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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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 |
|---|---|---|---|
| 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 |
|---|---|
| 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 (31)
| Country | Link |
|---|---|
| US (1) | US9914720B2 (show.php) |
| EP (1) | EP3077389B1 (show.php) |
| JP (1) | JP6496733B2 (show.php) |
| KR (1) | KR102361418B1 (show.php) |
| CN (1) | CN105793257B (show.php) |
| AU (1) | AU2014358742B2 (show.php) |
| CA (1) | CA2929423C (show.php) |
| CL (1) | CL2016001342A1 (show.php) |
| CY (1) | CY1119695T1 (show.php) |
| DK (1) | DK3077389T3 (show.php) |
| EA (1) | EA030137B1 (show.php) |
| ES (1) | ES2651475T3 (show.php) |
| HK (1) | HK1225731B (show.php) |
| HR (1) | HRP20171773T1 (show.php) |
| HU (1) | HUE035731T2 (show.php) |
| IL (1) | IL245923B (show.php) |
| LT (1) | LT3077389T (show.php) |
| MA (1) | MA39163B1 (show.php) |
| MX (1) | MX364208B (show.php) |
| MY (1) | MY179862A (show.php) |
| NO (1) | NO3077389T3 (show.php) |
| NZ (1) | NZ721438A (show.php) |
| PH (1) | PH12016500988A1 (show.php) |
| PL (1) | PL3077389T3 (show.php) |
| PT (1) | PT3077389T (show.php) |
| SA (1) | SA516371231B1 (show.php) |
| SI (1) | SI3077389T1 (show.php) |
| TW (1) | TWI664177B (show.php) |
| UA (1) | UA119549C2 (show.php) |
| WO (1) | WO2015083070A1 (show.php) |
| ZA (1) | ZA201604499B (show.php) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI510481B (zh) | 2012-06-04 | 2015-12-01 | Actelion Pharmaceuticals Ltd | 苯并咪唑脯胺酸衍生物 |
| 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 |
| LT3077391T (lt) | 2013-12-04 | 2018-10-25 | Idorsia Pharmaceuticals Ltd | Benzimidazolo prolino darinių panaudojimas |
| CN110612291B (zh) * | 2017-05-03 | 2024-02-13 | 爱杜西亚药品有限公司 | 2-([1,2,3]三唑-2-基)-苯甲酸衍生物的制备 |
| EP4138822A1 (en) * | 2020-04-19 | 2023-03-01 | 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 |
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| US3282927A (en) | 1964-05-21 | 1966-11-01 | Bristol Myers Co | 5-phenyl-4-thiazolylpenicillins |
| ATE293101T1 (de) | 2000-06-16 | 2005-04-15 | Smithkline Beecham Plc | Piperidine zur verwendung als orexin rezeptor antagonisten |
| CA2425185A1 (en) | 2000-10-06 | 2002-04-11 | Stephane De Lombaert | Benzimidazole and indole derivatives as crf receptor modulators |
| DE60108420T2 (de) | 2000-11-28 | 2005-12-22 | Smithkline Beecham P.L.C., Brentford | Morpholinderivate als antagonisten an orexinrezeptoren |
| ATE383359T1 (de) | 2001-05-05 | 2008-01-15 | Smithkline Beecham Plc | N-aroyl zyklische amine |
| JP2004534026A (ja) | 2001-05-05 | 2004-11-11 | スミスクライン ビーチャム パブリック リミテッド カンパニー | オレキシン受容体アンタゴニストとしてのｎ−アロイルサイクリックアミン誘導体 |
| GB0115862D0 (en) | 2001-06-28 | 2001-08-22 | Smithkline Beecham Plc | Compounds |
| ES2266549T3 (es) * | 2001-06-28 | 2007-03-01 | Smithkline Beecham Plc | Derivados de n-aroil-amina ciclicos como antagonistas del receptor de orexina. |
| 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 |
| JP2006504695A (ja) | 2002-09-18 | 2006-02-09 | グラクソ グループ リミテッド | オレキシン受容体アンタゴニストとしてのｎ−アロイル環状アミン |
| 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 |
| HRP20150371T1 (hr) | 2004-03-01 | 2015-05-08 | Actelion Pharmaceuticals Ltd. | Supstituirani derivati 1,2,3,4-tetrahidroizokinolina |
| AU2007226203A1 (en) | 2006-03-15 | 2007-09-20 | Actelion Pharmaceuticals Ltd | Tetrahydroisoquinoline derivatives to enhance memory function |
| WO2007135527A2 (en) * | 2006-05-23 | 2007-11-29 | Pfizer Products Inc. | Benzimidazolyl compounds |
| US7994336B2 (en) | 2006-08-15 | 2011-08-09 | Actelion Pharmaceuticals Ltd. | Azetidine compounds as orexin receptor antagonists |
| WO2008038251A2 (en) | 2006-09-29 | 2008-04-03 | 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 |
| 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. |
| US20100222328A1 (en) | 2007-05-14 | 2010-09-02 | Hamed Aissaoui | 2-cyclopropyl-thiazole derivatives |
