ES2617863T3 - Derivados de bencimidazol-prolina - Google Patents
Derivados de bencimidazol-prolina Download PDFInfo
- Publication number
- ES2617863T3 ES2617863T3 ES13744805T ES13744805T ES2617863T3 ES 2617863 T3 ES2617863 T3 ES 2617863T3 ES 13744805 T ES13744805 T ES 13744805T ES 13744805 T ES13744805 T ES 13744805T ES 2617863 T3 ES2617863 T3 ES 2617863T3
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- ES
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- Prior art keywords
- phenyl
- benzimidazol
- methanone
- alkyl
- alkoxy
- Prior art date
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- 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
-
- 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
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- 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)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Addiction (AREA)
- Hospice & Palliative Care (AREA)
- Anesthesiology (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Un compuesto de la fórmula (I)**Fórmula** en la que Ar1 representa - fenilo o un heteroarilo de 5 o 6 miembros, en el que dicho fenilo o heteroarilo de 5 o 6 miembros está independientemente mono-, di- o tri-sustituido; en el que - uno de dichos sustituyentes está unido en una posición orto al punto de unión de Ar1 al resto de la molécula; en la que dicho sustituyente es fenilo o un heteroarilo de 5 o 6 miembros, en el que dicho sustituyente fenilo o heteroarilo de 5 o 6 miembros está independientemente sin sustituir, mono-, di- o trisustituido, en el que los sustituyentes se seleccionan de manera independiente de alquilo (C1-4), alcoxi (C1-4), halógeno, ciano, fluoroalquilo (C1-3) y fluoroalcoxi (C1-3); o dicho sustituyente orto es benzo[1,3]dioxolilo, o 2-(3-metoxi-fenil)-etinilo; - y el otro de dichos sustituyentes, en caso de estar presente, se selecciona/n de alquilo (C1-4); alcoxi (C1-4); cicloalquilo (C3-6); halógeno; ciano; fluoroalquilo (C1-3); fluoroalcoxi (C1-3); -NR10R11, en el que R10 y R11 independientemente representan hidrógeno o alquilo (C1-4) o R10 y R11 junto con el nitrógeno al cual están unidos forman un anillo de pirrolidina, piridinilo sin sustituir y fenilo que está sin sustituir o mono- o di-sustituido, en el que los sustituyentes se seleccionan de manera independiente de alquilo (C1-4), alcoxi (C1-4), ciano y halógeno; uno de R2 y R3 representa hidrógeno y el otro representa hidrógeno o alquilo (C1-4); y uno de R4a y R4b representa hidrógeno y el otro representa hidrógeno, alcoxi (C1-4), o halógeno; o R4a y R4b juntos representan un grupo H2C>=; o ambos R4a y R4b representan flúor; en el que, en caso de que R3 sea diferente a hidrógeno, ambos R4a y R4b representan hidrógeno; R1 representa hidrógeno, alquilo (C1-4), cicloalquilo (C3-6)-(CH2)-, fluoroalquilo (C2-3), o alcoxi (C1-4)-alquilo (C2-4); y (R5)n representa uno a tres sustituyentes opcionales independientemente seleccionado de alquilo (C1-4), alcoxi (C1-4), halógeno, alquil (C1-4)-tio-, fluoroalquilo (C1-3), fluoroalcoxi (C1-3), fluoroalquil (C1-3)-tio-, hidroxi-alquilo (C1- 4)-, alcoxi (C1-4)-carbonilo-, nitro, hidroxi, y ciano; o (R5)n representa un grupo -O-CH2-CH2-O-; o (R5)n representa un grupo fenilo fusionado que, junto con el resto bencimidazol al cual se fusiona, forma un grupo 1H-nafto[2,3- d]imidazol-2-ilo; con la excepción de [2-(1H-bencimidazol-2-il)-1-pirrolidinil][2-(1H-pirazol-1-il)fenil]-metanona; [2-(1H-bencimidazol-2-il)-1-pirrolidinil][5-(2,5-dimetil-1H-pirrol-1-il)-1-metil-1H-pirazol-4-il]-metanona; [2-(1H-bencimidazol-2-il)-1-pirrolidinil][1,1'-bifenil]-2-il-metanona; [2-(6-metil-1H-bencimidazol-2-il)-pirrolidin-1-il][3-fenil-isoxazol-4-il]-metanona; [2-(1H-imidazol-2-il)fenil][2-(6-metil-1H-bencimidazol-2-il)-pirrolidin-1-il]-metanona; [2-(6-metil-1H-bencimidazol-2-il)-pirrolidin-1-il][3-(tien-2-il)-1H-pirazol-4-il]-metanona; [2-(6-metil-1H-bencimidazol-2-il)-pirrolidin-1-il][3-fenil-1H-pirazol-4-il]-metanona; [2-(1H-bencimidazol-2-il)-pirrolidin-1-il][3-ciclopropil-1-fenil-1H-pirazol-5-il]-metanona; y [2-(1H-bencimidazol-2-il)-pirrolidin-1-il][1-(2-fluorofenil)-5-(1H-pirrol-1-il)-1H-pirazol-4-il]-metanona; o una sal farmacéuticamente aceptable del mismo.
