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The discovery of 6-[2-(5-chloro-2-{[(2,4-difluorophenyl)methyl]oxy}phenyl)-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid, GW848687X, a potent and selective prostaglandin EP1 receptor antagonist for
TLDR
From this series of selective EP1 receptor antagonists, GW848687X was shown to have an excellent profile in models of inflammatory pain and was selected as a development candidate.
Dynamics of Aβ42 Reduction in Plasma, CSF and Brain of Rats Treated with the γ-Secretase Modulator, GSM-10h
TLDR
These findings support the γ-secretase modulator profile of GSM-10h, and highlight the utility of the rat for assessing the pre-clinical efficacy ofγ- secretase modulators, in a model of endogenous Aβ production.
Reversible Inhibition of Human Carboxylesterases by Acyl Glucuronides
TLDR
Drug-drug interaction studies may be warranted for drugs that metabolize to acyl glucuronides due to the potential inhibition of hCESs.
Piperidine-derived gamma-secretase modulators.
TLDR
Compound 10h was found to be a potent modulator in vitro, which on further profiling, was finding to decrease Abeta42, increase Abeta38 and have no effect on Abeta40 levels.
A General Method for the a-Acyloxylation of Carbonyl Compounds
A simple, one-pot method for the α-acyloxylation of carbonyl compounds that proceeds at room temperature in the presence of both moisture and air has been developed. Treatment of a variety of
Novel Strategies To Activate the Dopamine D1 Receptor: Recent Advances in Orthosteric Agonism and Positive Allosteric Modulation.
TLDR
This review highlights the recent progress in the field, covering both orthosteric and allosteric modes of activation, discusses the elucidation of theAllosteric binding sites, and summarizes the clinical development status of various compounds.
Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists.
Replacement of the carboxylic acid group in a series of previously described 1,5-biaryl pyrrole EP1 receptor antagonists led to the discovery of various novel non-acidic antagonists. Several
γ‐Secretase modulators do not induce Aβ‐rebound and accumulation of β‐C‐terminal fragment
J. Neurochem. (2012) 121, 277–286.
Discovery of novel biaryl heterocyclic EP1 receptor antagonists.
TLDR
The generation of novel EP(1) receptor antagonists by investigation of thiophene isosteres is described and preliminary in vitro and in vivo DMPK for selected compounds are disclosed.
Novel 4-(aryloxy)tetrahydropyridine analogs of MPTP as monoamine oxidase A and B substrates.
TLDR
The expected dihydropyridinium metabolites generated from these MAO-A- andMAO-B-catalyzed oxidations of the 4-(aryloxy)tetrahydropyridine analogs were found to undergo rapid hydrolytic cleavage to yield the corresponding arenol and 1-methyl-2,3-dihydro-4-pyridone, a species that could be monitored spectrophotometrically.
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