Conformationally Constrained ortho-Anilino Diaryl Ureas: Discovery of 1-(2-(1′-Neopentylspiro [indoline-3, 4′-piperidine]-1-yl) phenyl)-3-(4-(trifluoromethoxy) …

…, R Ruel, C Thibeault, A L'Heureux…

Index: Qiao, Jennifer X.; Wang, Tammy C.; Ruel, Rejean; Thibeault, Carl; L'Heureux, Alexandre; Schumacher, William A.; Spronk, Steven A.; Hiebert, Sheldon; Bouthillier, Gilles; Lloyd, John; Pi, Zulan; Schnur, Dora M.; Abell, Lynn M.; Hua, Ji; Price, Laura A.; Liu, Eddie; Wu, Qimin; Steinbacher, Thomas E.; Bostwick, Jeffrey S.; Chang, Ming; Zheng, Joanna; Gao, Qi; Ma, Baoqing; McDonnell, Patricia A.; Huang, Christine S.; Rehfuss, Robert; Wexler, Ruth R.; Lam, Patrick Y. S. Journal of Medicinal Chemistry, 2013 , vol. 56, # 22 p. 9275 - 9295

Full Text: HTML

Citation Number: 16

Abstract

Preclinical antithrombotic efficacy and bleeding models have demonstrated that P2Y1 antagonists are efficacious as antiplatelet agents and may offer a safety advantage over P2Y12 antagonists in terms of reduced bleeding liabilities. In this article, we describe the structural modification of the tert-butyl phenoxy portion of lead compound 1 and the subsequent discovery of a novel series of conformationally constrained ortho-anilino ...