UA102087C2 - 3-sulfonyl-pyrazolo[1,5-a] pyrimidines/antagonists of serotonin 5-ht6receptors, methods for the production and the use thereof - Google Patents
3-sulfonyl-pyrazolo[1,5-a] pyrimidines/antagonists of serotonin 5-ht6receptors, methods for the production and the use thereofInfo
- Publication number
- UA102087C2 UA102087C2 UAA201009958A UAA201009958A UA102087C2 UA 102087 C2 UA102087 C2 UA 102087C2 UA A201009958 A UAA201009958 A UA A201009958A UA A201009958 A UAA201009958 A UA A201009958A UA 102087 C2 UA102087 C2 UA 102087C2
- Authority
- UA
- Ukraine
- Prior art keywords
- serotonin
- optionally substituted
- novel
- pyrazolo
- pyrimidines
- Prior art date
Links
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 title abstract 6
- 229940076279 serotonin Drugs 0.000 title abstract 3
- 239000005557 antagonist Substances 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 150000003230 pyrimidines Chemical class 0.000 title abstract 2
- 108091005435 5-HT6 receptors Proteins 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 230000004913 activation Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000008506 pathogenesis Effects 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
- -1 sulphonyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
-
- 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
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Psychiatry (AREA)
- Obesity (AREA)
- Psychology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Данное изобретение касается 3-арилсульфонил-пиразоло[1,5-а]пиримидинов общей формулы 1 или их фармацевтически приемлемых солей и/или гидратов, антагонистов серотониновых 5-НТрецепторов, лекарственных субстанций, фармацевтических композиций, лекарственных препаратов и способов их получения и применения для лечения и предупреждения патологических состояний и заболеваний ЦНС, патогенез которых связан с нарушением активации серотониновых 5-НТрецепторов.В соединениях общей формулы 1(1)Ar является необязательно замещенным арилом или необязательно замещенным гетероциклилом; R, Ri Rнезависимо друг от друга являются атомом водорода, C-Салкилом или фенилом; Rявляется атомом водорода, необязательно замещенным С-Салкилом, замещенной гидроксильной группой или замещенной сульфонильной группой.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| RU2008102154/04A RU2369600C1 (ru) | 2008-01-24 | 2008-01-24 | ЗАМЕЩЕННЫЕ 4-СУЛЬФОНИЛ-ПИРАЗОЛЫ И 3-СУЛЬФОНИЛ-ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ5-HT6 РЕЦЕПТОРОВ, АКТИВНЫЙ КОМПОНЕНТ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ЛЕКАРСТВЕННОЕ СРЕДСТВО И СПОСОБЫ ИХ ПОЛУЧЕНИЯ |
| PCT/IB2009/050270 WO2009093206A2 (ru) | 2008-01-24 | 2009-01-23 | 3-CУЛЬФOHИЛ-ПИPAЗOЛO[1,5-a]ПИPИMИДИHЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA102087C2 true UA102087C2 (en) | 2013-06-10 |
Family
ID=40901496
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UAA201009961A UA100138C2 (ru) | 2008-01-24 | 2009-01-23 | ЗАМЕЩЕННЫЕ ЦИКЛОАЛКАНО[e АБО d]ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-НТ6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ |
| UAA201009960A UA101643C2 (en) | 2008-01-24 | 2009-01-23 | 2-ALKYLAMINO-3-ARYLSULFONYL-CYCLOALCANO [e OR d] PYRAZOLO[1,5-A]PYRIMIDINES AS ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, PROCESS FOR THE PREPARATION AND USE THEREOF |
| UAA201009959A UA100137C2 (en) | 2008-01-24 | 2009-01-23 | SUBSTITUTED 2-AMINO-3-SULFONYL-PYRAZOLO[1,5-a]PYRIMIDINES AS ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS AND USE THEREOF |
| UAA201009958A UA102087C2 (en) | 2008-01-24 | 2009-01-23 | 3-sulfonyl-pyrazolo[1,5-a] pyrimidines/antagonists of serotonin 5-ht6receptors, methods for the production and the use thereof |
Family Applications Before (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UAA201009961A UA100138C2 (ru) | 2008-01-24 | 2009-01-23 | ЗАМЕЩЕННЫЕ ЦИКЛОАЛКАНО[e АБО d]ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-НТ6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ |
| UAA201009960A UA101643C2 (en) | 2008-01-24 | 2009-01-23 | 2-ALKYLAMINO-3-ARYLSULFONYL-CYCLOALCANO [e OR d] PYRAZOLO[1,5-A]PYRIMIDINES AS ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, PROCESS FOR THE PREPARATION AND USE THEREOF |
| UAA201009959A UA100137C2 (en) | 2008-01-24 | 2009-01-23 | SUBSTITUTED 2-AMINO-3-SULFONYL-PYRAZOLO[1,5-a]PYRIMIDINES AS ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS AND USE THEREOF |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US8552005B2 (ru) |
