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WO2009093208A3 - ЗАМЕЩЕННЫЕ 2-AMИHO-3-CУЛЬФOHИЛ-ПИPAЗOЛO[1,5-a]ПИPИMИДИHЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ - Google Patents

ЗАМЕЩЕННЫЕ 2-AMИHO-3-CУЛЬФOHИЛ-ПИPAЗOЛO[1,5-a]ПИPИMИДИHЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ Download PDF

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Publication number
WO2009093208A3
WO2009093208A3 PCT/IB2009/050272 IB2009050272W WO2009093208A3 WO 2009093208 A3 WO2009093208 A3 WO 2009093208A3 IB 2009050272 W IB2009050272 W IB 2009050272W WO 2009093208 A3 WO2009093208 A3 WO 2009093208A3
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WIPO (PCT)
Prior art keywords
optionally substituted
serotonin
receptors
pyrazolo
pyrimidines
Prior art date
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Ceased
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PCT/IB2009/050272
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English (en)
French (fr)
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WO2009093208A2 (ru
Inventor
Андрей Александрович Иващенко
Александр Васильевич Иващенко
Николай Филиппович Савчук
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Alla Chem LLC
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Alla Chem LLC
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Publication date
Priority claimed from RU2008102154/04A external-priority patent/RU2369600C1/ru
Priority claimed from RU2008117846/04A external-priority patent/RU2376291C1/ru
Application filed by Alla Chem LLC filed Critical Alla Chem LLC
Priority to US12/812,733 priority Critical patent/US8309559B2/en
Priority to EP09704333.5A priority patent/EP2248817B1/en
Priority to EA201001180A priority patent/EA017968B1/ru
Priority to JP2010543610A priority patent/JP5575663B2/ja
Publication of WO2009093208A2 publication Critical patent/WO2009093208A2/ru
Publication of WO2009093208A3 publication Critical patent/WO2009093208A3/ru
Anticipated expiration legal-status Critical
Priority to US13/573,818 priority patent/US8829009B2/en
Ceased legal-status Critical Current

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    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A—HUMAN NECESSITIES
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Abstract

Данное изобретение относится к новым замещенным 2-aминo-З-cyльфoнил- пиpaзoлo[1,5-a]пиpимидинaм, к новым антагонистам серотониновых 5-HT6 рецепторов, к новым лекарственным субстанциям, фармацевтическим композициям, лекарственным препаратам, способам их получения, а также к способу лечения и предупреждения развития различных заболеваний ЦНС, патогенез которых связан с нарушением моноаминоэргических сигнальных путей, в частности гипер- или гипоактивацией серотониновых 5-HT6 рецепторов. В общей формуле 1 Ar представляет собой необязательно замещенный арил или необязательно замещенный гетероциклил; R1 и R3 независимо друг от друга представляют собой C1-C3 алкил или фенил; R2 представляет собой атом водорода или C1-C3 алкил; R4 1, R4 2 независимо друг от друга, представляют собой атом водорода, необязательно замещенный C1-C3 алкил или необязательно замещенный фенил, или R4 1 и R4 2 вместе с атомом азота, с которым они связаны, образуют необязательно замещенный гетероцикл.
PCT/IB2009/050272 2008-01-24 2009-01-23 ЗАМЕЩЕННЫЕ 2-AMИHO-3-CУЛЬФOHИЛ-ПИPAЗOЛO[1,5-a]ПИPИMИДИHЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ Ceased WO2009093208A2 (ru)

Priority Applications (5)

Application Number Priority Date Filing Date Title
US12/812,733 US8309559B2 (en) 2008-01-24 2009-01-23 (EN) substituted 2-amino-3-sulfonyl-pyrazolo[1,5-A] pyrimidines/antagonists of serotonin 5-HT6 receptors, methods for the production and the use thereof
EP09704333.5A EP2248817B1 (en) 2008-01-24 2009-01-23 Substituted 2-amino-3-sulfonyl-pyrazolo[1,5-a] pyrimidines/antagonists of serotonin 5-ht6 receptors, methods for the production and the use thereof
EA201001180A EA017968B1 (ru) 2008-01-24 2009-01-23 ЗАМЕЩЕННЫЕ 2-АМИНО-3-СУЛЬФОНИЛПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ-АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-НТРЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
JP2010543610A JP5575663B2 (ja) 2008-01-24 2009-01-23 置換された２−アミノ−３−（スルホニル）ピラゾロ［１，５−ａ］ピリミジン−セロトニン５−ＨＴ６受容体アンタゴニスト、その調製のための方法及び使用
US13/573,818 US8829009B2 (en) 2008-01-24 2012-10-09 Substituted 2-amino-3-(sulfonyl)pyrazolo[1,5-a]pyrimidines - serotonin 5-HT6 receptor antagonists, method for use thereof

