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1. 发明专利

JP2001270884A PYRIMIDONE DERIVATIVE 失效
公开(公告)号：JP2001270884A
公开(公告)日：2001-10-02
申请号：JP2000081938
申请日：2000-03-23
申请人： MITSUBISHI TOKYO PHARM INC , SANOFI SYNTHELABO
发明人： ANDO RYOICHI , WATANABE KAZUTOSHI , SAITO KENICHI
IPC分类号： C07D401/14 , A61K31/506 , A61P9/00 , A61P9/10 , A61P25/00 , A61P25/16 , A61P25/28 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To obtain a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal advance of a tau protein kinase 1 such as neurodegenerative diseases (e.g. Alzheimer disease), and the like, containing a pyrimidone derivative or its salt as an active ingredient. SOLUTION: This pyrimidone derivative is represented by formula (I) [wherein R1 is hydrogen atom or a 1-5C alkyl group; X is a pyridine ring which may be substituted; (n) is an integer of 1-10] or a salt thereof, or a solvate thereof or a hydrate thereof.

3. 发明专利

AU8148701A 2-amino-3-(alkyl)-pyrimidone derivatives as GSK3.beta. inhibitors 未知
公开(公告)号：AU8148701A
公开(公告)日：2001-10-03
申请号：AU8148701
申请日：2001-03-22
申请人： SANOFI SYNTHELABO , MITSUBISHI TOKYO PHARM INC
发明人： GARCIA ANTONIO ALMARIO , ANDO RYOICHI , ARITOMO KEIICHI , FROST JONATHAN REID , LI ADRIEN TAK , SHODA AYA , UEHARA FUMIAKI , WATANABE KAZUTOSHI
IPC分类号： A61K31/505 , A61K31/506 , A61P3/04 , A61P3/10 , A61P5/00 , A61P9/00 , A61P11/00 , A61P15/00 , A61P17/02 , A61P17/14 , A61P19/00 , A61P25/00 , A61P25/02 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/28 , A61P27/02 , A61P27/06 , A61P31/12 , A61P35/00 , A61P35/02 , A61P43/00 , C07D401/04 , C07D401/14 , C07D409/14 , A61K31/305
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein : R1 represents a hydrogen atom or a C1-6 alkyl group; R2 represents a C1-6 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula -(CH2)2-X-(CH2)2- or -(CH2)2 -X-(CH2)3- where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; and R4 represents a C1-6 alkyl group optionally substituted by a C6,10 aryl group which may be substituted. And a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3 beta such as Alzheimer's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents, brain and spinal trauma, and peripheral neuropathies.

4. 发明专利

AU1734401A Carboxyamido derivatives 未知
公开(公告)号：AU1734401A
公开(公告)日：2001-06-18
申请号：AU1734401
申请日：2000-12-08
申请人： MITSUBISHI TOKYO PHARM INC
发明人： ANDO RYOICHI , ARITOMO KEIICHI , SHODA AYA , WATANABE KAZUTOSHI , UEHARA FUMIAKI , SAITO KENICHI
IPC分类号： A61P7/04 , C07D235/02 , C07D235/26 , C07D401/12 , A61K31/4184

5. 发明专利

PL368816A1 3-SUBSTITUTED-4-PYRIMIDONE DERIVATIVES 未知
公开(公告)号：PL368816A1
公开(公告)日：2005-04-04
申请号：PL36881602
申请日：2002-09-20
申请人： MITSUBISHI PHARMA CORP , SANOFI SYNTHELABO
发明人： UEHARA FUMIAKI , ARITOMO KEIICHI , SHODA AYA , HIKI SHINSUKE , OKUYAMA MASAHIRO , USUI YOSHIHIRO , OOIZUMI MITSURU , WATANABE KAZUTOSHI
IPC分类号： C07D239/36 , A61K31/513 , A61K31/5377 , A61K31/5386 , A61P3/04 , A61P3/10 , A61P17/14 , A61P25/02 , A61P25/16 , A61P25/18 , A61P25/28 , A61P27/02 , A61P27/06 , A61P35/00 , A61P35/02 , A61P43/00 , C07D239/34 , C07D239/40 , C07D239/46 , C07D239/56 , C07D401/04 , C07D401/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D498/10 , A61K31/505
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R1 represents a C1-C12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group; R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.

