RU2010119458A - 1,3,5-тризамещенное производное триазола - Google Patents
1,3,5-тризамещенное производное триазола Download PDFInfo
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- RU2010119458A RU2010119458A RU2010119458/04A RU2010119458A RU2010119458A RU 2010119458 A RU2010119458 A RU 2010119458A RU 2010119458/04 A RU2010119458/04 A RU 2010119458/04A RU 2010119458 A RU2010119458 A RU 2010119458A RU 2010119458 A RU2010119458 A RU 2010119458A
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- compound
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- nicotinic receptor
- diseases
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- -1 1,3,5-TRI-SUBSTITUTED TRIAZOLE Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 6
- 102000019315 Nicotinic acetylcholine receptors Human genes 0.000 claims abstract 4
- 108050006807 Nicotinic acetylcholine receptors Proteins 0.000 claims abstract 4
- 230000009286 beneficial effect Effects 0.000 claims abstract 4
- 201000010099 disease Diseases 0.000 claims abstract 4
- 239000003937 drug carrier Substances 0.000 claims abstract 4
- 238000004519 manufacturing process Methods 0.000 claims abstract 4
- 229940122656 Alpha-7 nicotinic receptor agonist Drugs 0.000 claims abstract 2
- 239000007818 Grignard reagent Substances 0.000 claims abstract 2
- 201000006347 Intellectual Disability Diseases 0.000 claims abstract 2
- 239000004480 active ingredient Substances 0.000 claims abstract 2
- 230000003197 catalytic effect Effects 0.000 claims abstract 2
- 208000035475 disorder Diseases 0.000 claims abstract 2
- 239000003814 drug Substances 0.000 claims abstract 2
- 150000004795 grignard reagents Chemical class 0.000 claims abstract 2
- 239000008240 homogeneous mixture Substances 0.000 claims abstract 2
- 208000027866 inflammatory disease Diseases 0.000 claims abstract 2
- AQBLLJNPHDIAPN-LNTINUHCSA-K iron(3+);(z)-4-oxopent-2-en-2-olate Chemical compound [Fe+3].C\C([O-])=C\C(C)=O.C\C([O-])=C\C(C)=O.C\C([O-])=C\C(C)=O AQBLLJNPHDIAPN-LNTINUHCSA-K 0.000 claims abstract 2
- NXPHGHWWQRMDIA-UHFFFAOYSA-M magnesium;carbanide;bromide Chemical compound [CH3-].[Mg+2].[Br-] NXPHGHWWQRMDIA-UHFFFAOYSA-M 0.000 claims abstract 2
- 238000000034 method Methods 0.000 claims abstract 2
- 239000000203 mixture Substances 0.000 claims abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 2
- 230000002265 prevention Effects 0.000 claims abstract 2
- 208000020016 psychiatric disease Diseases 0.000 claims abstract 2
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 239000012453 solvate Substances 0.000 claims abstract 2
- 239000002904 solvent Substances 0.000 claims abstract 2
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
- A61P25/10—Antiepileptics; Anticonvulsants for petit-mal
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/22—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
-
- 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
- A61P25/34—Tobacco-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
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- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Medicinal Chemistry (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Addiction (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
1. Соединение формулы (I) !! или его фармацевтически приемлемая соль, или гидрат, или сольват. ! 2. Применение соединения для производства лекарственного средства для предотвращения или лечения, или профилактики психических расстройств, расстройств или заболеваний нарушения интеллекта, воспалительных заболеваний или состояний, при которых является благоприятной модуляция α7 никотинового рецептора, где соединение является соединением по п.1. ! 3. Фармацевтическая композиция, содержащая фармацевтически приемлемый носитель и, в качестве активного компонента терапевтически эффективное количество соединения по п.1. ! 4. Способ получения композиции по п.3, отличающийся тем, что фармацевтически приемлемый носитель смешивается до получения однородной смеси с терапевтически эффективным количеством соединения по п.1. ! 5. Продукт, содержащий ! (a) соединение по п.1 и ! (b) агонист α7 никотинового рецептора в качестве комбинированного препарата для одновременного, раздельного или последовательного применения при предотвращении или лечении заболеваний, при которых является благоприятной модуляция α7 никотинового рецептора. ! 6. Способ получения соединения по п.1, включающий стадию взаимодействия промежуточного соединения формулы (VI) с избытком реактива Гриньяра MeMgBr ! ! в присутствии каталитических количеств ацетилацетоната железа(III) в системе растворителей, состоящей из 75-85% ТГФ и 15-25% NМP по объему, в диапазоне температур от 0°C до 50°C.
Claims (6)
1. Соединение формулы (I)
или его фармацевтически приемлемая соль, или гидрат, или сольват.
