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.
Quaternary ammonium salts of aromatic amine compounds, their preparation and pharmaceutical compositions in which they are present
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, (2008/06/13)
The present invention relates to quaternary ammonium salts of the formula STR1 in which: J is either a group Ar--CXX''--CX"" or a group Ar--(CH 2) x CH 1, in which:Ar is a substituted or unsubstituted phenyl, a cycloalkyl, a pyridyl or a thienyl;X is hydrogen;X'' is hydrogen or is combined with X"" below to form a carbon-carbon bond, or else X and X'' together form an oxo group;X"" is hydrogen or forms a carbon-carbon bond with X'';X is zero or one; andX 1 is hydrogen (n=0), a hydroxyl, an alkoxy, an acyloxy, a carboxyl, a carbalkoxy, a cyano or an alkoxyamino group;Q is an alkyl group or a benzyl group;A is an anion;m is 2 or 3;Ar'', R, T and Z are as defined in the specification, are neurokinin receptor antagonists.