Macrocyclic immunomodulators with novel cyclohexyl ring replacem

Details Macrocyclic immunomodulators with novel cyclohexyl ring replacem Macrocyclic immunomodulators with novel cyclohexyl ring replacem

1995-04-19

1997-03-18

Bond, Robert T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

540456, A61K 31395

Patent

active

056123507

ABSTRACT:
Novel macrolide compounds of the formula ##STR1## and pharmaceutically acceptable salts, esters, amides and prodrugs thereof, wherein X is a substituent selected from among radicals having the subformulae ##STR2## and other heterocyclic radicals, as well as pharmaceutical compositions and methods of immunomodulatory treatment utilizing the same.

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patent: 5208241 (1992-11-01), Ok et al.
patent: 5262533 (1993-11-01), Sinclair et al.
Schreiber, S. L., et al., "The mechanism of action of Cyclosporin A and FK 506", Immunology Today, 13(4):136-142 (1992).
Hauske, J. R., et al., "Design and Synthesis of Novel FKBP inhibitors", J. Med. Chem., 35(23):4284-4296 (1992).
Schreiber, S. L., "Chemistry and Biology of the Immunophilins and Their Immunosuppressive Ligands", Science, 251:283-287 (Jan. 1991).
Batchelor, M. J., et al., "Total Synthesis of Close analogues of the Immunosupressant FK 506", Tetrahedron, 50(3):809-826 (1994).
Zimmer, R., et al., "Synthesis Modifications of Asomycin-I. A Chemoselective Removal of the Cyclohexyl Residue of Asomycin", Tetrahedron, 50(48):13655-13670 (1994).

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