713143-67-0Relevant articles and documents
Discovery of Potent Orally Active Protease-Activated Receptor 1 (PAR1) Antagonists Based on Andrographolide
Liu, Jun,Sun, Bin,Zhao, Xiaoyu,Xing, Jie,Gao, Yanhui,Chang, Wenqiang,Ji, Jianbo,Zheng, Hongbo,Cui, Changyi,Ji, Aiguo,Lou, Hongxiang
, p. 7166 - 7185 (2017/09/07)
Protease-activated receptor-1 (PAR1), a G-protein-coupled receptor, plays a critical role in thrombin-mediated platelet aggregation. It is regarded as a promising antithrombosis target that is unlikely to result in bleeding. Here, we describe the synthesi
Discovery of octahydroindenes as PAR1 antagonists
Lee, Sunkyung,Song, Jong-Hwan,Park, Chul Min,Kim, Jin-Seok,Jeong, Ji-Hye,Cho, Woo-Young,Lim, Dong-Chul
, p. 1054 - 1058 (2013/12/04)
Octahydroindene was identified as a novel scaffold for protease activated receptor 1 (PAR1) antagonists. Herein, the 2-position (C2) was explored for structure-activity relationship (SAR) studies. Compounds 14, 19, and 23b showed IC50 values of 1.3, 8.6, and 2.7 nM in a PAR1 radioligand binding assay, respectively, and their inhibitory activities on platelet activation were comparable to that of vorapaxar in a platelet rich plasma (PRP) aggregation assay. This series of compounds showed high potency and no significant cytotoxicity; however, the compounds were metabolically unstable in both human and rat liver microsomes. Current research efforts are focused on optimizing the compounds to improve metabolic stability and physicochemical properties as well as potency.
[6+5] FUSED BICYCLES AS A THROMBIN ANTAGONIST, PROCESS FOR PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE BICYCLES
-
, (2012/01/14)
The present invention relates to the new [6+5] fused bicycle derivatives, pharmaceutically acceptable salts or isomers thereof, processes for preparing the same, and pharmaceutical compositions comprising the same. The [6+5] fused bicycle derivatives can antagonize the thrombin receptor and thus may be effectively used for the treatment and prevention of thrombus, platelet aggregation, atherosclerosis, restenosis, blood coagulation, hypertension, arrhythmia, angina pectoris, heart failure, inflammation and cancer when used alone or with other cardiovascular agents.
Method for producing biaryl compounds
-
Page/Page column 25, (2008/06/13)
[PROBLEM TO BE SOLVED]: To provide method for producing biaryl compound in high purity and in high selectivity.[SOLUTION]: This method for producing the biaryl compound is characterized by coupling a halogenated aryl with a organomethallic aryl in the presence of a transition metal multidentate phosphite complex catalyst to obtain the biaryl compound.