Synthesis of pharmaceutical compositions with lactams and .beta.

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

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514183, 514200, 514359, 514430, 514438, 514444, 435117, 435128, 435130, 424114, 540304, 549 29, 549 32, A61K 3143, C12P 1700, C07D49900

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active

060158085

ABSTRACT:
Pharmaceutical compositions with heretofore unknown and enhanced physical, chemical, and biological properties are prepared by combining known biologically active parent compounds with oxo thia azabicyclo compounds, such as lactam and .beta.-lactam compounds, capable of rapidly transporting the parent compounds in undegraded form to their target sites of action. A process for combining the parent compound with .beta.-lactam compounds consists of dissolving the parent compound in a polar solvent, adding a .beta.-lactam compound, incubating the resulting mixture, followed by drying, and subjecting the remaining solid material to solvent washing or extraction to further purify the new pharmaceutical composition. The new pharmaceutical composition possesses the biological and therapeutic activity of the parent compound and the barrier penetrating characteristics of the .beta.-lactam compound, which results in improved pharmacodynamics, including bioavailability, and an improved chemotherapeutic index, such that lower amounts of the parent may be used to avoid the toxic effects of the parent compound. Some of the new pharmaceutical compounds provide for the first time parent compounds in an orally administerable form.

REFERENCES:
patent: 4508723 (1985-04-01), Schaffner et al.

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