公开(公告)号：US20230165932A1

公开(公告)日：2023-06-01

申请号：US18051250

申请日：2022-10-31

申请人： MERCK SHARP & DOHME LLC

发明人： Hubert Josien ,  Abbas Walji ,  Harold B. WOOD ,  Fa-Xiang Ding ,  Jian Liu ,  Thomas Joseph Tucker ,  Michael Man-Chu Lo ,  Liangqin Guo

IPC分类号： A61K38/12 ,  A61P3/06 ,  C07K9/00

CPC分类号： A61K38/12 ,  A61P3/06 ,  C07K9/006

摘要： Disclosed are compounds of Formula A, or a pharmaceutically acceptable salt thereof:




where A, X, R1, and R2 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.

公开(公告)号：US11484565B2

公开(公告)日：2022-11-01

申请号：US17005686

申请日：2020-08-28

申请人： MERCK SHARP & DOHME LLC

发明人： Hubert Josien ,  Abbas Walji ,  Harold B. Wood ,  Fa-Xiang Ding ,  Jian Liu ,  Thomas Joseph Tucker ,  Michael Man-Chu Lo ,  Liangqin Guo

IPC分类号： A61K38/00 ,  A61K38/12 ,  A61P3/06 ,  C07K9/00

摘要： Disclosed are compounds of Formula A, or a pharmaceutically acceptable salt thereof: where A, X, R1, and R2 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.