378185-92-3Relevant academic research and scientific papers
SELECTIVE FKBP51 LIGANDS FOR TREATMENT OF PSYCHIATRIC DISORDERS
-
Page/Page column 166, (2015/04/15)
The present invention relates to compounds of the general formula (I) having a selective FKBP51 ligand scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with
Stereospecific syntheses of 2-alkyl and 2-phenyl substituted 3-(2,6-dimethyl-4-hydroxyphenyl)propanoic acids
Lu,Schiller
, p. 1639 - 1644 (2007/10/03)
Stereospecific syntheses of 2-methyl-, 2-ethyl-, 2-cyclohexyland 2-phenyl- substituted 3-(2,6-dimethyl-4-hydroxyphenyl)propanoic acids were developed. The key steps for the formation of the stereogenic centers involved the utilization of Evans' 4-benzyl-2-oxazolidinone chiral auxiliary. These compounds were designed to replace the N-terminal tyrosine residue in opioid peptides.
The synthesis of novel matrix metalloproteinase inhibitors employing the Ireland-Claisen rearrangement
Pratt, Lisa M.,Beckett, R. Paul,Bellamy, Claire L.,Corkill, Dominic J.,Cossins, Judy,Courtney, Paul F.,Davies, Stephen J.,Davidson, Alan H.,Drummond, Alan H.,Helfrich, Karen,Lewis, Christopher N.,Mangan, Matthew,Martin, Fionna M.,Miller, Karen,Nayee, Prakash,Rickerts, Michelle L.,Thomas, Wayne,Todd, Richard S.,Whittaker, Mark
, p. 1359 - 1364 (2007/10/03)
Matrix metalloproteinase inhibitors of general formula (1) were synthesised by a route involving an Ireland-Claisen rearrangement which enables systematic modification of the substituent alpha to the hydroxamic acid. An analogue (12c) possessing an α-cyclopentyl group is a potent broad spectrum inhibitor that displays high and sustained blood levels following oral dosing in both the rat and marmoset ex-vivo bioassays. This compound and analogues are also potent inhibitors of TNFα release.
