申请人:KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
公开号:US20140228565A1
公开(公告)日:2014-08-14
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.
披露了作为对代谢型谷氨酸受体亚型1起作用的拮抗剂的噻吩嘧啶酮衍生物。这些噻吩嘧啶酮衍生物显示出对代谢型谷氨酸受体相关疾病的药理活性,包括疼痛,如神经病性疼痛和偏头痛,精神疾病,如焦虑症和精神分裂症,尿失禁,以及神经退行性疾病,如帕金森病和阿尔茨海默病。还披露了制备这些噻吩嘧啶酮衍生物的方法,以及含有这些噻吩嘧啶酮衍生物作为活性成分的药物组合物。