Following the discovery of the human histamine H 4 receptor, a high throughput screen of our
corporate compound collection identified compound 6 as a potential lead. Investigation of …

Orexins are peptides produced by lateral hypothalamic neurons that exert a prominent role
in the maintenance of wakefulness by activating orexin-1 (OX1R) and orexin-2 (OX2R) …

Ring‐closing metathesis was used as a key step in the first total syntheses of the streptogramin
antibiotics griseoviridin (1) and its C‐8 epimer starting from D‐and L‐cystine, respectively…

Three series of H 4 receptor ligands, derived from indoly-2-yl-(4-methyl-piperazin-1-yl)-methanones,
have been synthesized and their structure−activity relationships evaluated for …

In rodents 5-hydroxytryptamine type 7 (5-HT 7 ) receptor blockade has been shown to be
effective in models of depression and to increase the latency to rapid eye movement (REM) …

A single pot dipolar cycloaddition reaction/Cope elimination sequence was developed to
access novel 1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridine P2X7 antagonists that contain …

Two new conformationally-restricted chiral bicyclic thiazolium salts have been synthesized
by a concise, high-yielding route. These salts are effective catalysts for the benzoin …

GPR139 is an orphan G-protein–coupled receptor expressed in the central nervous system.
To identify its physiologic ligand, we measured GPR139 receptor activity from recombinant …

4-(Aminoalkoxy)benzylamines were prepared and screened for in vitro activity at the human
histamine H 3 receptor. Some members of this series exhibited subnanomolar binding …

The synthesis and preclinical characterization of novel 4-(R)-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridines
that are potent and selective brain penetrant P2X7 antagonists are described…