EA200501311A1 - ПРОИЗВОДНЫЕ ЗАМЕЩЁННОГО 8-ПЕРФТОРАЛКИЛ-6,7,8,9-ТЕТРАГИДРОПИРИМИДО[1,2-a]ПИРИМИДИН-4-ОНА - Google Patents

ПРОИЗВОДНЫЕ ЗАМЕЩЁННОГО 8-ПЕРФТОРАЛКИЛ-6,7,8,9-ТЕТРАГИДРОПИРИМИДО[1,2-a]ПИРИМИДИН-4-ОНА

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Publication number
EA200501311A1
EA200501311A1 EA200501311A EA200501311A EA200501311A1 EA 200501311 A1 EA200501311 A1 EA 200501311A1 EA 200501311 A EA200501311 A EA 200501311A EA 200501311 A EA200501311 A EA 200501311A EA 200501311 A1 EA200501311 A1 EA 200501311A1
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EA
Eurasian Patent Office
Prior art keywords
alkyl group
group
atom
hydrogen atom
substituted
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EA200501311A
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English (en)
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EA009198B1 (ru
Inventor
Алистер Локхид
Мурад Саади
Франк Словински
Филипп Йеш
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Санофи-Авентис
Мицубиси Фарма Корпорейшн
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Publication of EA200501311A1 publication Critical patent/EA200501311A1/ru
Publication of EA009198B1 publication Critical patent/EA009198B1/ru

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    • 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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P25/14—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
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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

Abstract

Настоящее изобретение относится к производному замещенного пиримидона, представленному формулой (I), или его соли, где X представляет собой два атома водорода, атом серы, атом кислорода или Cалкильную группу и атом водорода; Y представляет собой связь, карбонильную группу, возможно замещенную метиленовую группу; R1 представляет собой 2-, 3- или 4-пиридиновое кольцо либо 2-, 4- или 5-пиримидиновое кольцо, причем эти кольца возможно замещены; R2 представляет собой фенильную группу или нафталиновое кольцо, причем фенильная группа и нафталиновое кольцо возможно замещены; R3 представляет собой атом водорода или Cалкильную группу; R4 представляет собой Cпергалогенированную алкильную группу или Cгалогенированную алкильную группу; R5 представляет собой атом водорода, Cалкильную группу или атом галогена; n равно 0-3; и p+q равно от 0 до 3. Настоящее изобретение относится также к лекарственному средству, содержащему в качестве активного ингредиента указанное производное или его соль, которое используют для профилактического и/или терапевтического лечения нейродегенеративных заболеваний, вызванных аномальной активностью GSK3β, например, таких как болезнь Альцгеймера.
EA200501311A 2003-03-21 2004-03-19 ПРОИЗВОДНЫЕ ЗАМЕЩЕННОГО 8-ПЕРФТОРАЛКИЛ-6,7,8,9-ТЕТРАГИДРОПИРИМИДО[1,2-a]ПИРИМИДИН-4-ОНА EA009198B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP03290728A EP1460076A1 (en) 2003-03-21 2003-03-21 Substituted 8-perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives
PCT/EP2004/004013 WO2004083210A1 (en) 2003-03-21 2004-03-19 SUBSTITUTED 8-PERFLUOROALKYL-6,7,8,9-TETRAHYDROPYRIMIDO[1,2-a] PYRIMIDIN-4-ONE DERIVATIVES

Publications (2)

Publication Number Publication Date
EA200501311A1 true EA200501311A1 (ru) 2006-04-28
EA009198B1 EA009198B1 (ru) 2007-12-28

Family

ID=32799141

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200501311A EA009198B1 (ru) 2003-03-21 2004-03-19 ПРОИЗВОДНЫЕ ЗАМЕЩЕННОГО 8-ПЕРФТОРАЛКИЛ-6,7,8,9-ТЕТРАГИДРОПИРИМИДО[1,2-a]ПИРИМИДИН-4-ОНА

Country Status (26)

