Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1989-04-12
1991-08-20
Wax, Robert A.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514339, 514414, 514418, 546273, 548510, 548511, C07D20920, A61K33140
Patent
active
050414607
ABSTRACT:
This invention provides a series of novel heter-aliphatic carboxamides of formula I in which the group >Z--Y--X< is selected from >C.dbd.CH--N<, >N--CH.dbd.C<, >C.dbd.N--N< and >N--N.dbd.C< and the other radicals have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.
REFERENCES:
J. L. Marx, Science (1982) 215, 1380: "The Leukotrienes in Allergy and Inflammation".
J. A. Cook, et al., J Pharm. Exp. Ther. (1985) 235, 470: "Protective Effect of a Selective Leukotriene Antagonist in Endotoxemia in the Rat".
C. Denzlinger, et al., Science (1985) 230, 330: "Leukotrienes as Mediators in Tissue Trauma".
R. D. Krell, J. Pharm. Exp. Ther. (1979) 211, 436: "Pharmacologic Characterization of Isolated Rhesus Monkey Brochial Smooth Muscle".
D. Aharony, et al., Fed Proc. (1987) 46, 691: "Inhibition of .sup.3 H-Leukotriene (LT) D.sub.4 Binding to Guinea-pig Lung Membrane Receptors by the Novel Leukotriene Antagonist ICI 198,615".
Yung-chi Cheng and W. H. Prusoff, Biochem. Pharmacol. (1973) 22, 3099-3108: "Relationship Between the Inhibition Constant (K.sub.I) and the Concentration of Inhibitor Which Causes 50 Per Cent Inhibition (I.sub.50) of an Enzymatic Causes 50 Reaction".
ICI Americas Inc.
Jackson Thomas E.
Miano Rosemary M.
Tsung Frederick F.
Wax Robert A.
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