Applications Claiming Priority (4)

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
RU2008102154 2008-01-24
RU2008117846/04A RU2376291C1 (ru) 2008-05-07 2008-05-07 ЗАМЕЩЕННЫЕ 3,5-ДИАМИНО-4-СУЛЬФОНИЛ-ПИРАЗОЛЫ И 2-АМИНО-3-СУЛЬФОНИЛ-ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
RU2008117846 2008-05-07

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US12/812,733 A-371-Of-International US8309559B2 (en) 2008-01-24 2009-01-23 (EN) substituted 2-amino-3-sulfonyl-pyrazolo[1,5-A] pyrimidines/antagonists of serotonin 5-HT6 receptors, methods for the production and the use thereof
US13/573,818 Division US8829009B2 (en) 2008-01-24 2012-10-09 Substituted 2-amino-3-(sulfonyl)pyrazolo[1,5-a]pyrimidines - serotonin 5-HT6 receptor antagonists, method for use thereof

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WO2009093208A2 WO2009093208A2 (ru) 2009-07-30
WO2009093208A3 true WO2009093208A3 (ru) 2009-10-29

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PCT/IB2009/050272 Ceased WO2009093208A2 (ru) 2008-01-24 2009-01-23 ЗАМЕЩЕННЫЕ 2-AMИHO-3-CУЛЬФOHИЛ-ПИPAЗOЛO[1,5-a]ПИPИMИДИHЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ

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US (2) US8309559B2 (ru)
EP (1) EP2248817B1 (ru)
JP (1) JP5575663B2 (ru)
KR (1) KR20110000623A (ru)
EA (1) EA017968B1 (ru)
WO (1) WO2009093208A2 (ru)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2351756A4 (en) * 2008-10-06 2013-01-02 Ivashchenko Andrey Alexandrovich SUBSTITUTED 3-ARYLSULFONYL-PYRAZOLO [1,5-A] PYRIMIDINES, SEROTONIN-5-HT6 RECEPTOR ANTAGONISTS, AND METHOD FOR THEIR PREPARATION AND USE
RU2443697C1 (ru) * 2010-12-21 2012-02-27 Александр Васильевич Иващенко Замещенные метил-амины, антагонисты серотониновых 5-ht6 рецепторов, способы получения и применения
WO2013055386A2 (en) * 2011-10-03 2013-04-18 The University Of Utah Research Foundation Application of 5-ht6 receptor antagonists for the alleviation of cognitive deficits of down syndrome
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
JP7165126B2 (ja) * 2016-09-19 2022-11-02 バイエル・クロップサイエンス・アクチェンゲゼルシャフト ピラゾロ［１，５－ａ］ピリジン誘導体及びそれの殺有害生物剤としての使用

Citations (2)

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Publication number Priority date Publication date Assignee Title
EP0941994A1 (en) * 1998-03-11 1999-09-15 F. Hoffmann-La Roche Ag Pyrazolopyrimidines and pyrazolotriazines with 5-HT6 receptor affinity
EP1354884A1 (en) * 2000-12-28 2003-10-22 Ono Pharmaceutical Co., Ltd. Tricyclic and heterocyclic derivative compounds and drugs containing these compounds as the active ingredient

Family Cites Families (2)

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Publication number Priority date Publication date Assignee Title
AU7001396A (en) 1995-09-22 1997-04-09 Takeda Chemical Industries Ltd. Triazole compounds, their production and use
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0941994A1 (en) * 1998-03-11 1999-09-15 F. Hoffmann-La Roche Ag Pyrazolopyrimidines and pyrazolotriazines with 5-HT6 receptor affinity
EP1354884A1 (en) * 2000-12-28 2003-10-22 Ono Pharmaceutical Co., Ltd. Tricyclic and heterocyclic derivative compounds and drugs containing these compounds as the active ingredient

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of EP2248817A4 *

Also Published As

Publication number Publication date
EA201001180A1 (ru) 2011-02-28
US20100292245A1 (en) 2010-11-18
WO2009093208A2 (ru) 2009-07-30
EP2248817B1 (en) 2015-01-07
US8829009B2 (en) 2014-09-09
EP2248817A4 (en) 2011-01-12
US20130079350A1 (en) 2013-03-28
US8309559B2 (en) 2012-11-13
EA017968B1 (ru) 2013-04-30
JP2011510062A (ja) 2011-03-31
KR20110000623A (ko) 2011-01-04
EP2248817A2 (en) 2010-11-10
JP5575663B2 (ja) 2014-08-20

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