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1. 发明授权

US07378413B2 2-amino-3-(alkyl)-pyrimidone derivatives 失效
标题翻译： 2-氨基-3-（烷基） - 嘧啶酮衍生物
公开(公告)号：US07378413B2
公开(公告)日：2008-05-27
申请号：US11035264
申请日：2005-01-13
申请人： Antonio Almario Carcia , Ryoichi Ando , Keiichi Arimoto , Fumiaki Uehara , Adrien Tak Li , Aya Shoda , Jonathan Reid Frost , Kazutoshi Watanabe
发明人： Antonio Almario Carcia , Ryoichi Ando , Keiichi Arimoto , Fumiaki Uehara , Adrien Tak Li , Aya Shoda , Jonathan Reid Frost , Kazutoshi Watanabe
IPC分类号： A61K31/505 , C07D401/04
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 C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 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 halogen atom; and R4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or 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 GSK3β such as Alzheimer's disease.
摘要翻译：由式（I）表示的嘧啶酮衍生物或其盐：其中R1表示氢原子或可以被C 6-10取代的C 1-6烷基， / SUB>芳基; R 2表示可以被取代的C 1-10烷基，可以被取代的C 2-6亚烷基，C 3-6亚烷基，可以被取代的亚炔基，可被取代的C 3-6亚烷基或可以被取代的C 6〜6-亚芳基; 或者R 1和R 2一起形成可以被取代的C 2-6亚烷基; 或者R 1和R 2一起形成式 - （CH 2 CH 2）2 - （CH 2）2 - 或 - （CH 2）2 -X-（CH 2）3 - - 其中X表示氧原子，硫原子或可被取代的氮原子; 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; 并且R 4表示任选被羟基，氨基，C 1-6 - 单烷基氨基，C 2-12-12任意取代的C 1-10烷基。 >可以被取代的二烷基氨基或C 6,10 芳基。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如阿尔茨海默氏病的异常活性引起的神经变性疾病的预防和/或治疗性治疗。

2. 发明授权

US07427615B2 3-substituted-4-pyrimidone derivatives 有权
标题翻译： 3-取代-4-嘧啶酮衍生物
公开(公告)号：US07427615B2
公开(公告)日：2008-09-23
申请号：US10489606
申请日：2002-09-20
申请人： Fumiaki Uehara , Keiichi Aritomo , Aya Shoda , Shinsuke Hiki , Masahiro Okuyama , Yoshihiro Usui , Mitsuru Ooizumi , Kazutoshi Watanabe , Koichi Yamakoshi
发明人： Fumiaki Uehara , Keiichi Aritomo , Aya Shoda , Shinsuke Hiki , Masahiro Okuyama , Yoshihiro Usui , Mitsuru Ooizumi , Kazutoshi Watanabe , Koichi Yamakoshi
IPC分类号： C07D401/04 , C07D401/14 , A61K31/505
CPC分类号： C07D401/04 , C07D239/34 , C07D239/47 , C07D239/56 , C07D401/14 , C07D413/14
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.
摘要翻译：由式（I）表示的嘧啶酮衍生物或其盐，或其溶剂合物或其水合物对tau蛋白激酶1具有抑制活性：其中R 1表示C 1〜可以被取代的C 1 -C 12烷基; R表示例如由下式（II）表示的基团：其中R 2和R 3独立地表示氢原子或C 1〜 C 1 -C 8烷基; R 4表示可以被取代的苯环，可以被取代的萘环，可以被取代的茚满环，可被取代的四氢萘环，或具有1个的任选取代的杂环至4个选自氧原子，硫原子和氮原子的杂原子，并且总共具有5至10个环构成原子。

