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1. 发明授权

US09018238B2 Inhibitor of casein kinase 1δ and casein kinase 1ε 有权
标题翻译：酪蛋白激酶1δ和酪蛋白激酶1抑制剂
公开(公告)号：US09018238B2
公开(公告)日：2015-04-28
申请号：US13201309
申请日：2009-12-28
申请人： Masako Okamoto , Kiyoshi Takayama
发明人： Masako Okamoto , Kiyoshi Takayama
IPC分类号： A61K31/422 , A61K31/433 , A61K31/4439 , C07D413/06 , C07D413/14 , C07D417/14 , C07D413/04 , C07D263/18
CPC分类号： C07D413/04 , A61K31/422 , A61K31/433 , A61K31/4439 , C07D263/18 , C07D413/06 , C07D413/14 , C07D417/14
摘要： There is provided an inhibitor that inhibits casein kinase 1δ and casein kinase 1ε, and thus, there is also provided a pharmaceutical agent useful for the treatment and/or prevention of a disease, with the pathological condition of which the mechanism of activation of casein kinase 1δ or casein kinase 1ε is associated. Particularly, the above-described inhibitor is used to provide a pharmaceutical agent useful for the treatment of circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer.An inhibitor of casein kinase 1δ and casein kinase 1ε, which comprises, as an active ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: [wherein, in the formula (1), each of R1 and R2 independently represents any one of a substituted or unsubstituted 6-membered or 5-membered heterocyclic group optionally having a condensed ring, a substituted or unsubstituted aromatic hydrocarbon group optionally having a condensed ring, and a substituted or unsubstituted aromatic hydrocarbon lower alkyl group or aromatic hydrocarbon lower alkenyl group optionally having a condensed ring.]
摘要翻译：提供了抑制酪蛋白激酶1δ和酪蛋白激酶1的抑制剂，因此，还提供了可用于治疗和/或预防疾病的药剂，其病理状况是酪蛋白的活化机制激酶1δ或酪蛋白激酶1＆egr; 已关联的。特别地，上述抑制剂用于提供可用于治疗昼夜节律紊乱（包括睡眠障碍），中枢神经变性疾病和癌症的药剂。酪蛋白激酶1δ和酪蛋白激酶1抑制剂，其包含作为活性成分的由以下通式（1）表示的恶唑酮衍生物，其盐，其溶剂化物或其水合物：[其中，在式（1）中，R 1和R 2各自独立地表示任选具有稠环的取代或未取代的6元或5元杂环基，任选具有稠环的取代或未取代的芳香族烃基，取代或未取代的芳烃低级烷基或任选具有稠环的芳烃低级链烯基。

2. 发明申请

US20130137730A1 INHIBITOR OF CASEIN KINASE 1DELTA AND CASEIN KINASE 1E 有权
标题翻译： CASEIN KINASE 1DELTA和CASEIN KINASE 1E的抑制剂
公开(公告)号：US20130137730A1
公开(公告)日：2013-05-30
申请号：US13816180
申请日：2011-08-08
申请人： Masako Okamoto , Kiyoshi Takayama
发明人： Masako Okamoto , Kiyoshi Takayama
IPC分类号： A61K31/4439
CPC分类号： A61K31/4439 , C07D413/14
摘要： There is provided a novel oxazolone derivative having inhibitory activity against casein kinase 1δ and casein kinase 1ε. In addition, the present inhibitor inhibits casein kinase 1δ and casein kinase 1ε, and thus there is also provided a pharmaceutical agent useful for the treatment and/or prevention of diseases, with the pathological conditions of which the activation mechanism of casein kinase 1δ or casein kinase 1ε is associated. There is further provided a pharmaceutical agent useful for the treatment of particularly, circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer.An inhibitor of casein kinase 1δ and casein kinase 1ε comprising, as an act ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: wherein X represents a halogen atom (which may be any one of a fluorine atom, a chlorine atom, a bromine atom, and an iodine atom).
摘要翻译：提供了对酪蛋白激酶1delta和酪蛋白激酶1epsilon具有抑制活性的新型恶唑酮衍生物。此外，本发明的抑制剂抑制酪蛋白激酶1delta和酪蛋白激酶1β，因此还提供了可用于治疗和/或预防疾病的药剂，其病理条件是酪蛋白激酶1delta或酪蛋白的激活机制激酶1epon是相关的。还提供了用于特别治疗昼夜节律紊乱（包括睡眠障碍），中枢性神经变性疾病和癌症的药剂。酪蛋白激酶1delta和酪蛋白激酶1β的抑制剂，其包含作为成分的由以下通式（1）表示的恶唑酮衍生物，其盐，其溶剂合物或其水合物：其中X表示卤素原子（其可以是氟原子，氯原子，溴原子和碘原子中的任何一个）。

