists |
| 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 |
| GB0225884D0 (en) | 2002-11-06 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
| PT1751111E (pt) | 2004-03-01 | 2015-04-01 | Actelion Pharmaceuticals Ltd | Derivados de 1,2,3,4-tetrahidroisoquinolina substituída |
| US20090082394A1 (en) | 2006-03-15 | 2009-03-26 | Actelion Pharmaceuticals, Ltd. | Tetrahydroisoquinoline Derivatives to Enhance Memory Function |
| WO2007135527A2 (en) * | 2006-05-23 | 2007-11-29 | Pfizer Products Inc. | Benzimidazolyl compounds |
| DE602007012910D1 (de) | 2006-08-15 | 2011-04-14 | Actelion Pharmaceuticals Ltd | Azetidinverbindungen als orexin-rezeptor-antagonisten |
| TW200823227A (en) | 2006-09-29 | 2008-06-01 | Actelion Pharmaceuticals Ltd | 3-aza-bicyclo[3.1.0]hexane derivatives |
| PE20081229A1 (es) | 2006-12-01 | 2008-08-28 | Merck & Co Inc | Antagonistas de receptor de orexina de diazepam sustituido |
| CL2007003827A1 (es) | 2006-12-28 | 2008-09-26 | Actelion Pharmaceuticals Ltd | Compuestos derivados de n-(2-aza-biciclo(3.1.0)hex-3-ilmetil)amida; y su uso para prevenir o tratar la depresion, neurosis, esquizofrenia, ansiedad, adicciones, epilepsia, dolor, enfermedades cardiacas, entre otras. |
| 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. |
| ATE483707T1 (de) | 2007-05-14 | 2010-10-15 | Actelion Pharmaceuticals Ltd | 2-cyclopropylthiazolderivate |
| WO2008150364A1 (en) | 2007-05-23 | 2008-12-11 | Merck & Co., Inc. | Cyclopropyl pyrrolidine orexin receptor antagonists |
| ATE524466T1 (de) | 2007-07-03 | 2011-09-15 | Actelion Pharmaceuticals Ltd | 3-azabicycloä3.3.0üoktanverbindungen |
| GB0712888D0 (en) | 2007-07-03 | 2007-08-15 | Glaxo Group Ltd | Novel compounds |
| EP2176258A1 (en) | 2007-07-03 | 2010-04-21 | Glaxo Group Limited | Piperidine derivatives useful as orexin receptor antagonists |
| KR20100046047A (ko) | 2007-07-27 | 2010-05-04 | 액테리온 파마슈티칼 리미티드 | 2-아자-비시클로[3.3.0]옥탄 유도체 |
| CA2693817A1 (en) | 2007-07-27 | 2009-02-05 | Actelion Pharmaceuticals Ltd | Trans-3-aza-bicyclo[3.1.0]hexane derivatives |
| 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 |
| MX2010008993A (es) | 2008-02-21 | 2010-09-07 | Actelion Pharmaceuticals Ltd | Derivados de 2-aza-biciclo-[2.2.1]heptano. |
| GB0806536D0 (en) | 2008-04-10 | 2008-05-14 | Glaxo Group Ltd | Novel compounds |
| CN102083827A (zh) | 2008-07-07 | 2011-06-01 | 埃科特莱茵药品有限公司 | 作为食欲素受体拮抗剂的噻唑烷化合物 |
| WO2010038200A1 (en) | 2008-10-01 | 2010-04-08 | Actelion Pharmaceuticals Ltd | Oxazolidine compounds as orexin receptor antagonists |
| JP2012509910A (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 |
| 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 |
| WO2010060472A1 (en) | 2008-11-26 | 2010-06-03 | Glaxo Group Limited | Imidazopyridazine derivatives acting as orexin antagonists |
| 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 |
| JP2012510494A (ja) | 2008-12-02 | 2012-05-10 | グラクソ グループ リミテッド | Ｎ−｛［（ｉｒ、４ｓ、６ｒ）−３−（２−ピリジニルカルボニル）−３−アザビシクロ［４．１．０］ヘプタ−４−イル］メチル｝−２−ヘテロアリールアミン誘導体およびその使用 |
