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Title:
BIODEGRADABLE POLYETHYLENE GLYCOL DERIVATIVE HAVING CYCLIC BENZYLIDENE ACETAL LINKER
Document Type and Number:
WIPO Patent Application WO/2016/159071
Kind Code:
A1
Abstract:
Provided is a biodegradable polyethylene glycol derivative in which polyethylene glycol chains are linked by acetal linkers having a precisely controllable hydrolysis rate in environments of different pH within the body, and in which it is possible to precisely control the rate of splitting into low-molecular-weight polyethylene glycol chains within the body. The present invention is shown by formula (1) or formula (2). (In formula (1) and formula (2), R1-R6 are hydrogen atoms or the like; s = 1 or 2, t = 0 or 1, and s + t = 1 or 2; P1 and P2 are polyethylene glycol having three or more ethylene glycol units; w, u, and v are integers of 1 or the like; X1 is a functional group capable of chemical reaction; and Z1, Z2, and Z3 are divalent spacers.)

Inventors:
TSUBUSAKI TAKUMA (JP)
YAMAMOTO YUJI (JP)
Application Number:
PCT/JP2016/060377
Publication Date:
October 06, 2016
Filing Date:
March 30, 2016
Export Citation:
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Assignee:
NOF CORP (JP)
International Classes:
C08G65/333; A61K47/34
Domestic Patent References:
WO2014157150A12014-10-02
WO2015152182A12015-10-08
Other References:
SEDLAK, MILOS ET AL.: "Synthesis of pH-sensitive amphotericin B-poly(ethylene glycol) conjugates and study of their controlled release in vitro", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 15, no. 12, 5 May 2007 (2007-05-05), pages 4069 - 4076, XP022062539
CHEN, WEI ET AL.: "pH-Responsive Biodegradable Micelles Based on Acid-Labile Polycarbonate Hydrophobe: Synthesis and Triggered Drug Release", BIOMACROMOLECULES, vol. 10, no. 7, 13 July 2009 (2009-07-13), pages 1727 - 1735, XP055062990
GILLIES, ELIZABETH R. ET AL.: "pH-responsive copolymer assemblies for controlled release of doxorubicin", BIOCONJUGATE CHEMISTRY, vol. 16, no. 2, 2005, pages 361 - 368, XP055118301
HUANG,X. ET AL.: "pH-labile sheddable block copolymers by RAFT polymerization: Synthesis and potential use as siRNA conjugates", EUROPEAN POLYMER JOURNAL, vol. 49, no. 10, 2013, pages 2895 - 2905, XP028711629
See also references of EP 3279236A4
Attorney, Agent or Firm:
Shin-Ei Patent Firm, P. C. (JP)
Patent business corporation Shin-Ei Patent Firm (JP)
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