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Title:
POLYMER CONJUGATE OF BIOACTIVE SUBSTANCE HAVING HYDROXY GROUP
Document Type and Number:
WIPO Patent Application WO/2010/131675
Kind Code:
A1
Abstract:
Disclosed is a polymer conjugate of a bioactive substance, which enables drug release independent of a biological enzyme and can be expected to have a high therapeutic effect. Specifically disclosed is a polymer conjugate of a bioactive substance, in which a substituent represented by general formula (I) or (II) is linked, through an amide bond, to at least one of the side-chain carboxy groups of a block copolymer comprising a polyethylene glycol structural moiety and a polymer having two or more carboxy groups. In formulae (I) and (II), R8 and R9 each independently represent a hydrogen atom or a C1-C6 alkyl group which may have a substituent; R10 represents a hydrogen atom, a C1-C40 alkyl group which may have a substituent, a C1-C40 aralkyl group which may have a substituent, an aromatic group which may have a substituent, an amino acid residue having a protected carboxy group, or a sugar residue which may have a substituent; CX-CY represents CH-CH or C=C (double bond); A represents a residue obtained by removing, from a bioactive substance having one or more hydroxy groups, one of the one or more hydroxy groups.

Inventors:
KITAGAWA MASAYUKI (JP)
SENO CHIEKO (JP)
EBARA KEIKO (JP)
TAKASHIO KAZUTOSHI (JP)
Application Number:
PCT/JP2010/058034
Publication Date:
November 18, 2010
Filing Date:
May 12, 2010
Export Citation:
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Assignee:
NIPPON KAYAKU KK (JP)
KITAGAWA MASAYUKI (JP)
SENO CHIEKO (JP)
EBARA KEIKO (JP)
TAKASHIO KAZUTOSHI (JP)
International Classes:
C08G85/00; A61K31/167; A61K31/19; A61K31/195; A61K31/337; A61K31/365; A61K31/4745; A61K31/52; A61K31/573; A61K31/704; A61K31/7052; A61K31/7068; A61K47/34; A61K47/42; A61K47/48; A61P9/10; A61P17/14; A61P35/00; C08G69/48
Domestic Patent References:
WO2008056654A12008-05-15
WO2004039869A12004-05-13
WO2007111211A12007-10-04
WO2007135910A12007-11-29
WO2008010463A12008-01-24
WO2006120914A12006-11-16
Foreign References:
JPS63502037A1988-08-11
JPH08507558A1996-08-13
JP2002069184A2002-03-08
JP2007511586A2007-05-10
JP2694923B21997-12-24
Other References:
See also references of EP 2431403A4
J. MED. CHEM., vol. 38, 1995, pages 1666 - 1672
Attorney, Agent or Firm:
Kawaguti & Partners (JP)
In the patent business corporation Kawaguchi 國 case, it is a patent firm. (JP)
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Claims: