861673-68-9Relevant academic research and scientific papers
Studies towards the development of a PET radiotracer for imaging of the P2Y1 receptors in the brain: synthesis, 18F-labeling and preliminary biological evaluation
Moldovan, Rare?-Petru,Wenzel, Barbara,Teodoro, Rodrigo,Neumann, Wilma,Dukic-Stefanovic, Sladjana,Kraus, Werner,Rong, Peijing,Deuther-Conrad, Winnie,Hey-Hawkins, Evamarie,Krügel, Ute,Brust, Peter
, p. 142 - 159 (2019/01/23)
Purine nucleotides such as ATP and ADP are important extracellular signaling molecules in almost all tissues activating various subtypes of purinoreceptors. In the brain, the P2Y1 receptor (P2Y1R) subtype mediates trophic functions l
Design, synthesis, and biological evaluation of 2-(phenoxyaryl)-3-urea derivatives as novel P2Y1 receptor antagonists
Peng, Jingjing,Zhao, Lifen,Wang, Lanlan,Chen, Hui,Qiu, Yunguang,Wang, Jiang,Yang, Huaiyu,Liu, Jun,Liu, Hong
, p. 302 - 310 (2018/09/18)
A novel series of 2-(phenoxyaryl)-3-urea derivatives were designed, synthesized, and biologically evaluated for their anti-thrombotic activity. Most of compounds exhibited good inhibition against P2Y1 receptor. Among them, three compounds 11, 12, and 13 demonstrated good P2Y1 receptor antagonistic potency in vitro (IC50 = 0.62 μM, 0.82 μM, and 0.21 μM, respectively). In antiplatelet aggregation study, four compounds 2, 3, 9, and 13 showed good antiplatelet activity. The possible binding modes of compounds with P2Y1 receptor were also explored by molecular docking simulation. The docking studies demonstrated that compound 13 interacted well with Phe119 through hydrophobic interaction and modestly improved the P2Y1 receptor antagonistic activity, making it justifiable for further investigation.
2-Aminothiazole based P2Y1 antagonists as novel antiplatelet agents
Pi, Zulan,Sutton, James,Lloyd, John,Hua, Ji,Price, Laura,Wu, Qimin,Chang, Ming,Zheng, Joanna,Rehfuss, Robert,Huang, Christine S.,Wexler, Ruth R.,Lam, Patrick Y.S.
, p. 4206 - 4209 (2013/07/25)
ADP receptors, P2Y1 and P2Y12 have been recognized as potential targets for antithrombotic drugs. A series of P2Y1 antagonists that contain 2-aminothiazoles as urea surrogates were discovered. Extensive SAR of the thiazole
Discovery of diarylurea P2Y1 antagonists with improved aqueous solubility
Wang, Tammy C.,Qiao, Jennifer X.,Clark, Charles G.,Jua, Ji,Price, Laura A.,Wu, Qimin,Chang, Ming,Zheng, Joanna,Huang, Christine S.,Everlof, Gerry,Schumacher, William A.,Wong, Pancras C.,Seiffert, Dietmar A.,Stewart, Anne B.,Bostwick, Jeffrey S.,Crain, Earl J.,Watson, Carol A.,Rehfuss, Robert,Wexler, Ruth R.,Lam, Patrick Y.S.
, p. 3239 - 3243 (2013/06/27)
Preclinical data suggests that P2Y1 antagonists, such as diarylurea compound 1, may provide antithrombotic efficacy similar to P2Y 12 antagonists and may have the potential of providing reduced bleeding liabilities. This manuscript d
Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y 1 antagonists
Chao, Hannguang,Turdi, Huji,Herpin, Timothy F.,Roberge, Jacques Y.,Liu, Yalei,Schnur, Dora M.,Poss, Michael A.,Rehfuss, Robert,Hua, Ji,Wu, Qimin,Price, Laura A.,Abell, Lynn M.,Schumacher, William A.,Bostwick, Jeffrey S.,Steinbacher, Thomas E.,Stewart, Anne B.,Ogletree, Martin L.,Huang, Christine S.,Chang, Ming,Cacace, Angela M.,Arcuri, Maredith J.,Celani, Deborah,Wexler, Ruth R.,Lawrence, R. Michael
, p. 1704 - 1714 (2013/04/10)
Two distinct G protein-coupled purinergic receptors, P2Y1 and P2Y12, mediate ADP-driven platelet activation. The clinical effectiveness of P2Y12 blockade is well established. Recent preclinical data suggest that P2Y1
Linear urea mimics antagonists of P2Y1 receptor useful in the treatment of thrombotic condition
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Page/Page column 23-24, (2010/11/25)
The present invention provides novel urea mimics and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, W, and R6 are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.
Heteroaryl compounds as P2Y1 receptor inhibitors
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Page/Page column 40, (2008/06/13)
The present invention provides novel heteroaryl compounds and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.
Carbocycle and heterocycle antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
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Page/Page column 19, (2010/11/25)
The present invention provides novel urea mimics and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, W, and R6 are as defined herein. These compounds a
AMINO-BENZAZOLES AS P2Y1 RECEPTOR INHIBITORS
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Page/Page column 64-65, (2008/06/13)
The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating dis
