公开(公告)号：US09493423B2

公开(公告)日：2016-11-15

申请号：US14632839

申请日：2015-02-26

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Ghil Soo Nam ,  Kyung Il Choi ,  Jung Hyun Kim ,  Ae Nim Pae ,  Jin Ri Hong ,  Jae Kyun Lee

IPC: C07D231/12 ,  C07D417/14 ,  C07D401/12 ,  C07D417/06

CPC classification number: C07D231/12 ,  C07D401/12 ,  C07D417/06 ,  C07D417/14

Abstract: Disclosed herein are an N-(pyrazolylmethyl)arylsulfonamide derivative useful as a calcium ion channel blocker, a pharmaceutically acceptable salt thereof, and the medicinal use thereof as a therapeutic agent using its calcium ion channel blocking effect.

Abstract translation: 本文公开了可用作钙离子通道阻断剂的N-（吡唑基甲基）芳基磺酰胺衍生物及其药学上可接受的盐，其药物用途为其钙离子通道阻断作用的治疗剂。

公开(公告)号：US12050224B2

公开(公告)日：2024-07-30

申请号：US17021438

申请日：2020-09-15

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Ghil Soo Nam ,  Hyun Ah Choo ,  Ahmed A. Elbatrawy ,  Gyo Chang Keum ,  Yun Kyung Kim ,  Sung Su Lim ,  Jae Kyun Lee ,  Eun Kyoung Bang

IPC: G01N33/68 ,  C07D215/20 ,  C07D215/48 ,  C07D401/06 ,  G01N33/58

CPC classification number: G01N33/6896 ,  C07D215/20 ,  C07D215/48 ,  C07D401/06 ,  G01N33/582 ,  G01N2800/2814 ,  G01N2800/2821 ,  G01N2800/2835

Abstract: Disclosed are a compound with near-infrared fluorescence that selectively binds to tau aggregates, a method for preparing the same, a tau-targeting near-infrared fluorescent probe including the compound, a composition for detecting a tau fiber protein containing the near-infrared fluorescent probe as an active ingredient, and the use of the composition for the diagnosis of tauopathy. In particular, the compound does not bind to an amyloid beta protein and has high selectivity to a tau aggregate, specifically reported as an etiology of the initial state of tauopathy, thus being useful as a near-infrared fluorescent detector for detecting a tau fiber protein for early diagnosis of a tauopathy including Alzheimer's disease.

公开(公告)号：US08946431B2

公开(公告)日：2015-02-03

申请号：US13943019

申请日：2013-07-16

Applicant: Korea Institute of Science and Technology

Inventor： Sun Joon Min ,  Yong Seo Cho ,  Ae Nim Pae ,  Eun Jeong Lim ,  Ji Yeong Kim ,  Myung Hee Son ,  Jae Kyun Lee

IPC: C07D215/06 ,  A61K31/04 ,  C07D215/20 ,  C07D401/06

CPC classification number: C07D215/06 ,  C07D215/20 ,  C07D401/06

Abstract: Provided is a 2-(substituted ethynyl)quinoline derivative having an mGluR5 antagonistic activity and pharmaceutically acceptable salts thereof. The compound of the present invention can be useful as a medicament for treating and preventing mGluR5 receptor-mediated diseases such as Alzheimer's disease, senile dementia, Parkinson's disease, L-DOPA-induced dyskinesia, Huntington's chorea, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, anxiety disorder, depression, neuropathic pain, drug dependence, fragile X syndrome, autism, migraine and gastroesophageal reflux disease (GERD).

Abstract translation: 本发明提供具有mGluR5拮抗活性的2-（取代乙炔基）喹啉衍生物及其药学上可接受的盐。 本发明的化合物可用作治疗和预防mGluR5受体介导的疾病如阿尔茨海默氏病，老年性痴呆，帕金森病，L-DOPA诱导的运动障碍，亨廷顿舞蹈病，肌萎缩性侧索硬化，多发性硬化，精神分裂症 ，焦虑症，抑郁症，神经性疼痛，药物依赖，脆性X综合征，自闭症，偏头痛和胃食管反流病（GERD）。