公开(公告)号：EP1136489A1

公开(公告)日：2001-09-26

申请号：EP00400802.5

申请日：2000-03-23

申请人： SANOFI-SYNTHELABO ,  Mitsubishi-Tokyo Pharmaceuticals, Inc.

发明人： Almario-Garcia, Antonio ,  Frost, Jonathan Reid ,  Li-Tak, Adrien

IPC分类号： C07D401/14 ,  C07D401/04 ,  A61K31/506 ,  A61P25/28

CPC分类号： C07D401/04 ,  C07D401/14

摘要： The invention relates to pyrimidone derivative represented by formula (I) or a salt thereof:
   wherein:

R1 represents

* a C 6,10 aryl group,
* a heterocyclic ring having 1-4 hetero atoms selected from oxygen atom, sulfur atom, and nitrogen atom, and having total ring-constituting atoms of 5-10, or
* a C 1-6 alkyl group substituted by 1 to 3 substituents selected from

a hydroxyl group,
a C 3-6 cycloalkyl group
a C 6,10 aryl group and
a heterocyclic ring as defined above,


the C 6,10 aryl groups and heterocyclic rings being optionally substituted by 1 to 3 substituents.
The invention relates also to 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 GSK3β, such as Alzheimer's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents, brain and spinal trauma, and peripheral neuropathies.

摘要翻译： 本发明涉及由式（I）表示的嘧啶酮衍生物或其盐：其中：R1表示C6,10芳基，具有1-4个选自氧原子，硫原子和氮原子的杂原子的杂环 原子，并且具有5-10个整体构成的原子，或被1至3个选自羟基，C 3-6环烷基，C 6,10芳基和杂环的取代基取代的C 1-6烷基作为 C6,10芳基和杂环任选被1至3个取代基取代。 本发明还涉及包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3β异常活动引起的神经变性疾病，例如阿尔茨海默病，帕金森病，前额叶 痴呆，皮质基底膜变性，皮克病，脑血管意外，脑和脊髓损伤以及周围神经病变。

公开(公告)号：EP1136483A1

公开(公告)日：2001-09-26

申请号：EP00400801.7

申请日：2000-03-23

申请人： SANOFI-SYNTHELABO ,  Mitsubishi-Tokyo Pharmaceuticals, Inc.

发明人： Almario-Garcia, Antonio ,  Frost, Jonathan Reid ,  Li, Adrien-Tak ,  Ando, Ryoichi, Mitsubishi-Tokyo Pharm., Inc. ,  Shoda, Aya, Mitsubishi-Tokyo Pharmaceuticals, Inc.

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D495/04 ,  A61K31/506 ,  A61P25/28

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D495/04

摘要： A pyrimidone derivative represented by formula (I) or a salt thereof:
wherein R1 represents

* a C 6,10 aryl group,
* a heterocyclic ring having 1-4 hetero atoms selected from oxygen atom, sulfur atom, and nitrogen atom, and having total ring-constituting atoms of 5-10, or
* a C 1-6 alkyl group substituted by one C 6,10 aryl group,
the C 6,10 aryl groups and heterocyclic ring being optionally substituted by 1 to 3 substituents selected from a C 1-6 alkyl group, halogen atom, a C 1-2 perhalogenated alkyl group, a C 1-3 halogenated alkyl group, a hydroxyl group, a C 1-6 alkoxy group, methylenedioxy group, a nitro, a cyano or a phenyl group;

R2 represents a 2, 3 or 4-pyridyl group optionally substituted by a C 1-2 alkyl, group, C 1-2 alkoxy group or a halogen atom; and
n represents 1 or 2.

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 GSK3β such as Alzheimer's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents, brain and spinal trauma, and peripheral neuropathies.

