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.
PIPERIDINE DERIVATIVES, PROCESS FOR OBTAINING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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, (2008/06/13)
Piperidine derivatives, process for obtaining them and pharmaceutical compositions containing them, of formula STR1 used as neurokinin receptor antagonists, which are, in particular, useful for the treatment of all substance P-and neurokinin-dependent pathologies.
Aryl substituted heterocycles
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, (2008/06/13)
The present invention concerns the novel use of aryl substituted heterocycles of formula I, set out below, which antagonize the pharmacological actions of one of ent endogenous neuropeptide tachykinins an the neurokinin 2 (NK2) receptor making them useful whenever such antagonism is desired, such as in the treatment of asthma and related conditions. The invention also provides pharmaceutical compositions containing the aryl substituted heterocycles for use in such treatment. Certain novel aryl substituted heterocycles of formula I and novel intermediates for their manufacture are also provided. STR1