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1. 发明授权

US07166617B2 Cyclic amide derivatives 有权
标题翻译：环状酰胺衍生物
公开(公告)号：US07166617B2
公开(公告)日：2007-01-23
申请号：US10220359
申请日：2001-02-26
申请人： Haruko Yamabe , Masahiro Okuyama , Akira Nakao , Mitsuru Ooizumi , Ken-ichi Saito
发明人： Haruko Yamabe , Masahiro Okuyama , Akira Nakao , Mitsuru Ooizumi , Ken-ichi Saito
IPC分类号： A61K31/445 , C07D401/06
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D491/04 , C07D495/04
摘要： Novel compounds represented by the following formula (I) that act as a ligand to sigma receptor/binding cite and a medicament comprising the same as an active ingredient: wherein X represents an alkyl group, an aryl group, a heterocyclic group or the like; Q represents a group represented by —CH2—, —CO—, —O—, —CH(OR7)— or the like wherein R7 represents a hydrogen atom, an alkyl group or the like; n represents an integer of from 0 to 5; R1 and R2 each represent a hydrogen atom, an alkyl group or the like; B represents either of the following groups: wherein R3, R4, R5, and R6 each represent a hydrogen atom, a halogen atom, an alkoxyl group or the like; m represents 1 or 2; and the ring of: represents an aromatic heterocyclic ring.
摘要翻译：作为σ受体/结合物的配体的下述式（I）表示的新型化合物和含有该活性成分的药物，其中X表示烷基，芳基，杂环基等; Q表示由-CH 2 - ， - CO - ， - O - ， - CH（OR 7） - 表示的基团，其中R 7， / SUB表示氢原子，烷基等; n表示0〜5的整数， R 1和R 2各自表示氢原子，烷基等; B表示以下基团中的任一个：其中R 3，R 4，R 5和R 6各自表示氢原子，卤素原子，烷氧基等; m表示1或2; 且环：表示芳族杂环。

2. 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。

3. 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。

4. 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。

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. 发明授权

US08293796B2 Modulator 有权
标题翻译：调制器
公开(公告)号：US08293796B2
公开(公告)日：2012-10-23
申请号：US12707812
申请日：2010-02-18
申请人： Masahiro Okuyama , David Selwood , Cristina Visintin , David Baker , Gareth Pryce
发明人： Masahiro Okuyama , David Selwood , Cristina Visintin , David Baker , Gareth Pryce
IPC分类号： A01N37/18
CPC分类号： C07C235/42 , A61K31/165 , C07C69/76 , C07C69/78 , C07C233/11 , C07C233/65 , C07C233/66 , C07C233/69 , C07C235/34 , C07C235/78 , C07C235/84 , C07C237/32 , C07C237/38 , C07C237/42 , C07C255/41 , C07C255/44
摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR1 or NR1R2 wherein each of R1 and R2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X—Y is other than meta-C≡—C—(CH2)2CO2H, meta-C≡—C—(CH2)2OH, meta-C≡C—(CH2)2CO2Me, meta-(CH2)4CO2H, ortho-CH2CO2H, ortho-(CH2)2CO2H and ortho-(CH2)4CO2H; and (ii) when A is phenyl, n is 0, and Z is OMe, X—Y is other than meta-C≡C—(CH2)4OH. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中Z为OR 1或NR 1 R 2，其中R 1和R 2各自独立地为H或烃基; X是亚烷基，亚烯基或亚炔基，其各自可以任选地被一个或多个选自烷基，COOH，CO 2 - 烷基，烯基，CN，NH 2，羟基，卤素，烷氧基，CF 3和硝基的取代基取代; Y是选自OH，NO2，CN，COR3，COOR3，NR3R4，CONR3R4，SO3H，SO2-R3，SO2NR3R4和CF3的极性官能团，其中R3和R4各自独立地为H或烃基; A是芳基或杂芳基，其各自可以任选被取代; 和B是（CH 2）n，其中n是0,1,2,3,4或5; 条件是：（i）当A是苯基时，n是0，Z是OH，X-Y不是间位-C≡-C-（CH 2）2 CO 2 H，间-C≡C-（CH 2）（CH 2）2 CO 2 Me，间 - （CH 2）4 CO 2 H，邻-CH 2 CO 2 H，邻 - （CH 2）2 CO 2 H和邻 - （CH 2）4 CO 2 H; 和（ii）当A是苯基时，n是0，Z是OMe，X-Y不是间位-C≡C-（CH 2）4 OH。本发明的其它方面涉及这样的化合物在制备用于治疗肌肉疾病，胃肠道疾病或用于控制痉挛或震颤的药物中的用途。

