AR036600A1 - Derivados de 2-piridinil-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 - Google Patents

Derivados de 2-piridinil-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

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Publication number
AR036600A1
AR036600A1 ARP020103541A ARP020103541A AR036600A1 AR 036600 A1 AR036600 A1 AR 036600A1 AR P020103541 A ARP020103541 A AR P020103541A AR P020103541 A ARP020103541 A AR P020103541A AR 036600 A1 AR036600 A1 AR 036600A1
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Argentina
Prior art keywords
group
ring
alkyl group
optionally substituted
atom
Prior art date
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ARP020103541A
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English (en)
Inventor
Sebastien Gallet
Patrick Lardenois
Alistair Lochead
Alain Nedelec
Severine Marguerie
Mourad Saady
Philippe Yaiche
Franck Slowinski
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Sanofi Aventis
Mitsubishi Pharma Corp
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Priority claimed from EP01402432A external-priority patent/EP1295885A1/en
Priority claimed from EP02290489A external-priority patent/EP1340761A1/en
Application filed by Sanofi Aventis, Mitsubishi Pharma Corp filed Critical Sanofi Aventis
Publication of AR036600A1 publication Critical patent/AR036600A1/es

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    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
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    • 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
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/46—Oxygen atoms
    • C07D213/50—Ketonic radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • 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

Un derivado de pirimidona representado por la fórmula (1) o una sal del mismo, o un solvato del mismo o un hidrato del mismo, en la cual: X representa dos átomos de hidrógeno, un átomo de azufre, un átomo de oxígeno o un grupo alquilo C1-2 y un átomo de hidrógeno; Y representa un enlace, un grupo etenileno, un grupo etinileno, un átomo de oxígeno, un átomo de azufre, un grupo sulfonilo, un grupo sulfóxido, un grupo carbonilo, un grupo hidroxiiminometileno, un grupo dioxolano, un átomo de nitrógeno opcionalmente sustituido por un grupo alquilo C1-6, un grupo fenilo o un grupo bencilo; o un grupo metileno opcionalmente sustituido por uno o dos grupos elegidos entre un grupo alquilo C1-6, un grupo bencilo, un grupo hidroxilo, un grupo alcoxi C1-4, un grupo alquilo perhalogenado C1-2, un grupo amino, un grupo acetilamino o un grupo fenilo; R1 representa un anillo 2-, 3- ó 4-piridina opcionalmente sustituido por un grupo cicloalquilo C3-6, un grupo alquilo C1-4, un grupo alcoxi C1-4, un grupo bencilo o un átomo de halógeno; cuando Y representa un enlace, un grupo metileno opcionalmente sustituido, un grupo hidroxiiminometileno, un grupo dioxolano o un grupo carbonilo, entonces R2 representa un grupo alquilo C1-6 opcionalmente sustituido por un grupo hidroxi, un grupo ariloxi C6-10 o un grupo arilamino C6-10, un grupo cicloalquilo C3-6, un grupo alquiltio C1-4, un grupo alcoxi C1-4, un grupo alquilo perhalogenado C1-2, un grupo alquilo halogenado C1-3, un grupo feniltio, un grupo bencilo, un anillo fenilo, un anillo indanilo, un anillo 5,6,7,8-tetrahidronaftilo, un anillo naftilo, un anillo piridina, un anillo pirrol, un anillo tiofeno, un anillo furano o un anillo imidazol; siendo el grupo bencilo o los anillos opcionalmente sustituidos por 1 a 4 sustituyentes seleccionados entre un grupo alquilo C1-6, un grupo metilenodioxi, 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 nitro, un ciano, un amino, un grupo monoalquilamino C1-5, un grupo dialquilamino C2-10, un grupo alquilcarbonilamino C1-6, un grupo arilcarbonilamino C6-10, un grupo alquilsulfonilo C1-4, un grupo alquilsulfoniloxi C1-4 o un grupo fenilo; cuando Y representa un grupo etenileno, un grupo etinileno, un átomo de oxígeno, un átomo de azufre, un grupo sulfonilo, un grupo sulfóxido o un átomo de nitrógeno opcionalmente sustituido, entonces R2 representa un grupo alquilo C1-6 opcionalmente sustituido por un grupo hidroxi, un grupo ariloxi C6-10 o un grupo arilamino C6-10; un grupo cicloalquilo C3-6, un grupo alquilo perhalogenado C1-2, un grupo alquilo halogenado C1-3, un grupo bencilo, un anillo fenilo, un anillo indanilo, un anillo 5,6,7,8-tetrahidronaftilo, un anillo naftilo, un arilamino C6-10, un anillo piridina, un anillo pirrol, un anillo tiofeno, un anillo furano o un anillo imidazol; siendo el grupo bencilo o los anillos opcionalmente sustituidos por 1 a 4 sustituyentes seleccionados entre un grupo alquilo C1-6, un grupo metilenodioxi, 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 nitro, un ciano, un amino, un grupo monoalquilamino C1-5, un grupo dialquilamino C2-10, un grupo alquilcarbonilamino C1-6, un grupo arilcarbonilamino C6-10, un grupo alquilsulfonilo C1-4, un grupo alquilsulfoniloxi C1-4 o un grupo fenilo; R3 representa un átomo de hidrógeno, un grupo alquilo C1-6, un grupo hidroxi, un grupo alcoxi C1-4, o un átomo de halógeno; R4 representa un átomo de hidrógeno, un grupo alquilo C1-6, un grupo hidroxi, un grupo alcoxi C1-4, o un átomo de halógeno; R5 representa un átomo de hidrógeno, un grupo alquilo C1-6 o un átomo de halógeno; con la condición de que cuando R3 y R4 representan cada uno un átomo de hidrógeno, entonces R5 no es un átomo de hidrógeno; cuando m es igual a 0, p es igual a 1, 2 ó 3; cuando m es igual a 1, p es igual a 0, 1 ó 2; cuando m es igual a2, p es igual a 0 ó 1; y n representa 0 a 3. Un medicamento que comprende como ingrediente activo el derivado de pirimidona o sales del mismo, o un solvato del mismo o un hidrato del mismo; un inhibidor de la GSK3beta o la de la GSK3beta y la cdk5/p25 seleccionado entre el grupo del derivado de pirimidona representado por la fórmula (1) o sales del mismo, o un solvato del mismo o un hidrato del mismo; y sus usos para la preparación de medicamentos. El derivado de pirimidona, sal, solvato o hidrato del mismo son útiles como ingrediente activo para el tratamiento preventivo y/o terapéutico de una enfermedad neurodegenerativa provocada por la actividad anormal de la GSK3beta o la GSK3beta y la cdk5/p25, tal como la enfermedad de Alzheimer.
ARP020103541A 2001-09-21 2002-09-20 Derivados de 2-piridinil-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 AR036600A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP01402432A EP1295885A1 (en) 2001-09-21 2001-09-21 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
EP02290489A EP1340761A1 (en) 2002-02-28 2002-02-28 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

