530441-99-7Relevant articles and documents
Two complementary, diversity-driven asymmetric syntheses of a 2,2-disubstituted piperidine NK1 antagonist
Xiao, Dong,Wang, Cheng,Palani, Anandan,Reichard, Gregory,Aslanian, Robert,Shih, Neng-Yang,Buevich, Alexei
, p. 2596 - 2598 (2007/10/03)
Two diversity-driven asymmetric syntheses of a potent NK1 receptor antagonist 1 were achieved. These syntheses provided two complementary approaches that were well positioned for further modifications of several different sites of medicinal che
Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions
Shue, Ho-Jane,Chen, Xiao,Schwerdt, John H.,Paliwal, Sunil,Blythin, David J.,Lin, Ling,Gu, Danlin,Wang, Cheng,Reichard, Gregory A.,Wang, Hongwu,Piwinski, John J.,Duffy, Ruth A.,Lachowicz, Jean E.,Coffin, Vicki L.,Nomeir, Amin A.,Morgan, Cynthia A.,Varty, Geoffrey B.,Shih, Neng-Yang
, p. 1065 - 1069 (2007/10/03)
A series of novel five-membered urea derivatives as potent NK1 receptor antagonists is described. The effects of substitution of a 4-fluoro group at the phenyl ring and the introduction of an α-methyl group at the benzylic position to improve p
Cyclobutane derivatives as potent NK1 selective antagonists
Wrobleski, Michelle Laci,Reichard, Gregory A.,Paliwal, Sunil,Shah, Sapna,Tsui, Hon-Chung,Duffy, Ruth A.,Lachowicz, Jean E.,Morgan, Cynthia A.,Varty, Geoffrey B.,Shih, Neng-Yang
, p. 3859 - 3863 (2007/10/03)
A series of novel cyclobutane derivatives as potent and selective NK1 receptor antagonists is described. Several compounds in this series exhibited high in vitro binding affinity (Ki {less-than or slanted equal to} 1 nM), and potent