3. 发明申请

US20070282189A1 Method For Transforming Head Surface Coordinates To Brain Surface Coordinates And Transcranial Brain Function Measuring Method Using The Transformation Data 有权
标题翻译：使用变换数据将头部表面坐标转换为脑表面坐标和经颅脑功能测量方法的方法
公开(公告)号：US20070282189A1
公开(公告)日：2007-12-06
申请号：US10579463
申请日：2004-11-12
申请人： Ippeita Dan , Kuniko Sakamoto , Masako Okamoto , Seiichiro Isobe , Kaoru Kohyama , Koji Shimizu , Kazubiro Takeo
发明人： Ippeita Dan , Kuniko Sakamoto , Masako Okamoto , Seiichiro Isobe , Kaoru Kohyama , Koji Shimizu , Kazubiro Takeo
IPC分类号： A61B6/00
CPC分类号： A61B5/0059 , A61B5/0042 , A61B5/061 , A61B5/14553 , A61B5/4064 , A61B5/7445
摘要： Data collected by a transcranial brain function measuring/stimulating method is accurately projected and displayed onto a brain surface. If there is no three-dimensional head image, data is projected and displayed onto the brain surface of a standard brain. The head surface coordinates are transformed to the brain surface coordinates of the brain surface underlying the head surface by, e.g., a minimum distance search method. The coordinates of a projected point on the brain surface of the head surface and the probability distribution are determined for a standard brain normalized with data on subjects.
摘要翻译：通过经颅脑功能测量/刺激方法收集的数据被精确投影并显示在脑表面上。如果没有三维头像，则将数据投影并显示在标准脑的脑表面上。头表面坐标通过例如最小距离搜索方法转换到头表面下面的脑表面的脑表面坐标。确定头部表面的脑表面上的投影点的坐标和概率分布，以便根据受试者数据进行标准化的标准脑。

4. 发明授权

US08180426B2 Method for transforming head surface coordinates to brain surface coordinates and transcranial brain function measuring method using the transformation data 有权
标题翻译：使用转换数据将头面坐标转换为脑表面坐标和经颅脑功能测量方法
公开(公告)号：US08180426B2
公开(公告)日：2012-05-15
申请号：US10579463
申请日：2004-11-12
申请人： Ippeita Dan , Kuniko Sakamoto , Masako Okamoto , Seiichiro Isobe , Kaoru Kohyama , Koji Shimizu , Kazuhiro Takeo
发明人： Ippeita Dan , Kuniko Sakamoto , Masako Okamoto , Seiichiro Isobe , Kaoru Kohyama , Koji Shimizu , Kazuhiro Takeo
IPC分类号： A61B5/05
CPC分类号： A61B5/0059 , A61B5/0042 , A61B5/061 , A61B5/14553 , A61B5/4064 , A61B5/7445
摘要： Data collected by a transcranial brain function measuring/stimulating method is accurately projected and displayed onto a brain surface. If there is no three-dimensional head image, data is projected and displayed onto the brain surface of a standard brain. The head surface coordinates are transformed to the brain surface coordinates of the brain surface underlying the head surface by, e.g., a minimum distance search method. The coordinates of a projected point on the brain surface of the head surface and the probability distribution are determined for a standard brain normalized with data on subjects.
摘要翻译：通过经颅脑功能测量/刺激方法收集的数据被精确投影并显示在脑表面上。如果没有三维头像，则将数据投影并显示在标准脑的脑表面上。头表面坐标通过例如最小距离搜索方法转换到头表面下面的脑表面的脑表面坐标。确定头部表面的脑表面上的投影点的坐标和概率分布，以便根据受试者数据进行标准化的标准脑。

