EA200400937A1 - ПРОИЗВОДНЫЕ 1-[АЛКИЛ]-, 1-[(ГЕТЕРОАРИЛ)АЛКИЛ]- И 1-[(АРИЛ)АЛКИЛ]-7-(ПИРИМИДИН-4-ИЛ)ИМИДАЗО[1,2-a]ПИРИМИДИН-5(1H)-ОНА - Google Patents

ПРОИЗВОДНЫЕ 1-[АЛКИЛ]-, 1-[(ГЕТЕРОАРИЛ)АЛКИЛ]- И 1-[(АРИЛ)АЛКИЛ]-7-(ПИРИМИДИН-4-ИЛ)ИМИДАЗО[1,2-a]ПИРИМИДИН-5(1H)-ОНА

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Publication number
EA200400937A1
EA200400937A1 EA200400937A EA200400937A EA200400937A1 EA 200400937 A1 EA200400937 A1 EA 200400937A1 EA 200400937 A EA200400937 A EA 200400937A EA 200400937 A EA200400937 A EA 200400937A EA 200400937 A1 EA200400937 A1 EA 200400937A1
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Eurasian Patent Office
Prior art keywords
ring
group
alkil
possibly substituted
pyrimidin
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EA200400937A
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English (en)
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EA007459B1 (ru
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Алистер Локхид
Мурад Саади
Филипп Йеш
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Санофи-Авентис
Мицубиси Фарма Корпорейшн
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Publication of EA200400937A1 publication Critical patent/EA200400937A1/ru
Publication of EA007459B1 publication Critical patent/EA007459B1/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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • 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
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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

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
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  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
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  • Pain & Pain Management (AREA)
  • Hematology (AREA)
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  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
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  • Child & Adolescent Psychology (AREA)
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  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Данное изобретение относится к производному имидазо[1,2-a]пиримидона, представленному формулой (I), или его соли R, где X представляет собой связь, этениленовую группу, этиниленовую группу, метиленовую группу, возможно замещенную; карбонильную группу, атом кислорода, атом серы, сульфонильную группу, сульфоксидную группу или атом азота, возможно замещенный; Rпредставляет собой 2-, 4- или 5-пиримидинил, возможно замещенный; Rпредставляет собой Cалкильную группу, Cпергалогенированную алкильную группу, Cгалогенированную алкильную группу, бензильную группу, бензольное кольцо, нафталиновое кольцо, 5,6,7,8-тетрагидронафталиновое кольцо, пиридиновое кольцо, индольное кольцо, пиррольное кольцо, тиофеновое кольцо, фурановое кольцо или имидазольное кольцо, причем бензильная группа и кольца возможно замещены; и n равен от 0 до 3. Данное изобретение также относится к лекарству, содержащему указанное производное или его соль в качестве активного ингредиента, которое используют для профилактического и/или терапевтического лечения нейродегенеративного заболевания, вызванного аномальной активностью гликоген-синтазы-киназы 3β (GSK3β), такого как болезнь Альцгеймера.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200400937A 2002-02-28 2003-02-26 Производные 1-[алкил]-, 1-[(гетероарил)алкил]- и 1-[(арил)алкил]-7-(пиримидин-4-ил)имидазо[1,2-a]пиримидин-5(1h)-она EA007459B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02290487A EP1340759A1 (en) 2002-02-28 2002-02-28 1-[alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7-(pyrimidin-4-yl)-imidazo[1,2-a]pyrimidin-5(1H)-one derivatives
PCT/EP2003/002652 WO2003072580A1 (en) 2002-02-28 2003-02-26 1-[ALKYL], 1-[HETEROARYL)ALKYL] AND 1-[ARYL)ALKYL]-7-(PYRIMIDIN-4-YL)-IMADAZO[1,2-a]PYRIMIDIN-5(1H)-ONE DERIVATIVES

Publications (2)

Publication Number Publication Date
EA200400937A1 true EA200400937A1 (ru) 2005-02-24
EA007459B1 EA007459B1 (ru) 2006-10-27

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ID=27675771

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EA200400937A EA007459B1 (ru) 2002-02-28 2003-02-26 Производные 1-[алкил]-, 1-[(гетероарил)алкил]- и 1-[(арил)алкил]-7-(пиримидин-4-ил)имидазо[1,2-a]пиримидин-5(1h)-она

Country Status (23)

Country Link
US (2) US7429663B2 (ru)
EP (2) EP1340759A1 (ru)
JP (1) JP4484524B2 (ru)
KR (1) KR100935262B1 (ru)
CN (1) CN100441581C (ru)
AR (1) AR038620A1 (ru)
AT (1) ATE309246T1 (ru)
AU (1) AU2003214127C1 (ru)
BR (1) BR0308106A (ru)
CA (1) CA2474875C (ru)
DE (1) DE60302220T2 (ru)
DK (1) DK1480981T3 (ru)
EA (1) EA007459B1 (ru)
ES (1) ES2250876T3 (ru)
IL (1) IL163288A (ru)
MX (1) MXPA04008365A (ru)
NO (1) NO329756B1 (ru)
NZ (1) NZ534467A (ru)
PL (1) PL372664A1 (ru)
SI (1) SI1480981T1 (ru)
TW (1) TWI305534B (ru)
WO (1) WO2003072580A1 (ru)
ZA (1) ZA200406154B (ru)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2696492C2 (ru) * 2014-05-13 2019-08-02 Ф. Хоффманн-Ля Рош Аг Дейтрированные гетероциклические соединения и их применение в качестве средств визуализации
RU2791900C1 (ru) * 2014-05-13 2023-03-14 Ф. Хоффманн-Ля Рош Аг Дейтрированные гетероциклические соединения и их применение в качестве средств визуализации

