Pentadieneamides

Details Pentadieneamides Pentadieneamides

1987-07-10

1988-11-29

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514351, 514352, 514357, 514332, 546291, 546300, 546301, 546302, 546303, 546304, 546305, 546309, 546329, 546331, 546334, 546255, 546264, 546266, C07D21300, A61K 3144

Patent

active

047882069

ABSTRACT:
Compounds of the formula ##STR1## Y is O ir S, *A is paraphenylene or *----(CH.sub.2)n----(X).sub.m --(CH.sub.2).sub.r ----, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het, aryl, R.sub.3, R.sub.4 and R.sub.8, independently, are hydrogen, lower alkyl, aryl, R.sub.5 and R.sub.6, independently, are hydrogen or lower alkyl, R.sub.7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment,
and when R.sub.6 and R.sub.7 are different, their enantiomers and racemic mixtures thereof, when R.sub.1 and R.sub.2 are different, their geometric isomers, and pharmaceutically acceptable acid addition salts thereof, are described.
The compounds of formula I exhibit activity as platelet activating factor (PAF) antagonists and are, therefore, useful in disease states characerized by excess platelet activating factor or for the prevention and treatment of cardiovascular disease, pulmonary diseases, immunological disorders, inflammatory diseases, dermatological disorders, shock or transplant rejection.

REFERENCES:
patent: 3072649 (1963-01-01), Semb et al.
patent: 4542145 (1985-09-01), Wright, Jr. et al.
patent: 4568685 (1986-02-01), Wright, Jr. et al.
patent: 4568687 (1986-02-01), Wright, Jr. et al.
Chemical Abstracts; CA 104:168177c, 1986.
Chemical Abstracts; 107:154084v, 1987.
Chemical Abstracts; 97:6167j, 1982.
Japanese 82-81, 973, C.A. 96:178,218x.
5-Phenyl-2,4-Pentadienamides as Potential Antimalarial Agents, Werbel et al, Journal of Med. Chem., vol. 10, pp. 366-370.

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