527693-93-2Relevant academic research and scientific papers
Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis
Cumming, John G.,Tucker, Howard,Oldfield, John,Fielding, Colin,Highton, Adrian,Faull, Alan,Wild, Martin,Brown, Dearg,Wells, Stuart,Shaw, John
, p. 1655 - 1659 (2012/04/04)
Modifications to a series of potent and selective substituted 1-(3,3-diphenylpropyl)-piperidine phenylacetamide CCR5 antagonists were explored with the aim of reducing affinity at the hERG cardiac ion channel. Replacement of one aromatic ring in the diphe
Evaluation of amide replacements in CCR5 antagonists as a means to increase intrinsic permeability. Part 2: SAR optimization and pharmacokinetic profile of a homologous azacyle series
Wanner, Jutta,Chen, Lijing,Lemoine, Rémy C.,Kondru, Rama,Jekle, Andreas,Heilek, Gabrielle,Derosier, André,Ji, Changhua,Berry, Pamela W.,Rotstein, David M.
scheme or table, p. 6802 - 6807 (2011/01/04)
Replacement of a secondary amide with a piperidine or azetidine moiety in a series of CCR5 antagonists led to the discovery of compounds with increased intrinsic permeability. This effort led to the identification of a potent CCR5 antagonist which exhibited an improved in vivo pharmacokinetic profile.
OCTAHYDROPYRROLO [3, 4-C] PYRROLE DERIVATIVES AN THEIR USE AS ANTIVIRAL AGENTS
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Page/Page column 68-69, (2008/06/13)
Chemokine receptor antagonists, in particular, 3,7-diazabicyclo [3.3.0] octane compounds according to formula (I) wherein R1-R3 and Ar are as defined herein are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula (I).
Chemical compounds
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Page/Page column 37, (2008/06/13)
Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
