Immunosuppressive 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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514330, 514428, 546226, 546245, 548533, C07D21132, C07D21104, C07D26708

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active

051927730

ABSTRACT:
This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.

REFERENCES:
D. R. Williams et al., Synthesis of the .alpha.,.beta.-Diketo Amide Segment of the Novel Immuno Suppressive FK506, J. Org. Chem., vol. 53, No. 19, 1988.
Egbertson et al., J. Org. Chem. 54:11-12 (1989).
Coleman et al., Heterocycles 28:157-61 (1989).
Finberg et al., Science, 249:287-291 (Jul. 20, 1990).
Kaczmar et al., Makromol. Chem. 177:1981-9 (1976).
Blaschke et al., Chemical Abstracts, 85:78405k (Sep. 20, 1976).
Effenberger et al., Chemical Abstracts 110:154847h.
J. Chem. Soc. Chem. Commun. 15:1016-17 (1984).
J. Chem. Soc. Perkin Trans. I 4:769-772 (1985).
Bull. Soc. Cim. Fr. 2:185-91 (1989).

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