HRP20171772T1 - Kristalični oblik soli od (s)-(2-(6-kloro-7-metil-1h-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2h-1,2,3-triazol-2-il)fenil)metanona koji služi kao antagonist receptora oreksina - Google Patents
Kristalični oblik soli od (s)-(2-(6-kloro-7-metil-1h-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2h-1,2,3-triazol-2-il)fenil)metanona koji služi kao antagonist receptora oreksina Download PDFInfo
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- HRP20171772T1 HRP20171772T1 HRP20171772TT HRP20171772T HRP20171772T1 HR P20171772 T1 HRP20171772 T1 HR P20171772T1 HR P20171772T T HRP20171772T T HR P20171772TT HR P20171772 T HRP20171772 T HR P20171772T HR P20171772 T1 HRP20171772 T1 HR P20171772T1
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- methylpyrrolidin
- triazol
- imidazol
- benzo
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- 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 2
- 150000003839 salts Chemical group 0.000 title claims 2
- 229940123730 Orexin receptor antagonist Drugs 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
- 208000035475 disorder Diseases 0.000 claims 9
- HJVGDXBEMFHGKI-BQAIUKQQSA-N [(2s)-2-(5-chloro-4-methyl-1h-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-[5-methoxy-2-(triazol-2-yl)phenyl]methanone;hydrochloride Chemical compound Cl.N1([C@](CCC1)(C)C=1NC2=CC=C(Cl)C(C)=C2N=1)C(=O)C1=CC(OC)=CC=C1N1N=CC=N1 HJVGDXBEMFHGKI-BQAIUKQQSA-N 0.000 claims 7
- 208000019116 sleep disease Diseases 0.000 claims 5
- 230000006806 disease prevention Effects 0.000 claims 4
- 208000019901 Anxiety disease Diseases 0.000 claims 3
- 206010012335 Dependence Diseases 0.000 claims 3
- 238000000634 powder X-ray diffraction Methods 0.000 claims 3
- 208000019022 Mood disease Diseases 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 238000010586 diagram Methods 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000000843 powder Substances 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- 206010013980 Dyssomnias Diseases 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical class Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- 208000006199 Parasomnias Diseases 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 230000004630 mental health Effects 0.000 claims 1
- 230000000446 orexinergic effect Effects 0.000 claims 1
- 208000020685 sleep-wake disease Diseases 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive 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
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/28—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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (9)
1. Kristalični oblik spoja (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanona, pri čemu je spomenuti spoj prisutan u obliku soli klorovodične kiseline, te je pritom spomenuti kristalični oblik soli, naznačen time, da pokazuje vršne vrijednosti u difrakcijskom dijagramu praha X-zraka, uz sljedeće refrakcijske kutove 2θ: 11,0°, 24,1° i 24,5°, dok se navedeni dijagram difrakcije praha X-zraka dobiva pomoću uporabe kombinirane radijacije Cu Kα1 i Cu Kα2, bez Kα2-strippinga; a preciznost za 2θ-vrijednosti leži u rasponu od 2θ +/- 0,2°.
2. Kristalični oblik od (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanonhidroklorida prema zahtjevu 1, naznačen time, da pokazuje vršne vrijednosti u difrakcijskom dijagramu praha X-zraka, uz sljedeće refrakcijske kutove 2θ: 9,2°, 11,0°, 13,8°, 15,1°, 16,3°, 16,8°, 19,8°, 24,1°, 24,5°, i 27,3°, gdje se navedeni dijagram difrakcije praha X-zraka dobiva pomoću kombinirane radijacije Cu Kα1 i Cu Kα2, bez Kα2-strippinga; a preciznost za 2θ-vrijednosti leži u rasponu od 2θ +/- 0,2°.
3. Kristalični oblik od (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanonhidroklorida prema zahtjevima 1 ili 2, naznačen time, da u biti pokazuje uzorak difrakcije praha X-zraka kao što je prikazano na Slici 2.
4. Farmaceutski sastav, naznačen time, da obuhvaća kristalični oblik od (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanonhidroklorida prema bilo kojem od zahtjeva 1 do 3, i farmaceutski prikladan nosač.
5. Farmaceutski sastav prema zahtjevu 4, naznačen time, da se upotrebljava u liječenju ili prevenciji bolesti ili poremećaja mentalnog zdravlja u odnosu na oreksinergijske disfunkcije.
6. Kristalični oblik od (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanonhidroklorida prema bilo kojem od zahtjeva 1 do 3, naznačen time, da se upotrebljava kao lijek.
