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WO2009093210A3 - ЗАМЕЩЕННЫЕ ЦИKЛOAЛKAHO[e ИЛИ d]ПИPAЗOЛO[l,5-a]ПИPИMИДИHЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ - Google Patents

ЗАМЕЩЕННЫЕ ЦИKЛOAЛKAHO[e ИЛИ d]ПИPAЗOЛO[l,5-a]ПИPИMИДИHЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ Download PDF

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Publication number
WO2009093210A3
WO2009093210A3 PCT/IB2009/050275 IB2009050275W WO2009093210A3 WO 2009093210 A3 WO2009093210 A3 WO 2009093210A3 IB 2009050275 W IB2009050275 W IB 2009050275W WO 2009093210 A3 WO2009093210 A3 WO 2009093210A3
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receptors
alkyl
substituted
cycloalcano
pyrazolo
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WO2009093210A2 (ru
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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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Priority claimed from RU2008102154/04A external-priority patent/RU2369600C1/ru
Priority claimed from RU2008137217/04A external-priority patent/RU2374249C1/ru
Application filed by Alla Chem LLC filed Critical Alla Chem LLC
Priority to EA201001181A priority Critical patent/EA017818B1/ru
Priority to EP09703618A priority patent/EP2248814A4/en
Priority to JP2010543612A priority patent/JP5584627B2/ja
Priority to US12/863,192 priority patent/US8629154B2/en
Publication of WO2009093210A2 publication Critical patent/WO2009093210A2/ru
Publication of WO2009093210A3 publication Critical patent/WO2009093210A3/ru
Anticipated expiration legal-status Critical
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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
    • 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
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
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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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
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Abstract

Данное изобретение относится к антагонистам серотониновых 5-HT6 рецепторов - замещенным 2-aлкилcyльфaнил-3-apилcyльфoнил-циклoaлкaнo[e и d]пиpaзoлo[1,5- a]пиpимидинaм, новым лекарственным началам и фармацевтическим композициям, содержащим лекарственные начала в виде указанных соединений, а также к новым лекарственным средствам и способу лечения и предупреждения развития заболеваний ЦНС людей и теплокровных животных, патогенез которых связан с 5-HT6 рецепторами. В общих формулах 1 и 2 R1 представляет собой атом водорода или C1-C3алкил; R представляет собой C1-C3 алкил; R 2 представляет собой атом водорода, один или два необязательно одинаковых атома галогена, C1-C3 алкил или необязательно замещенный C1-C3 алкилом гидроксил; n представляет собой целое число 1, 2 или 3.
PCT/IB2009/050275 2008-01-24 2009-01-23 ЗАМЕЩЕННЫЕ ЦИKЛOAЛKAHO[e ИЛИ d]ПИPAЗOЛO[l,5-a]ПИPИMИДИHЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ Ceased WO2009093210A2 (ru)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EA201001181A EA017818B1 (ru) 2008-01-24 2009-01-23 ЗАМЕЩЕННЫЕ ЦИКЛОАЛКАНО[e ИЛИ d]ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-НТРЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
EP09703618A EP2248814A4 (en) 2008-01-24 2009-01-23 SUBSTITUTED CYCLOALKAN [E AND D] PYRAZOLO [1,5-A] PYRIMIDINES / ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS AND PROCESS FOR THEIR PREPARATION AND THEIR USE
JP2010543612A JP5584627B2 (ja) 2008-01-24 2009-01-23 置換されたシクロアルキル［ｅ又はｄ］ピラゾロ［１，５−ａ］ピリミジン−セロトニン５−ＨＴ６受容体のアンタゴニスト、その調製の方法及び使用
US12/863,192 US8629154B2 (en) 2008-01-24 2009-01-23 Substituted cycloalcano[e and d] pyrazolo [1,5-a]pyrimidines/antagonists of serotonin 5-HT6 receptors and methods for production and the 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
RU2008137217/04A RU2374249C1 (ru) 2008-09-17 2008-09-17 ЗАМЕЩЕННЫЕ ЦИКЛОАЛКАНО[е ИЛИ d]ПИРАЗОЛО[1,5-а]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-НТ6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
RU2008137217 2008-09-17

Publications (2)

Publication Number Publication Date
WO2009093210A2 WO2009093210A2 (ru) 2009-07-30
WO2009093210A3 true WO2009093210A3 (ru) 2009-10-08

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PCT/IB2009/050275 Ceased WO2009093210A2 (ru) 2008-01-24 2009-01-23 ЗАМЕЩЕННЫЕ ЦИKЛOAЛKAHO[e ИЛИ d]ПИPAЗOЛO[l,5-a]ПИPИMИДИHЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ

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US (1) US8629154B2 (ru)
EP (1) EP2248814A4 (ru)
JP (1) JP5584627B2 (ru)
KR (1) KR20100119777A (ru)
EA (1) EA017818B1 (ru)
WO (1) WO2009093210A2 (ru)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9533984B2 (en) 2013-04-19 2017-01-03 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors

Families Citing this family (22)

* 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
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
UA125503C2 (uk) 2012-06-13 2022-04-13 Інсайт Холдинґс Корпорейшн Заміщені трициклічні сполуки як інгібітори fgfr
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
UA121669C2 (uk) 2015-02-20 2020-07-10 Інсайт Корпорейшн Біциклічні гетероцикли як інгібітори fgfr
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
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CN112566912A (zh) 2018-05-04 2021-03-26 因赛特公司 Fgfr抑制剂的盐
SI3788047T1 (sl) 2018-05-04 2024-11-29 Incyte Corporation Trdne oblike inhibitorja fgfr in postopki priprave le-teh
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4045151A1 (en) 2019-10-14 2022-08-24 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4069695A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Derivatives of an fgfr inhibitor
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors

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RU2003129060A (ru) * 2001-03-14 2005-04-10 Грюненталь ГмбХ (DE) Замещенные пиразоло-и тиазолопиримидины

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9533984B2 (en) 2013-04-19 2017-01-03 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors

Also Published As

Publication number Publication date
EA017818B1 (ru) 2013-03-29
WO2009093210A2 (ru) 2009-07-30
EP2248814A2 (en) 2010-11-10
US8629154B2 (en) 2014-01-14
JP2011510064A (ja) 2011-03-31
EP2248814A4 (en) 2011-01-12
US20110059997A1 (en) 2011-03-10
KR20100119777A (ko) 2010-11-10
JP5584627B2 (ja) 2014-09-03
EA201001181A1 (ru) 2011-02-28

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