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1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 发明授权

US07994315B2 Intermediate compound for synthesizing pharmaceutical agent and production method thereof 失效
标题翻译：用于合成药剂的中间体化合物及其制备方法
公开(公告)号：US07994315B2
公开(公告)日：2011-08-09
申请号：US11996205
申请日：2006-07-21
申请人： Masahiro Okuyama , Fumiaki Uehara , Hiroshi Iwamura , Kazutoshi Watanabe
发明人： Masahiro Okuyama , Fumiaki Uehara , Hiroshi Iwamura , Kazutoshi Watanabe
IPC分类号： C07D265/30
CPC分类号： C07D265/30 , C07D265/32
摘要： Production method of an optically active morpholine compound represented by the formula 10, or a compound represented by the formula 55, which includes the following steps: or wherein each symbol is as defined in the specification. An optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4′]bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.
摘要翻译：由式10表示的光学活性吗啉化合物的制备方法或由式55表示的化合物，其包括以下步骤：或其中每个符号如说明书中所定义。光学活性的2-芳基取代的吗啉化合物和3-氧代-3-（嘧啶-4-基）丙酸酯，其作为合成2-（2-芳基吗啉-4-基）-1-甲基 - 可以通过工业上有利的方法以高产率制备具有tau蛋白激酶1抑制活性并且可用作阿尔茨海默氏病等的治疗药物的1H- [4,4']联嘧啶基-6-酮。

8. 发明申请

US20090156804A1 INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF 失效
标题翻译：用于合成药物代理的中间体化合物及其生产方法
公开(公告)号：US20090156804A1
公开(公告)日：2009-06-18
申请号：US11996205
申请日：2006-07-21
申请人： Masahiro Okuyama , Fumiaki Uehara , Hiroshi Iwamura , Kazutoshi Watanabe
发明人： Masahiro Okuyama , Fumiaki Uehara , Hiroshi Iwamura , Kazutoshi Watanabe
IPC分类号： C07D413/14 , C07C211/43 , C07D265/30 , C07D265/32 , C07D239/24
CPC分类号： C07D265/30 , C07D265/32
摘要： The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification.The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification.According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4′]bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.
摘要翻译：本发明涉及由式10表示的光学活性吗啉化合物的制备方法，其包括以下步骤：其中每个符号如说明书中所定义。本发明还涉及由式55表示的化合物的制备方法，其包括以下步骤：其中每个符号如说明书中所定义。根据本发明的制备方法，光学活性2-芳基取代的吗啉化合物和3-氧代-3-（嘧啶-4-基）丙酸酯作为合成2-（2-芳基吗啉） -4-基）-1-甲基-1H- [4,4']二嘧啶基-6-酮，其具有tau蛋白激酶1抑制活性，可用作阿尔茨海默氏病等的治疗药物，可以以高通过工业上有利的方法得到。

9. 发明授权

US07683069B2 3-substituted-4-pyrimidone derivatives 失效
标题翻译： 3-取代-4-嘧啶酮衍生物
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。

10. 发明申请

US20070142409A1 3-Substituted-4-pyrimidone derivatives 失效
标题翻译： 3-取代的-4-嘧啶酮衍生物
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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