IL245923B - Crystalline form of (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidine-1-yl)(5-methoxy-2-(2h- 3,2,1-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-methylpyrrolidine-1-yl)(5-methoxy-2-(2h- 3,2,1-triazol-2-yl)phenyl)methanone and its use as orexin receptor antagonistsInfo
- Publication number
- IL245923B IL245923B IL245923A IL24592316A IL245923B IL 245923 B IL245923 B IL 245923B IL 245923 A IL245923 A IL 245923A IL 24592316 A IL24592316 A IL 24592316A IL 245923 B IL245923 B IL 245923B
- Authority
- IL
- Israel
- Prior art keywords
- methylpyrrolidin
- methanone
- triazol
- imidazol
- benzo
- Prior art date
Links
- 229940123730 Orexin receptor antagonist Drugs 0.000 title 1
- 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 title 1
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)
- 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 (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
|---|---|
| IL245923A0 IL245923A0 (en) | 2016-08-02 |
| IL245923B true IL245923B (en) | 2019-09-26 |
Family
ID=52282786
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL245923A IL245923B (en) | 2013-12-03 | 2016-05-30 | Crystalline form of (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidine-1-yl)(5-methoxy-2-(2h- 3,2,1-triazol-2-yl)phenyl)methanone and its use as orexin receptor antagonists |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US9914720B2 (Direct) |
| EP (1) | EP3077389B1 (Direct) |
| JP (1) | JP6496733B2 (Direct) |
| KR (1) | KR102361418B1 (Direct) |
| CN (1) | CN105793257B (Direct) |
| AU (1) | AU2014358742B2 (Direct) |
| CA (1) | CA2929423C (Direct) |
| CL (1) | CL2016001342A1 (Direct) |
| CY (1) | CY1119695T1 (Direct) |
| DK (1) | DK3077389T3 (Direct) |
| EA (1) | EA030137B1 (Direct) |
| ES (1) | ES2651475T3 (Direct) |
| HR (1) | HRP20171773T1 (Direct) |
| HU (1) | HUE035731T2 (Direct) |
| IL (1) | IL245923B (Direct) |
| LT (1) | LT3077389T (Direct) |
| MA (1) | MA39163B1 (Direct) |
| MX (1) | MX364208B (Direct) |
| MY (1) | MY179862A (Direct) |
| NO (1) | NO3077389T3 (Direct) |
| NZ (1) | NZ721438A (Direct) |
| PH (1) | PH12016500988A1 (Direct) |
| PL (1) | PL3077389T3 (Direct) |
| PT (1) | PT3077389T (Direct) |
| SA (1) | SA516371231B1 (Direct) |
| SI (1) | SI3077389T1 (Direct) |
| TW (1) | TWI664177B (Direct) |
| UA (1) | UA119549C2 (Direct) |
| WO (1) | WO2015083070A1 (Direct) |
| ZA (1) | ZA201604499B (Direct) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2873341C (en) | 2012-06-04 | 2018-01-02 | Actelion 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 |
| MX366642B (es) | 2013-12-04 | 2019-07-17 | Idorsia Pharmaceuticals Ltd | Uso de derivados de bencimidazol-prolina. |
| CA3059394C (en) | 2017-05-03 | 2023-09-12 | Idorsia Pharmaceuticals Ltd | Preparation of 2-([1,2,3]triazol-2-yl)-benzoic acid derivatives |
| MX2022011179A (es) * | 2020-04-19 | 2022-10-07 | Idorsia Pharmaceuticals Ltd | Uso medico de daridorexant. |
| KR20230142554A (ko) * | 2021-02-02 | 2023-10-11 | 메드샤인 디스커버리 아이엔씨. | 테트라하이드로피롤로사이클릭 화합물 및 이의 용도 |
| 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 |
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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 |
| 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 |
| WO2002044172A1 (en) | 2000-11-28 | 2002-06-06 | Smithkline Beecham P.L.C. | Morpholine derivatives as antagonists of orexin receptors |
| US20040192673A1 (en) | 2001-05-05 | 2004-09-30 | Pascale Gaillard | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
| MXPA03010129A (es) | 2001-05-05 | 2004-03-10 | Smithkline Beecham Plc | N-aroilaminas-ciclicas. |
| GB0115862D0 (en) | 2001-06-28 | 2001-08-22 | Smithkline Beecham Plc | Compounds |
| CZ20033437A3 (cs) * | 2001-06-28 | 2004-09-15 | Smithkline Beecham P.L.C. | N-Aroylové cyklické aminové deriváty jako antagonisté orexinového receptoru |
| 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 |
| 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 |
| CA2644010A1 (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 |
| KR101113626B1 (ko) | 2006-08-15 | 2012-02-17 | 액테리온 파마슈티칼 리미티드 | 오렉신 수용체 길항제로서 아제티딘 화합물 |
| US20100016401A1 (en) | 2006-09-29 | 2010-01-21 | Actelion Phamaceuticals 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. |