6. 发明专利

CA2460177A1 3-SUBSTITUTED-4-PYRIMIDONE DERIVATIVES 未知
公开(公告)号：CA2460177A1
公开(公告)日：2003-04-03
申请号：CA2460177
申请日：2002-09-20
申请人： MITSUBISHI PHARMA CORP , SANOFI SYNTHELABO
发明人： SHODA AYA , HIKI SHINSUKE , OKUYAMA MASAHIRO , ARITOMO KEIICHI , UEHARA FUMIAKI , OOIZUMI MITSURU , WATANABE KAZUTOSHI , USUI YOSHIHIRO
IPC分类号： C07D239/36 , A61K31/513 , A61K31/5377 , A61K31/5386 , A61P3/04 , A61P3/10 , A61P17/14 , A61P25/02 , A61P25/16 , A61P25/18 , A61P25/28 , A61P27/02 , A61P27/06 , A61P35/00 , A61P35/02 , A61P43/00 , C07D239/34 , C07D239/40 , C07D239/46 , C07D239/56 , C07D401/04 , C07D401/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D498/10 , A61K31/505
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1:wherein R1 represents a C1-C12 alkyl group which may be substituted;R represents, for example, a group represented by the following formula (II):wherein R2 and R3 independently represent a hydrogen atom or a C1- C8 alkyl group; R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.

7. 发明专利

CA2460177C 3-SUBSTITUTED-4-PYRIMIDONE DERIVATIVES 未知
公开(公告)号：CA2460177C
公开(公告)日：2010-03-23
申请号：CA2460177
申请日：2002-09-20
申请人： MITSUBISHI PHARMA CORP , SANOFI SYNTHELABO
发明人： UEHARA FUMIAKI , ARITOMO KEIICHI , SHODA AYA , HIKI SHINSUKE , OKUYAMA MASAHIRO , USUI YOSHIHIRO , OOIZUMI MITSURU , WATANABE KAZUTOSHI
IPC分类号： C07D239/36 , C07D413/14 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/5386 , A61P3/04 , A61P3/10 , A61P17/14 , A61P25/02 , A61P25/16 , A61P25/18 , A61P25/28 , A61P27/02 , A61P27/06 , A61P35/00 , A61P35/02 , A61P43/00 , C07D239/34 , C07D239/40 , C07D239/46 , C07D239/47 , C07D239/56 , C07D401/04 , C07D401/14 , C07D413/04 , C07D417/14 , C07D498/10
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1:wherein R1 represents a C1-C12 alkyl group which may be substituted;R represents, for example, a group represented by the following formula (II):wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group; R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.

8. 发明专利

DE60131844D1 未知
公开(公告)号：DE60131844D1
公开(公告)日：2008-01-24
申请号：DE60131844
申请日：2001-03-22
申请人： SANOFI SYNTHELABO , MITSUBISHI PHARMA CORP
发明人： ALMARIO GARCIA ANTONIO , ANDO RYOICHI , ARITOMO KEIICHI , FROST JONATHAN REID , LI ADRIEN TAK , SHODA AYA , UEHARA FUMIAKI , WATANABE KAZUTOSHI
IPC分类号： C07D401/04 , A61K31/505 , A61K31/506 , A61P3/04 , A61P3/10 , A61P5/00 , A61P9/00 , A61P11/00 , A61P15/00 , A61P17/02 , A61P17/14 , A61P19/00 , A61P25/00 , A61P25/02 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/28 , A61P27/02 , A61P27/06 , A61P31/12 , A61P35/00 , A61P35/02 , A61P43/00 , C07D401/14 , C07D409/14
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein : R1 represents a hydrogen atom or a C1-6 alkyl group; R2 represents a C1-6 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula -(CH2)2-X-(CH2)2- or -(CH2)2 -X-(CH2)3- where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; and R4 represents a C1-6 alkyl group optionally substituted by a C6,10 aryl group which may be substituted. And a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3 beta such as Alzheimer's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents, brain and spinal trauma, and peripheral neuropathies.

9. 发明专利

PL368671A1 3-SUBSTITUTED-4-PYRIMIDONE DERIVATIVES 未知
公开(公告)号：PL368671A1
公开(公告)日：2005-04-04
申请号：PL36867102
申请日：2002-09-20
申请人： MITSUBISHI PHARMA CORP , SANOFI SYNTHELABO
发明人： UEHARA FUMIAKI , ARITOMO KEIICHI , SHODA AYA , HIKI SHINSUKE , OKUYAMA MASAHIRO , USUI YOSHIHIRO , OOIZUMI MITSURU , WATANABE KAZUTOSHI , YAMAKOSHI KOICHI
IPC分类号： C07D239/40 , A61K31/513 , A61K31/5377 , A61K31/5386 , A61P3/04 , A61P3/10 , A61P9/10 , A61P17/14 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P35/00 , A61P35/02 , A61P43/00 , C07D239/34 , C07D239/46 , C07D239/56 , C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D498/10 , A61K31/505
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R 1 represents a C 1 -C 12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein R 2 and R 3 independently represent a hydrogen atom or a C 1 -C 8 alkyl group; R 4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.

