AR043485A1 - Derivados del 8'-piridinil-dihidrospiro-[cicloalquil]-pirimido[1,2a]pirimidin-6-ona y 8´-pirimidinil-dihidrospiro-[cicloalquil]-pirimido[1,2a]pirimidin-6-ona substituidos - Google Patents

Derivados del 8'-piridinil-dihidrospiro-[cicloalquil]-pirimido[1,2a]pirimidin-6-ona y 8´-pirimidinil-dihidrospiro-[cicloalquil]-pirimido[1,2a]pirimidin-6-ona substituidos

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Publication number
AR043485A1
AR043485A1 ARP040100694A ARP040100694A AR043485A1 AR 043485 A1 AR043485 A1 AR 043485A1 AR P040100694 A ARP040100694 A AR P040100694A AR P040100694 A ARP040100694 A AR P040100694A AR 043485 A1 AR043485 A1 AR 043485A1
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AR
Argentina
Prior art keywords
group
alkyl group
atom
dihidrospiro
pirimido
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ARP040100694A
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English (en)
Inventor
Pascal George
Alistair Lochead
Mourad Saady
Franck Slowinski
Philippe Yaiche
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Sanofi Aventis
Mitsubishi Pharma Corp
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Application filed by Sanofi Aventis, Mitsubishi Pharma Corp filed Critical Sanofi Aventis
Publication of AR043485A1 publication Critical patent/AR043485A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/16Anti-Parkinson drugs
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61P25/28Drugs 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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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente se refiere a compuestos que se utilizan para el tratamiento preventivo y/o terapéutico de una enfermedad neurodegenerativa causada por la actividad anormal de la GSK3beta, como ser enfermedad de Alzheimer. Reivindicación 1: Un derivado de dihidrospiro-[cicloalquil]-pirimidona representado por la fórmula (1) o una sal del mismo; donde: X representa dos átomos de H, un átomo de S, un átomo de O o un grupo alquilo C1-2 y un átomo de H; Y representa un enlace, un grupo carbonilo, un grupo metileno opcionalmente sustituido por uno o dos grupos seleccionados entre un grupo alquilo C1-6, un grupo hidroxilo, un grupo alcoxi C1-4, un grupo alquilo perhalogenado C1-2 o un grupo amino; R1 representa un anillo de 2m 3 o 4-piridina o un anillo de 2, 4 o 5-pirimidina, y el anillo está opcionalmente sustituido por un grupo alquilo C1-4, un grupo alcoxi C1-4 o un átomo de halógeno; R2 representa un anillo de benceno o un anillo de naftaleno; los anillos están opcionalmente sustituidos por 1 a 4 sustituyentes seleccionados entre un grupo alquilo c1-6, un grupo metilendioxi, un átomo de halógeno, un grupo alquilo perhalogenado c1-2, un grupo alquilo halogenado C1-3, un grupo hidroxilo, un grupo alcoxi C1-4, un grupo nitro, un grupo ciano, un grupo amino, un grupo monoalquilamino C1-5 o un grupo dialquilamino C2-10; R3 representa un átomo de H, un grupo alquilo C1-6 o un átomo de halógeno; m representa 1 a 4; n representa 0 a 3; p representa 0 a 2; y q representa 0 a 2, y p + q es inferior a 4.
ARP040100694A 2003-03-07 2004-03-05 Derivados del 8'-piridinil-dihidrospiro-[cicloalquil]-pirimido[1,2a]pirimidin-6-ona y 8´-pirimidinil-dihidrospiro-[cicloalquil]-pirimido[1,2a]pirimidin-6-ona substituidos AR043485A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP03290569A EP1454909B1 (en) 2003-03-07 2003-03-07 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

Publications (1)

Publication Number Publication Date
AR043485A1 true AR043485A1 (es) 2005-08-03

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ID=32799103

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Application Number Title Priority Date Filing Date
ARP040100694A AR043485A1 (es) 2003-03-07 2004-03-05 Derivados del 8'-piridinil-dihidrospiro-[cicloalquil]-pirimido[1,2a]pirimidin-6-ona y 8´-pirimidinil-dihidrospiro-[cicloalquil]-pirimido[1,2a]pirimidin-6-ona substituidos

Country Status (26)

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US (2) US7294632B2 (es)
EP (2) EP1454909B1 (es)
JP (1) JP4639182B2 (es)
KR (1) KR101069984B1 (es)
CN (1) CN100463908C (es)
AR (1) AR043485A1 (es)
AT (1) ATE469153T1 (es)
AU (1) AU2004218250B2 (es)
BR (1) BRPI0408189A (es)
CA (1) CA2516937C (es)
CY (1) CY1111057T1 (es)
DE (1) DE602004027354D1 (es)
DK (1) DK1603915T3 (es)
EA (1) EA008172B1 (es)
ES (1) ES2346311T3 (es)
HK (1) HK1085740A1 (es)
IL (1) IL170461A (es)
MX (1) MXPA05009574A (es)
NO (1) NO20054140L (es)
NZ (1) NZ542135A (es)
PL (1) PL1603915T3 (es)
PT (1) PT1603915E (es)
SI (1) SI1603915T1 (es)
TW (1) TWI320785B (es)
WO (1) WO2004078760A1 (es)
ZA (1) ZA200507107B (es)

