- 4-Amino-2-(aryl)-butylbenzamides and their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK2) receptor
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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.
- MacKenzie, A. Roderick,Marchington, Allan P.,Middleton, Donald S.,Newman, Sandra D.,Selway, Christopher N.,Terrett, Nicholas K.
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p. 2211 - 2215
(2007/10/03)
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- PIPERIDINE DERIVATIVES, PROCESS FOR OBTAINING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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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.
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- Substituted heteroalkyleneamine neurokinin antagonists
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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.
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- SALTS OF SUBSTITUTED NITROGENOUS HETEROAROMATIC COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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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.
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- Quaternary ammonium salts of aromatic amine compounds, their preparation and pharmaceutical compositions in which they are present
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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.
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- Aryl substituted heterocycles
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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
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- Process for the preparation of an optically pure aminoalcohol
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A process is described for the preparation of (+)-2-(3,4-dichlorophenyl)-4-hydroxybutylamine (I) by reaction of 3,4-dichlorophenylacetonitrile (II) with an alkali metal halogenoacetate, treatment of the 3-cyano-3-(3,4-dichlorophenyl)propionic acid (III) w
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- Therapeutic heterocycles which antagonize neurokinin receptors
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Compounds of formula I STR1 wherein G, J, L, M, m and D have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
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- AROMATIC AMINE COMPOUNDS THEIR METHOD OF PREPARATION AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE PRESENT
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Aromatic amine derivatives of the general formula (I) STR1 or salts of the derivatives with mineral or organic acids are useful as neurokinin receptor antagonists.
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