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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。
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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。
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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。
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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。
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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。
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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。
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公开(公告)号:US08569294B2
公开(公告)日:2013-10-29
申请号:US12282396
申请日:2007-03-14
申请人: Kenji Fukunaga , Toshiyuki Kohara , Kazutoshi Watanabe , Yoshihiro Usui , Fumiaki Uehara , Satoshi Yokoshima , Daiki Sakai , Shin-ichi Kusaka , Kazuki Nakayama
发明人: Kenji Fukunaga , Toshiyuki Kohara , Kazutoshi Watanabe , Yoshihiro Usui , Fumiaki Uehara , Satoshi Yokoshima , Daiki Sakai , Shin-ichi Kusaka , Kazuki Nakayama
IPC分类号: A61K31/535
CPC分类号: C07D413/14 , C07D401/04 , C07D401/14 , C07D403/14 , C07D409/14 , C07D453/06 , C07D493/04
摘要: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
摘要翻译: 由式(I)表示的化合物或其光学活性异构体或其药学上可接受的盐:其中R2表示氢等; R3表示甲基等; R 20表示卤素原子等; q表示0〜3的整数, Z表示氮原子,CH等; R4表示氢等; R5表示氢等; R6表示取代的烷氧基等; p表示0〜3的整数, X表示键,CH2,氧原子,NH等; R 5和R 6,R 5和R 4,R 6和R 4,X和R 5,X和R 4,X和R 6以及R 6和R 6中的任何一个或多个可以彼此结合形成环,其用于预防和/ 或治疗由tau蛋白激酶1多动症如神经变性疾病(例如阿尔茨海默病)引起的疾病。
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公开(公告)号:US20090233918A1
公开(公告)日:2009-09-17
申请号:US12282396
申请日:2007-03-14
申请人: Kenji Fukunaga , Toshiyuki Kohara , Kazutoshi Watanabe , Yoshihiro Usui , Fumiaki Uehara , Satoshi Yokoshima , Daiki Sakai , Shin-ichi Kusaka , Kazuki Nakayama
发明人: Kenji Fukunaga , Toshiyuki Kohara , Kazutoshi Watanabe , Yoshihiro Usui , Fumiaki Uehara , Satoshi Yokoshima , Daiki Sakai , Shin-ichi Kusaka , Kazuki Nakayama
IPC分类号: A61K31/538 , C07D403/02 , A61K31/506 , A61P25/00 , A61P3/00
CPC分类号: C07D413/14 , C07D401/04 , C07D401/14 , C07D403/14 , C07D409/14 , C07D453/06 , C07D493/04
摘要: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
摘要翻译: 由式(I)表示的化合物或其光学活性异构体或其药学上可接受的盐:其中R2表示氢等; R3表示甲基等; R 20表示卤素原子等; q表示0〜3的整数, Z表示氮原子,CH等; R4表示氢等; R5表示氢等; R6表示取代的烷氧基等; p表示0〜3的整数, X表示键,CH2,氧原子,NH等; R 5和R 6,R 5和R 4,R 6和R 4,X和R 5,X和R 4,X和R 6以及R 6和R 6中的任何一个或多个可以彼此结合形成环,其用于预防和/ 或治疗由tau蛋白激酶1多动症如神经变性疾病(例如阿尔茨海默病)引起的疾病。
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公开(公告)号:US07683069B2
公开(公告)日:2010-03-23
申请号:US10538766
申请日:2003-12-12
申请人: Yoshihiro Usui , Masahiro Okuyama , Tokushi Hanano
发明人: Yoshihiro Usui , Masahiro Okuyama , Tokushi Hanano
IPC分类号: C07D401/14 , A61K31/505
CPC分类号: C07D401/14 , C07D409/14 , C07D413/14
摘要: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof useful as a tau protein kinase 1 inhibitor: wherein X represents CH or nitrogen atom; R1 represents a C?1#191-C?12#191 alkyl group which may be substituted; R2 represents a C?1#191-C?8#191 alkyl group which may be substituted, 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: 用作tau蛋白激酶1抑制剂的由式(I)表示的嘧啶酮衍生物或其盐或其溶剂合物或其水合物:其中X表示CH或氮原子; R1表示可被取代的C 1〜191-C 12〜191烷基; R2表示可被取代的C 1〜191-C 18〜191烷基,可被取代的苯环,可被取代的萘环,可被取代的茚满环,可以被取代的四氢萘环, 或具有1〜4个选自氧原子,硫原子和氮原子的杂原子的任意取代的杂环,并且总共具有5〜10个构成环的原子。
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公开(公告)号:US20070142409A1
公开(公告)日:2007-06-21
申请号:US10538766
申请日:2003-12-12
申请人: Yoshihiro Usui , Masahiro Okuyama , Tokushi Hanano
发明人: Yoshihiro Usui , Masahiro Okuyama , Tokushi Hanano
IPC分类号: A61K31/513 , C07D403/14
CPC分类号: C07D401/14 , C07D409/14 , C07D413/14
摘要: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof useful as a tau protein kinase 1 inhibitor:wherein X represents CH or nitrogen atom; R1 represents a C?1#191-C?12#191 alkyl group which may be substituted; R2 represents a C?1#191-C?8#191 alkyl group which may be substituted, 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: 用作tau蛋白激酶1抑制剂的由式(I)表示的嘧啶酮衍生物或其盐或其溶剂合物或其水合物:其中X表示CH或氮原子; R 1表示可被取代的C 1〜1 191〜C 12〜191烷基; R 2表示可以被取代的C 1〜191-C 18〜191烷基,可被取代的苯环,可被取代的萘环,可以被取代的萘环 可被取代的四氢萘环,或具有1-4个选自氧原子,硫原子和氮原子的杂原子的任意取代的杂环,并且总共具有5至10个环构成原子 。
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