KR102361418B1 - (S)-(2-(6-클로로-7-메틸-1H-벤조[d]이미다졸-2-일)-2-메틸피롤리딘-1- 일)(5-메톡시-2-(2H-1,2,3-트리아졸-2-일)페닐)메타논의 결정형 및 오렉신 수용체 길항제로서의 그 용도 - Google Patents
(S)-(2-(6-클로로-7-메틸-1H-벤조[d]이미다졸-2-일)-2-메틸피롤리딘-1- 일)(5-메톡시-2-(2H-1,2,3-트리아졸-2-일)페닐)메타논의 결정형 및 오렉신 수용체 길항제로서의 그 용도 Download PDFInfo
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- KR102361418B1 KR102361418B1 KR1020167017644A KR20167017644A KR102361418B1 KR 102361418 B1 KR102361418 B1 KR 102361418B1 KR 1020167017644 A KR1020167017644 A KR 1020167017644A KR 20167017644 A KR20167017644 A KR 20167017644A KR 102361418 B1 KR102361418 B1 KR 102361418B1
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- South Korea
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- crystalline form
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- compound
- methyl
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- UMKSAURFQFUULT-UHFFFAOYSA-N COc(cc1)cc(C(O)=O)c1N Chemical compound COc(cc1)cc(C(O)=O)c1N UMKSAURFQFUULT-UHFFFAOYSA-N 0.000 description 1
- NBGABHGMJVIVBW-QHCPKHFHSA-N C[C@](CCC1)(c2nc(c(C)c(cc3)Cl)c3[nH]2)N1C(c(cc(cc1)OC)c1-[n]1nccn1)=O Chemical compound C[C@](CCC1)(c2nc(c(C)c(cc3)Cl)c3[nH]2)N1C(c(cc(cc1)OC)c1-[n]1nccn1)=O NBGABHGMJVIVBW-QHCPKHFHSA-N 0.000 description 1
- ITFDEQAHMJTBKT-ZDUSSCGKSA-N C[C@]1(c2nc(c(C)c(cc3)Cl)c3[nH]2)NCCC1 Chemical compound C[C@]1(c2nc(c(C)c(cc3)Cl)c3[nH]2)NCCC1 ITFDEQAHMJTBKT-ZDUSSCGKSA-N 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4192—1,2,3-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Anesthesiology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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 (2)
| Publication Number | Publication Date |
|---|---|
| KR20160092015A KR20160092015A (ko) | 2016-08-03 |
| KR102361418B1 true KR102361418B1 (ko) | 2022-02-09 |
Family
ID=52282786
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020167017644A Active KR102361418B1 (ko) | 2013-12-03 | 2014-12-02 | (S)-(2-(6-클로로-7-메틸-1H-벤조[d]이미다졸-2-일)-2-메틸피롤리딘-1- 일)(5-메톡시-2-(2H-1,2,3-트리아졸-2-일)페닐)메타논의 결정형 및 오렉신 수용체 길항제로서의 그 용도 |
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 |
|---|---|---|---|---|
| MY169986A (en) * | 2012-06-04 | 2019-06-19 | Idorsia Pharmaceuticals Ltd | Benzimidazole-proline derivatives |
| 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 |
| JP6421185B2 (ja) | 2013-12-04 | 2018-11-07 | イドーシア ファーマシューティカルズ リミテッドIdorsia Pharmaceuticals Ltd | ベンゾイミダゾール−プロリン誘導体の使用 |
| PT3619199T (pt) * | 2017-05-03 | 2021-10-01 | Idorsia Pharmaceuticals Ltd | Preparação de derivados de ácido 2-([1,2,3]triazol-2-il)- benzoico |
| BR112022020924A2 (pt) | 2020-04-19 | 2023-02-14 | Idorsia Pharmaceuticals Ltd | Métodos de tratamento de um transtorno do sono, a sonolência diurna em um indivíduo, a insônia, e, daridorexante na forma de sal livre ou farmaceuticamente aceitável |
| 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 |
| 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 |
Citations (2)
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|---|---|---|---|---|
| WO2010072722A1 (en) | 2008-12-23 | 2010-07-01 | Glaxo Group Limited | Piperidine derivatives useful as orexin antagonists |
| WO2013182972A1 (en) | 2012-06-04 | 2013-12-12 | Actelion Pharmaceuticals Ltd | Benzimidazole-proline derivatives |
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| US3282927A (en) | 1964-05-21 | 1966-11-01 | Bristol Myers Co | 5-phenyl-4-thiazolylpenicillins |
| EP1289955B1 (en) | 2000-06-16 | 2005-04-13 | Smithkline Beecham Plc | Piperidines for use as orexin receptor antagonists |
| MXPA03003039A (es) | 2000-10-06 | 2003-10-15 | Neurogen Corp | Derivados de indola y bencimidazola como moduladores del receptor crf. |
| EP1353918B1 (en) | 2000-11-28 | 2005-01-12 | Smithkline Beecham Plc | Morpholine derivatives as antagonists of orexin receptors |
| WO2002090355A1 (en) | 2001-05-05 | 2002-11-14 | Smithkline Beecham P.L.C. | N-aroyl cyclic amines |
| US20040192673A1 (en) | 2001-05-05 | 2004-09-30 | Pascale Gaillard | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
| 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 |
| GB0130393D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| GB0130335D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| WO2004026866A1 (en) | 2002-09-18 | 2004-04-01 | Glaxo Group Limited | N-aroyl cyclic amines as orexin receptor antagonists |
| 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 |
| PT1751111E (pt) | 2004-03-01 | 2015-04-01 | Actelion Pharmaceuticals Ltd | Derivados de 1,2,3,4-tetrahidroisoquinolina substituída |
