EA200300151A1 - ПРОИЗВОДНЫЕ 2-ПИРИДИНИЛ-6,7,8,9-ТЕТРАГИДРОПИРИМИДО[1,2-a]ПИРИМИДИН-4-ОНА И 7-ПИРИДИНИЛ-2,3-ДИГИДРОИМИДАЗО[1,2-a]ПИРИМИДИН-5(1H)ОНА - Google Patents

ПРОИЗВОДНЫЕ 2-ПИРИДИНИЛ-6,7,8,9-ТЕТРАГИДРОПИРИМИДО[1,2-a]ПИРИМИДИН-4-ОНА И 7-ПИРИДИНИЛ-2,3-ДИГИДРОИМИДАЗО[1,2-a]ПИРИМИДИН-5(1H)ОНА

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Publication number
EA200300151A1
EA200300151A1 EA200300151A EA200300151A EA200300151A1 EA 200300151 A1 EA200300151 A1 EA 200300151A1 EA 200300151 A EA200300151 A EA 200300151A EA 200300151 A EA200300151 A EA 200300151A EA 200300151 A1 EA200300151 A1 EA 200300151A1
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group
ring
atom
alkyl group
possibly substituted
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EA200300151A
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English (en)
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EA005297B1 (ru
Inventor
Антонио Альмарио Гарсия
Тьерри Галле
Адриен Так Ли
Алистер Локхид
Северен Маргери
Ален Неделек
Мурад Саади
Филипп Йеш
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Санофи-Синтелябо
Мицубиси Фарма Корпорейшн
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Priority claimed from EP00402410A external-priority patent/EP1184383A1/en
Priority claimed from EP00402412A external-priority patent/EP1184385A1/en
Application filed by Санофи-Синтелябо, Мицубиси Фарма Корпорейшн filed Critical Санофи-Синтелябо
Publication of EA200300151A1 publication Critical patent/EA200300151A1/ru
Publication of EA005297B1 publication Critical patent/EA005297B1/ru

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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
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61P25/16—Anti-Parkinson drugs
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    • A61P25/00—Drugs for disorders of the nervous system
    • 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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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • A—HUMAN NECESSITIES
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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
    • A—HUMAN NECESSITIES
    • 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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  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Данное изобретение относится к производному пиримидона, представленному формулой (I), или к его соли, где X представляет собой атомы водорода, атом серы, атом кислорода или Cалкильную группу и атом водорода; Y является связью, этениленовой группой, этиниленовой группой, 1,2-циклопропиленом, атомом кислорода, атомом серы, сульфонильной группой, сульфинильной группой, карбонильной группой, возможно замещенным атомом азота или возможно замещенной метиленовой группой; R1 является 2-, 3- или 4-пиридильной группой, возможно замещенной Cциклоалкильной группой, Cалкильной группой, Cалкоксигруппой, бензильной группой или атомом галогена; когда Y представляет собой связь, возможно замещенную метиленовую группу или карбонильную группу, тогда R2 является Cалкильной группой, Cциклоалкильной группой, Cалкилтиогруппой, Cалкоксигруппой, Cпергалогенированной алкильной группой, Cгалогенированной алкильной группой, 5,6,7,8-тетрагидронафтильным кольцом, нафтильным кольцом, фенилтиогруппой, бензильной группой, фенильным кольцом, пиридильным кольцом, индольным кольцом, пиррольным кольцом, тиофеновым кольцом, фурановым кольцом или имидазольным кольцом; когда Y представляет собой этениленовую группу, этиниленовую группу, атом кислорода, атом серы, сульфонильную группу, сульфинильную группу или возможно замещенный атом азота, тогда R2 является Cалкильной группой, Cциклоалкильной группой, Cпергалогенированной алкильной группой, Cгалогенированной алкильной группой, нафтильным кольцом, 5,6,7,8-тетрагидронафтильным кольцом, бензильной группой, фенильным кольцом, пиридильным кольцом, индольным кольцом, пиррольным кольцом, тиофеновым кольцом, фурановым кольцом или имидазольным
EA200300151A 2000-09-01 2001-08-31 ПРОИЗВОДНЫЕ 2-ПИРИДИНИЛ-6,7,8,9-ТЕТРАГИДРОПИРИМИДО[1,2-a]ПИРИМИДИН-4-ОНА И 7-ПИРИДИНИЛ-2,3-ДИГИДРОИМИДАЗО[1,2-a]ПИРИМИДИН-5(1H)ОНА EA005297B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP00402410A EP1184383A1 (en) 2000-09-01 2000-09-01 9-[Alkyl], 9-[(heteroaryl)alkyl] and 9-[(aryl)alkyl]-2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives
EP00402412A EP1184385A1 (en) 2000-09-01 2000-09-01 1-[Alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7-pyridin-4-yl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one derivatives
PCT/EP2001/010726 WO2002018386A1 (en) 2000-09-01 2001-08-31 2-PYRIDINYL-6,7,8,9-TETRAHYDROPYRIMIDO[1,2-a]PYRIMIDIN-4-ONE AND 7-PYRIDINYL-2,3-DIHYDROIMIDAZO[1,2-a]PYRIMIDIN-5(1H)ONE DERIVATI VES

