SI3077389T1 - (S) - (2- (6-CHLORO-7-METHYL-1 H-BENZO (D) IMIDAZOL-2-YL) -2-METHYLPYROLIDIN-1-YL (5-METHOXY-2- (2H- , 2,3-TRIAZOL-2-IL) PHENYL) METHANONE AND ITS USE AS ANTAGONISTS OF OREXIN RECEPTOR - Google Patents
(S) - (2- (6-CHLORO-7-METHYL-1 H-BENZO (D) IMIDAZOL-2-YL) -2-METHYLPYROLIDIN-1-YL (5-METHOXY-2- (2H- , 2,3-TRIAZOL-2-IL) PHENYL) METHANONE AND ITS USE AS ANTAGONISTS OF OREXIN RECEPTOR Download PDFInfo
- Publication number
- SI3077389T1 SI3077389T1 SI201430489T SI201430489T SI3077389T1 SI 3077389 T1 SI3077389 T1 SI 3077389T1 SI 201430489 T SI201430489 T SI 201430489T SI 201430489 T SI201430489 T SI 201430489T SI 3077389 T1 SI3077389 T1 SI 3077389T1
- Authority
- SI
- Slovenia
- Prior art keywords
- crystalline form
- methylpyrrolidin
- triazol
- imidazol
- benzo
- Prior art date
Links
- 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 claims abstract 8
- 229940123730 Orexin receptor antagonist Drugs 0.000 title claims abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 6
- 239000003814 drug Substances 0.000 claims abstract 3
- 238000002360 preparation method Methods 0.000 claims abstract 2
- 150000001875 compounds Chemical class 0.000 claims 16
- WSFSSNUMVMOOMR-BJUDXGSMSA-N methanone Chemical compound O=[11CH2] WSFSSNUMVMOOMR-BJUDXGSMSA-N 0.000 claims 12
- 238000000634 powder X-ray diffraction Methods 0.000 claims 12
- 238000010586 diagram Methods 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- -1 (S) - (2- (6-chloro-7-methyl-1H-benzo [d] imidazol-2- yl) -2- methylpyrrolidin-1-yl) (2H-1,2,3-triazol-2-yl) phenyl Chemical group 0.000 claims 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 230000005855 radiation Effects 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
- 208000019901 Anxiety disease Diseases 0.000 claims 3
- 238000003756 stirring Methods 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000001035 drying Methods 0.000 claims 2
- 239000000463 material Substances 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 206010012335 Dependence Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 208000006199 Parasomnias Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 238000002425 crystallisation Methods 0.000 claims 1
- 230000008025 crystallization Effects 0.000 claims 1
- 238000001914 filtration Methods 0.000 claims 1
- 238000011010 flushing procedure Methods 0.000 claims 1
- 230000007257 malfunction Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 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)
- Pain & Pain Management (AREA)
- Anesthesiology (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 |
|---|---|---|---|
| IB2013060596 | 2013-12-03 | ||
| EP14824107.8A EP3077389B1 (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 |
| 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 (1)
| Publication Number | Publication Date |
|---|---|
| SI3077389T1 true SI3077389T1 (en) | 2018-01-31 |
Family
ID=52282786
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI201430489T SI3077389T1 (en) | 2013-12-03 | 2014-12-02 | (S) - (2- (6-CHLORO-7-METHYL-1 H-BENZO (D) IMIDAZOL-2-YL) -2-METHYLPYROLIDIN-1-YL (5-METHOXY-2- (2H- , 2,3-TRIAZOL-2-IL) PHENYL) METHANONE AND ITS USE AS ANTAGONISTS OF OREXIN RECEPTOR |
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 |
|---|---|---|---|---|
| HRP20170351T1 (hr) | 2012-06-04 | 2017-04-21 | Actelion Pharmaceuticals Ltd. | Derivati benzimidazol-prolina |
| 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 |
| JP7182562B2 (ja) * | 2017-05-03 | 2022-12-02 | イドーシア ファーマシューティカルズ リミテッド | ２－（［１，２，３］トリアゾール－２－イル）－安息香酸誘導体の製造 |
| JP2023521492A (ja) | 2020-04-19 | 2023-05-24 | イドーシア ファーマシューティカルズ リミテッド | ダリドレキサントの医学的用途 |
| EP4289834B1 (en) * | 2021-02-02 | 2025-11-26 | Medshine Discovery Inc. | Tetrahydropyrrolocyclic compound and application thereof |
| 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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| WO2002028839A1 (en) | 2000-10-06 | 2002-04-11 | Neurogen Corporation | Benzimidazole and indole derivatives as crf receptor modulators |
| AU2002224885A1 (en) | 2000-11-28 | 2002-06-11 | Smithkline Beecham Plc | Morpholine derivatives as antagonists of orexin receptors |
| 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 |
| 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 |
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| HRP20170351T1 (hr) * | 2012-06-04 | 2017-04-21 | Actelion Pharmaceuticals Ltd. | Derivati benzimidazol-prolina |
| EP2906553B1 (en) | 2012-10-10 | 2019-06-26 | Idorsia Pharmaceuticals Ltd | Orexin receptor antagonists which are [ortho bi (hetero )aryl]-[2-(meta bi (hetero)aryl)-pyrrolidin-1-yl]-methanone derivatives |
| 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 |
| HRP20181710T1 (hr) | 2013-12-04 | 2018-12-28 | Idorsia Pharmaceuticals Ltd | Uporaba derivata benzimidazol-prolina |
-
2014
- 2014-12-02 NO NO14824107A patent/NO3077389T3/no unknown
- 2014-12-02 MY MYPI2016701997A patent/MY179862A/en unknown
- 2014-12-02 MA MA39163A patent/MA39163B1/fr unknown
- 2014-12-02 LT LTEP14824107.8T patent/LT3077389T/lt unknown
- 2014-12-02 JP JP2016536109A patent/JP6496733B2/ja active Active
- 2014-12-02 DK DK14824107.8T patent/DK3077389T3/da active
- 2014-12-02 ES ES14824107.8T patent/ES2651475T3/es active Active
- 2014-12-02 PT PT148241078T patent/PT3077389T/pt unknown
- 2014-12-02 SI SI201430489T patent/SI3077389T1/en unknown
- 2014-12-02 PL PL14824107T patent/PL3077389T3/pl unknown
- 2014-12-02 CA CA2929423A patent/CA2929423C/en active Active
- 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 EP EP14824107.8A patent/EP3077389B1/en active Active
- 2014-12-02 US US15/101,768 patent/US9914720B2/en active Active
- 2014-12-02 UA UAA201607114A patent/UA119549C2/uk unknown
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