Piperidinyl compounds as neurokinin receptor antagonists

Details Piperidinyl compounds as neurokinin receptor antagonists Piperidinyl compounds as neurokinin receptor antagonists

1994-05-16

1996-05-28

Chang, Ceila

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546233, A61K 31445, C07D21126

Patent

active

055211992

ABSTRACT:
The present invention concerns the novel alkyl substituted heterocycles of formula I, set out below, wherein Q, Q.sup.1, Q.sup.2 and R have the values defined herein, which antagonize the pharmacological actions of one of the endogenous neuropeptide tachykinins at the neurokinin 2 (NK.sup.2) 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 alkyl substituted heterocycles for use in such treatment, methods for their use, and processes and novel intermediates for their manufacture. ##STR1##

REFERENCES:
patent: 5236921 (1993-08-01), Emonds-Alt et al.
patent: 5300648 (1994-04-01), Emonds-Alt
patent: 5350852 (1994-09-01), Emonds-Alt
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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