Cytostatic conjugates with integrin ligands

Details Cytostatic conjugates with integrin ligands Cytostatic conjugates with integrin ligands

2007-12-04

2007-12-04

Russel, Jeffrey Edwin (Department: 1654)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

C514S283000, C514S401000, C514S539000, C514S562000, C530S330000, C530S331000, C530S345000

Reexamination Certificate

active

10096120

ABSTRACT:
The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to αvβ3integrin antagonists via preferred linking units which can be selectively cleaved by elastase, i.e. by an enzyme which can especially be found in tumor tissue. The preferred linking units provide sufficient stability of the conjugate of cytostatic and αvβ3integrin antagonist in biological fluids and, at the same time, the desired intracellular action within tumor cells as a result of its specific enzymatic or hydrolytic cleavability with release of the cytostatic.

REFERENCES:
patent: 4757072 (1988-07-01), Kabbe et al.
patent: 4975278 (1990-12-01), Senter et al.
patent: 4980343 (1990-12-01), Stella et al.
patent: 5464796 (1995-11-01), Petersen et al.
patent: 5561119 (1996-10-01), Jacquesy et al.
patent: 5955100 (1999-09-01), Bosslet et al.
patent: 6271342 (2001-08-01), Lerchen et al.
patent: 6291503 (2001-09-01), Schoop et al.
patent: 4229903 (1994-03-01), None
patent: 0511917 (1992-11-01), None
patent: 0516861 (1992-12-01), None
patent: 0520240 (1992-12-01), None
patent: 0595133 (1994-05-01), None
patent: 8807378 (1988-10-01), None
patent: 9602546 (1996-02-01), None
patent: 9631532 (1996-10-01), None
patent: 9810795 (1998-03-01), None
patent: 9851703 (1998-11-01), None
patent: 9951638 (1999-10-01), None
patent: 0041469 (2000-07-01), None
patent: 0069472 (2000-11-01), None
patent: 0117563 (2001-03-01), None
De Marre, A., Soyez, H., Schacht, E., Shoaibi, M., Seymour, L., Rihova, B., “Synthesis and Evaluation of Macromolecular Prodrugs of Mitomycin C”, J. of Controlled Release, 36:87-97 (1995).
Soyez, H., Seymour, L., Schacht, E., “Macromolecular Derivatives of N,N-di-(2-chloroethyl)-4-phenylene Diamine Mustard. 2. In Vitro Cytotoxicity and In Vivo Anticancer Efficacy”, J. of Controlled Release, 57:187-196 (1999).
Kasafirek, E., Fric, P., Slaby, J., “Role of Amino Acid Residues in Chromogenic Substrates Cleaved by Pancreatic Elastase”, Collection Czechoslovak Chem. Commun., 52:1625-1633 (1987).
Fields, G., “Integrins: Cell Adhesion Molecules in Cancer”, Exp. Opin. Ther. Patents 8: 633-644, (1998).
Ashwell, G., Harford, J., “Carbohydrate-Specific Receptors of the Liver”, Ann. Rev. Biochem., 51: 531-554 (1982).
Aminoff, D., Bruegge, W., Bell, W., Sarpolis, K., Williams, R., “Role of Sialic Acid in Survival of Erythrocytes in the Circulation: Interaction of Neuraminidase-Treated and Untreated Erythrocytes With Spleen and Liver at the Cellular Level”, Proc. Natl. Acad. Sci. USA, 74: 1521-1524 (1977).
Haltiwanger, R., Lehrman, M., Eckhardt, A., Hill, R., “The Distribution and Localization of the Fucose-Binding Lectin in Rat Tissues and the Identification of a High Affinity Form of the Mannose/N-Acetylglucosamine-Binding Lectin in Rat Liver”, J. Biol. Chem., 261: 7433-7439 (1986).
Jansen, R., Molema, G., Ching, T., Oosting, R., Harms, G., Moolenaar, F., Hardonk, M., Meijer, D., “Hepatic Endocytosis of Various Types of Mannose-Terminated Alburnins”, J. Biol. Chem., 266: 3343-3348 (1991).
Wall, J., Wani, M., Cook, C., Palmer, K., McPhail, A., Sim, G., “Plant Antitumor Agents. I. The Isolation and Structure of Camptothecin, A Novel Alkaloidal Leukemia and Tumor Inhibitor fromCamptotheca acuminata”, J. Am. Chem. Soc., 88: 3888-3890 (1966).
Brooks, P., Montgomery, A., Rosenfeld, M., Reisfeld, R., Hu, T., Klier, G., Cheresh, D., “Integrin αvβ3 Antagonists Promote Tumor Regression by Inducing Apoptosis of Angiogenic Blood Vessels”, Cell, 79: 1157-1164 (1994).
Brooks, P., Stromblad, S., Lemke, R., Visscher, D., Sarkar, F., Cheresh, D., “Antiintegrin αvβ3 Blocks Human Breast Cancer Growth and Angiogenesis in Human Skin”, J. Clin. Invest., 96: 1815-1822 (1995).
Fitzpatrick, J., Garnett, M., “Design, Synthesis andIn VitroTesting of Methotrexate Carrier Conjugates Linked Via Oligopeptide Spacers”, Anti-Cancer Drug Design, 10: 1-9 (1995).
March, J., Advanced Organic Chemistry, 3rd. Ed., John Wiley & Sons, pp. 370-371, 802-803, no date.
Jiang, J., Li, W., Przeslawski, R., Joullie, M., “Comparative Study of Selected Reagents for Carboxyl Activation”, Tetrahedr. Lett., 34: 6705-6708 (1993).
Rodionow, W., Postovskaja, E., “The Mechanism of Formation of Beta-Aryl-Beta-Amino Fatty Acids by the Condensation of Aromatic Aldehydes With Malonic Acid and its Derivatives”, J. Am. Chem. Soc., 51: 841-847 (1929).
Ishihara, K., Hanaki, N., Funahashi, M., Miyata, M., Yamamoto, H., “Tris (pentafluorophenyl) Boron as an Efficient, Air Stable, and Water Tolerant Lewis Acid Catalyst”, Bull. Chem. Soc. Jpn., 68: 1721-1730 (1995).
Arlt, D., Bomer, B., Grosser, R., Lange, W., “New Chiral Polyamide Stationary Phases for Chromatographic Enantiomer Separation”, Angew. Chem. Ed. Engl., 30: 1662-1664 (1991).
Kunz, H., Muller, B., Schanzenbach, D., “Diastereoselective Diels—Alder Reaction on Carbohydrate Matrices”, Angew. Chem. Int. Ed. Engl., 26: 267-269 (1987).
Gabius, H.J., “Endogene Lektine in Tumoren und Ihre Mogliche Bedeutung Fur Diagnose und Therapie Von Krebserkrankungen”,Onkologie, 12: 175-181 (1989).

Affiliated with

Also associated with

Rating

Cytostatic conjugates with integrin ligands does not yet have a rating. At this time, there are no reviews or comments for this patent.

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

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-3832094