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 (1)
| Publication Number | Publication Date |
|---|---|
| ES2617863T3 true ES2617863T3 (es) | 2017-06-20 |
Family
ID=48914370
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES13744805T Active ES2617863T3 (es) | 2012-06-04 | 2013-06-03 | Derivados de bencimidazol-prolina |
Country Status (33)
| Country | Link |
|---|---|
| US (3) | US9732075B2 (es) |
| EP (1) | EP2855453B1 (es) |
| JP (1) | JP5814491B2 (es) |
| KR (3) | KR101689093B1 (es) |
| CN (1) | CN104334544B (es) |
| AR (1) | AR091257A1 (es) |
| AU (1) | AU2013273222B2 (es) |
| BR (1) | BR112014030173B1 (es) |
| CA (1) | CA2873341C (es) |
| CL (1) | CL2014003294A1 (es) |
| CY (1) | CY1118735T1 (es) |
| DK (1) | DK2855453T3 (es) |
| EA (2) | EA029899B1 (es) |
| ES (1) | ES2617863T3 (es) |
| FR (1) | FR22C1047I2 (es) |
| HK (1) | HK1208449A1 (es) |
| HR (1) | HRP20170351T1 (es) |
| HU (2) | HUE031753T2 (es) |
| IL (1) | IL236024A (es) |
| LT (2) | LT2855453T (es) |
| MX (1) | MX354102B (es) |
| MY (1) | MY169986A (es) |
| NL (1) | NL301197I2 (es) |
| NO (1) | NO2022044I1 (es) |
| NZ (1) | NZ703448A (es) |
| PH (1) | PH12014502540A1 (es) |
| PL (1) | PL2855453T3 (es) |
| PT (1) | PT2855453T (es) |
| SG (2) | SG11201408004SA (es) |
| SI (1) | SI2855453T1 (es) |
| TW (2) | TWI510481B (es) |
| WO (1) | WO2013182972A1 (es) |
| ZA (1) | ZA201409422B (es) |
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| CN104334544B (zh) | 2012-06-04 | 2016-10-19 | 埃科特莱茵药品有限公司 | 苯并咪唑脯氨酸衍生物 |
| EA201500399A1 (ru) | 2012-10-10 | 2015-09-30 | Актелион Фармасьютиклз Лтд. | Антагонисты рецептора орексина, которые представляют собой производные [орто-би-(гетеро)арил]-[2-(мета-би-(гетеро)арил)пирролидин-1-ил]метанона |
| CA2902135A1 (en) | 2013-03-12 | 2014-09-18 | Actelion Pharmaceuticals Ltd | Azetidine amide derivatives as orexin receptor antagonists |
| EA030067B1 (ru) | 2013-07-22 | 2018-06-29 | Идорсиа Фармасьютиклз Лтд | Производные 1-(пиперазин-1-ил)-2-([1,2,4]триазол-1-ил)этанона |
| 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 |
| TWI664177B (zh) | 2013-12-03 | 2019-07-01 | 瑞士商愛杜西亞製藥有限公司 | 晶形 |
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| 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 |
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| 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 |
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