Piperidine derivatives useful as neurokinin antagonists

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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Details

544315, 544316, 544318, A61K 31505, C07D23910

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active

056355092

ABSTRACT:
Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 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.

REFERENCES:
patent: 4782061 (1988-11-01), Kruse et al.
patent: 5236921 (1993-08-01), Emonds-Alt et al.
A. Graham et al., "Isolation and Characterisation of the Human Lung NK-2 Receptor Gene Using Rapid Amplification of cDNA Ends", Biochemical and Biophysical Research Communications, (1991), vol. 177, No. 1, 8-16.
X. Emonds-Alt et al., "Pharmacological Profile and Chemical Synthesis of SR 48968, a Non-Peptide Antagonist of the Neurokinin A (NK.sub.2) Receptor", Biorganic & Medicinal Chemistry Letters, (1993), vol. 3, No. 5, 925-930.
D. Aharony et al., "Pharmacologic Characterization of the Novel Ligand [4,5-.sup.3 H-LEU.sup.9 ]Neurokinin-A Binding to NK-2 Receptors on Hamster Urinary Bladder Membranes", Neuropeptides, (1992), 23, 121-130.
M. Needham et al., "LCR/MEL: A Versatile System for High-Level Expression of Heterologous Proteins in Erythroid Cells", Nucleic Acids Research, (1992), vol. 20, No. 5, 997-1003.

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