Publications (1)

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AR036600A1 true AR036600A1 (es) 2004-09-22

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ARP020103541A AR036600A1 (es) 2001-09-21 2002-09-20 Derivados de 2-piridinil-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

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US (2) US7214682B2 (es)
EP (2) EP1430057B1 (es)
JP (3) JP4570362B2 (es)
KR (1) KR100868841B1 (es)
CN (2) CN1247585C (es)
AR (1) AR036600A1 (es)
AT (2) ATE303388T1 (es)
AU (1) AU2002350487C1 (es)
BR (1) BR0212896A (es)
CA (1) CA2457965C (es)
CY (1) CY1108341T1 (es)
DE (2) DE60205921T2 (es)
DK (2) DK1430057T3 (es)
EA (1) EA006859B1 (es)
ES (2) ES2247398T3 (es)
HK (1) HK1091208A1 (es)
HU (1) HUP0500328A3 (es)
IL (2) IL160402A0 (es)
MX (1) MXPA04002629A (es)
NO (1) NO329565B1 (es)
NZ (2) NZ547205A (es)
PL (1) PL370349A1 (es)
PT (1) PT1674456E (es)
SI (1) SI1430057T1 (es)
WO (1) WO2003027116A2 (es)

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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
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)
SI2655375T1 (sl) 2010-12-23 2015-03-31 Sanofi Derivati pirimidinona, njihova priprava in njihova farmacevtska uporaba
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
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
CN109836427B (zh) * 2017-11-29 2022-04-15 暨南大学 嘧啶并嘧啶酮类化合物及其应用

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