7. Kristalični oblik od (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanonhidroklorida prema bilo kojem od zahtjeva 1 do 3, naznačen time, da se upotrebljava u liječenju ili prevenciji bolesti ili poremećaja odabranih iz skupine koju čine: poremećaji spavanja, poremećaji anksioznosti, poremećaji ovisnosti, kognitivne disfunkcije, poremećaji raspoloženja, i poremećaji teka.
8. Kristalični oblik od (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanonhidroklorida prema bilo kojem od zahtjeva 1 do 3, naznačen time, da se upotrebljava u liječenju ili prevenciji bolesti ili poremećaja odabranih iz skupine koju čine: poremećaj spavanja koji se odabire iz skupine koja se sastoji od disomnija, parasomnija, poremećaja spavanja povezanih s općim medicinskim stanjem i poremećaja spavanja izazvanih supstancama; poremećaj anksioznosti; i poremećaj ovisnosti.
9. Uporaba kristaličnog oblika od (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanonhidroklorida prema bilo kojem od zahtjeva 1 do 3, naznačena time, da je za proizvodnju lijeka za liječenje ili prevenciju bolesti ili poremećaja odabranih iz skupine koju čine: poremećaji spavanja, poremećaji anksioznosti, poremećaji ovisnosti, kognitivne disfunkcije, poremećaji raspoloženja, i poremećaji teka.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IB2013060595 | 2013-12-03 | ||
| PCT/IB2014/066509 WO2015083071A1 (en) | 2013-12-03 | 2014-12-02 | Crystalline salt form of (s)-(2-(6-chloro-7-methyl-1 h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1 -yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone as orexin receptor antagonist |
| EP14824108.6A EP3077390B1 (en) | 2013-12-03 | 2014-12-02 | Crystalline salt 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 as orexin receptor antagonist |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20171772T1 true HRP20171772T1 (hr) | 2017-12-29 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20171772TT HRP20171772T1 (hr) | 2013-12-03 | 2017-11-16 | Kristalični oblik soli od (s)-(2-(6-kloro-7-metil-1h-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2h-1,2,3-triazol-2-il)fenil)metanona koji služi kao antagonist receptora oreksina |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US9790208B2 (hr) |
| EP (1) | EP3077390B1 (hr) |
| JP (1) | JP6091716B2 (hr) |
| KR (1) | KR101839716B1 (hr) |
| CN (1) | CN105793258B (hr) |
| AU (1) | AU2014358743B2 (hr) |
| CA (1) | CA2929720C (hr) |
| CL (1) | CL2016001348A1 (hr) |
| CY (1) | CY1119687T1 (hr) |
| DK (1) | DK3077390T3 (hr) |
| EA (1) | EA030109B1 (hr) |
| ES (1) | ES2651508T3 (hr) |
| HK (1) | HK1225736B (hr) |
| HR (1) | HRP20171772T1 (hr) |
| HU (1) | HUE034656T2 (hr) |
| IL (1) | IL245922B (hr) |
| LT (1) | LT3077390T (hr) |
| MA (1) | MA39164B1 (hr) |
| MX (1) | MX362701B (hr) |
| MY (1) | MY176244A (hr) |
| NO (1) | NO3077390T3 (hr) |
| NZ (1) | NZ721493A (hr) |
| PH (1) | PH12016500989B1 (hr) |
| PL (1) | PL3077390T3 (hr) |
| PT (1) | PT3077390T (hr) |
| SA (1) | SA516371248B1 (hr) |
| SG (1) | SG11201604541WA (hr) |
| SI (1) | SI3077390T1 (hr) |
| TW (1) | TWI636982B (hr) |
| UA (1) | UA119151C2 (hr) |
| WO (1) | WO2015083071A1 (hr) |
| ZA (1) | ZA201604501B (hr) |
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| 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 |
| NZ721438A (en) * | 2013-12-03 | 2021-12-24 | Idorsia Pharmaceuticals Ltd | 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 |
| KR102330133B1 (ko) | 2013-12-04 | 2021-11-23 | 이도르시아 파마슈티컬스 리미티드 | 벤즈이미다졸-프롤린 유도체의 용도 |
| MX2019012902A (es) | 2017-05-03 | 2019-12-16 | Idorsia Pharmaceuticals Ltd | Preparacion de derivados de acido 2-([1,2,3]triazol-2-il)-benzoico . |
| EP4138822A1 (en) | 2020-04-19 | 2023-03-01 | Idorsia Pharmaceuticals Ltd | Medical use of daridorexant |
| 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 |
| CN117736193B (zh) * | 2023-12-19 | 2024-07-23 | 南京知和医药科技有限公司 | 一种氘代稠环化合物及其制备方法与用途 |
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