Publications (2)

Publication Number Publication Date
EA200300151A1 true EA200300151A1 (ru) 2003-08-28
EA005297B1 EA005297B1 (ru) 2004-12-30

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ID=26073571

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Application Number Title Priority Date Filing Date
EA200300151A EA005297B1 (ru) 2000-09-01 2001-08-31 ПРОИЗВОДНЫЕ 2-ПИРИДИНИЛ-6,7,8,9-ТЕТРАГИДРОПИРИМИДО[1,2-a]ПИРИМИДИН-4-ОНА И 7-ПИРИДИНИЛ-2,3-ДИГИДРОИМИДАЗО[1,2-a]ПИРИМИДИН-5(1H)ОНА

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US (3) US6974819B2 (ru)
EP (1) EP1315731B1 (ru)
JP (1) JP2004507546A (ru)
KR (1) KR100800250B1 (ru)
CN (2) CN1267432C (ru)
AR (1) AR030587A1 (ru)
AT (1) ATE269333T1 (ru)
AU (2) AU1224902A (ru)
CA (1) CA2419880C (ru)
DE (1) DE60103909T2 (ru)
DK (1) DK1315731T3 (ru)
EA (1) EA005297B1 (ru)
ES (1) ES2222396T3 (ru)
SI (1) SI1315731T1 (ru)
TR (1) TR200402342T4 (ru)
WO (1) WO2002018386A1 (ru)