2. Применение соединения для производства лекарственного средства для предотвращения или лечения, или профилактики психических расстройств, расстройств или заболеваний нарушения интеллекта, воспалительных заболеваний или состояний, при которых является благоприятной модуляция α7 никотинового рецептора, где соединение является соединением по п.1.
3. Фармацевтическая композиция, содержащая фармацевтически приемлемый носитель и, в качестве активного компонента терапевтически эффективное количество соединения по п.1.
4. Способ получения композиции по п.3, отличающийся тем, что фармацевтически приемлемый носитель смешивается до получения однородной смеси с терапевтически эффективным количеством соединения по п.1.
5. Продукт, содержащий
(a) соединение по п.1 и
(b) агонист α7 никотинового рецептора в качестве комбинированного препарата для одновременного, раздельного или последовательного применения при предотвращении или лечении заболеваний, при которых является благоприятной модуляция α7 никотинового рецептора.
6. Способ получения соединения по п.1, включающий стадию взаимодействия промежуточного соединения формулы (VI) с избытком реактива Гриньяра MeMgBr
в присутствии каталитических количеств ацетилацетоната железа(III) в системе растворителей, состоящей из 75-85% ТГФ и 15-25% NМP по объему, в диапазоне температур от 0°C до 50°C.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07118822.1 | 2007-10-18 | ||
| EP07118822 | 2007-10-18 | ||
| PCT/EP2008/063844 WO2009050185A1 (en) | 2007-10-18 | 2008-10-15 | 1,3,5-trisubstituted triazole derivative |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2010119458A true RU2010119458A (ru) | 2011-11-27 |
| RU2476433C2 RU2476433C2 (ru) | 2013-02-27 |
Family
ID=39047591
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2010119458/04A RU2476433C2 (ru) | 2007-10-18 | 2008-10-15 | 1,3,5-тризамещенное производное триазола |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8404851B2 (ru) |
| EP (1) | EP2205594B1 (ru) |
| JP (1) | JP2011500624A (ru) |
| CN (1) | CN101827839B (ru) |
| AR (1) | AR068919A1 (ru) |
| AT (1) | ATE522523T1 (ru) |
| AU (1) | AU2008313775B2 (ru) |
| CA (1) | CA2697982C (ru) |
| CL (1) | CL2008003067A1 (ru) |
| ES (1) | ES2371863T3 (ru) |
| IL (1) | IL205102A (ru) |
| JO (1) | JO2784B1 (ru) |
| MX (1) | MX2010004176A (ru) |
| PA (1) | PA8799901A1 (ru) |
| PE (1) | PE20091080A1 (ru) |
| RU (1) | RU2476433C2 (ru) |
| TW (1) | TW200934491A (ru) |
| WO (1) | WO2009050185A1 (ru) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ576570A (en) * | 2006-10-19 | 2010-11-26 | Takeda Pharmaceutical | 7-sulfonylamino-2-thiazol and 2-thiadiazol -indole compounds |
| CA2697974C (en) * | 2007-10-18 | 2015-06-30 | Janssen Pharmaceutica Nv | Trisubstituted 1,2,4-triazoles |
| KR101564303B1 (ko) * | 2008-03-19 | 2015-11-06 | 얀센 파마슈티카 엔.브이. | 니코틴성 아세틸콜린 수용체 조절제로서의 삼치환된 1,2,4-트리아졸 |
| WO2009135944A1 (en) * | 2008-05-09 | 2009-11-12 | Janssen Pharmaceutica Nv | Trisubstituted pyrazoles as acetylcholine receptor modulators |
| CN103443092B (zh) | 2011-02-03 | 2015-11-25 | 鲁平有限公司 | 用作α7胆碱受体调节剂的吡咯衍生物 |
| CU24177B1 (es) | 2011-02-23 | 2016-04-25 | Lupin Ltd | Derivados de heteroarilo como moduladores de nachr alfa 7 |
| CA2824350C (en) | 2011-02-25 | 2019-07-02 | Janssen Pharmaceutica Nv | (pyridin-4-yl)benzylamides as allosteric modulators of alpha 7 nachr |
| JP2014509641A (ja) | 2011-03-31 | 2014-04-21 | ルピン・リミテッド | アルツハイマー病やパーキンソン病などの神経変性疾患の治療に用いられるニコチン性アセチルコリン受容体モジュレータとしてのピロール誘導体 |
| WO2013005153A1 (en) | 2011-07-05 | 2013-01-10 | Lupin Limited | Biaryl derivatives as nachr modulators |
