Pharmaceutical compositions of-2,2-1,1-[bis-2,2'-(3,1-benzoxazin

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

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514218, 5142282, 5142305, 544 586, 544 73, A61K 31535, C07D26536

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active

048227919

ABSTRACT:
This invention relates to pharmaceutical compositions of compounds of the general formula: ##STR1## wherein R.sup.1 is an aryl group or a substituted aryl group wherein the substituent is halogen, hydroxy, C.sub.(1-6) lower alkoxy, C.sub.(1-6) lower alkylenedioxy, halo C.sub.(1-6) lower alkyl, cyano, nitro, mono- or di-C.sub.(1-6) alkylamino or C.sub.(1-6) lower alkanoylamino; or a 5-membered or 6-membered C.sub.(1-6) alkyl substituted or unsubstituted heterocyclic group containing a heteroatom selected from oxygen, nitrogen, and sulfur, or a condensed heterocyclic group consisting of a heterocycle as defined above and a benzene nucleus, and R.sup.2 and R.sup.2' are, independently, hydrogen, halogen, nitro, C.sub.(1-6) lower alkyl or C.sub.(1-6) lower alkoxy. These compounds have been found to exhibit hyaluronidase inhibiting activity, anti-allergic activity and anti-ulcerous activity. The present invention further contemplates processes for the preparation of said compounds and their pharmaceutical compositions.

REFERENCES:
Shepel et al., "N,N'-Malonybis(Aminoterephthalic Acid)", Chem Abstracts, 70, 15:67926v, (1969).
Black et al., "Metal Template Reactions. XV The Scope of Macrocyclic Metal Complex Formation from Malonamido Dicarbonyl Precursors.": Australian J. Chem., 36, pp. 1133-1140.
Satoh et al., "Studies on Methodology of Finding Novel Anti-Allergenic Agents with the Guidance of Anti-Hyaluronidase Activity", VIIIth International Symposium on Medicinal Chemistry, Aug. 27-31, 1984.

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