摘要翻译： 由式（I）表示的嘧啶酮衍生物或其盐：其中R1表示C6,10芳基，具有1-4个选自氧原子，硫原子和氮原子的杂原子的杂环，并且具有 总环成键原子为5-10，或被一个C6,10芳基取代的C1-6烷基，C6,10芳基和杂环任选被1至3个选自C 1-6烷基的取代基取代 基团，卤素原子，C1-2全卤代烷基，C1-3卤代烷基，羟基，C1-6烷氧基，亚甲二氧基，硝基，氰基或苯基; R2表示任选被C 1-2烷基，C 1-2烷氧基或卤素原子取代的2,3或4-吡啶基; 并且n表示1或2.并且包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3β的异常活性引起的神经变性疾病，例如阿尔茨海默病，帕金森病 ，前额叶痴呆，皮质基底变性，皮克病，脑血管意外，脑和脊髓损伤以及周围神经病变。

公开(公告)号：EP1136484A1

公开(公告)日：2001-09-26

申请号：EP00400804.1

申请日：2000-03-23

申请人： SANOFI-SYNTHELABO ,  Mitsubishi-Tokyo Pharmaceuticals, Inc.

发明人： Almario-Garcia, Antonio ,  Frost, Jonathan Reid ,  Li, Adrien-Tak ,  Ando, Ryoichi, c/o Mitsubishi-Tokyo Pharm., Inc. ,  Watanabe, Kazutoshi, Mitsubishi-Tokyo Pharm., Inc.

IPC分类号： C07D401/04 ,  C07D401/14 ,  A61K31/506 ,  A61P25/28

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14

摘要： A pyrimidone derivative represented by formula (I) or a salt thereof:
wherein :

When n represents 1 to 5, then R1 represents an unsubstituted napht-1-yl group, an unsubstituted napht-2-yl group or a C 6,10 aryl group substituted by 1 to 3 substituents selected from a C 1-6 alkyl group, halogen atom, a C 1-2 perhalogenated alkyl group, a C 1-3 halogenated alkyl group, a hydroxyl group, a C 1-6 alkoxy group, methylenedioxy group, a nitro, a cyano, an amino, a C 1-6 monoalkylamino group, a C 2-12 dialkylamino group, a (C 1-6 -alkyl)carbonylamino group, a (C 6,10 -aryl)carbonylamino group, a (C 1-6 -alkoxy)carbonylamino group, aminocarbonyl group, a (C 1-6 monoalkylamino)carbonyl group, a (C 2-12 dialkylamino)carbonyl group, a formyl, a C 1-6 alkylcarbonyl group, a (C 6,10 -aryl)carbonyl group, a C 1-6 alkylsulfonyl group, a C 6,10 arylsulfonyl group, an aminosulfonyl group, a C 1-6 monoalkylaminosulfonyl group, a C 2-12 dialkylaminosulfonyl group, or a phenyl group;the C 1-6 alkyl groups and the C 1-6 alkoxy groups being optionally substituted; or
When n represents 4 or 5 then R1 can represent an unsubstituted phenyl group;
R2 represents a hydrogen atom or a C 1-6 alkyl; and
R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C 1-4 alkyl, group, C 1-4 alkoxy group or a halogen atom.

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 GSK3β.

摘要翻译： 由式（I）表示的嘧啶酮衍生物或其盐：其中：当n表示1至5时，则R1表示未取代的萘-1-基，未取代的萘-2-基或C6， 被1〜3个选自C 1-6烷基，卤素原子，C1-2全卤代烷基，C 1-3卤代烷基，羟基，C 1-6烷氧基，亚甲二氧基 ，硝基，氰基，氨基，C 1-6单烷基氨基，C 2-12二烷基氨基，（C 1-6 - 烷基）羰基氨基，（C 6-10芳基）羰基氨基，（C1- 羰基氨基，氨基羰基，（C1-6单烷基氨基）羰基，（C2-12二烷基氨基）羰基，甲酰基，C1-6烷基羰基，（C6,10-芳基）羰基 ，C 1-6烷基磺酰基，C 6,10芳基磺酰基，氨基磺酰基，C 1-6单烷基氨基磺酰基，C 2-12二烷基氨基磺酰基或苯基; C 1-6烷基和C 1-6烷基 烷氧基任选被取代; 或当n表示4或5时，则R1可以表示未取代的苯基; R2表示氢原子或C1-6烷基; 并且R 3表示任选被C 1-4烷基，C 1-4烷氧基或卤素原子取代的2,3或4-吡啶基。 以及包含所述衍生物或其盐作为活性成分的药物，其用于由GSK3β的异常活性引起的神经变性疾病的预防和/或治疗性治疗。

