公开(公告)号：US20100055691A1

公开(公告)日：2010-03-04

申请号：US12439760

申请日：2007-08-24

申请人： Akira Nakagawara ,  Tian-Ling Liu ,  Tadayuki Koda

发明人： Akira Nakagawara ,  Tian-Ling Liu ,  Tadayuki Koda

IPC分类号： C12Q1/68 ,  G01N33/53

CPC分类号： G01N33/6896 ,  G01N2333/9121 ,  G01N2800/2814

摘要： The objective of the present invention is to provide methods of screening therapeutic agents for juvenile familial amyotrophic lateral sclerosis (ALS2). The invention provides a method of screening therapeutic agents for juvenile familial amyotrophic lateral sclerosis, comprising a step of assessing a substance that suppresses the expression of Tollip in cells as a therapeutic agent for juvenile familial amyotrophic lateral sclerosis; a method of screening therapeutic agents for juvenile familial amyotrophic lateral sclerosis, comprising a step of assessing a substance that promotes migration of Tollip in cells from the cytoplasm to the cell nucleus as a therapeutic agent for juvenile familial amyotrophic lateral sclerosis; and a method of screening therapeutic agents for juvenile familial amyotrophic lateral sclerosis, comprising a step of assessing a substance that inhibits the interaction between Tollip and IRAK-1 in cells as a therapeutic agent for juvenile familial amyotrophic lateral sclerosis.

摘要翻译： 本发明的目的是提供筛选青少年家族性肌萎缩性侧索硬化症（ALS2）的治疗剂的方法。 本发明提供一种筛选青少年家族性肌萎缩性侧索硬化症的治疗剂的方法，包括评估抑制作为幼年家族性肌萎缩性侧索硬化症的治疗剂的细胞中Tollip的表达的物质的步骤; 筛选青少年家族性肌萎缩性侧索硬化症的治疗剂的方法，包括评估促进细胞中细胞中Tollip从细胞质迁移到细胞核的物质的步骤，作为青少年家族性肌萎缩性侧索硬化症的治疗剂; 以及筛选用于青少年家族性肌萎缩性侧索硬化症的治疗剂的方法，包括评估抑制细胞中Tollip和IRAK-1之间相互作用的物质作为幼年家族性肌萎缩性侧索硬化症的治疗剂的步骤。

公开(公告)号：US06218402B1

公开(公告)日：2001-04-17

申请号：US09328643

申请日：1999-06-09

申请人： Derek T. Chalmers ,  Susumo Sato ,  Tadayuki Koda

发明人： Derek T. Chalmers ,  Susumo Sato ,  Tadayuki Koda

IPC分类号： A61K314545

CPC分类号： C07D471/04

摘要： Disclosed herein are quinoline derivatives having dual mechanistic properties, referred to in this patent document as “acetylcholine enhancers”, i.e., compounds which evidence acetylcholinesterase (AChE) inhibition activity, and 5-HT3 receptor antagonist activity. A particularly preferred compound is 2-[2-(1-benzylpiperizin-4-yl) ethyl]-2,3-dihydro-9-methoxy-1H-pyrrolo [3,4-b] quinolin-1-one hemifumarate, referred to herein as Compound A (“Cm.A”).

摘要翻译： 本文公开了具有双重机械性质的喹啉衍生物，在该专利文献中称为“乙酰胆碱增强剂”，即证实乙酰胆碱酯酶（AChE）抑制活性的化合物和5-HT 3受体拮抗剂活性。 特别优选的化合物是2- [2-（1-苄基哌嗪-4-基）乙基] -2,3-二氢-9-甲氧基-1H-吡咯并[3,4-b]喹啉-1-酮半富马酸盐， 作为化合物A（“Cm.A”）。

公开(公告)号：US06586596B2

公开(公告)日：2003-07-01

申请号：US09836069

申请日：2001-04-17

申请人： Derek T. Chalmers ,  Susumo Sato ,  Tadayuki Koda

发明人： Derek T. Chalmers ,  Susumo Sato ,  Tadayuki Koda

IPC分类号： C07D40106

CPC分类号： C07D471/04

摘要： Disclosed herein are quinoline derivatives having dual mechanistic properties, referred to in this patent document as “acetylcholine enhancers”, i.e., compounds which evidence acetylcholinesterase (AChE) inhibition activity, and 5-HT3 receptor antagonist activity. A particularly preferred compound is 2-[2-(1-benzylpiperizin-4-yl)ethyl]-2,3-dihydro-9-methoxy-1H-pyrrolo [3,4-b] quinolin-1-one hemifumarate, referred to herein as Compound A (“Cm.A”).

摘要翻译： 本文公开了具有双重机械性质的喹啉衍生物，在该专利文献中称为“乙酰胆碱增强剂”，即证实乙酰胆碱酯酶（AChE）抑制活性的化合物和5-HT 3受体拮抗剂活性。 特别优选的化合物是2- [2-（1-苄基哌嗪-4-基）乙基] -2,3-二氢-9-甲氧基-1H-吡咯并[3,4-b]喹啉-1-酮半富马酸盐， 作为化合物A（“Cm.A”）。