205999-74-2Relevant academic research and scientific papers
NOVEL OPIOID ANTAGONISTS
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Page/Page column 30; 47-48, (2008/06/13)
Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.
Substituted piperidine compounds
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Page/Page column 18; 22, (2008/06/13)
Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, in
trans-3,4-Dimethyl-4-(3-carboxamidophenyl)piperidines: A novel class of μ-Selective opioid antagonists
Le Bourdonnec, Bertrand,Belanger, Serge,Cassel, Joel A.,Stabley, Gabriel J.,DeHaven, Robert N.,Dolle, Roland E.
, p. 4459 - 4462 (2007/10/03)
trans-3,4-Dimethyl-4-(3-carboxamidophenyl)piperidines constitute a novel class of μ opioid receptor antagonists. The CONH2 group was found to be an effective isostere of the phenolic OH moiety. Structure-activity relationships at the piperidine
Investigation of the N-substituent conformation governing potency and μ receptor subtype-selectivity in (+)-(3R,4R)-dimethyl-4-(3- hydroxyphenyl)piperidine opioid antagonists
Thomas, James B.,Wayne Mascarella,Rothman, Richard B.,Partilla, John S.,Xu, Heng,McCullough, Karen B.,Dersch, Christina M.,Cantrell, Buddy E.,Zimmerman, Dennis M.,Carroll, F. Ivy
, p. 1980 - 1990 (2007/10/03)
A study of the binding site requirements associated with the N- substituent of (+)-(3R,4R)dimethyl-4-(3-hydroxyphenyl)piperidine (4) derivatives was undertaken using a set of rigid vs flexible N-substituents. The study showed that compounds 7-9 bearing th