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JP2007508290A (ja) * 2003-10-10 2007-04-05 ファイザー・プロダクツ・インク ＧＳＫ−３阻害剤としての置換２Ｈ−［１，２，４］トリアゾロ［４，３−ａ］ピラジン
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス，インコーポレイティド ムスカリン性受容体調節による神経発生
CA2625153A1 (en) 2005-10-21 2007-04-26 Braincells, Inc. Modulation of neurogenesis by pde inhibition
US20070112017A1 (en) 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP2377531A2 (en) 2006-05-09 2011-10-19 Braincells, Inc. Neurogenesis by modulating angiotensin
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
AU2009260526A1 (en) * 2008-05-30 2009-12-23 Merck Sharp & Dohme Corp. Novel substituted indoles
EP2138494A1 (en) * 2008-06-26 2009-12-30 Sanofi-Aventis Substituted alkyl pyrimidin-4-one derivatives
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
PL2448939T3 (pl) * 2009-07-02 2017-08-31 Sanofi Pochodne 2,3-dihydro-1h-imidazo {1,2-a} pirymidyn-5-onu, ich wytwarzanie i ich zastosowanie farmaceutyczne
CN112574219A (zh) * 2021-01-31 2021-03-30 湖北大学 一种苯并咪唑并嘧啶酮衍生物的合成方法
CN115448921B (zh) * 2021-06-08 2023-08-01 四川大学 一类咪唑烷并嘧啶酮化合物及在治疗HsClpP介导的疾病中的用途

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CZ296911B6 (cs) * 1996-12-05 2006-07-12 Amgen Inc. Substituovaný pyrimidin, jeho pouzití a farmaceutický prostredek na jeho bázi
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EP1184384A1 (en) * 2000-09-01 2002-03-06 Sanofi-Synthelabo 1-(Alkyl), 1-((heteroaryl)alkyl) and 1-((aryl)alkyl)-7-pyridin-4-ylimidazo(1,2a)pyrimidin-5(1H)-one derivatives
EP1295884A1 (en) * 2001-09-21 2003-03-26 Sanofi-Synthelabo 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]Pyrimidin-4-one and 7-Pyrimidinyl-2,3-Dihydroimidazo[1,2-a]Pyrimidin-5(1H)one derivatives

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2696492C2 (ru) * 2014-05-13 2019-08-02 Ф. Хоффманн-Ля Рош Аг Дейтрированные гетероциклические соединения и их применение в качестве средств визуализации
RU2791900C1 (ru) * 2014-05-13 2023-03-14 Ф. Хоффманн-Ля Рош Аг Дейтрированные гетероциклические соединения и их применение в качестве средств визуализации

Also Published As

Publication number Publication date
IL163288A (en) 2009-12-24
DE60302220D1 (de) 2005-12-15
CA2474875C (en) 2011-04-12
KR100935262B1 (ko) 2010-01-06
DE60302220T2 (de) 2006-07-27
CN100441581C (zh) 2008-12-10
TW200418859A (en) 2004-10-01
EA007459B1 (ru) 2006-10-27
JP2005519087A (ja) 2005-06-30
AU2003214127A1 (en) 2003-09-09
ZA200406154B (en) 2005-08-02
EP1480981A1 (en) 2004-12-01
DK1480981T3 (da) 2006-03-20
ES2250876T3 (es) 2006-04-16
CN1646533A (zh) 2005-07-27
NZ534467A (en) 2006-07-28
US20050119280A1 (en) 2005-06-02
KR20040087328A (ko) 2004-10-13
US7429663B2 (en) 2008-09-30
JP4484524B2 (ja) 2010-06-16
TWI305534B (en) 2009-01-21
AU2003214127C1 (en) 2009-02-05
AU2003214127B2 (en) 2008-07-03
PL372664A1 (en) 2005-07-25
ATE309246T1 (de) 2005-11-15
WO2003072580A1 (en) 2003-09-04
AR038620A1 (es) 2005-01-19
NO20043567L (no) 2004-11-26
NO329756B1 (no) 2010-12-13
BR0308106A (pt) 2005-01-04
CA2474875A1 (en) 2003-09-04
SI1480981T1 (sl) 2006-04-30
US20080318980A1 (en) 2008-12-25
EP1340759A1 (en) 2003-09-03
MXPA04008365A (es) 2005-07-26
EP1480981B1 (en) 2005-11-09

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