Anthracycline prodrugs, method for preparation as well as their

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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536 64, 536 185, 536 186, A61K 3170, C07H 1524

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057101353

ABSTRACT:
Anthracycline derivatives are disclosed which are coupled to an enzymatically cleavable N-phenyl-O-glycosyl carbamate spacer group, which derivatives are represented by the formula ##STR1## as well as the acid addition salts thereof. Further the synthesis of these derivatives and their use, alone or in combination with enzymes or antibody enzyme conjugates are disclosed.

REFERENCES:
Kita et al, Facile and Efficient Syntheses of Carboxylic Anhydrides and Amides Using (Trimethylsilyl) Ethoxyacetylene, J.Org.Chem., vol. 51 No. 22, pp. 4150-4158, Dec. 19, 1985.
Andrianomenjanahary et al, Syntheses of Novel Targeted Pro-Prodrugs of Anthracyclines Potentially Activated by a Monoclonal Antibody Galactosidase Conjugate (Part 1), Biorganic & Medical Chemistry vol. 2, No. 9, pp. 1093-1096, 1992.
Bosslet et al, Tumor-Selective Prodrug Activation by Fusion Protein-Mediated Catalysis, Cancer Reasearch, vol. 54, pp. 2151-2159, Apr. 15, 1994.
Carl et al, Journal of Medical Chemistry, vol. 24, No. 5, May 1981.
Gesson et al, Prodrugs of Anthracycline for Chemotherapy via Enzyme-Monclonal Antibody Conjugates, Anti-Cancer Drug Design, vol. 9, pp. 409-423, 1994.
Jungheim et al, Design of ANtitumor Prodrugs: Substrates for Antibody Targeted Enzymes, Chem. Rev., vol. 94 pp. 1553-1556, Jan. 21, 1994.
Senter et al, Generation of Cytotoxic Agents by Targeted Enzymes, Bioconjugate Chem. vol. 4, pp. 3-9 1993.
Haisma et al, A Monoclonal Antibody-.beta.-Glucuronidase Conjugate as Activator of the Prodrug Epirubicin-Glucuronide for Specific Treatment of Cancer, Br. J. Cancer, vol. 66, pp. 474-478, 1992.
Jungheim et al, Synthesis of Acylhyhydrazido-Substituted Cephemus. Design of Cephalosporin-Vinca Alkaloid Prodrugs: Substrates for an Antibody-Targeted Enzyme, J. Org. Chem. vol. 57, pp. 2334-2340, 1992.
Senter et al, Enhancement of the in Vitro and in Vitro Antitumor Activities of Phosphorylated Mitomycin C and Etoposide Derivativesby Monoclonal Antibod-Alkaline Phosphatase Conjugates, vol. 49, pp. 5789-5792, Nov. 1, 1989.
Senter et al, Anti-Tumor Effects of Antibody-Alkaline Phosphatase Conjugates in Combination with Etopside Phosphate, Proc. Natl. Acad. Sci., vol. 85, pp. 4842-4846, Jul. 1988.
Vingerhoeds et al, A New Application for Liposomes in Cancer Therapy, FEBS, vol. 336, No. 3, pp. 485-490, Dec. 1993.
Miyashita et al, Prodrug Activation via Catalytic Antibodies, Proc. Natl. Sci. vol. 90, pp. 5337-5340, 1993.
Wallace et al, In Vitro and in Vivo Activities of Monoclonal Antibody-Alkaline Phosphate Conjugates in Combination with Phenol Mustard Phosphatase, Bioconjugate Chem., vol. 2, pp. 349-352, Jun. 24, 1991.

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