10. 发明专利

AR036604A1 DERIVADOS DE 4-PIRIMIDONA 3-SUSTITUIDA 未知
公开(公告)号：AR036604A1
公开(公告)日：2004-09-22
申请号：ARP020103547
申请日：2002-09-20
申请人： MITSUBISHI PHARMA CORP , SANOFI SYNTHELABO
发明人： UEHARA FUMIAKI , SHODA AYA , HIKI SHINSUKE , OKUYAMA MASAHIRO , OOIZUMI MITSURU , WATANABE KAZUTOSHI , USUI YOSHIHIRO , ARITOMO KEIICHI
IPC分类号： C07D239/36 , A61K31/513 , A61K31/5377 , A61K31/5386 , A61P3/04 , A61P3/10 , A61P17/14 , A61P25/02 , A61P25/16 , A61P25/18 , A61P25/28 , A61P27/02 , A61P27/06 , A61P35/00 , A61P35/02 , A61P43/00 , C07D239/34 , C07D239/40 , C07D239/46 , C07D239/56 , C07D401/04 , C07D401/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D498/10 , A61K31/505
摘要： Un derivado de pirimidona representado por la fórmula (1) o una sal del mismo, o un solvato del mismo, o un hidrato del mismo que tiene una actividad inhibidora contra la cinasa proteínica tau 1. También se reivindican un medicamento y un inhibidor de la cinasa proteínica tau 1. Dicho medicamento se usa para el tratamiento preventivo y/o terapéutico de una enfermedad causada por la hiper actividad de la cinasa proteínica tau 1, tales como: mal de Alzheimer, accidentes cerebrovasculares isquémicos, síndrome de Down, complejo de demencia y parkinsonismo de Guam, demencia vascular, danos traumáticos, traumas cerebrales y de la médula espinal, retinopatía y glaucoma. Reivindicación 1: Un derivado de pirimidona representado por la fórmula (1) o una sal del mismo, o un solvato del mismo, o un hidrato del mismo, caracterizada porque R1 representa un grupo alquilo C1-12 que puede ser sustituido; R representa cualquiera de los grupos representados por las siguientes fórmulas (2) a (5) caracterizadas porque R2 y R3 independientemente representan un átomo de hidrógeno o un grupo alquilo C1-8; R4 representa un anillo de benceno que puede ser sustituido, un anillo de naftaleno que puede ser sustituido, un anillo de indano que puede ser sustituido, un anillo de tetrahidronaftaleno que puede ser sustituido, o un anillo heterocíclico opcionalmente sustituido que tiene de 1 a 4 heteroátomos seleccionados del grupo que consiste de un átomo de oxígeno, un átomo de azufre, un átomo de nitrógeno, y tiene de 5 a 10 átomos, en total. R5 representa un grupo alquilo C1-8 que puede ser sustituido, un grupo cicloalquilo C3-8 que puede ser sustituido, un anillo de benceno que puede ser sustituido, un anillo de naftaleno que puede ser sustituido, un anillo de indano que puede ser sustituido, un anillo de tetrahidronaftaleno que puede ser sustituido, o un anillo heterocíclico opcionalmente sustituido que tiene de 1 a 4 heteroátomos seleccionados del grupo que consiste de un átomo de oxígeno, un átomo de azufre, un átomo de nitrógeno, y tiene de 5 a 10 átomos, en total. R6 representa un átomo de hidrógeno, un grupo alquilo C1-8 que puede ser sustituido, un anillo de benceno que puede ser sustituido; ó R5 y R6 pueden unirse para formar, junto con el carbono al cual se unen, un anillo espiro cíclico opcionalmente sustituido, que tiene de 3 a 11 átomos, en total, que constituyen el anillo; R7 y R8 independientemente representan un átomo de hidrógeno, o un grupo alquilo C1-8, o R7 y R8 pueden combinarse para formar un grupo alquileno C2-6; R9 y R10 representan un grupo alquilo C1-8 que puede ser sustituido, un grupo cicloalquilo C3-8 que puede ser sustituido, un anillo de benceno que puede ser sustituido, un anillo de naftaleno que puede ser sustituido, o un anillo heterocíclico opcionalmente sustituido que tiene de 1 a 4 heteroátomos seleccionados del grupo que consiste de un átomo de oxígeno, un átomo de azufre, un átomo de nitrógeno, y tiene de 5 a 10 átomos, en total, o R9 y R10 representan -N(R11)R12) caracterizados porque R11 representa un átomo de hidrógeno, un grupo alquilo C1-8; y R12 representa un grupo alquilo C1-8, un anillo de benceno que puede ser sustituido, un anillo de naftaleno que puede ser sustituido, o un anillo heterocíclico opcionalmente sustituido que tiene de 1 a 4 heteroátomos seleccionados del grupo que consiste de un átomo de oxígeno, un átomo de azufre, un átomo de nitrógeno, y que tiene de 5 a 10 átomos en total, que constituyen el anillo; y X representa CH2, O ó NR13 caracterizados porque R13 representa un átomo de hidrógeno o un grupo alquilo C1-8.

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