CA2929423C - 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 - Google Patents
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 Download PDFInfo
- Publication number
- CA2929423C CA2929423C CA2929423A CA2929423A CA2929423C CA 2929423 C CA2929423 C CA 2929423C CA 2929423 A CA2929423 A CA 2929423A CA 2929423 A CA2929423 A CA 2929423A CA 2929423 C CA2929423 C CA 2929423C
- Authority
- CA
- Canada
- Prior art keywords
- crystalline form
- compound
- disorders
- methyl
- triazol
- 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.)
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Links
Classifications
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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 (2)
| Publication Number | Publication Date |
|---|---|
| CA2929423A1 CA2929423A1 (en) | 2015-06-11 |
| CA2929423C true CA2929423C (en) | 2021-12-07 |
Family
ID=52282786
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2929423A Active CA2929423C (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 |
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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