公开(公告)号：EP1136099A1

公开(公告)日：2001-09-26

申请号：EP00400805.8

申请日：2000-03-23

申请人： SANOFI-SYNTHELABO ,  Mitsubishi-Tokyo Pharmaceuticals, Inc.

发明人： Almario-Garcia, Antonio ,  Frost, Jonathan Reid ,  Li, Adrien-Tak

IPC分类号： A61P25/28 ,  C07D401/14 ,  A61K31/505

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14

摘要： A pyrimidone derivative represented by formula (I) or a salt thereof:
wherein:

R1 represents a hydrogen atom or a C 1-6 alkyl group;
R2 represents a hydrogen atom or a C 1-6 alkyl group;
R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C 1-4 alkyl group, a C 1-4 alkoxy group or a halogen atom;
R4 represents a hydrogen atom, a C 1-6 alkyl group, a halogen atom, a C 1-2 perhalogenated alkyl group, a C 1-3 halogenated alkyl group, a hydroxyl group, a C 1-6 alkoxy group, methylenedioxy group, a nitro, a cyano, an amino, a C 1-6 monoalkylamino group, C 2-12 dialkylamino group, a C 1-6 alkylcarbonylamino group, C 6-10 arylcarbonylamino group, a phenyl group or a benzyloxy group; and
n represents 1 to 5.

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 GSK3β such as Alzheimer's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents, brain and spinal cord trauma and peripheral neuropathies.

摘要翻译： 由式（I）表示的嘧啶酮衍生物或其盐：其中：R1表示氢原子或C1-6烷基; R2表示氢原子或C 1-6烷基; R 3表示任选被C 1-4烷基，C 1-4烷氧基或卤素原子取代的2,3或4-吡啶基; R4表示氢原子，C1-6烷基，卤素原子，C1-2全卤代烷基，C1-3卤代烷基，羟基，C1-6烷氧基，亚甲二氧基，硝基， 氰基，氨基，C 1-6单烷基氨基，C 2-12二烷基氨基，C 1-6烷基羰基氨基，C 6-10芳基羰基氨基，苯基或苄氧基; 并且n表示1至5.并且包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3β的异常活性引起的神经变性疾病，例如阿尔茨海默氏病，帕金森病 ，前额叶痴呆，皮质基底变性，皮克病，脑血管意外，脑和脊髓创伤和周围神经病变。

公开(公告)号：EP1136491A1

公开(公告)日：2001-09-26

申请号：EP00400806.6

申请日：2000-03-23

申请人： SANOFI-SYNTHELABO ,  Mitsubishi-Tokyo Pharmaceuticals, Inc.

发明人： Almario-Garcia, Antonio ,  Frost, Jonathan Reid ,  Li, Adrien-Tak

IPC分类号： C07D405/14 ,  C07D409/14 ,  C07D401/14 ,  A61K31/506 ,  A61P25/28

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

摘要： The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof:
wherein:

R1 represents a hydrogen atom or a C 1-6 alkyl group;
R2 represents a furan ring, thiophene ring, pyrrole ring or imidazole ring, the rings being optionally substituted by 1 to 3 substituents selected from a C 1-6 alkyl group, a halogen atom, a C 1 - 2 perhalogenated alkyl group, a C 1 - 3 halogenated alkyl group, a hydroxyl group, a C 1-6 alkoxy group, a nitro, a cyano an amino, a C 1-6 monoalkylamino group, a C 2-10 dialkylamino group, a C 1-6 alkylcarbonylamino group, a C 6,10 arylcarbonylamino group or a phenyl group;
R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C 1-4 alkyl, group, C 1-4 alkoxy group or a halogen atom;
n represents 1 to 5.