| WO2008150364A1 (en) | 2007-05-23 | 2008-12-11 | Merck & Co., Inc. | Cyclopropyl pyrrolidine orexin receptor antagonists |
| EP2176258A1 (en) | 2007-07-03 | 2010-04-21 | Glaxo Group Limited | Piperidine derivatives useful as orexin receptor antagonists |
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| GB0712888D0 (en) | 2007-07-03 | 2007-08-15 | Glaxo Group Ltd | Novel compounds |
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| CA2693817A1 (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 |
| 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 |
| 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 |
| 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 |
| CA2745433A1 (en) | 2008-12-02 | 2010-06-10 | Glaxo Group Ltd. | N-{[(ir,4s,6r-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0]hept-4-yl] methyl}-2-heteroarylamine derivatives and uses thereof |
| UY32276A (es) | 2008-12-02 | 2010-05-31 | Glaxo Group Ltd | Derivados de n-{[1s,4s,6s)-3-(2-piridinilcarbonil)-3-azabiciclo[4.1.0]hept-4-il}metil}-2heteroarilamina y uso de los mismos |
| GB0823467D0 (en) * | 2008-12-23 | 2009-01-28 | Glaxo Group Ltd | Novel Compounds |
| SG175026A1 (en) | 2009-04-24 | 2011-11-28 | Glaxo Group Ltd | 3 -azabicyclo [4.1.0] heptanes used as orexin antagonists |
| WO2012025877A1 (en) | 2010-08-24 | 2012-03-01 | Actelion Pharmaceuticals Ltd | Proline sulfonamide derivatives as orexin receptor antagonists |
| JP5847830B2 (ja) | 2010-11-10 | 2016-01-27 | 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 | オレキシン受容体拮抗薬として有用なラクタム誘導体 |
| CN103380130B (zh) | 2011-02-18 | 2015-06-17 | 埃科特莱茵药品有限公司 | 用作为食欲素拮抗剂的新颖的吡唑和咪唑衍生物 |
| DK2776430T3 (en) | 2011-11-08 | 2016-05-09 | Actelion Pharmaceuticals Ltd | 2- (1,2,3-triazol-2-yl) benzamide and 3- (1,2,3-triazol-2-yl) PICOLINAMIDDERIVATER AS orexin receptor antagonists |
| TWI510481B (zh) * | 2012-06-04 | 2015-12-01 | Actelion Pharmaceuticals Ltd | 苯并咪唑脯胺酸衍生物 |
| MX2015004638A (es) | 2012-10-10 | 2015-07-14 | 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. |
| JP2016510810A (ja) | 2013-03-12 | 2016-04-11 | 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 | オレキシン受容体アンタゴニストとしてのアゼチジンアミド誘導体 |
| 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 |
| LT3077391T (lt) | 2013-12-04 | 2018-10-25 | Idorsia Pharmaceuticals Ltd | Benzimidazolo prolino darinių panaudojimas |
-
2014
- 2014-12-02 HU HUE14824107A patent/HUE035731T2/hu unknown
- 2014-12-02 US US15/101,768 patent/US9914720B2/en active Active
- 2014-12-02 UA UAA201607114A patent/UA119549C2/uk unknown
- 2014-12-02 MA MA39163A patent/MA39163B1/fr unknown
- 2014-12-02 HK HK16114145.7A patent/HK1225731B/en unknown
- 2014-12-02 KR KR1020167017644A patent/KR102361418B1/ko active Active
- 2014-12-02 CN CN201480065274.7A patent/CN105793257B/zh active Active
- 2014-12-02 NO NO14824107A patent/NO3077389T3/no unknown
- 2014-12-02 ES ES14824107.8T patent/ES2651475T3/es active Active
- 2014-12-02 JP JP2016536109A patent/JP6496733B2/ja active Active
- 2014-12-02 AU AU2014358742A patent/AU2014358742B2/en active Active
- 2014-12-02 PT PT148241078T patent/PT3077389T/pt unknown
- 2014-12-02 PL PL14824107T patent/PL3077389T3/pl unknown
- 2014-12-02 CA CA2929423A patent/CA2929423C/en active Active
- 2014-12-02 TW TW103141828A patent/TWI664177B/zh active
- 2014-12-02 MX MX2016007215A patent/MX364208B/es active IP Right Grant
- 2014-12-02 LT LTEP14824107.8T patent/LT3077389T/lt unknown
- 2014-12-02 MY MYPI2016701997A patent/MY179862A/en unknown
- 2014-12-02 SI SI201430489T patent/SI3077389T1/en unknown
- 2014-12-02 HR HRP20171773TT patent/HRP20171773T1/hr unknown
- 2014-12-02 EA EA201600435A patent/EA030137B1/ru not_active IP Right Cessation
- 2014-12-02 EP EP14824107.8A patent/EP3077389B1/en active Active
- 2014-12-02 DK DK14824107.8T patent/DK3077389T3/da active
- 2014-12-02 WO PCT/IB2014/066508 patent/WO2015083070A1/en not_active Ceased
- 2014-12-02 NZ NZ721438A patent/NZ721438A/en unknown
-
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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