| EP (1) | EP2248815B1 (ru) |
| JP (1) | JP5690594B2 (ru) |
| KR (1) | KR101526930B1 (ru) |
| CA (1) | CA2749742C (ru) |
| DK (1) | DK2248815T3 (ru) |
| EA (1) | EA017817B1 (ru) |
| RU (1) | RU2369600C1 (ru) |
| UA (4) | UA100138C2 (ru) |
| WO (1) | WO2009093206A2 (ru) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20110069148A (ko) * | 2008-10-06 | 2011-06-22 | 알라 캠, 엘엘씨 | 치환된 3-아릴설포닐-피라졸로[1,5-a]피리미딘, 세로토닌 5-HT6 수용체의 길항제, 물질의 제조방법 및 이의 용도 |
| US10864191B2 (en) | 2016-05-11 | 2020-12-15 | H. Lundbeck A/S | 5-HT6 receptor antagonists for use in the treatment of Alzheimer's disease with apathy as comorbidity |
| WO2018050825A1 (de) * | 2016-09-19 | 2018-03-22 | Bayer Cropscience Aktiengesellschaft | Pyrazolo[1,5-a]pyridin- derivative und ihre verwendung als schädlingsbekämpfungsmittel |
| MX385719B (es) | 2017-05-24 | 2025-03-18 | H Lundbeck As | Combinacion de un antagonista del receptor 5-ht6 y un inhibidor de acetilcolinesterasa para su uso en el tratamiento de la enfermedad de alzheimer en una subpoblacion de pacientes portadores de alelos apoe4 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8531485D0 (en) * | 1985-12-20 | 1986-02-05 | May & Baker Ltd | Compositions of matter |
| JPH09143181A (ja) * | 1995-09-22 | 1997-06-03 | Takeda Chem Ind Ltd | 新規トリアゾール系化合物、その製造法、中間体および農薬 |
| AU7001396A (en) * | 1995-09-22 | 1997-04-09 | Takeda Chemical Industries Ltd. | Triazole compounds, their production and use |
| US6194410B1 (en) * | 1998-03-11 | 2001-02-27 | Hoffman-La Roche Inc. | Pyrazolopyrimidine and pyrazolines and process for preparation thereof |
| EP1212304A2 (en) * | 1999-08-27 | 2002-06-12 | Eli Lilly And Company | Hypoglycemic sulfonyl pyrazolones and pyrazolines |
| DE60130924T2 (de) * | 2000-12-28 | 2008-07-17 | Ono Pharmaceutical Co. Ltd. | Cyclopentaädüpyrazoloä1,5-aüpyrimidin-verbindung als crf-rezeptor antagonist |
| EP1368355B1 (de) * | 2001-03-14 | 2006-06-07 | Grünenthal GmbH | Substituierte pyrazolo- und thiazolopyrimidine als analgetika |
| EP1465872A1 (en) | 2001-12-28 | 2004-10-13 | Bayer Pharmaceuticals Corporation | 4-sulfide/sulfoxide/sulfonyl-1h-pyrazolyl derivative compounds, for use in diseases associated with the 5-ht2c receptor |
| JP2005527542A (ja) * | 2002-03-27 | 2005-09-15 | グラクソ グループ リミテッド | キノリンおよびアザインドール誘導体およびその5−ht6リガンドとしての使用 |
| JP2004277337A (ja) * | 2003-03-14 | 2004-10-07 | Sumitomo Pharmaceut Co Ltd | ピラゾロ[1,5−a]ピリミジン誘導体 |
| AU2006305104B2 (en) * | 2005-10-21 | 2009-10-22 | Mitsubishi Tanabe Pharma Corporation | Pyrazolo[1,5-a]pyrimidine compounds as cannabinoid receptor antagonists |
| JP4847275B2 (ja) * | 2005-10-21 | 2011-12-28 | 田辺三菱製薬株式会社 | ピラゾロ[1,5−a]ピリミジン化合物 |
| CA2709784A1 (en) * | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
-
2008
- 2008-01-24 RU RU2008102154/04A patent/RU2369600C1/ru not_active IP Right Cessation
-
2009
- 2009-01-23 EP EP09703835.0A patent/EP2248815B1/en not_active Not-in-force
- 2009-01-23 KR KR1020107018828A patent/KR101526930B1/ko not_active Expired - Fee Related
- 2009-01-23 UA UAA201009961A patent/UA100138C2/ru unknown
- 2009-01-23 EA EA201001179A patent/EA017817B1/ru not_active IP Right Cessation
- 2009-01-23 WO PCT/IB2009/050270 patent/WO2009093206A2/ru not_active Ceased
- 2009-01-23 DK DK09703835.0T patent/DK2248815T3/en active
- 2009-01-23 UA UAA201009960A patent/UA101643C2/ru unknown
- 2009-01-23 US US12/812,728 patent/US8552005B2/en active Active
- 2009-01-23 UA UAA201009959A patent/UA100137C2/ru unknown
- 2009-01-23 CA CA2749742A patent/CA2749742C/en not_active Expired - Fee Related
- 2009-01-23 JP JP2010543609A patent/JP5690594B2/ja not_active Expired - Fee Related
- 2009-01-23 UA UAA201009958A patent/UA102087C2/ru unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP2248815A4 (en) | 2012-02-15 |
| EP2248815A2 (en) | 2010-11-10 |
| UA101643C2 (en) | 2013-04-25 |
| EP2248815B1 (en) | 2014-09-24 |
| KR20100137428A (ko) | 2010-12-30 |
| EA201001179A1 (ru) | 2011-02-28 |
| CA2749742C (en) | 2016-04-26 |
| US20100331347A1 (en) | 2010-12-30 |
| RU2369600C1 (ru) | 2009-10-10 |
| CA2749742A1 (en) | 2009-07-30 |
| WO2009093206A2 (ru) | 2009-07-30 |
| KR101526930B1 (ko) | 2015-06-08 |
| JP2011510061A (ja) | 2011-03-31 |
| EA017817B1 (ru) | 2013-03-29 |
| RU2008102154A (ru) | 2009-07-27 |
| UA100138C2 (ru) | 2012-11-26 |
| UA100137C2 (en) | 2012-11-26 |
| US8552005B2 (en) | 2013-10-08 |
| WO2009093206A3 (ru) | 2009-10-29 |
| JP5690594B2 (ja) | 2015-03-25 |
| DK2248815T3 (en) | 2014-11-17 |
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