The invention relates also to 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 GSK3β such as Alzheimer's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents, brain and spinal trauma, and peripheral neuropathies.

摘要翻译： 本发明涉及由式（I）表示的嘧啶酮衍生物或其盐：其中：R1表示氢原子或C1-6烷基; R 2表示呋喃环，噻吩环，吡咯环或咪唑环，所述环任选被1〜3个选自C 1-6烷基，卤素原子，C 1-2-2全卤代烷基，C 1-3 卤代烷基，羟基，C 1-6烷氧基，硝基，氰基氨基，C 1-6单烷基氨基，C 2-10二烷基氨基，C 1-6烷基羰基氨基，C 6-10芳基羰基氨基 或苯基; R3表示任选被C 1-4烷基，C 1-4烷氧基或卤素原子取代的2,3或4-吡啶基; 本发明还涉及包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3β异常活动引起的神经变性疾病如阿尔茨海默病 帕金森病，前额叶痴呆，皮质基底变性，皮克病，脑血管意外，脑和脊髓损伤以及周围神经病变。

公开(公告)号：EP1136486A1

公开(公告)日：2001-09-26

申请号：EP00400808.2

申请日：2000-03-23

申请人： SANOFI-SYNTHELABO ,  Mitsubishi-Tokyo Pharmaceuticals, Inc.

发明人： Almario-Garcia, Antonio ,  Frost, Jonathan Reid ,  Li, Adrien-Tak

IPC分类号： C07D401/04 ,  A61K31/506 ,  A61P25/28

CPC分类号： C07D401/04

摘要： The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof:
wherein

R1 represents a hydrogen atom or a C 1-6 alkyl group;
R2 represents a hydrogen atom or 1 to 3 substituents selected from a C 1-6 alkyl group, halogen atom, a C 1-2 perhalogenated alkyl group, a C 1-3 halogenated alkyl group, a hydroxyl group, a C 1-6 alkoxy group, methylenedioxy group, a nitro, a cyano, an amino, a C 1-6 monoalkylamino group, C 2-10 dialkylamino group ; C 1-6 alkylcarbonylamino group, C 6,10 arylcarbonylamino group;
R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C 1-4 alkyl group, C 1-4 alkoxy group or a halogen atom and n represents 0 or 1, when n represents 0 then m is 2 or 3, and when n represents 1 then m is 1 or 2.

The invention relates also to 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 GSK3β such as Alzheimer's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents and brain and spinal trauma and peripheral neuropathies.

摘要翻译： 本发明涉及由式（I）表示的嘧啶酮衍生物或其盐：其中R1表示氢原子或C1-6烷基; R2表示氢原子或1〜3个选自C 1-6烷基，卤素原子，C1-2全卤代烷基，C1-3卤代烷基，羟基，C1-6烷氧基， 亚甲二氧基，硝基，氰基，氨基，C 1-6单烷基氨基，C 2-10二烷基氨基; C 1-6烷基羰基氨基，C 6,10芳基羰基氨基; R3表示任选被C 1-4烷基，C 1-4烷氧基或卤素原子取代的2,3或4-吡啶基，n表示0或1，当n表示0时，m表示2或3，当 n表示1，则m为1或2.本发明还涉及包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3β的异常活性引起的神经变性疾病 如阿尔茨海默病，帕金森病，前额叶痴呆，皮质基底变性，皮克病，脑血管意外以及脑和脊髓创伤及周围神经病变。

公开(公告)号：EP1184383A1

公开(公告)日：2002-03-06

申请号：EP00402410.5

申请日：2000-09-01

申请人： SANOFI-SYNTHELABO ,  Mitsubishi-Tokyo Pharmaceuticals, Inc.