| EP2822946A1 (en) | 2012-03-06 | 2015-01-14 | Lupin Limited | Thiazole derivatives as alpha 7 nachr modulators |
| EP2945936A1 (en) | 2012-11-12 | 2015-11-25 | Lupin Limited | Thiazole derivatives as alpha 7 nachr modulators |
| WO2014111839A1 (en) | 2013-01-16 | 2014-07-24 | Lupin Limited | Pyrrole derivatives as alpha 7 nachr modulators |
| CA2892682A1 (en) | 2013-03-13 | 2014-09-18 | Lupin Limited | Pyrrole derivatives as alpha 7 nachr modulators |
| TW201446243A (zh) | 2013-06-03 | 2014-12-16 | Lupin Ltd | 4-(5-(4-氯苯基)-2-(2-環丙基乙醯基)-1,4-二甲基-1氫-吡咯-3-基)苯磺醯胺作為α7尼古丁乙醯膽鹼受體調節劑 |
| AU2014282886A1 (en) | 2013-06-17 | 2015-12-17 | Lupin Limited | Pyrrole derivatives as alpha 7 nAChR modulators |
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| ES2392795T3 (es) | 2008-04-17 | 2012-12-13 | Proximagen Limited | Indoles como moduladores del receptor nicotínico de acetilcolina de subtipo alfa-7 |
| WO2009135944A1 (en) * | 2008-05-09 | 2009-11-12 | Janssen Pharmaceutica Nv | Trisubstituted pyrazoles as acetylcholine receptor modulators |
| CN102574832B (zh) * | 2009-09-17 | 2014-09-24 | 詹森药业有限公司 | 取代的n-苯基-1-(4-吡啶基)-1h-吡唑-3-胺 |
| JO3078B1 (ar) * | 2009-11-27 | 2017-03-15 | Janssen Pharmaceutica Nv | مورفولينوثيازولات بصفتها منظمات الوستيرية نوع الفا 7 موجبة |
| CA2824350C (en) | 2011-02-25 | 2019-07-02 | Janssen Pharmaceutica Nv | (pyridin-4-yl)benzylamides as allosteric modulators of alpha 7 nachr |
-
2008
- 2008-09-15 JO JO2008412A patent/JO2784B1/en active
- 2008-10-15 RU RU2010119458/04A patent/RU2476433C2/ru active
- 2008-10-15 AU AU2008313775A patent/AU2008313775B2/en not_active Ceased
- 2008-10-15 CN CN2008801119538A patent/CN101827839B/zh not_active Expired - Fee Related
- 2008-10-15 CA CA2697982A patent/CA2697982C/en not_active Expired - Fee Related
- 2008-10-15 EP EP08805280A patent/EP2205594B1/en active Active
- 2008-10-15 AT AT08805280T patent/ATE522523T1/de not_active IP Right Cessation
- 2008-10-15 MX MX2010004176A patent/MX2010004176A/es active IP Right Grant
- 2008-10-15 WO PCT/EP2008/063844 patent/WO2009050185A1/en active Application Filing
- 2008-10-15 JP JP2010529360A patent/JP2011500624A/ja active Pending
- 2008-10-15 US US12/738,725 patent/US8404851B2/en active Active
- 2008-10-15 ES ES08805280T patent/ES2371863T3/es active Active
- 2008-10-16 CL CL2008003067A patent/CL2008003067A1/es unknown
- 2008-10-17 PA PA20088799901A patent/PA8799901A1/es unknown
- 2008-10-17 TW TW097139807A patent/TW200934491A/zh unknown
- 2008-10-17 PE PE2008001789A patent/PE20091080A1/es active IP Right Grant
- 2008-10-17 AR ARP080104545A patent/AR068919A1/es not_active Application Discontinuation
-
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- 2010-04-15 IL IL205102A patent/IL205102A/en active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| CA2697982A1 (en) | 2009-04-23 |
| IL205102A (en) | 2015-04-30 |
| IL205102A0 (en) | 2010-11-30 |
| CN101827839A (zh) | 2010-09-08 |
| AR068919A1 (es) | 2009-12-16 |
| PE20091080A1 (es) | 2009-08-03 |
| ATE522523T1 (de) | 2011-09-15 |
| CA2697982C (en) | 2015-09-22 |
| WO2009050185A1 (en) | 2009-04-23 |
| TW200934491A (en) | 2009-08-16 |
| US20100240707A1 (en) | 2010-09-23 |
| RU2476433C2 (ru) | 2013-02-27 |
| US8404851B2 (en) | 2013-03-26 |
| PA8799901A1 (es) | 2009-05-15 |
| JO2784B1 (en) | 2014-03-15 |
| JP2011500624A (ja) | 2011-01-06 |
| MX2010004176A (es) | 2010-05-03 |
| EP2205594B1 (en) | 2011-08-31 |
| ES2371863T3 (es) | 2012-01-10 |
| CN101827839B (zh) | 2012-10-24 |
| CL2008003067A1 (es) | 2009-11-27 |
| AU2008313775A1 (en) | 2009-04-23 |
| EP2205594A1 (en) | 2010-07-14 |
| AU2008313775B2 (en) | 2012-12-13 |
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