Aryl substituted heterocycles

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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5142278, 5142315, 514255, 514278, 514316, 514317, 514318, 514319, 514320, 514321, 514326, 514327, 514329, 514330, 546 16, 546 17, 546186, 546187, 546188, 546190, 546192, 546194, 546195, 546196, 546198, 546201, 546205, 546206, 546207, 546208, 546213, 546214, 546216, 546217, 546223, 544 60, 544 66, 544129, 544244, 544360, A61K 31445, A61K 3154, C07D21106, C07D27304

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active

056542992

ABSTRACT:
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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X. Emonds-Alt et al., "Pharmacological Profile and Chemical Synthesis of SR 48968, a Non-Peptide Antagonist of the Neurokinin A (NK.sub.2-l) 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.
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