| 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 |
| TW201209037A (en) | 2010-08-24 | 2012-03-01 | Actelion Pharmaceuticals Ltd | Proline sulfonamide derivatives as orexin receptor antagonists |
| CN103201261A (zh) | 2010-11-10 | 2013-07-10 | 埃科特莱茵药品有限公司 | 用作为食欲素受体拮抗剂的内酰胺衍生物 |
| KR101873083B1 (ko) | 2011-02-18 | 2018-06-29 | 이도르시아 파마슈티컬스 리미티드 | 오렉신 길항제로서 유용한 신규 피라졸 및 이미다졸 유도체 |
| TWI565703B (zh) | 2011-11-08 | 2017-01-11 | 艾克泰聯製藥有限公司 | ２-（１，２，３-三唑-２-基）苯甲醯胺及３-（１，２，３-三唑-２-基）吡啶醯胺衍生物 |
| KR101689093B1 (ko) * | 2012-06-04 | 2016-12-22 | 액테리온 파마슈티칼 리미티드 | 벤즈이미다졸-프롤린 유도체 |
| BR112015007516A2 (pt) | 2012-10-10 | 2017-07-04 | Actelion Pharmaceuticals Ltd | antagonistas do receptor de orexina que são derivados de [orto bi-(hetero-)aril]-[2-(meta bi-(hetero-)aril)- pirrolidin-1-il]-metanona |
| CA2902135A1 (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 |
| HRP20181710T1 (hr) | 2013-12-04 | 2018-12-28 | Idorsia Pharmaceuticals Ltd | Uporaba derivata benzimidazol-prolina |
-
2014
- 2014-12-02 HK HK16114145.7A patent/HK1225731B/en unknown
- 2014-12-02 JP JP2016536109A patent/JP6496733B2/ja active Active
- 2014-12-02 CN CN201480065274.7A patent/CN105793257B/zh active Active
- 2014-12-02 EP EP14824107.8A patent/EP3077389B1/en active Active
- 2014-12-02 HU HUE14824107A patent/HUE035731T2/hu unknown
- 2014-12-02 US US15/101,768 patent/US9914720B2/en active Active
- 2014-12-02 PT PT148241078T patent/PT3077389T/pt unknown
- 2014-12-02 UA UAA201607114A patent/UA119549C2/uk unknown
- 2014-12-02 NZ NZ721438A patent/NZ721438A/en unknown
- 2014-12-02 WO PCT/IB2014/066508 patent/WO2015083070A1/en not_active Ceased
- 2014-12-02 PL PL14824107T patent/PL3077389T3/pl unknown
- 2014-12-02 MA MA39163A patent/MA39163B1/fr unknown
- 2014-12-02 ES ES14824107.8T patent/ES2651475T3/es active Active
- 2014-12-02 DK DK14824107.8T patent/DK3077389T3/da active
- 2014-12-02 HR HRP20171773TT patent/HRP20171773T1/hr unknown
- 2014-12-02 SI SI201430489T patent/SI3077389T1/en unknown
- 2014-12-02 CA CA2929423A patent/CA2929423C/en active Active
- 2014-12-02 NO NO14824107A patent/NO3077389T3/no unknown
- 2014-12-02 MX MX2016007215A patent/MX364208B/es active IP Right Grant
- 2014-12-02 KR KR1020167017644A patent/KR102361418B1/ko active Active
- 2014-12-02 EA EA201600435A patent/EA030137B1/ru not_active IP Right Cessation
- 2014-12-02 TW TW103141828A patent/TWI664177B/zh active
- 2014-12-02 LT LTEP14824107.8T patent/LT3077389T/lt unknown
- 2014-12-02 MY MYPI2016701997A patent/MY179862A/en unknown
- 2014-12-02 AU AU2014358742A patent/AU2014358742B2/en active Active
-
2016
- 2016-05-26 PH PH12016500988A patent/PH12016500988A1/en unknown
- 2016-05-30 SA SA516371231A patent/SA516371231B1/ar unknown
- 2016-05-30 IL IL245923A patent/IL245923B/en active IP Right Grant
- 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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