Derivatives of (E)-3-(4-oxo-4H-quinazolin-3-yl)-2-propenamide

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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514242, 514253, 544182, 544284, 544286, A61K 31505, C07D40112

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active

045993360

ABSTRACT:
Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, lower cycloalkyl, lower alkoxy, hydroxy, halo, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, di-(C.sub.1 -C.sub.7) alkyl-N(CH.sub.2).sub.n O-- or 2-hydroxyethoxy; n is 2 to 7; R.sub.2 is hydrogen, lower alkyl or lower alkoxy; R.sub.3 is hydrogen or methyl; R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen or lower alkyl provided however if R.sub.2 is other than hydrogen R.sub.5 is hydrogen; m is 1 to 7; Y is ##STR2## --O-- or --S--; w is zero or one; and A is an unsubstituted or substituted aromatic 5- or 6-membered heterocyclic radical;
or pharmaceutically acceptable addition salts thereof are described. The compounds of formula I are useful for treating allergic conditions and vascular disorders.

REFERENCES:
patent: 4281127 (1981-07-01), LeMahieu et al.
patent: 4451467 (1984-05-01), Ishikawa et al.
Iizuka, et al., "J. Med. Chem.", vol. 24, 1981, pp. 1139-1148.
Tanouchi, et al., "J. Med. Chem.", vol. 24, 1981, pp. 1149-1155.
LeMahieu, et al., "J. Med. Chem.", vol. 26, 1983, pp. 420-425.

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