Country Link
US (2) US7217715B2 (ru)
EP (2) EP1460076A1 (ru)
JP (1) JP4572194B2 (ru)
KR (1) KR101070075B1 (ru)
CN (1) CN100368412C (ru)
AR (1) AR053082A1 (ru)
AT (1) ATE433977T1 (ru)
AU (1) AU2004222105B2 (ru)
BR (1) BRPI0408605A (ru)
CA (1) CA2517774C (ru)
CY (1) CY1109345T1 (ru)
DE (1) DE602004021572D1 (ru)
DK (1) DK1608653T3 (ru)
EA (1) EA009198B1 (ru)
ES (1) ES2328812T3 (ru)
HK (1) HK1088893A1 (ru)
IL (1) IL170634A (ru)
MX (1) MXPA05010112A (ru)
NO (1) NO20054331L (ru)
NZ (1) NZ542224A (ru)
PL (1) PL1608653T3 (ru)
PT (1) PT1608653E (ru)
SI (1) SI1608653T1 (ru)
TW (1) TWI322809B (ru)
WO (1) WO2004083210A1 (ru)
ZA (1) ZA200507192B (ru)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US9708735B2 (en) 2005-06-23 2017-07-18 Sumitomo Electric Industries, Ltd. Group III nitride crystal substrate, epilayer-containing group III nitride crystal substrate, semiconductor device and method of manufacturing the same
US8771552B2 (en) * 2005-06-23 2014-07-08 Sumitomo Electric Industries, Ltd. Group III nitride crystal substrate, epilayer-containing group III nitride crystal substrate, semiconductor device and method of manufacturing the same
JP4277826B2 (ja) 2005-06-23 2009-06-10 住友電気工業株式会社 窒化物結晶、窒化物結晶基板、エピ層付窒化物結晶基板、ならびに半導体デバイスおよびその製造方法
EP2258357A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
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
AU2006304787A1 (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
EP1790649A1 (en) * 2005-11-21 2007-05-30 Sanofi-Aventis Substituted bicyclic pyrimidone derivatives
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP2021000A2 (en) 2006-05-09 2009-02-11 Braincells, Inc. Neurogenesis by modulating angiotensin
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
EP1939187A1 (en) 2006-12-20 2008-07-02 Sanofi-Aventis Substituted heteroaryl pyridopyrimidone derivatives
EP2138485A1 (en) 2008-06-26 2009-12-30 sanofi-aventis Substituted N-Oxide pyrazine derivatives
EP2138492A1 (en) 2008-06-26 2009-12-30 Sanofi-Aventis Substituted pyrimidin-4-one derivatives
EP2138495A1 (en) 2008-06-26 2009-12-30 sanofi-aventis Substituted pyrimido[2,1-a]isoquinolin-4-one derivatives
EP2138498A1 (en) 2008-06-26 2009-12-30 sanofi-aventis Substituted tricyclic derivatives against neurodegenerative diseases
EP2138493A1 (en) 2008-06-26 2009-12-30 Sanofi-Aventis Substituted pyrimidone derivatives
EP2138494A1 (en) * 2008-06-26 2009-12-30 Sanofi-Aventis Substituted alkyl pyrimidin-4-one derivatives
EP2138488A1 (en) 2008-06-26 2009-12-30 sanofi-aventis 4-(pyridin-4-yl)-1H-[1,3,5]triazin-2-one derivatives as GSK3-beta inhibitors for the treatment of neurodegenerative diseases
US8846670B2 (en) 2009-07-02 2014-09-30 Sanofi 1,2,3,4-tetrahydro-pyrimido(1,2-a)pyrimidin-6-one derivatives, preparation thereof, and pharmaceutical use thereof
SI2655375T1 (sl) 2010-12-23 2015-03-31 Sanofi Derivati pirimidinona, njihova priprava in njihova farmacevtska uporaba
FR2992316A1 (fr) 2012-06-22 2013-12-27 Sanofi Sa Derives de pyrimidinones, leur preparation et leur application en therapeutique
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

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2001270884A (ja) * 2000-03-23 2001-10-02 Mitsubishi-Tokyo Pharmaceuticals Inc ピリミドン誘導体
EP1136482A1 (en) * 2000-03-23 2001-09-26 Sanofi-Synthelabo 2-Amino-3-(alkyl)-pyrimidone derivatives as GSK3beta inhibitors
EP1184383A1 (en) * 2000-09-01 2002-03-06 Sanofi-Synthelabo 9-[Alkyl], 9-[(heteroaryl)alkyl] and 9-[(aryl)alkyl]-2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives
DE60103909T2 (de) * 2000-09-01 2005-09-22 Sanofi-Aventis 2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-on- und 7-pyridinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5 1honderivate
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

Also Published As

Publication number Publication date
NO20054331L (no) 2005-12-21
CN1784407A (zh) 2006-06-07
JP2006520766A (ja) 2006-09-14
AR053082A1 (es) 2007-04-25
NO20054331D0 (no) 2005-09-20
CN100368412C (zh) 2008-02-13
HK1088893A1 (en) 2006-11-17
AU2004222105B2 (en) 2010-03-04
EA009198B1 (ru) 2007-12-28
WO2004083210A1 (en) 2004-09-30
EP1608653B1 (en) 2009-06-17
JP4572194B2 (ja) 2010-10-27
TWI322809B (en) 2010-04-01
US20060035910A1 (en) 2006-02-16
CA2517774C (en) 2011-10-18
IL170634A (en) 2012-02-29
SI1608653T1 (sl) 2009-12-31
PL1608653T3 (pl) 2009-12-31
US7393853B2 (en) 2008-07-01
ZA200507192B (en) 2007-03-28
ATE433977T1 (de) 2009-07-15
KR20050111781A (ko) 2005-11-28
DK1608653T3 (da) 2009-10-05
TW200505922A (en) 2005-02-16
CY1109345T1 (el) 2014-07-02
DE602004021572D1 (de) 2009-07-30
ES2328812T3 (es) 2009-11-18
US7217715B2 (en) 2007-05-15
KR101070075B1 (ko) 2011-10-04
PT1608653E (pt) 2009-09-07
US20070191384A1 (en) 2007-08-16
BRPI0408605A (pt) 2006-03-07
EP1460076A1 (en) 2004-09-22
AU2004222105A1 (en) 2004-09-30
CA2517774A1 (en) 2004-09-30
EP1608653A1 (en) 2005-12-28
MXPA05010112A (es) 2006-05-17
NZ542224A (en) 2008-11-28

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