Polymer-bound paclitaxel derivatives

Details Polymer-bound paclitaxel derivatives Polymer-bound paclitaxel derivatives

1993-06-16

1994-11-08

Page, Thurman K.

Synthetic resins or natural rubbers -- part of the class 520 ser

Synthetic resins

Polymers from only ethylenic monomers or processes of...

5263074, 5263073, 424 7832, 424 7808, A61K 31765, C80F22238

Patent

active

053628314

ABSTRACT:
A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4## wherein R is a phenyl or t-butoxy group, R.sub.3 is H or an acetyl group, A and A.sub.1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from .beta. Ala, Gly, Phe-Gly, Phe-Phe-, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe,-.beta.Ala, Phe-Gly-.beta.Ala, Phe-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Val-Ala-.beta.Ala, Phe-Ala-.beta.Ala, Leu-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Phe-Leu-Gly-.beta.Ala, Phe-Phe-Leu .beta.Ala, Leu-Leu-Gly-.beta.Ala, Phe-Tyr-Ala-.beta.Ala, Phe-Gly-Phe-.beta., Phe-Phe-Gly .beta.Ala, Phe-Leu-Gly-Phe-.beta.Ala or Gly-Phe-Leu-Gly-Phe-.beta.Ala. The compounds are endowed with antitumor activity and show improved water solubility and decreased toxicity in comparison with paclitaxel or its known analogs. A method for their preparation and pharmaceutical compositions containing them are also described.

REFERENCES:
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Journal of Controlled Release, vol. 16, 1991, pp. 121-136, R. Duncan, et al., "Macromolecular Prodrugs for Use in Targeted Cancer Chemotherapy: Melphalan Covalently Coupled to HMPA Copolymers".
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Journal of Controlled Release, vol. 18, No. 2, Feb. 1992, pp. 123-132, V. Subr, et al., "Polymers Containing Enzymatically Degradable Bonds, XII. Effect of Spacer Structure on the Rate of Release of Daunomycin and Adriamycin from HMPA Copolymer Drug Carriers in Vitro and Antitumor Measured in Vivo".

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