3. 发明申请

US20060252768A1 2,3,6-Trisubstituted-4-pyrimidone derivatives 失效
标题翻译： 2,3,6-三取代-4-嘧啶酮衍生物
公开(公告)号：US20060252768A1
公开(公告)日：2006-11-09
申请号：US10550299
申请日：2004-03-26
申请人： Kazutoshi Watanabe , Fumiaki Uehara , Shinsuke Hiki , Satoshi Yokoshima , Yoshihiro Usui , Masahiro Okuyama , Aya Shoda , Keiichi Aritomo , Toshiyuki Kohara , Kenji Fukunaga
发明人： Kazutoshi Watanabe , Fumiaki Uehara , Shinsuke Hiki , Satoshi Yokoshima , Yoshihiro Usui , Masahiro Okuyama , Aya Shoda , Keiichi Aritomo , Toshiyuki Kohara , Kenji Fukunaga
IPC分类号： A61K31/513 , C07D403/14
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof; useful for prventive and/or therapeutic treatment of diseass such as neurodegenerative diseases (e.g. Alzheimer disease); wherein Q represents CH or nitrogen atom; R represents a C1-C12 alkyl group; the ring of Formula (I): represents piperazine ring or piperidine ring; each X independently represents a C1-C8 alkyl group, an optionally partially hydrogenated C6-C10 aryl ring, an indan ring or the like; m represents an integer of 1 to 3; each independently represents a halogen atom, a hydroxy group, a cyano group, a C1-C6 alkyl group or the like; n represents an integer of 0 to 8; when X and Y or two Y groups are attached on the same carbon atom, they may combine to each other to form a C2-C6 alkylene group.
摘要翻译：具有由式（I）表示的tau蛋白激酶1抑制活性的嘧啶酮衍生物或其盐或其溶剂合物或其水合物; 可用于疾病的预防和/或治疗性治疗，例如神经变性疾病（例如阿尔茨海默病）; 其中Q表示CH或氮原子; R表示C 1 -C 12烷基; 式（I）的环表示哌嗪环或哌啶环; 每个X独立地表示C 1 -C 8烷基，任选部分氢化的C 6 -C 10烷基，芳环，茚满环等; m表示1〜3的整数，各自独立地表示卤素原子，羟基，氰基，C 1 -C 6烷基等; n表示0〜8的整数，当X和Y或两个Y基团连接在同一个碳原子上时，它们可以彼此结合形成C 2 -C 6亚烷基。

4. 发明授权

US07504411B2 2,3,6-Trisubstituted-4-pyrimidone derivatives 失效
标题翻译： 2,3,6-三取代-4-嘧啶酮衍生物
公开(公告)号：US07504411B2
公开(公告)日：2009-03-17
申请号：US10550299
申请日：2004-03-26
申请人： Kazutoshi Watanabe , Fumiaki Uehara , Shinsuke Hiki , Satoshi Yokoshima , Yoshihiro Usui , Masahiro Okuyama , Aya Shoda , Keiichi Aritomo , Toshiyuki Kohara , Kenji Fukunaga
发明人： Kazutoshi Watanabe , Fumiaki Uehara , Shinsuke Hiki , Satoshi Yokoshima , Yoshihiro Usui , Masahiro Okuyama , Aya Shoda , Keiichi Aritomo , Toshiyuki Kohara , Kenji Fukunaga
IPC分类号： C07D401/14 , C07D403/14 , A61K31/496 , A61K31/506 , A61P3/10 , A61P25/28
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof; useful for prventive and/or therapeutic treatment of diseass such as neurodegenerative diseases (e.g. Alzheimer disease); wherein Q represents CH or nitrogen atom; R represents a C1-C12 alkyl group; the ring of Formula (I): represents piperazine ring or piperidine ring; each X independently represents a C1-C8 alkyl group, an optionally partially hydrogenated C6-C10 aryl ring, an indan ring or the like; m represents an integer of 1 to 3; each independently represents a halogen atom, a hydroxy group, a cyano group, a C1-C6 alkyl group or the like; n represents an integer of 0 to 8; when X and Y or two Y groups are attached on the same carbon atom, they may combine to each other to form a C2-C6 alkylene group.
摘要翻译：具有由式（I）表示的tau蛋白激酶1抑制活性的嘧啶酮衍生物或其盐或其溶剂合物或其水合物; 可用于疾病的预防和/或治疗性治疗，例如神经变性疾病（例如阿尔茨海默病）; 其中Q表示CH或氮原子; R代表C1-C12烷基; 式（I）的环表示哌嗪环或哌啶环; 每个X独立地表示C1-C8烷基，任选部分氢化的C 6 -C 10芳基环，茚满环等; m表示1〜3的整数，各自独立地表示卤素原子，羟基，氰基，C1-C6烷基等; n表示0〜8的整数，当X和Y或两个Y基团连接在同一个碳原子上时，它们可以彼此结合形成C 2 -C 6亚烷基。

