Thiepane compounds

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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549 9, A61K 3138, C07D33700

Patent

active

058114505

ABSTRACT:
Tri- and tetra substituted thiepane compositions having use as immunogens, therapeutics, diagnostics and for other industrial purposes are disclosed. The compositions inhibit proteolytic activity of viral enzymes and are useful for the inhibition of such enzymes as well as in assays for the detection of such enzymes. Embodiments in which antigenic polypeptides are bonded to the compositions are useful in raising antibodies against the thiepane haptens or the polypeptide. Labeled thiepanes of this invention are useful as diagnostic reagents.

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Billich et al., "Review: Antiviral Assays, No. 1--Assay systems for HIV-1 proteinase and their use for evaluation of inhibitors," Antiviral Chem & Chemo 2(2):65-73 (1991).
Matayoshi et al., "Novel Fluorogenic Substrates for Assaying Retroviral Proteases by Resonance Energy Transfer," Science 247:954-958 (Feb. 23, 1990).
Wang et al., "Design and Synthesis of New Fluorogenic HIV Protease Substrates Based on Resonance Energy Transfer," TET LETT 31(45):6493-6496 (1990).
Wong et al., "A Pharmacokinetic Evaluation of HIV Protease Inhibitors, Cyclic Ureas, in Rats and Dogs," Biochem Pharm 15:535-544 (1994).

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