Immunosuppressive compounds

Details Immunosuppressive compounds Immunosuppressive compounds

1994-04-11

1996-05-14

O'Sullivan, Peter

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

514330, 514423, 514428, 514534, 514538, 514547, 514549, 514551, 514465, 514466, 549441, 560 39, 560 43, 560170, A61K 31445, A61K 3140, A61K 3122, A61K 3124

Patent

active

055167977

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:
G. Blaschke et. al., "Investigation of Chromatographic Resolutions of Racemates, VI. Polymeric Amino Acid Derivatives As Optically Active Adsorbents", Chem. Ber., 109(6), pp. 1967-1975 (1976).
A. Boulmedais et. al., "Stereochemistry of Electrochemical Reduction of Optically Active Alfa-Ketoamides. II. Electro-Reduction of Benzoylformamides Derived from S-(-)-Proline", Bull. Soc. Chim. Fr., 2, pp. 189-191 (1989).
R. S. Coleman et. al., "Degradation and Manipulations of the Immunosuppressant FK506: Preparation of Potential Synthetic Intermediates", Heterocycles, 28, pp. 157-161 (1989).
F. Effenberger et. al., "Amino Acids. 14. Diastereoselective Addition of Benzenesulfenyl Chloride to 1-Acryloylproline Esters", Chem. Ber., 122(3), pp. 545-551 (1989).
M. Egbertson and S. J. Danishefsky, "Synthetic Route to the Tricarbonyl Region of FK-506", J. Org. Chem. 54, pp. 11-12 (1989).
G. Feutren, "The Optimal Use of Cyclosporin A in Autoimmune Diseases", J. Autoimmun., 5, pp. 183-195 (1992).
R. W. Finberg et. al., "Prevention of HIV-1 Infection and Preservation of CD4 Function by the Binding of CPFs to gp120", Science, 249, pp. 287-291 (1990).
L. Fry, "Psoriasis: Immunopathology and Long-term Treatment with Cyclosporin", J. Autoimmun., 5, pp. 277-283 (1982).
M. W. Harding et. al., "A Receptor for the Immunosuppressant FK-506 is a Cis-Trans Peptidyl-Prolyl Isomerase", Nature, 341, pp. 758-760 (1989).
B. U. Kaczmar et. al., "Snake-Cage Polymers, 1. Synthesis of Various Snake-Cage Polyelectrolytes Consisting of Polyacrylamides and an Anion Exchanger", Makromol. Chem., 177(7), pp. 1981-1989 (1976).
C. Ponticelli, "Treatment of the Nephrotic Syndrome with Cyclosporin A", J. Autoimmun., 5, pp. 315-324 (1992).
K. Soai et. al., "Diastereoselective Asymmetric Allylation of Chiral .alpha.-Keto-amides with Allyltrimethylsilane. Preparation of Protected Homoallylic Alcohols", J. Chem. Commun., 4, pp. 769-772 (1984).
K. Soai et. al., "Diastereoselective Reduction of Chiral Alpha-Ketoamides Derived from (S)-Proline Esters with Sodium Borohydride. Preparation of Optically Active Alpha-Hydroxy Acids", J. Chem. Soc., Perkins Trans., 4, pp. 769-772 (1985).
R. S. A Tindall, "Immunointervention with Cyclosporin A in Autoimmune Neurological Disorders", J. Autoimmun., 5, pp. 301-313 (1992).
P. Tugwell, "Cyclosporin in the Treatment of Rheumatoid Arthritis", J. Autoimmun., 5, pp. 231-240 (1992).
D. R. Williams et. al., "Synthesis of the .alpha.,.beta.-Diketo Amide Segment of the Novel Immuno Suppressive FK506", J. Org. Chem., 53, pp. (1988).

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