5. 发明申请

US20050090490A1 3-Substituted-4-pyrimidone derivatives 有权
标题翻译： 3-取代的-4-嘧啶酮衍生物
公开(公告)号：US20050090490A1
公开(公告)日：2005-04-28
申请号：US10489606
申请日：2002-09-20
申请人： Fumiaki Uehara , Keiichi Aritomo , Aya Shoda , Shinsuke Hiki , Masahiro Okuyama , Yoshihiro Usui , Mitsuru Ooizumi , Kazutoshi Watanabe , Koichi Yamakoshi
发明人： Fumiaki Uehara , Keiichi Aritomo , Aya Shoda , Shinsuke Hiki , Masahiro Okuyama , Yoshihiro Usui , Mitsuru Ooizumi , Kazutoshi Watanabe , Koichi Yamakoshi
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 , A61K31/541 , C07D43/14
CPC分类号： C07D401/04 , C07D239/34 , C07D239/47 , C07D239/56 , C07D401/14 , C07D413/14
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 heteno atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.
摘要翻译：由式（I）表示的嘧啶酮衍生物或其盐，或其对tau蛋白激酶1具有抑制活性的溶剂合物或其水合物：其中R 1表示C 1〜可以被取代的C 1 -C 12烷基; R表示例如由下式（II）表示的基团：其中R 2和R 3独立地表示氢原子或C 1〜 C 1 -C 8烷基; R 4表示可以被取代的苯环，可以被取代的萘环，可以被取代的茚满环，可被取代的四氢萘环，或具有1个的任选取代的杂环至4个选自氧原子，硫原子和氮原子的Heteno原子，并且总共具有5至10个构成环的原子。

6. 发明授权

US07256199B1 Pyrimidone derivatives 失效
标题翻译：嘧啶衍生物
公开(公告)号：US07256199B1
公开(公告)日：2007-08-14
申请号：US09787426
申请日：1999-09-24
申请人： Kazutoshi Watanabe , Ryoichi Ando , Ken-ichi Saito , Rie Kawamoto , Aya Shoda
发明人： Kazutoshi Watanabe , Ryoichi Ando , Ken-ichi Saito , Rie Kawamoto , Aya Shoda
IPC分类号： C07D401/04 , A61K31/506
CPC分类号： C07D401/04 , C07D401/14 , C07D409/14
摘要： A pyrimidone derivative represented by the formula (I) or a salts thereof: wherein R1 represents an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group and the like; R2 represents a hydrogen atom, hydroxyl group, an alkyl group, an alkenyl group and the like, R3 represents a pyridyl group, and a medicament comprising said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as Alzheimer disease.
摘要翻译：由式（I）表示的嘧啶酮衍生物或其盐：其中R 1表示烷基，烯基，炔基，环烷基，芳基等; R 2表示氢原子，羟基，烷基，烯基等，R 3表示吡啶基，并且包含所述衍生物或其盐作为活性成分，用于预防和/或治疗由tau蛋白激酶1多动症如阿尔茨海默病引起的疾病。

7. 发明申请

US20050130998A1 2-amino-3-(alkyl)-pyrimidone derivatives 失效
标题翻译： 2-氨基-3-（烷基） - 嘧啶酮衍生物
公开(公告)号：US20050130998A1
公开(公告)日：2005-06-16
申请号：US11035264
申请日：2005-01-13
申请人： Antonio Almario Carcia , Ryoichi Ando , Keiichi Arimoto , Fumiaki Uehara , Adrien Li , Aya Shoda , Jonathan Frost , Kazutoshi Watanabe
发明人： Antonio Almario Carcia , Ryoichi Ando , Keiichi Arimoto , Fumiaki Uehara , Adrien Li , Aya Shoda , Jonathan Frost , Kazutoshi Watanabe
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 , A61K31/513 , C07D43/02
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 C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 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 halogen atom; and R4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or 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 GSK3β such as Alzheimer's disease.
摘要翻译：由式（I）表示的嘧啶酮衍生物或其盐：其中R1表示氢原子或可以被C 6-10取代的C 1-6烷基， / SUB>芳基; R 2表示可以被取代的C 1-10烷基，可以被取代的C 2-6亚烷基，C 3-6亚烷基，可以被取代的亚炔基，可被取代的C 3-6亚烷基或可以被取代的C 6〜6-亚芳基; 或者R 1和R 2一起形成可以被取代的C 2-6亚烷基; 或者R 1和R 2一起形成式 - （CH 2 CH 2）2 - （CH 2）2 - 或 - （CH 2）2 -X-（CH 2）3 - - 其中X表示氧原子，硫原子或可被取代的氮原子; 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; 并且R 4表示任选被羟基，氨基，C 1-6 - 单烷基氨基，C 2-12-12任意取代的C 1-10烷基。 >可以被取代的二烷基氨基或C 6,10 芳基。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如阿尔茨海默氏病的异常活性引起的神经变性疾病的预防和/或治疗性治疗。

