Heterocyclic esters and amides

Details Heterocyclic esters and amides Heterocyclic esters and amides

1996-09-25

1998-09-01

Ivy, C. Warren

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

548201, 5462697, 514342, A61K 31425, C07D27704

Patent

active

058011870

ABSTRACT:
This invention relates to neurotrophic low molecular weight, small molecule heterocyclic esters and amides having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.

REFERENCES:
patent: 4374829 (1983-02-01), Harris et al.
patent: 4808573 (1989-02-01), Gold et al.
patent: 4818749 (1989-04-01), Gold et al.
patent: 5147877 (1992-09-01), Goulet
patent: 5192773 (1993-03-01), Armistead et al.
patent: 5252579 (1993-10-01), Skotnicki et al.
patent: 5294603 (1994-03-01), Rinehart
patent: 5319098 (1994-06-01), Burbaum et al.
patent: 5330993 (1994-07-01), Armistead et al.
patent: 5359138 (1994-10-01), Takeuchi et al.
patent: 5385918 (1995-01-01), Connell et al.
patent: 5424454 (1995-06-01), Burbaum et al.
patent: 5447915 (1995-09-01), Schreiber et al.
patent: 5516797 (1996-05-01), Armistead et al.
patent: 5543423 (1996-08-01), Zelle et al.
Gold, B.G. et al.: The immunosuppressant FK506 Increases Functional Recovery and Nerve Regeneration Following Peripheral Nerve Injury. Restorative Neurology and Neuroscience vol. 6, pp. 287-296, 1994.
Dumont, Francis J. et al., "The Immunosuppressive and Toxic Effects of FK-506 are Mechanistically Related: Pharmacology of a Novel Antagonist of FK-506 and Rapamycin," J. Exp. Med., 1992, 176, 751-760.
Schreiber, Stuart L., "Chemistry and Biology of the Immunophilins and Their Immunosuppressive Ligands," Science, 1991, 251, 282-287.
Hauske, james R. et al., "Design and Synthesis of Novel FKBP Inhibitors," J. Med. Chem., 1992, 35, pp. 4284-4296.
Teague, Simon J. et al. "The Affinity of Excised Binding Dommain of FK-506 for the Immunophilin FKBP12," Bioorganic & Medicinal Chemistry Letters, 1993, vol. 3, No. 10, pp. 1947-1950.
Snyder, Solomon H. and Sabatini David M., "Immunophilins and the Nervous System," Nature Medicine, 1995, vol. 1, No. 1, pp. 32-37.
Tanaka, H. et al., "Structure of FK506, a novel immunosuppressant isolated from Streptomyces," J. Am. Chem. Soc., 1987, 109(16), 5031-3.
Holt, Dennis A. et al., "Structure-activity of synthetic FKBP ligands as peptidyl-prolyl isomerase inhibitors," Bioorg. Med. Chem. Lett., 1994, 4(2), 315-20.
Steiner, Joseph P. et al., "High brain densities of the immunophilin FKBP colocalized with calcineurin," Nature Lett., 1992, 358, 584-7.
Furber, M. et al., "Studies relating to the immunosuppressive activity of FK506," Tetrahedron Lett., 1993, 34(8), 1351-4.
Armistead, D.M. et al., "Design, synthesis and structure of non-macrocyclic inhibitors of FKBP12, the major binding protin for the immunosuppressant FK506," Acta Crystallogr. 1995, D51(4), 522-8.
Chakraborty, TK et al., "Design and Synthesis of a rapamycin-based high affinity binding FKBP12 ligand," Chem. Biol., 1995, 2(3), 157-61.
Steiner, J.P. et al., "Nonimmunosuppressive Ligands for Neuroimmunophilins Promote Nerve Extension In Vitro and In Vivo," Society for Neuroscience Abstracts, 1996, 22, 297.13.
Lyons, W. Ernest et al., "Neronal Regeneration Enhances the Expression of the Immunophilin FKBP-12," The Journal of Neuroscience, 1995, 15, 2985-94.

Affiliated with

Also associated with

Rating

Heterocyclic esters and amides does not yet have a rating. At this time, there are no reviews or comments for this patent.

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

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-270625