Tetrazole-containing rapamycin analogs with shortened half-lives

Details Tetrazole-containing rapamycin analogs with shortened half-lives Tetrazole-containing rapamycin analogs with shortened half-lives

1998-09-24

2000-01-18

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

540456, C07D49116, C07D49818, A61K 31445

Patent

active

060158158

ABSTRACT:
A compound having the formula ##STR1## or a pharmaceutically acceptible salt or prodrug thereof, is an immunomodulatory agent and is usefull in the treatment of restenosis and immune and autoimmune diseases. Also disclosed are cancer-, fungal growth-, restenosis-, post-transplant tissue rejection- and immune- and autoimmune disease-inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosois, post-transplant tissue rejection, and immune and autoimmune disease in a mammal.

REFERENCES:
patent: 3929992 (1975-12-01), Sehgal et al.
patent: 3993749 (1976-11-01), Sehgal et al.
patent: 4316885 (1982-02-01), Rakhit
patent: 4401653 (1983-08-01), Eng
patent: 4650803 (1987-03-01), Stella et al.
patent: 4885171 (1989-12-01), Surendra et al.
patent: 5023262 (1991-06-01), Caufield et al.
patent: 5120725 (1992-06-01), Kao et al.
patent: 5120727 (1992-06-01), Kao et al.
patent: 5120842 (1992-06-01), Failli et al.
patent: 5177203 (1993-01-01), Failli et al.
patent: 5457111 (1995-10-01), Luly et al.
patent: 5527907 (1996-06-01), Or et al.
Prescott, ed., Methods in Cell Biology, vol. XIV, Academic Press, New York, NY (1976), p. 33 et seq.
C. Vezina et al., "Rapamycin (AY-22,989), A New Antifungal Antibiotic I", Journal of Antibiotics, vol. 28, (1975), pp. 721-726.
S.N. Sehgal et al., "Rapamycin (AY-22,989), A New Antifungal Antibiotic II", Journal of Antibiotics, vol. 28, (1975), pp. 727-732.
H.A. Baker et al., "Rapamycin (AY-22,989), a New Antifungal Antibiotic III", Journal of Antibiotics, vol. 31, (1978), pp. 539-545.
J.J. Siekierka et al., "A Cytosolic Binding Protein for the Immunosuppressant FK506 has Peptidyl-prolyl Isomerase Activity but is Distinct from Cyclophilin", Nature, vol. 341, (1989), pp. 755-757.
M.W. Harding et al., "A Receptor for the Immunosuppressant FK506 is a cis-trans Peptidyl-prolyl Isomerase", Nature, vol. 341 (1989), 758-760.
N.L. Pavia et al., "Incorporation into Rapamycin", Journal of Natural Products--Lloydia, vol. 54, No. 1, (1991), pp. 167-177.
E.J. Brown et al., "A Mammalian Protein Targeted by G1-arresting Rapamycin-Receptor Complex", Nature, vol. 369, (1994), pp. 756-758.
S.J. Danishefsky et al., "Total Synthesis of Rapamycin vis a Novel Titanium-Mediated Aldol Macrocyclization Reaction", Journal of the American Chemical Society, vol. 115 (1993), pp. 9345-9346.
S.L. Schreiber et al., "Total Synthesis of (-)-Rapamycin Using an Evans-Tishchenko Fragment Coupling", Journal of the American Chemical Society, vol. 115, (1993), pp. 7906-7907.
K.C. Nicolau et al., "Total Synthesis of Rapamycin", Journal of the American Chemical Society, vol. 115, (1993), pp. 4419-4420.
H. Fretz et al., "Rapamycin and FK506 Binding Proteins (Immunophilins)", Journal of the American Chemical Society, vol. 113 (1991), pp. 1409-1411.
F.J. Dumont et al., "The Immunosuppressive Macrolides FK-506 and Rapamycin Act as Reciprocal Antagonists in Murine T Cells", Journal of Immunology, vol. 144, (1990), pp. 1418-1424.
M. Shichiri et al., "Endothelin-1 is an Autocrine/Paracrine Growth Factor for Human Cancer Cell Lines", Journal of Clinical Investigation, vol. 87, (1991), pp. 1867-1871.
B.E. Bierer et al., "The Effect of the Immunosuppressant FK-506 on Alternate Pathways of T Cell Activation", European Journal of Immunology, vol. 21, (1991), pp. 439-445.
S.N. Sehgal et al., "Demethoxyrapamycin (AY-24,668), A New Antofungal Antibiotic", Journal of Antibiotics, vol. 36, No. 4, (1983), pp. 351-354.
D.M. Sabatini et al., "RAFT1: A Mammalian Protein that Binds to FKBP12 in a Rapamycin-Dependent Fashion and is Homologous to Yeast TORs", Cell, vol. 78, (1994), pp.35-43.
R. Martel et al., "Inhibition of the Immune Response by Rapamycin, a New Antifungal Antibiotic", Canadian Journal of Physiology and Pharmacology, vol. 55, (1977), pp. 48-51.
S. Yamagishi et al., "Endothelin 1 Mediates Endothelial Cell-Dependent Proliferation of Vascular Pericytes", Biochemical and Biophysical Research Communications, vol. 191, (1993), pp. 840-846.
T. Kino et al., "Effect of FK-506 on Human Mixed Lymphocyte Reaction in Vitro", Transplantation Proceedings, vol. XIX, No. 5 sup. 6, (1987), pp. 36-39.
T.E. Bunchman et al., "Smooth Muscle Cell Proliferation by Conditioned Media from Cyclosporine-Treated Endothelial Cells: A Role of Endothelin", Transplantation Proceedings, vol. 23, No. 1, (1991), pp. 967-968.
R.E. Morris, "Rapamycins: Antofungal Antitumor, Antiproliferative, and Immunosuppressive Macrolides", Transplantation Reviews, vol. 6, No. 1, (1992), pp. 39-87.
R. Morris et al., "Identification of a New Pharmacologic Action for an Old Compound", Medical Science Research, vol. 17, (1989), pp. 877-879.
M.J. Strauch, FASEB, 3(3): 3411 (1989).

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