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* Cited by examiner, † Cited by third party
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MX2007016182A (es) 2005-06-14 2008-03-07 Schering Corp Inhibidores de aspartil proteasas.
WO2007025177A2 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
EP2377530A3 (en) 2005-10-21 2012-06-20 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
EP1992625A1 (en) * 2007-05-16 2008-11-19 Sanofi-Aventis Arylamide pyrimidone compounds
EP1992621A1 (en) 2007-05-16 2008-11-19 Sanofi-Aventis Heteroarylamide-substituted pyrimidone derivatives for the treatment of neurodegenerative diseases
EP1992620A1 (en) * 2007-05-16 2008-11-19 Sanofi-Aventis Arylamide pyrimidone derivatives for the treatment of neurodegenerative diseases
EP1992624A1 (en) 2007-05-16 2008-11-19 Sanofi-Aventis Heteroarylamide pyrimidone compounds
EP2138493A1 (en) 2008-06-26 2009-12-30 Sanofi-Aventis Substituted pyrimidone 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
EP2138498A1 (en) * 2008-06-26 2009-12-30 sanofi-aventis Substituted tricyclic derivatives against neurodegenerative diseases
EP2138494A1 (en) 2008-06-26 2009-12-30 Sanofi-Aventis Substituted alkyl pyrimidin-4-one derivatives
EP2138485A1 (en) 2008-06-26 2009-12-30 sanofi-aventis Substituted N-Oxide pyrazine derivatives
EP2138495A1 (en) 2008-06-26 2009-12-30 sanofi-aventis Substituted pyrimido[2,1-a]isoquinolin-4-one derivatives
EP2138492A1 (en) 2008-06-26 2009-12-30 Sanofi-Aventis Substituted pyrimidin-4-one derivatives
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
CN102482286B (zh) 2009-07-02 2015-07-15 赛诺菲 新型1,2,3,4-四氢嘧啶并{1,2-a}嘧啶-6-酮衍生物、其制备以及其医药用途
PL2655375T3 (pl) 2010-12-23 2015-05-29 Sanofi Sa Pochodne pirymidynonu, ich wytwarzanie i ich farmaceutyczne zastosowanie
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
FR2992316A1 (fr) 2012-06-22 2013-12-27 Sanofi Sa Derives de pyrimidinones, leur preparation et leur application en therapeutique
WO2015155738A2 (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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FR2812636A1 (fr) * 2000-08-02 2002-02-08 Novapharme Nouveaux derives 2-phenyl imidazo[1.2-a]pyrimidin-5-ones et 2-phenyl 2,3-dihydro imidazo[1,2-a]pyrimidin-5-ones
EP1184385A1 (en) * 2000-09-01 2002-03-06 Sanofi-Synthelabo 1-[Alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7-pyridin-4-yl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)-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
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
SI1430057T1 (sl) * 2001-09-21 2006-02-28 Sanofi Aventis Substituirani 2-piridinil-6,7,8,9-tetrahidropirimido -(1,2-a)pirimidin-4-onski in 7-piridinil-2,3-dihidroimidazo -(1,2-a)pirimidin-5(1H)onski derivati
IL160397A0 (en) * 2001-09-21 2004-07-25 Sanofi Synthelabo Substituted 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 for neurodegenerative disorders
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
EP1295885A1 (en) * 2001-09-21 2003-03-26 Sanofi-Synthelabo Substituted 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 derivatives

Also Published As

Publication number Publication date
MXPA05009574A (es) 2006-05-19
DE602004027354D1 (de) 2010-07-08
BRPI0408189A (pt) 2006-03-21
KR20050106500A (ko) 2005-11-09
EP1454909A1 (en) 2004-09-08
NO20054140L (no) 2005-12-02
ATE469153T1 (de) 2010-06-15
PL1603915T3 (pl) 2010-10-29
US7294632B2 (en) 2007-11-13
CN100463908C (zh) 2009-02-25
AU2004218250A1 (en) 2004-09-16
CA2516937A1 (en) 2004-09-16
TWI320785B (en) 2010-02-21
CA2516937C (en) 2011-10-25
CY1111057T1 (el) 2015-06-11
IL170461A (en) 2011-11-30
PT1603915E (pt) 2010-07-22
KR101069984B1 (ko) 2011-10-04
AU2004218250B2 (en) 2010-02-25
EP1454909B1 (en) 2008-08-20
EA200501241A1 (ru) 2006-04-28
TW200510418A (en) 2005-03-16
WO2004078760A1 (en) 2004-09-16
JP2006519814A (ja) 2006-08-31
US7507743B2 (en) 2009-03-24
CN1777607A (zh) 2006-05-24
US20080081819A1 (en) 2008-04-03
JP4639182B2 (ja) 2011-02-23
EA008172B1 (ru) 2007-04-27
EP1603915A1 (en) 2005-12-14
NZ542135A (en) 2008-06-30
SI1603915T1 (sl) 2010-08-31
HK1085740A1 (en) 2006-09-01
ES2346311T3 (es) 2010-10-14
DK1603915T3 (da) 2010-08-30
ZA200507107B (en) 2006-11-29
EP1603915B1 (en) 2010-05-26
NO20054140D0 (no) 2005-09-06
US20060025431A1 (en) 2006-02-02

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