EA201401351A1 - Производные бензимидазол-пролина - Google Patents
Производные бензимидазол-пролинаInfo
- Publication number
- EA201401351A1 EA201401351A1 EA201401351A EA201401351A EA201401351A1 EA 201401351 A1 EA201401351 A1 EA 201401351A1 EA 201401351 A EA201401351 A EA 201401351A EA 201401351 A EA201401351 A EA 201401351A EA 201401351 A1 EA201401351 A1 EA 201401351A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- benzimidazol
- proline
- derivatives
- compounds
- formula
- Prior art date
Links
- UBSOHWJGTKOSAS-VWMHFEHESA-N 1H-benzimidazole (2S)-pyrrolidine-2-carboxylic acid Chemical class OC(=O)[C@@H]1CCCN1.c1nc2ccccc2[nH]1 UBSOHWJGTKOSAS-VWMHFEHESA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229940123730 Orexin receptor antagonist Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- 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
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- 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
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- C07D403/02—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 two hetero rings
- C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Anesthesiology (AREA)
- Addiction (AREA)
- Hospice & Palliative Care (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Изобретение относится к соединениям формулы (I)где Ar, R, R, R, R, Rи (R)имеют значения, как описано в описании, к их получению, к их фармацевтически приемлемым солям, и к их применению в качестве фармацевтических средств, к фармацевтическим композициям, содержащим одно или более соединений формулы (I), и в особенности к их применению в качестве антагонистов рецептора орексина.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12170748 | 2012-06-04 | ||
| EP13158520 | 2013-03-11 | ||
| PCT/IB2013/054567 WO2013182972A1 (en) | 2012-06-04 | 2013-06-03 | Benzimidazole-proline derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201401351A1 true EA201401351A1 (ru) | 2015-05-29 |
| EA028046B1 EA028046B1 (ru) | 2017-10-31 |
Family
ID=48914370
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201600366A EA029899B1 (ru) | 2012-06-04 | 2013-06-03 | Производные бензимидазол-пролина |
| EA201401351A EA028046B1 (ru) | 2012-06-04 | 2013-06-03 | Производные бензимидазол-пролина |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201600366A EA029899B1 (ru) | 2012-06-04 | 2013-06-03 | Производные бензимидазол-пролина |
Country Status (33)
| Country | Link |
|---|---|
| US (3) | US9732075B2 (ru) |
| EP (1) | EP2855453B1 (ru) |
| JP (1) | JP5814491B2 (ru) |
| KR (3) | KR101689093B1 (ru) |
| CN (1) | CN104334544B (ru) |
| AR (1) | AR091257A1 (ru) |
| AU (1) | AU2013273222B2 (ru) |
| BR (1) | BR112014030173B1 (ru) |
| CA (1) | CA2873341C (ru) |
| CL (1) | CL2014003294A1 (ru) |
| CY (2) | CY1118735T1 (ru) |
| DK (1) | DK2855453T3 (ru) |
| EA (2) | EA029899B1 (ru) |
| ES (1) | ES2617863T3 (ru) |
| FR (1) | FR22C1047I2 (ru) |
| HR (1) | HRP20170351T1 (ru) |
| HU (2) | HUE031753T2 (ru) |
| IL (1) | IL236024A (ru) |
| LT (2) | LT2855453T (ru) |
| LU (1) | LUC00279I2 (ru) |
| MX (1) | MX354102B (ru) |
| MY (1) | MY169986A (ru) |
| NL (1) | NL301197I2 (ru) |
| NO (1) | NO2022044I1 (ru) |
| NZ (1) | NZ703448A (ru) |
| PH (1) | PH12014502540A1 (ru) |
| PL (1) | PL2855453T3 (ru) |
| PT (1) | PT2855453T (ru) |
| SG (2) | SG10201702540UA (ru) |
| SI (1) | SI2855453T1 (ru) |