5. 发明申请

US20110294857A1 INHIBITOR OF CASEIN KINASE 1DELTA AND CASEIN KINASE 1EPSILON 有权
标题翻译： CASEIN KINASE 1DELTA和CASEIN KINASE 1EPSILON的抑制剂
公开(公告)号：US20110294857A1
公开(公告)日：2011-12-01
申请号：US13201309
申请日：2009-12-28
申请人： Masako Okamoto , Kiyoshi Takayama
发明人： Masako Okamoto , Kiyoshi Takayama
IPC分类号： A61K31/422 , A61P35/00 , A61P43/00 , A61P25/28 , A61K31/4439 , A61K31/433
CPC分类号： C07D413/04 , A61K31/422 , A61K31/433 , A61K31/4439 , C07D263/18 , C07D413/06 , C07D413/14 , C07D417/14
摘要： There is provided an inhibitor that inhibits casein kinase 1δ and casein kinase 1ε, and thus, there is also provided a pharmaceutical agent useful for the treatment and/or prevention of a disease, with the pathological condition of which the mechanism of activation of casein kinase 1δ or casein kinase 1ε is associated. Particularly, the above-described inhibitor is used to provide a pharmaceutical agent useful for the treatment of circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer.An inhibitor of casein kinase 1δ and casein kinase 1ε, which comprises, as an active ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: [wherein, in the formula (1), each of R1 and R2 independently represents any one of a substituted or unsubstituted 6-membered or 5-membered heterocyclic group optionally having a condensed ring, a substituted or unsubstituted aromatic hydrocarbon group optionally having a condensed ring, and a substituted or unsubstituted aromatic hydrocarbon lower alkyl group or aromatic hydrocarbon lower alkenyl group optionally having a condensed ring.]
摘要翻译：提供了抑制酪蛋白激酶1δ和酪蛋白激酶1的抑制剂，因此，还提供了可用于治疗和/或预防疾病的药剂，其病理状况是酪蛋白的活化机制激酶1δ或酪蛋白激酶1＆egr; 已关联的。特别地，上述抑制剂用于提供可用于治疗昼夜节律紊乱（包括睡眠障碍），中枢神经变性疾病和癌症的药剂。酪蛋白激酶1δ和酪蛋白激酶1抑制剂，其包含作为活性成分的由以下通式（1）表示的恶唑酮衍生物，其盐，其溶剂化物或其水合物：[其中，在式（1）中，R 1和R 2各自独立地表示任选具有稠环的取代或未取代的6元或5元杂环基，任选具有稠环的取代或未取代的芳香族烃基，取代或未取代的芳烃低级烷基或任选具有稠环的芳烃低级链烯基。

6. 发明授权

US08710231B2 Inhibitor of casein kinase 1delta and casein kinase 1E 有权
标题翻译：酪蛋白激酶1delta和酪蛋白激酶1E的抑制剂
公开(公告)号：US08710231B2
公开(公告)日：2014-04-29
申请号：US13816180
申请日：2011-08-08
申请人： Masako Okamoto , Kiyoshi Takayama
发明人： Masako Okamoto , Kiyoshi Takayama
IPC分类号： C07D413/00 , C07D419/00 , C07D409/00 , C07D411/00 , A61K31/44 , A01N43/40
CPC分类号： A61K31/4439 , C07D413/14
摘要： There is provided a novel oxazolone derivative having inhibitory activity against casein kinase 1δ and casein kinase 1ε. In addition, the present inhibitor inhibits casein kinase 1δ and casein kinase 1ε, and thus there is also provided a pharmaceutical agent useful for the treatment and/or prevention of diseases, with the pathological conditions of which the activation mechanism of casein kinase 1δ or casein kinase 1ε is associated. There is further provided a pharmaceutical agent useful for the treatment of, particularly, circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer. An inhibitor of casein kinase 1δ and casein kinase 1ε comprising, as an active ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: wherein X represents a halogen atom which is fluorine, chlorine, bromine or iodine.
摘要翻译：提供了一种对酪蛋白激酶1δ和酪蛋白激酶1具有抑制活性的新型恶唑酮衍生物。此外，本发明的抑制剂抑制酪蛋白激酶1δ和酪蛋白激酶1和egr，因此还提供了可用于治疗和/或预防疾病的药剂，其病理条件是酪蛋白激酶1δ或酪蛋白激酶1 已关联的。还提供了用于治疗，特别是昼夜节律紊乱（包括睡眠障碍），中枢神经变性疾病和癌症的药剂。酪蛋白激酶1δ和酪蛋白激酶1的抑制剂作为活性成分，含有下述通式（1）表示的恶唑酮衍生物，其盐，溶剂化物或其水合物：其中，X表示氟，氯，溴或碘的卤素原子。

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