| CA2685743A1 (en) | 2007-05-14 | 2008-11-20 | Actelion Pharmaceuticals Ltd | 2-cyclopropyl-thiazole derivatives |
| US8030495B2 (en) | 2007-05-23 | 2011-10-04 | Coleman Paul J | Cyclopropyl pyrrolidine orexin receptor antagonists |
| TW200911242A (en) | 2007-07-03 | 2009-03-16 | Glaxo Group Ltd | Novel compounds |
| CN101730696B (zh) | 2007-07-03 | 2013-01-09 | 埃科特莱茵药品有限公司 | 3-氮杂-二环[3.3.0]辛烷化合物 |
| GB0712888D0 (en) | 2007-07-03 | 2007-08-15 | Glaxo Group Ltd | Novel compounds |
| DE602008004265D1 (de) | 2007-07-27 | 2011-02-10 | Actelion Pharmaceuticals Ltd | Trans-3-aza-bicyclo-ä3.1.0ü-hexan-derivate |
| NZ583487A (en) | 2007-07-27 | 2011-09-30 | Actelion Pharmaceuticals Ltd | 2-aza-bicyclo[3.3.0]octane derivatives |
| EP2207778A2 (en) | 2007-09-24 | 2010-07-21 | Actelion Pharmaceuticals Ltd. | Pyrrolidines and piperidines as orexin receptor antagonists |
| PE20091010A1 (es) | 2007-10-10 | 2009-08-08 | Actelion Pharmaceuticals Ltd | Derivados de tetrahidroquinolina |
| AU2009215243A1 (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 |
| 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 |
| EP2358711A1 (en) | 2008-11-26 | 2011-08-24 | Glaxo Group Limited | Piperidine derivatives useful as orexin receptor antagonists |
| WO2010060472A1 (en) | 2008-11-26 | 2010-06-03 | Glaxo Group Limited | Imidazopyridazine derivatives acting as orexin antagonists |
| WO2010063663A1 (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 |
| EP2370427A1 (en) | 2008-12-02 | 2011-10-05 | 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 |
| GB0823467D0 (en) * | 2008-12-23 | 2009-01-28 | Glaxo Group Ltd | Novel Compounds |
| EA201171293A1 (ru) | 2009-04-24 | 2012-05-30 | Глэксо Груп Лимитед | 3-азабицикло[4.1.0]гептаны, применяемые в качестве антагонистов орексина |
| CA2807000C (en) | 2010-08-24 | 2018-12-04 | 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 |
| CA2823877C (en) | 2011-02-18 | 2020-01-07 | Actelion Pharmaceuticals Ltd | Novel pyrazole and imidazole derivatives useful as orexin antagonists |
| AR088692A1 (es) | 2011-11-08 | 2014-06-25 | Actelion Pharmaceuticals Ltd | Derivados de 2-(1,2,3-triazol-2-il)benzamina y 3-(1,2,3-triazol-2-il)picolinamida |
| CA2873341C (en) * | 2012-06-04 | 2018-01-02 | Actelion Pharmaceuticals Ltd | Benzimidazole-proline derivatives |
| AU2013328301A1 (en) | 2012-10-10 | 2015-05-28 | Actelion Pharmaceuticals Ltd | Orexin receptor antagonists which are [ortho bi (hetero-)aryl]-[2-(meta bi (hetero-)aryl)-pyrrolidin-1-yl]-methanone derivatives |
| EP2970241A1 (en) | 2013-03-12 | 2016-01-20 | 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 |
| MX366642B (es) | 2013-12-04 | 2019-07-17 | Idorsia Pharmaceuticals Ltd | Uso de derivados de bencimidazol-prolina. |
-
2014
- 2014-12-02 UA UAA201607114A patent/UA119549C2/uk unknown
- 2014-12-02 SI SI201430489T patent/SI3077389T1/en unknown
- 2014-12-02 NO NO14824107A patent/NO3077389T3/no unknown
- 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 CN CN201480065274.7A patent/CN105793257B/zh active Active
- 2014-12-02 DK DK14824107.8T patent/DK3077389T3/da active
- 2014-12-02 KR KR1020167017644A patent/KR102361418B1/ko active Active
- 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 MY MYPI2016701997A patent/MY179862A/en unknown
- 2014-12-02 HU HUE14824107A patent/HUE035731T2/hu unknown
- 2014-12-02 ES ES14824107.8T patent/ES2651475T3/es active Active
- 2014-12-02 LT LTEP14824107.8T patent/LT3077389T/lt unknown
- 2014-12-02 TW TW103141828A patent/TWI664177B/zh active
- 2014-12-02 MX MX2016007215A patent/MX364208B/es active IP Right Grant
- 2014-12-02 JP JP2016536109A patent/JP6496733B2/ja active Active
- 2014-12-02 US US15/101,768 patent/US9914720B2/en active Active
- 2014-12-02 CA CA2929423A patent/CA2929423C/en active Active
- 2014-12-02 AU AU2014358742A patent/AU2014358742B2/en active Active
- 2014-12-02 EP EP14824107.8A patent/EP3077389B1/en active Active
- 2014-12-02 PT PT148241078T patent/PT3077389T/pt unknown
- 2014-12-02 HR HRP20171773TT patent/HRP20171773T1/hr unknown
- 2014-12-02 PL PL14824107T patent/PL3077389T3/pl unknown
-
2016
- 2016-05-26 PH PH12016500988A patent/PH12016500988A1/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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