| TW (2) | TWI510481B (ru) |
| WO (1) | WO2013182972A1 (ru) |
| ZA (1) | ZA201409422B (ru) |
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| EP2608787B1 (en) | 2010-08-24 | 2019-11-20 | Idorsia Pharmaceuticals Ltd | Proline sulfonamide derivatives as orexin receptor antagonists |
| MY169986A (en) | 2012-06-04 | 2019-06-19 | Idorsia Pharmaceuticals Ltd | Benzimidazole-proline derivatives |
| AR092955A1 (es) | 2012-10-10 | 2015-05-06 | 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 |
| WO2014141065A1 (en) | 2013-03-12 | 2014-09-18 | Actelion Pharmaceuticals Ltd | Azetidine amide derivatives as orexin receptor antagonists |
| CN105658649B (zh) | 2013-07-22 | 2019-03-22 | 爱杜西亚药品有限公司 | 1-(哌嗪-1-基)-2-([1,2,4]三唑-1-基)-乙酮衍生物 |
| 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 |
| 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 |
| JP6421185B2 (ja) * | 2013-12-04 | 2018-11-07 | イドーシア ファーマシューティカルズ リミテッドIdorsia Pharmaceuticals Ltd | ベンゾイミダゾール−プロリン誘導体の使用 |
| TW201613864A (en) * | 2014-02-20 | 2016-04-16 | Takeda Pharmaceutical | Novel compounds |
| PE20161374A1 (es) * | 2014-02-20 | 2016-12-17 | Takeda Pharmaceuticals Co | Ciclopentanos, tetrahidrofuranos y pirrolidinas sustituidas como antagonistas del receptor de orexina |
| AR103399A1 (es) | 2015-01-15 | 2017-05-10 | Actelion Pharmaceuticals Ltd | Derivados de (r)-2-metil-piperazina como moduladores del receptor cxcr3 |
| MY187614A (en) * | 2015-01-15 | 2021-10-04 | Idorsia Pharmaceuticals Ltd | Hydroxyalkyl-piperazine derivatives as cxcr3 receptor modulators |
| AU2016295693B2 (en) | 2015-07-17 | 2020-05-21 | Sunshine Lake Pharma Co., Ltd. | Substituted quinazoline compounds and preparation and uses thereof |
| EA038492B1 (ru) | 2015-10-01 | 2021-09-07 | Байокрист Фармасьютикалз, Инк. | Ингибиторы плазменного калликреина человека |
| CN106749269B (zh) | 2015-11-23 | 2019-01-04 | 广东东阳光药业有限公司 | 八氢吡咯并[3,4-c]吡咯衍生物及其用途 |
| PT3619199T (pt) | 2017-05-03 | 2021-10-01 | Idorsia Pharmaceuticals Ltd | Preparação de derivados de ácido 2-([1,2,3]triazol-2-il)- benzoico |
| WO2019002344A1 (en) | 2017-06-29 | 2019-01-03 | Lonza Guangzhou Nansha Ltd. | PROCESS FOR THE PREPARATION OF ALPHA-METHYL-L-PROLINE |
| WO2020007964A1 (en) | 2018-07-05 | 2020-01-09 | Idorsia Pharmaceuticals Ltd | 2-(2-azabicyclo[3.1.0]hexan-1-yl)-1h-benzimidazole derivatives |
| WO2020007977A1 (en) | 2018-07-06 | 2020-01-09 | Idorsia Pharmaceuticals Ltd | 7-trifluoromethyl-[1,4]diazepan derivatives |
| CN108997308A (zh) * | 2018-07-09 | 2018-12-14 | 西藏大学 | 一种苯并咪唑类衍生物及其制备方法和应用 |
| WO2020099511A1 (en) | 2018-11-14 | 2020-05-22 | Idorsia Pharmaceuticals Ltd | Benzimidazole-2-methyl-morpholine derivatives |
| BR112022020924A2 (pt) | 2020-04-19 | 2023-02-14 | Idorsia Pharmaceuticals Ltd | Métodos de tratamento de um transtorno do sono, a sonolência diurna em um indivíduo, a insônia, e, daridorexante na forma de sal livre ou farmaceuticamente aceitável |
| 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 |
| 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 |
| TW202400149A (zh) | 2022-05-13 | 2024-01-01 | 瑞士商愛杜西亞製藥有限公司 | 經噻唑并芳基-甲基取代之環狀肼-n-甲醯胺衍生物 |
| CN116239575B (zh) * | 2023-03-13 | 2025-05-23 | 南开大学 | 一种联萘咪唑啉三齿手性配体的制法及其应用 |
| 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 |
| 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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