Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor β ligands
We recently discovered the isoform selective RARβ2 ligand 4′-octyl-4-biphenylcarboxylic acid (3, AC-55649). Although 3 is highly potent at RARβ2 and displays excellent selectivity, solubility issues make it unsuitable for drug development. Herein we descr
Lund, Birgitte W.,Knapp, Anne Eeg,Piu, Fabrice,Gauthier, Natalie K.,Begtrup, Mikael,Hacksell, Uli,Olsson, Roger
supporting information; experimental part
p. 1540 - 1545
(2009/12/25)
COMPOUNDS WITH ACTIVITY AT RETINOIC ACID RECEPTORS
Disclosed herein are novel compounds with activity at RARβ 2 receptors. Further disclosed are the use of such compounds for treatment of or to alleviate symptoms of cancer, neurological disorders such as memory deficits and schizophrenia, neurodegenerative disorders such as Parkinson's and Alzheimer's diseases, inflammatory disorders such as psoriasis and rheumatoid arthritis, eye disorders and depression.
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Page/Page column 45
(2008/06/13)
Discovery of a potent, orally available, and isoform-selective retinoic acid β2 receptor agonist
4′-Octyl-4-biphenylcarboxylic acid (1g, AC-55649) was identified as a highly isoform-selective agonist at the human RARβ2 receptor in a functional intact cell-based screening assay. The subsequent hit to lead optimization transformed the lipophilic, poorl
Lund, Birgitte W.,Piu, Fabrice,Gauthier, Natalie K.,Eeg, Anne,Currier, Erika,Sherbukhin, Vladimir,Brann, Mark R.,Hacksell, Uli,Olsson, Roger
p. 7517 - 7519
(2007/10/03)
N-acylamino acid amide compounds and intermediates for preparation thereof
The present invention discloses the compound represented by the formula (I): wherein A represents the following formula (a-1) or the following formula (a-2): B represents the following formula (b): (wherein the symbols are each as defined in the specification) or a pharmaceutically acceptable salts thereof, and intermediates for the preparation thereof, which have excellent platelet aggregation inhibitory activity and other properties and useful as prophylactic or therapeutic agents for diseases associated with a fibrinogen receptor, thrombosis, infarction and the like.
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(2008/06/13)
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