152298-51-6Relevant articles and documents
4-Amino-2-(aryl)-butylbenzamides and their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK2) receptor
MacKenzie, A. Roderick,Marchington, Allan P.,Middleton, Donald S.,Newman, Sandra D.,Selway, Christopher N.,Terrett, Nicholas K.
, p. 2211 - 2215 (2007/10/03)
A library, evaluating a range of piperazines, piperidines and acyclic amines, as replacements for the 4-hydroxy-4-phenylpiperidine moiety in lead (1b) was prepared. These efforts identified the 4-((N)-benzimidazolone)piperidine analogue (2a) which was further optimised using classical single-compound synthesis to yield the 3-((N)-morpholino)azetidine (2j). Conformationally constrained analogues of (2j), generally offered no potency advantage in this particular series.
Substituted heteroalkyleneamine neurokinin antagonists
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, (2008/06/13)
Compounds of formula I STR1 wherein Q1, Q2, Q3, and Q4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP and NKA are useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
SALTS OF SUBSTITUTED NITROGENOUS HETEROAROMATIC COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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, (2008/06/13)
The invention concerns compounds of formula: STR1 in which Am + represents a substituted 1-pyridylium radical, a substituted 3-thiazolylium radical, a substituted 1-pyridazinylium radical or a substituted 3-imidazolylium radical, and their salts with mineral or organic acids, whether in their optically pure or racemic form. The invention also concerns a process for the preparation of these compounds and pharmaceutical compositions containing them. Activity: antagonists of neurokinin receptors.