1.2.3.4-四氫異喹啉衍生物其製備方法及含彼之醫藥組合物

專利類型

發明

專利國別 (專利申請國家)

中華民國

專利申請案號

097116047

專利證號

I 364279

專利獲證名稱

1.2.3.4-四氫異喹啉衍生物其製備方法及含彼之醫藥組合物

專利所屬機關 (申請機關)

國防醫學院

獲證日期

2012/05/21

技術說明

本發明提供一類1,2,3,4-四氫異喹碄(1,2,3,4-tetrahydroisoquinoline)衍生物,該衍生物系如圖示支結構.其中R1為丙炔基或環丙烯甲基,其中R2為N-乙基-N-甲氨基或1-砒咯烷基或1-呱啶基或1-嗎碄基之一取代基.本發明並提供該類衍生物之製備方法及含彼之醫藥組合物,該些衍生物可用於調控類澱粉前驅蛋白的蛋白水解過程,進而提供治療阿茲海默症的新穎化合物. 1,2,3,4-四氫異喹碄作為反應起始物利用化學合成反應,進行不同官能基之修飾,以產生新穎1,2,3,4-四氫異喹碄燕生物. A type of new 1,2,3,4-tetrahydroisoquinoline derivatives was synthesized via concise procedure from commercially available tetrahydroisoquinoline. These derivatives were delicately designed to possess propargyl-related pharmacophores simulated with a monoamine oxidase inhibitor rasagiline. They effectively modulate the regulation of proteolytic processing of amyloid precursor protein (APP) by an ERK-dependent signaling pathway. Additionally, these compounds also displayed gamma-secretase inhibitory effetcs. The results suggested that certain compounds might be explored to possess both sAPPa-releasing stimulation and gamma-secretase inhibitory potency, which contribute the synergetic potential of neuroprotective activities for the treatment of Alzheimer’s disease.

備註

本部(收文號1070014974)備查該校107年2月27日國院研發字第1070000772號函通報終止維護專利(國防醫)

連絡單位 (專責單位/部門名稱)

研究發展室

連絡電話

(02)8792-3100分機18079