7. 发明申请

US20050001961A1 Display 审中-公开
标题翻译：显示
公开(公告)号：US20050001961A1
公开(公告)日：2005-01-06
申请号：US10826388
申请日：2004-04-19
申请人： Norio Koma , Shinji Ogawa , Kazuyuki Maeda , Nobuhiko Oda , Kazuhiro Inoue , Tsutomu Yamada , Masahiro Okuyama
发明人： Norio Koma , Shinji Ogawa , Kazuyuki Maeda , Nobuhiko Oda , Kazuhiro Inoue , Tsutomu Yamada , Masahiro Okuyama
IPC分类号： G02F1/1333 , G02F1/1335
CPC分类号： G02F1/133555 , G02F1/133371
摘要： There is provide a display which can prevent lowering of display quality caused by fluctuation of thickness of an orientation film. The display includes a display region having a reflective region and a transmissive region and comprises a first region having a convex insulating film formed in a region corresponding to the reflective region on a substrate, and an orientation film formed so as to cover the convex insulating film. A second region in which the convex insulating film is not formed is continuously formed among adjacent pixels.
摘要翻译：提供了可以防止由取向膜的厚度的波动引起的显示质量降低的显示。显示器包括具有反射区域和透射区域的显示区域，并且包括形成在与基板上的反射区域对应的区域中的凸形绝缘膜的第一区域和形成为覆盖凸状绝缘膜的取向膜。在相邻像素之间连续地形成没有形成凸状绝缘膜的第二区域。

8. 发明授权

US06801181B2 Level shifter for use in active matrix display apparatus 有权
标题翻译：用于有源矩阵显示装置的电平移位器
公开(公告)号：US06801181B2
公开(公告)日：2004-10-05
申请号：US09881113
申请日：2001-06-14
申请人： Shoichiro Matsumoto , Naoaki Komiya , Masahiro Okuyama , Koji Hirosawa
发明人： Shoichiro Matsumoto , Naoaki Komiya , Masahiro Okuyama , Koji Hirosawa
IPC分类号： G09G336
CPC分类号： G09G3/3677 , G09G2310/0289
摘要： Between a positive power supply 18 and a negative power supply 19, a p-channel transistor 11 and an n-channel transistor 14 are connected in series while a p-channel transistor 12 and an n-channel transistor 15 are also connected in series. An inverted input signal *Sig1 is input to the respective gates of the transistors 11 and 14, while an input signal Sig1 is input to the respective gates of the transistors 12 and 15. As a result, of a pair of the transistors connected in series, namely either the transistors 11 and 14 or the transistors 12 and 15, when one transistor turns ON, the other transistor turns OFF. Thus, generation of through currents is prevented.
摘要翻译：在正电源18和负电源19之间，p沟道晶体管11和n沟道晶体管14串联连接，同时p沟道晶体管12和n沟道晶体管15串联连接。反相输入信号* Sig1输入到晶体管11和14的各个栅极，而输入信号Sig1被输入到晶体管12和15的各个栅极。结果是，串联的一对晶体管，即晶体管11和14或晶体管12和15，当一个晶体管导通时，另一个晶体管截止。因此，防止通过电流的产生。

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。

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