公开(公告)号：US09980954B2

公开(公告)日：2018-05-29

申请号：US15403404

申请日：2017-01-11

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Hyunah Choo ,  Sun-Joon Min ,  Yun Kyung Kim ,  Hoon Ryu ,  Hyemyung Seo ,  Juhyeon Kim ,  Jihoon Jang ,  Sungsu Lim ,  Younghee Kim ,  Yu Jin Hwang ,  Yong Seo Cho

IPC: A61K31/47 ,  A61K31/4709 ,  A61K31/5377

CPC classification number: A61K31/47 ,  A61K31/4709 ,  A61K31/5377

Abstract: The present disclosure relates to a quinoline derivative which inhibits the activity of histone methyltransferases (ESET/SETDB1) specific for the histone molecule H3K9 or a pharmaceutically acceptable salt thereof and a use thereof.

公开(公告)号：US10435408B2

公开(公告)日：2019-10-08

申请号：US15738225

申请日：2017-11-06

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Hyunah Choo ,  Youngjae Kim ,  Jihye Seong ,  Ghil Soo Nam ,  Yong Seo Cho

IPC: C07D487/04 ,  C07D498/04 ,  A61K31/55 ,  A61K31/4162 ,  A61P25/22 ,  A61P25/24

Abstract: Azepine derivatives acting on 5-HT7 receptors and pharmaceutically acceptable salts thereof are disclosed. The azepine derivatives and the pharmaceutically acceptable salts thereof have high binding affinities for and high antagonistic activities on 5-HT7 receptors. Due to these advantages, the azepine derivatives and the pharmaceutically acceptable salts thereof can be applied to therapeutic or prophylactic agents for central nervous system diseases, such as depression, migraine, anxiety, pain, inflammatory pain, neuropathic pain, body temperature dysregulation, biorhythm dysregulation, sleep disturbance, and smooth muscle diseases where 5-HT7 receptors antagonistic activity is required.

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）。