397277-60-0

Upstream product

• 3612-20-2 1-phenylmethyl-4-piperidone 
• 333954-90-8 4-(4-cyanophenoxy)piperidine· hydrochloride 
• 100-52-7 benzaldehyde 
• 623-03-0 4-Cyanochlorobenzene 
• 333954-86-2 4-(4-cyano phenoxy)piperidine-1-carboxylic acid tert-butyl ester 
• 4727-72-4 1-benzyl-4-hydroxypiperidine 
• 1194-02-1 4-fluorobenzonitrile 
• 109384-19-2 t-butyl 4-hydroxy piperidine-1-carboxylate 

Relevant academic research and scientific papers

COMPOUNDS AND METHODS OF USE

Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X1, X2, X3, X4, X5, A, L, R1, R2, R5, m and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

Compounds and methods of use

Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X1, X2, X3, X4, Y, A, L1, L2, R1, R2, R5, m and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

NPY ANTAGONISTS, PREPARATION AND USES

The present invention concerns novel compounds, their preparation and their uses, therapeutic uses in particular. More specifically it concerns derivative compounds having at least two aromatic cycles, their preparation and their uses, in particular in the area of human or animal health. These compounds have an affinity for the biological receptors of neuropeptide Y, NPY, present in the central and peripheral nervous systems. The compounds of the invention are preferably NPY antagonists, and more particularly antagonists of sub-type NPY Y1, and can therefore be used for the therapeutic or prophylactic treatment of any disorder involving NPY. The present invention also concerns pharmaceutical compositions containing said compounds, their preparation and their uses, as well as treatment methods using said compounds.

4-Phenoxypiperidines: Potent, conformationally restricted, non-imidazole histamine H3 antagonists

Two new series of 4-(1-alkyl-piperidin-4-yloxy)-benzonitriles and 4-(1-isopropyl-piperidin-4-yloxy)-benzylamines have been prepared. In vitro activity was determined at the recombinant human H3 receptor and several members of these new series were found to be potent H3 antagonists. The present compounds contain a 4-phenoxypiperidine core, which behaves as a conformationally restricted version of the 3-amino-1-propanol moiety common to the many previously described non-imidazole histamine H 3 ligands. One selected member of the new series, 4-[4-(1-isopropyl-piperidin-4-yloxy)-benzyl]-morpholine (13g), was found to be a potent, highly selective H3 receptor antagonist with in vivo efficacy in a rat EEG model of wakefulness at doses as low as 1 mg/kg sc.

OPIOID RECEPTOR ANTAGONISTS

A compound of the formula (I) wherein the variables X1 to X5, R1 to R7 including R3', E, q, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, dia