415936-57-1Relevant articles and documents
Novel and highly potent histamine H3 receptor ligands. Part 3: An alcohol function to improve the pharmacokinetic profile
Labeeuw, Olivier,Levoin, Nicolas,Poupardin-Olivier, Olivia,Calmels, Thierry,Ligneau, Xavier,Berrebi-Bertrand, Isabelle,Robert, Philippe,Lecomte, Jeanne-Marie,Schwartz, Jean-Charles,Capet, Marc
, p. 2548 - 2554 (2013/06/27)
Synthesis and biological evaluation of potent histamine H3 receptor antagonists incorporating a hydroxyl function are described. Compounds in this series exhibited nanomolar binding affinities for human receptor, illustrating a new possible component for the H3 pharmacophore. As demonstrated with compound BP1.4160 (cyclohexanol 19), the introduction of an alcohol function counter-intuitively allowed to reach high in vivo efficiency and favorable pharmacokinetic profile with reduced half-life.
COMBINATION OF MODAFINIL AND AN ANTAGONIST OR INVERSE AGONIST OF THE H3 RECEPTOR
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, (2009/12/27)
The invention relates to a combination of modafinil and at least one histamine H3 receptor antagonist or inverse agonist, which can be used in particular for the treatment of narcolepsy-cataplexy and more generally for disorders of sleep, wakefulness and vigilance.
Phenoxypropylpiperidines and -pyrrolidines and their use as histamine H3-receptor ligands
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Page/Page column 25, (2008/06/13)
The present patent application concerns compounds of formula (I), with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.