公开(公告)号：US20140228565A1

公开(公告)日：2014-08-14

申请号：US14038324

申请日：2013-09-26

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Hyunah CHOO ,  Sun Joon Min ,  Seon Hee Seo ,  Jee Yeon Kim ,  Yoo Ran Ki ,  Min Joo Kim ,  Sora Kim ,  Youngjae Kim

IPC: C07D495/04

CPC classification number: C07D495/04 ,  A61K31/519

Abstract: Disclosed are thienopyrimidinone derivatives as antagonists that act on metabotropic glutamate receptor subtype 1. The thienopyrimidinone derivatives show pharmacological activity against metabotropic glutamate receptor-related diseases, including pain, such as neuropathic pain and migraine, psychiatric diseases, such as anxiety disorder and schizophrenia, urinary incontinence, and neurodegenerative diseases, such as Parkinson's disease and Alzheimer's disease. Also disclosed are methods for preparing the thienopyrimidinone derivatives, and pharmaceutical compositions containing the thienopyrimidinone derivatives as active ingredients.

Abstract translation: 公开了作为代谢型谷氨酸受体亚型1的拮抗剂的噻吩并嘧啶酮衍生物。噻吩并嘧啶酮衍生物显示针对代谢型谷氨酸受体相关疾病的药理学活性，包括疼痛，如神经性疼痛和偏头痛，精神疾病如焦虑障碍和精神分裂症，尿 失禁和神经变性疾病，如帕金森病和阿尔茨海默病。 还公开了制备噻吩并嘧啶酮衍生物的方法和含有噻吩并嘧啶酮衍生物作为活性成分的药物组合物。

公开(公告)号：US09260448B2

公开(公告)日：2016-02-16

申请号：US14038324

申请日：2013-09-26

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Hyunah Choo ,  Sun Joon Min ,  Seon Hee Seo ,  Jee Yeon Kim ,  Yoo Ran Ki ,  Min Joo Kim ,  Sora Kim ,  Youngjae Kim

IPC: A01N43/90 ,  A61K31/519 ,  C07D491/00 ,  C07D495/00 ,  C07D495/04

CPC classification number: C07D495/04 ,  A61K31/519

Abstract: Disclosed are thienopyrimidinone derivatives as antagonists that act on metabotropic glutamate receptor subtype 1. The thienopyrimidinone derivatives show pharmacological activity against metabotropic glutamate receptor-related diseases, including pain, such as neuropathic pain and migraine, psychiatric diseases, such as anxiety disorder and schizophrenia, urinary incontinence, and neurodegenerative diseases, such as Parkinson's disease and Alzheimer's disease. Also disclosed are methods for preparing the thienopyrimidinone derivatives, and pharmaceutical compositions containing the thienopyrimidinone derivatives as active ingredients.

Abstract translation: 公开了作为代谢型谷氨酸受体亚型1的拮抗剂的噻吩并嘧啶酮衍生物。噻吩并嘧啶酮衍生物显示针对代谢型谷氨酸受体相关疾病的药理学活性，包括疼痛，如神经性疼痛和偏头痛，精神疾病如焦虑障碍和精神分裂症，尿 失禁和神经变性疾病，如帕金森病和阿尔茨海默病。 还公开了制备噻吩并嘧啶酮衍生物的方法和含有噻吩并嘧啶酮衍生物作为活性成分的药物组合物。

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）。