Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists
In the design of potent and selective sphingosine-1-phosphate receptor agonists, we were able to identify two series of molecules based on phenylamide and phenylimidazole analogs of FTY-720. Several designed molecules in these scaffolds have demonstrated selectivity for S1P receptor subtype 1 versus 3 and excellent in vivo activity in mouse. Two molecules PPI-4621 (4b) and PPI-4691 (10a), demonstrated dose responsive lymphopenia, when administered orally.
Evindar, Ghotas,Bernier, Sylvie G.,Kavarana, Malcolm J.,Doyle, Elisabeth,Lorusso, Jeanine,Kelley, Michael S.,Halley, Keith,Hutchings, Amy,Wright, Albion D.,Saha, Ashis K.,Hannig, Gerhard,Morgan, Barry A.,Westlin, William F.
scheme or table
p. 369 - 372
(2011/03/18)
METHODS AND COMPOSITIONS FOR MODULATING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR ACTIVITY
The present invention relates to compounds which modulate the activity of the SI P1 receptor, the use of these compounds for treating conditions associated with signaling through the S1 P1 receptor, and pharmaceutical compositions comprising these compounds.
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Page/Page column 61-62
(2010/10/20)
PHENACYL ESTERS - A NEW TYPE OF LUQUID-CRYSTALLINE COMPOUND
The reaction of aliphatic, alicyclic, and aromatic acids with 4-substituted α-bromoacetophenones gave a series of new liquid-crystalline phenacyl esters.Their mesomorphous characteristics are discussed in relation to the structures of the acid and ketone parts of the molecule.
Torgova, S. I.,Karamysheva, L. A.,Agafonova, I. F.
p. 1162 - 1168
(2007/10/02)
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