公开(公告)号：US09907799B2

公开(公告)日：2018-03-06

申请号：US14781897

申请日：2014-04-02

申请人： THE DOSHISHA ,  National Center for Geriatrics and Gerontology

发明人： Tomohiro Miyasaka ,  Hachiro Sugimoto ,  Rie Tokizane ,  Yuki Shinzaki ,  Yohei Oe ,  Tetsuo Ota ,  Akihiko Takashima ,  Yoshiyuki Soeda ,  Yasuo Ihara ,  Yoshikazu Inoue

IPC分类号： A61K31/5375 ,  A61K31/05 ,  A61K31/055 ,  A61K31/11 ,  A61K31/12 ,  A61K31/136 ,  A61K31/085 ,  A61K31/137

CPC分类号： A61K31/5375 ,  A61K31/05 ,  A61K31/055 ,  A61K31/085 ,  A61K31/11 ,  A61K31/12 ,  A61K31/136 ,  A61K31/137

摘要： A tau aggregation inhibitor can sufficiently inhibit a tau protein from aggregating in cells. The inhibitor includes a 4-substituted catechol structure compound, having, at position 4 of its catechol ring, an electron-donating substituent R other than a hydrocarbon group, or a salt thereof. The 4-substituted catechol structure compound is preferably 4-aminocatechol or 1,2,4-benzenetriol. Examples of tauopathies to which this inhibitor is applicable include AD, Down's syndrome, frontotemporal dementia, cotricobasal degeneration (CBD) and progressive supranuclear palsy (PSP).

公开(公告)号：US20160030437A1

公开(公告)日：2016-02-04

申请号：US14781897

申请日：2014-04-02

申请人： NATIONAL CENTER FOR GERIATRICS AND GERONTOLOGY ,  THE DOSHISHA

发明人： Tomohiro Miyasaka ,  Hachiro Sugimoto ,  Rie Tokizane ,  Yuki Shinzaki ,  Yohei Oe ,  Tetsuo Ota ,  Akihiko Takashima ,  Yoshiyuki Soeda ,  Yasuo Ihara ,  Yoshikazu Inoue

IPC分类号： A61K31/5375 ,  A61K31/05 ,  A61K31/055 ,  A61K31/11 ,  A61K31/12 ,  A61K31/136 ,  A61K31/085

CPC分类号： A61K31/5375 ,  A61K31/05 ,  A61K31/055 ,  A61K31/085 ,  A61K31/11 ,  A61K31/12 ,  A61K31/136 ,  A61K31/137

摘要： A tau aggregation inhibitor can sufficiently inhibit a tau protein from aggregating in cells. The inhibitor includes a 4-substituted catechol structure compound, having, at position 4 of its catechol ring, an electron-donating substituent R other than a hydrocarbon group, or a salt thereof. The 4-substituted catechol structure compound is preferably 4-aminocatechol or 1,2,4-benzenetriol. Examples of tauopathies to which this inhibitor is applicable include AD, Down's syndrome, frontotemporal dementia, cotricobasal degeneration (CBD) and progressive supranuclear palsy (PSP).

摘要翻译： tau聚集抑制剂可以充分抑制tau蛋白在细胞中的聚集。 抑制剂包括4-取代的邻苯二酚结构化合物，其在其邻苯二酚环的4位具有除烃基以外的给电子取代基R或其盐。 4-取代的邻苯二酚结构化合物优选为4-氨基邻苯二酚或1,2,4-苯三醇。 这种抑制剂适用的tau蛋白病的实例包括AD，唐氏综合征，额颞叶痴呆，小叶蜕膜变性（CBD）和进行性核上麻痹（PSP）。