发明人： Almario-Garcia, Antonio ,  Li, Adrien-Tak ,  Lochead, Alistair ,  Marguerie, Séverine ,  Saady, Mourad ,  Yaiche, Philippe

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/00

CPC分类号： C07D487/04

摘要： The invention relates to a 6,7,8,9-tetrahydropyrimido [1,2- a ] pyrimidone derivative represented by formula (I) or a salt thereof:
wherein:

X represents hydrogen atoms, a sulphur atom or an oxygen atom;
Y represents a bond, a double bond, a triple bond, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxyde group, a carbonyl group, a nitrogen atom being optionally substituted by a C 1-6 alkyl group, a phenyl or a benzyl group; or a methylene group optionally substituted by one or two substituents;
R1 represents a 2, 3 or 4-pyridyl group optionally substituted by a C 1-4 alkyl group, a C 1-4 alkoxy group or a halogen atom;

when Y represents a bond, a methylene group optionally substituted or a carbonyl group then R2 represents a C 1-6 alkyl group, a C 1-4 alkylthio group, a C 1-4 alkoxy group, a C 3-6 cycloalkyl group, a naphthyl group, a phenylthio group, a benzyl group, a phenyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring ; the benzyl group, the phenyls, the naphthyl or the rings being optionally substituted by 1 to 3 substituents;
when Y represents a double bond, a triple bond, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxyde group or a nitrogen atom being optionally substituted then R2 represents a C 1-6 alkyl group, a C 3-6 cycloalkyl group, a naphthyl group, a benzyl group, a phenyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group or the phenyls, the naphthyl or the rings being optionally substituted by 1 to 3 substituents ;

and n represents 0 to 3.

The invention relates also to 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 GSK3β.

摘要翻译： 本发明涉及由式（I）表示的6,7,8,9-四氢嘧啶并嘧啶酮衍生物或其盐：其中：X表示氢原子，硫原子或氧原子; Y表示键，双键，三键，氧原子，硫原子，磺酰基，亚砜基，羰基，任选被C 1-6烷基取代的氮原子，苯基或 苄基; 或任选被一个或两个取代基取代的亚甲基; R1表示任选被C 1-4烷基，C 1-4烷氧基或卤素原子取代的2,3或4-吡啶基; 当Y表示键，亚甲基任意取代或羰基时，则R2表示C1-6烷基，C1-4烷硫基，C1-4烷氧基，C3-6环烷基，萘基， 苯硫基，苄基，苯环，吡啶环，吲哚环，吡咯环，噻吩环，呋喃环或咪唑环; 苄基，苯基，萘基或环任选被1至3个取代基取代; 当Y表示双键时，任选被取代的三键，氧原子，硫原子，磺酰基，亚砜基或氮原子，则R2表示C1-6烷基，C3-6环烷基， 萘基，苄基，苯环，吡啶环，吲哚环，吡咯环，噻吩环，呋喃环或咪唑环，苄基或苯基，萘基或环任选地 被1-3个取代基取代; 并且n表示0至3.本发明还涉及包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3β的异常活性引起的神经变性疾病。

公开(公告)号：EP1136493A1

公开(公告)日：2001-09-26

申请号：EP00400803.3

申请日：2000-03-23

申请人： SANOFI-SYNTHELABO ,  Mitsubishi-Tokyo Pharmaceuticals, Inc.

