TH13694A - Polymer-bound paclitacel derivatives - Google Patents

Abstract

Derivatives of polytacell bound to polymeric conjugate polymers containing critical parts of 90 to 99.9 mol% of the portion expressed by the formula (chemical formula) from 0.1 to 5. The mole% of the unit represented by the formula (chemical formula), where one of R1 and R2 is the formula's (chemical formula) residcopolymers and the other is the hydrogen atom from 0 to 9.9 mol%. Of the units represented by the formula (chemical formula) where R is the phenyl or ethiary-butoxi group, R3 is H or the acetyl group A and A1, may be the same or different instead of a single bond. chemical An amino acid resin or a selectable peptide spacer from B-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-Gly-BAla, Phe-Gly-Bala, Phe-Phe-BAla, Leu-Gly-BAla, Val-Ala-BAla, Phe-Ala-BAla, Leu-Phe-BAla, Leu- Gly-BAla, Phe-Leu-Gly-BAla, Phe-Phe-Leu BAla, Leu-Leu-Gly-BAla, Phe-Leu-Gly-BAla, Phe-Gly-Phe-B, Phe-Phe-Phe-Gly BAla, Phe-Ley-Gly-Phe-BAla, or Gly-Phe-Leu-Gly-Phe-BAla. This compound has anti-tumor action. And has improved water solubility and With reduced toxicity Compare with known paclitacel or paclitacel-like preparation method. And pharmaceutical ingredients containing these substances;

Claims (3)

1.Polymer conjugate Containing the prime fraction of 90 to 99.9 mol% of the unit represented by the formula (chemical formula) from 0.1 to 5 mol% of the unit represented by the formula (chemical formula), where one of R1 and R2 is us. The sitiocopolymer of the formula (chemical formula) and the other It is a hydrogen atom from 0 to 9.9 mol% of the unit represented by the formula (chemical formula) where R is the phenyl group. Or tertari-butoxi, R3 or H, or acetyl groups A and A1, which may be the same or different. Instead of a single chemical bond, amino resin or peptide spacer selected from B 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-Gly-BAla, Phe-Gly-Bala, Phe-Phe-BAla, Leu-Gly-BAla, Val-Ala-BAla, Phe-Ala-BAla, Leu-Phe-BAla , Leu-Gly-BAla, Phe-Leu-Gly-BAla, Phe-Phe-Leu BAla, Leu-Leu-Gly-BAla, Phe-Leu-Gly-BAla, Phe-Gly-Phe-B, Phe-Phe- Phe-Gly BAla, Phe-Ley-Gly-Phe-BAla, or Gly-Phe-Leu-Gly-Phe-BAla. 2. The conjugate polymer according to claim 1, where R represents the phenyl group, R3 is the acetyl group and A is the Phe-Leu-Gly resin or Phe-Leu resin. -Gly-B Ala 3.Polymer conjugate according to claim 1 or 2, which is the copolymer of 1-methacryloyl amino-2-hydroxypropane (methacryloyl glycyl-phenylalanilylusyl glycyl) 3 \ ' \ '- Amino-2-hydroxypropane and 2 \' \ '- (methacryloyl glycyl phenylalanil-liucyl glycyl-B a Lanil) Paclitacel