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ES2247398T3 (es) * 2001-09-21 2006-03-01 Sanofi-Aventis Derivados de 2-piridini9l-6,7,8,9-tetrahidropirimido(1,2-a)pirimidin-4-ona y 7-piridinil-2,3-dihidroimidazo(1,2-a)pirimidin-5(1h)ona sustituidos.
EA007737B1 (ru) 2002-02-28 2006-12-29 Санофи-Авентис ГЕТЕРОАРИЛЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 2-ПИРИДИНИЛ- И 2-ПИРИМИДИНИЛ-6,7,8,9-ТЕТРАГИДРОПИРИМИДО[1,2-a]ПИРИМИДИН-4-ОНА
EP1454909B1 (en) * 2003-03-07 2008-08-20 Sanofi Aventis 8'-pyridinyl-dihydrospiro (cycloalkyl) -pyrimido (1,2-a) pyrimidin-6-one and 8'-pyrimidinyl-dihydrospiro (cycloalkyl) pyrimido (1,2-a) pyrimidin-6 derivatives -one and their use against neurodegenerative diseases
EP1460075A1 (en) * 2003-03-21 2004-09-22 Sanofi-Synthelabo Substituted 8-Pyridinyl-6,7,8,9-Tetrahydropyrimido[1,2-a]Pyrimidin-4-one and 8-Phenyl-6-7,8,9-Tetrahydropyrimido[1,2-a]Pyrimidin-4-one derivatives
EP1460076A1 (en) * 2003-03-21 2004-09-22 Sanofi-Synthelabo Substituted 8-perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives
EP1557417B1 (en) * 2003-12-19 2007-03-07 Sanofi-Aventis Substituted 8'-pyri(mi)dinyl-dihydrospiro-[cycloalkylamine]-pyrimido[1,2-a] pyrimidin-6-one derivatives
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
EP2275095A3 (en) 2005-08-26 2011-08-17 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
JP2009512711A (ja) 2005-10-21 2009-03-26 ブレインセルス，インコーポレイティド Ｐｄｅ阻害による神経新生の調節
CA2625210A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
WO2007134136A2 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
MY155661A (en) * 2009-07-02 2015-11-13 Sanofi Sa Novel 1,2,3,4-tetrahydropyrimido{1,2-a}pyrimidin-6-one derivatives, preparation thereof and pharmaceutical use thereof
DK2448939T3 (en) 2009-07-02 2017-06-19 Sanofi Sa DERIVATIVES OF 2,3-DIHYDRO-1H-IMIDAZO {1,2-A} PYRIMIDIN-5-ON, PREPARATION AND PHARMACEUTICAL USE thereof
FR2947550B1 (fr) * 2009-07-02 2012-05-18 Sanofi Aventis Nouveaux derives de 2,3-dihydro-1h-imidazo{1,2-a}pyrimidin-5-one, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt (pkb)
FR2947551B1 (fr) * 2009-07-02 2012-05-18 Sanofi Aventis Nouveaux derives de 1,2,3,4-tetrahydro-pyrimido{1,2-a)pyrimidin-6-one, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt (pkb)
ES2553610T3 (es) * 2010-12-14 2015-12-10 Electrophoretics Limited Inhibidores de la caseína cinasa 1 delta (CK1delta)
DK2655375T3 (en) * 2010-12-23 2015-03-09 Sanofi Sa PYRIMIDINON DERIVATIVES, PREPARATION AND PHARMACEUTICAL USE THEREOF
FR2992314B1 (fr) 2012-06-22 2015-10-16 Sanofi Sa Nouveaux derives de 2,3-dihydro-1h-imidazo{1,2-a}pyrimidin-5-one et 1,2,3,4-tetrahydro-pyrimido{1,2-a}pyrimidin-6-one comportant une morpholine substituee, leur preparation et leur utilisation pharmaceutique
CA2945263A1 (en) 2014-04-09 2015-10-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity

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US6004814A (en) 1998-09-25 1999-12-21 Isis Pharmaceuticals Inc. Antisense modulation of CD71 expression

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CN100339379C (zh) 2007-09-26
DE60103909D1 (de) 2004-07-22
AU2002212249B2 (en) 2006-11-30
ATE269333T1 (de) 2004-07-15
JP2004507546A (ja) 2004-03-11
EP1315731B1 (en) 2004-06-16
AU2002212249B9 (en) 2007-01-18
US7566720B2 (en) 2009-07-28
DK1315731T3 (da) 2004-10-11
EA005297B1 (ru) 2004-12-30
EP1315731A1 (en) 2003-06-04
US6974819B2 (en) 2005-12-13
DE60103909T2 (de) 2005-09-22
KR20030027103A (ko) 2003-04-03
SI1315731T1 (en) 2005-02-28
CN1267432C (zh) 2006-08-02
KR100800250B1 (ko) 2008-02-01
WO2002018386A1 (en) 2002-03-07
US20080027078A1 (en) 2008-01-31
ES2222396T3 (es) 2005-02-01
CA2419880C (en) 2010-04-20
TR200402342T4 (tr) 2004-11-22
CN1449398A (zh) 2003-10-15
CA2419880A1 (en) 2002-03-07
AU1224902A (en) 2002-03-13
US20040087598A1 (en) 2004-05-06
CN1680379A (zh) 2005-10-12
AR030587A1 (es) 2003-08-27
US20060014762A1 (en) 2006-01-19

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