167485-86-1Relevant articles and documents
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 1: Discovery and initial structure-activity relationships for 1-amino-2-phenyl-4-(piperidin-1-yl) butanes
Dorn, Conrad P.,Finke, Paul E.,Oates, Bryan,Budhu, Richard J.,Mills, Sander G.,MacCoss, Malcolm,Malkowitz, Lorraine,Springer, Martin S.,Daugherty, Bruce L.,Gould, Sandra L.,DeMartino, Julie A.,Siciliano, Salvatore J.,Carella, Anthony,Carver, Gwen,Holmes, Karen,Danzeisen, Renee,Hazuda, Daria,Kessler, Joseph,Lineberger, Janet,Miller, Michael,Schleif, William A.,Emini, Emilio A.
, p. 259 - 264 (2001)
Screening of the Merck sample collection for compounds with CCR5 receptor binding afforded (2S)-2-(3,4-dichlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2 ,3-dihydrobenzthiophene-3,4′-piperidin-1′-yl)]butane S-oxide (4) as a potent lead structure having an IC50 binding affinity of 35 nM. Herein, we describe the discovery of this lead structure and our initial structure-activity relationship studies directed toward the requirement for and optimization of the 1-amino fragment.
Spiro-substituted azacycles as neurokinin antagonists
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, (2008/06/13)
Disclosed are spiro-substituted azacycles of formula I are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma. In particular compounds of formula I are shown to be neurokinin antagonists.
Piperidine derivatives useful as neurokinin antagonists
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, (2008/06/13)
Compounds of formula I STR1 wherein Q1, Q2, Q3, and Q4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
