Immunosuppressive compounds

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

514330, 514423, 546226, 548533, A61K 31445, A61K 3140, C07D21160, C07D20716

Patent

active

056229704

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:
patent: 5192773 (1993-03-01), Armistead et al.
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. 185-191 (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).
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).
M.W. Harding et al., "A Receptor for the Immunosuppresant 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).
K. Soai et al., "Diastereoselective Asymmetric Allylation of Chiral .alpha.-Keto-amides with Allyltrimethylsilane, Preparation of Protected Homoallyllic Acohols," J. Chem. Soc., Chem. Commun., 15, pp. 1016-1017 (1984).
K. Soai et al., "Diastereoselective Reduction of Chiral Alpha-Ketoamides Derived from (S)-Proline Esters with Sodium Borohydride. Prepparation of Optically Active Alha-Hydroxy Acids," J. Chem. Soc., Perkins Trans., 4, pp. 769-772 (1985).
D. R. Williams et al., "Synthethis of the .alpha.,.beta.-Diketo Amide Segment of the Novel Immuno Suppressive FK506," J. Org. Chem., 53, pp. 4643-4644 (1988).

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Immunosuppressive compounds does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Immunosuppressive compounds, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Immunosuppressive compounds will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-341961

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.