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| 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 |
| 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. |
| JP2010526869A (ja) | 2007-05-14 | 2010-08-05 | アクテリオン ファーマシューティカルズ リミテッド | 2−シクロプロピル−チアゾール誘導体 |
| JP2010528007A (ja) | 2007-05-23 | 2010-08-19 | メルク・シャープ・エンド・ドーム・コーポレイション | シクロプロピルピロリジンオレキシン受容体アンタゴニスト |
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| GB0712888D0 (en) | 2007-07-03 | 2007-08-15 | Glaxo Group Ltd | Novel compounds |
| EA201070091A1 (ru) | 2007-07-03 | 2010-06-30 | Глэксо Груп Лимитед | Производные пиперидина, пригодные в качестве антагонистов рецептора орексина |
| WO2009016560A2 (en) | 2007-07-27 | 2009-02-05 | Actelion Pharmaceuticals Ltd | Trans-3-aza-bicyclo[3.1.0]hexane derivatives |
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| WO2009104155A1 (en) | 2008-02-21 | 2009-08-27 | Actelion Pharmaceuticals Ltd | 2-aza-bicyclo[2.2.1]heptane derivatives |
| 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 |
| WO2010060471A1 (en) | 2008-11-26 | 2010-06-03 | Glaxo Group Limited | Piperidine derivatives useful as orexin receptor antagonists |
| 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 |
| 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 |
| 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 |
| CA2745420A1 (en) | 2008-12-02 | 2010-06-10 | Glaxo Group Limited | N-{[(ir,4s,6r-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0] hept-4-yl] methyl}-2-heteroarylamine derivatives and uses thereof |
| MX2011011127A (es) | 2009-04-24 | 2011-11-18 | Glaxo Group Ltd | 3-azabiciclo[4.1.0] heptanos usados como antagonistas de orexina. |
| EP2608787B1 (en) | 2010-08-24 | 2019-11-20 | Idorsia Pharmaceuticals Ltd | Proline sulfonamide derivatives as orexin receptor antagonists |
| US9242970B2 (en) | 2010-11-10 | 2016-01-26 | 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 |
| KR101676930B1 (ko) | 2011-11-08 | 2016-11-16 | 액테리온 파마슈티칼 리미티드 | 오렉신 수용체 길항제로서의 2-(1,2,3-트리아졸-2-일)벤즈아미드 및 3-(1,2,3-트리아졸-2-일)피콜린아미드 유도체 |
| AR092955A1 (es) | 2012-10-10 | 2015-05-06 | Actelion Pharmaceuticals Ltd | Antagonistas de receptores de orexina los cuales son derivados de [orto bi-(hetero-)aril]-[2-(meta bi-(hetero-)aril)-pirrolidin-1-il]-metanona |
| 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 |
| JP6421185B2 (ja) | 2013-12-04 | 2018-11-07 | イドーシア ファーマシューティカルズ リミテッドIdorsia Pharmaceuticals Ltd | ベンゾイミダゾール−プロリン誘導体の使用 |
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2014
- 2014-12-02 NZ NZ721438A patent/NZ721438A/en unknown
- 2014-12-02 PT PT148241078T patent/PT3077389T/pt unknown
- 2014-12-02 AU AU2014358742A patent/AU2014358742B2/en active Active
- 2014-12-02 PL PL14824107T patent/PL3077389T3/pl unknown
- 2014-12-02 LT LTEP14824107.8T patent/LT3077389T/lt unknown
- 2014-12-02 HR HRP20171773TT patent/HRP20171773T1/hr unknown
- 2014-12-02 US US15/101,768 patent/US9914720B2/en active Active
- 2014-12-02 HU HUE14824107A patent/HUE035731T2/hu unknown
- 2014-12-02 MY MYPI2016701997A patent/MY179862A/en unknown
- 2014-12-02 UA UAA201607114A patent/UA119549C2/uk unknown
- 2014-12-02 CA CA2929423A patent/CA2929423C/en active Active
- 2014-12-02 MX MX2016007215A patent/MX364208B/es active IP Right Grant
- 2014-12-02 MA MA39163A patent/MA39163B1/fr unknown
- 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 TW TW103141828A patent/TWI664177B/zh active
- 2014-12-02 ES ES14824107.8T patent/ES2651475T3/es 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 WO PCT/IB2014/066508 patent/WO2015083070A1/en not_active Ceased
- 2014-12-02 SI SI201430489T patent/SI3077389T1/en unknown
- 2014-12-02 KR KR1020167017644A patent/KR102361418B1/ko active Active
- 2014-12-02 DK DK14824107.8T patent/DK3077389T3/da active
- 2014-12-02 JP JP2016536109A patent/JP6496733B2/ja active Active
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2016
- 2016-05-26 PH PH12016500988A patent/PH12016500988B1/en unknown
- 2016-05-30 IL IL245923A patent/IL245923B/en active IP Right Grant
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| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2010072722A1 (en) | 2008-12-23 | 2010-07-01 | Glaxo Group Limited | Piperidine derivatives useful as orexin antagonists |
| WO2013182972A1 (en) | 2012-06-04 | 2013-12-12 | Actelion Pharmaceuticals Ltd | Benzimidazole-proline derivatives |
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