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 thereof

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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
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UA
Ukraine
Prior art keywords
serotonin
optionally substituted
novel
pyrazolo
pyrimidines
Prior art date
Application number
UAA201009958A
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English (en)
Ukrainian (uk)
Inventor
Андрей Александрович Иващенко
Александр Васильевич Иващенко
Николай Филиппович Савчук
Original Assignee
Общество С Ограниченной Ответственностью "Инновационная Фармацевтика"
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Application filed by Общество С Ограниченной Ответственностью "Инновационная Фармацевтика" filed Critical Общество С Ограниченной Ответственностью "Инновационная Фармацевтика"
Publication of UA102087C2 publication Critical patent/UA102087C2/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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

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  • 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.
UAA201009958A 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 UA102087C2 (en)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

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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