发明人： Almario-Garcia, Antonio ,  Frost, Jonathan Reid ,  Li, Adrien-Tak

IPC分类号： C07D495/04 ,  A61K31/513 ,  C07D471/04 ,  C07D401/14 ,  C07D491/04 ,  A61P25/28 ,  A61P25/16

CPC分类号： C07D401/14 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04

摘要： A pyrimidone derivative represented by formula (I) or a salt thereof:
wherein:
R1 represents a pyridyl ring optionally substituted by a C 1-4 alkyl group, C 1-4 alkoxy group or a halogen atom, and The heterocyclic ring of formula :
is selected from the group : 2,3,4,9-tetrahydro-1 H -pyrido[3,4- b ]indole, 1,2,3,4-tetrahydroisoquinoline, 4,5,6,7-tetrahydrothieno[2,3- c ]pyridine or 4,5,6,7-tetrahydrofuro[2,3- c ]pyridine.
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 GSK3β such as Alzheimer's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents, brain and spinal trauma, and peripheral neuropathies.

摘要翻译： 式（I）表示的嘧啶酮衍生物或其盐：其中：R 1表示任选被C 1-4烷基，C 1-4烷氧基或卤素原子取代的吡啶基，式 ：选自2,3,4,9-四氢-1H-吡啶并[3,4-b]吲哚，1,2,3,4-四氢异喹啉，4,5,6,7-四氢噻吩并[ cu吡啶或4,5,6,7-四氢呋喃并[2,3-c]吡啶。 以及包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3β的异常活性引起的神经变性疾病，例如阿尔茨海默氏病，帕金森氏病，前额叶痴呆，皮质基底变性， 皮克病，脑血管意外，脑和脊髓损伤以及周围神经病变。

公开(公告)号：EP1136482A1

公开(公告)日：2001-09-26

申请号：EP00400800.9

申请日：2000-03-23

申请人： SANOFI-SYNTHELABO ,  Mitsubishi-Tokyo Pharmaceuticals, Inc.

发明人： Almario-Garcia, Antonio ,  Frost, Jonathan Reid ,  Li, Adrien-Tak ,  Ando, Ryoichi ,  Watanabe, Kazutoshi

IPC分类号： C07D401/04 ,  A61K31/505 ,  A61P25/28

CPC分类号： A61K31/505 ,  C07D401/04 ,  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 C 1-6 alkyl group;
R2 represents a C 1-6 alkyl group which may be substituted, a C 2-6 alkenyl group which may be substituted, a C 3-6 alkynyl group which may be substituted, a C 3-6 cycloalkyl group which may be substituted, or a C 6-10 ARYL group which may be substituted;
or R1 and R2 form together a C 2-6 alkylene group which may be substituted;
or R1 and R2 form together a chain of formula -(CH 2 ) 2 -X-(CH 2 ) 2 - or
-(CH 2 ) 2 -X-(CH 2 ) 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 C 1-4 alkyl group, C 1-4 alkoxy group or a halogen atom; and
R4 represents a C 1-6 alkyl group optionally substituted by a C 6,10 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 GSK3β such as Alzheimer's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents, brain and spinal trauma, and peripheral neuropathies.

摘要翻译： 由式（I）表示的嘧啶酮衍生物或其盐：其中：R1表示氢原子或C1-6烷基; R 2表示可被取代的C 1-6烷基，可被取代的C 2-6烯基，可被取代的C 3-6炔基，可被取代的C 3-6环烷基，或C 6〜 10可以替代的ARYL组; 或R 1和R 2一起形成可被取代的C 2-6亚烷基; 或者R 1和R 2一起形成式 - （CH 2）2 -X-（CH 2）2 - 或 - （CH 2）2 -X-（CH 2）3 - 的链，其中X表示氧原子，硫原子或 可被取代的氮原子; R3表示任选被C 1-4烷基，C 1-4烷氧基或卤素原子取代的2,3或4-吡啶基; 并且R 4表示任选被可被取代的C 6,10芳基取代的C 1-6烷基。 以及包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3β的异常活性引起的神经变性疾病，例如阿尔茨海默氏病，帕金森氏病，前额叶痴呆，皮质基底变性， 皮克病，脑血管意外，脑和脊髓损伤以及周围神经病变。