8. 发明授权

US07572793B2 3-Substituted-4-pyrimidone derivatives 有权
标题翻译： 3-取代的-4-嘧啶酮衍生物
公开(公告)号：US07572793B2
公开(公告)日：2009-08-11
申请号：US10489607
申请日：2002-09-20
申请人： Fumiaki Uehara , Keiichi Aritomo , Aya Shoda , Shinsuke Hiki , Masahiro Okuyama , Yoshihiro Usui , Mitsuru Ooizumi , Kazutoshi Watanabe
发明人： Fumiaki Uehara , Keiichi Aritomo , Aya Shoda , Shinsuke Hiki , Masahiro Okuyama , Yoshihiro Usui , Mitsuru Ooizumi , Kazutoshi Watanabe
IPC分类号： A61K31/535 , A61K31/54 , C07D403/00 , C07D237/02 , C07D265/30 , C07D295/00 , C07D413/00
CPC分类号： A61K31/535 , C07D239/34 , C07D239/47 , C07D239/56 , C07D401/04 , C07D401/14 , C07D413/14
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.
摘要翻译：由式（I）表示的嘧啶酮衍生物或其盐，或其溶剂化物或其水合物对tau蛋白激酶1具有抑制活性：其中R1表示可被取代的C1-C12烷基; R表示例如由下式（II）表示的基团：其中R2和R3独立地表示氢原子或C1-C8烷基; R4表示可被取代的苯环，可被取代的萘环，可被取代的茚满环，可被取代的四氢萘环，或具有1-4个选自下述基团的杂原子的任意取代的杂环由氧原子，硫原子和氮原子构成，并且总共具有5〜10个构成环的原子。

9. 发明申请

US20050130967A1 3-Substituted-4-pyrimidone derivatives 有权
标题翻译： 3-取代的-4-嘧啶酮衍生物
公开(公告)号：US20050130967A1
公开(公告)日：2005-06-16
申请号：US10489607
申请日：2002-09-20
申请人： Fumiaki Uehara , Keiichi Aritomo , Aya Shoda , Shinsuke Hiki , Masahiro Okuyama , Yoshihiro Usui , Mitsuru Ooizumi , Kazutoshi Watanabe
发明人： Fumiaki Uehara , Keiichi Aritomo , Aya Shoda , Shinsuke Hiki , Masahiro Okuyama , Yoshihiro Usui , Mitsuru Ooizumi , Kazutoshi Watanabe
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 , C07D43/14
CPC分类号： A61K31/535 , C07D239/34 , C07D239/47 , C07D239/56 , C07D401/04 , C07D401/14 , C07D413/14
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.
摘要翻译：由式（I）表示的嘧啶酮衍生物或其盐，或其溶剂合物或其水合物对tau蛋白激酶1具有抑制活性：其中R 1表示C 1〜可以被取代的C 1 -C 12烷基; R表示例如由下式（II）表示的基团：其中R 2和R 3独立地表示氢原子或C 1 -C 3烷基， 8个烷基; R 4表示可以被取代的苯环，可以被取代的萘环，可以被取代的茚满环，可被取代的四氢萘环，或具有1个的任选取代的杂环至4个选自氧原子，硫原子和氮原子的杂原子，并且总共具有5至10个环构成原子。

10. 发明授权

US06844335B2 2-amino-3-(alkyl)-pyrimidone derivatives as GSK3.β.inhibitors 失效
标题翻译： 2-氨基-3-（烷基） - 嘧啶酮衍生物作为GSK3.beta.抑制剂
公开(公告)号：US06844335B2
公开(公告)日：2005-01-18
申请号：US10221598
申请日：2001-03-22
申请人： Antonio Almario Garcia , Ryoichi Ando , Keiichi Arimoto , Fumiaki Uehara , Adrien Tak Li , Aya Shoda , Jonathan Reid Frost , Kazutoshi Watanabe
发明人： Antonio Almario Garcia , Ryoichi Ando , Keiichi Arimoto , Fumiaki Uehara , Adrien Tak Li , Aya Shoda , Jonathan Reid Frost , Kazutoshi Watanabe
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
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 C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 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 halogen atom; and R4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or 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 GSK3β such as Alzheimer's disease.
摘要翻译：由式（I）表示的嘧啶酮衍生物或其盐：其中：R1表示氢原子或可被C6,10芳基取代的C1-6烷基; R2表示可以被C 1-6烷基取代的C 1-10烷基，可被取代的C2-6烯基，可被取代的C3-6炔基，可被取代的C3-6环烷基或可被取代的C6-10ArYL基;或R1 并且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-其中X表示氧原子，硫原子或可被取代的氮原子; R 3表示任选被C 1-4烷基，C 1-4烷氧基或卤素取代的2,3或4-吡啶基原子; R 4表示可以被羟基任选取代的C 1-10烷基，可以被取代的氨基，C 1-6单烷基氨基，C 2-12二烷基氨基或C 6〜10芳基。并且包含所述衍生物或其盐作为用于预防和/或治疗由GSK3β如阿尔茨海默病异常活动引起的神经变性疾病的活性成分。

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