872879-86-2Relevant 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
PROCESS FOR PREPARING BETA- (FLUOROPHENYL) -PROPANOATE ESTER DERIVATIVES
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Page/Page column 11-12, (2008/06/13)
A process for preparing a compound of formula (I) comprising reacting a compound of formula (II) with a fluorinated boron species of formula (III) in the presence of: an alcohol; a rhodium (I) pre-catalyst species; a suitable ligand that binds to the rhodium (I) pre-catalyst species to form a catalyst complex; a base; and, a suitable solvent; the process being carried out at a temperature in the range 40 to 110oC. The compounds of formula (I) are useful in the preparation of pharmaceutically active compounds.
CHEMICAL COMPOUNDS I
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Page/Page column 31, (2010/02/15)
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).
