Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1988-10-27
1990-07-03
Berch, Mark L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514225, 514226, 514228, 514230, 514231, 514232, 514234, 514236, 514241, 514242, 514243, 514248, 544 3, 544 8, 544 11, 544 12, 544 49, 544 50, 544 51, 544 54, 544 586, 544 63, 544 66, 544 67, 544 73, 544 80, 544 96, 544105, C07D23732, C07D51900, A61K 3150
Patent
active
049391402
ABSTRACT:
A heterocyclic oxophthalazinyl acetic acid having aldose reductast inhibitory activity of the formula ##STR1## wherein X is oxygen or sulfur; Z is a covalent bond, O, S, NH or CH.sub.2 or CHR.sub.5 Z is vinyl; R.sub.1 is hydroxy, or a prodrug group; R.sub.2 is a heterocyclic group, R.sub.3 and R.sub.4 are hydrogen or the same or a different substituent, and R.sub.5 is hydrogen, methyl or trifluoromethyl. The pharmaceutically acceptable acid addition salts of the above compounds wherein R.sub.1 is di(C.sub.1 -C.sub.4)alkylamino or (C.sub.1 -C.sub.4)alkoxy substituted by N-morpholino or di(C.sub.1 -C.sub.4)alkylamino and the pharmaceutically active base addition salts of the above compounds wherein R.sub.1 is hydroxy are also aldose reductase inhibitors.
REFERENCES:
patent: 4120960 (1978-10-01), Bristow
Foldeak, Khim. Pharm. Zh., 1970, 4(5), 22-6, 1970-English Translation.
Mylari, Chem. Abs. 107, 176055p, (May 20, 1977).
Foldeak, Chem. Abs. 73, 77173y, (1970).
Larson Eric R.
Mylari Banavara L.
Berch Mark L.
Ginsburg Paul H.
Holtrust Gezina
Pfizer Inc.
Richardson Peter C.
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