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POLYOXAZOLINE POLYMERS AND METHODS FOR THEIR PREPARATION, CONJUGATES OF THESE POLYMERS AND MEDICAL USES THEREOF
专利权人:
发明人:
申请号:
EP12821204.0
公开号:
EP2800773A1
申请日:
2012.12.28
申请国别(地区):
EP
年份:
2014
代理人:
摘要:
The present invention relates to functionalized ploy(2-oxazoline) polymers, which are very suitable as a carrier and/or delivery vehicle (conjugate) of drugs, such as small therapeutic molecules and bio-pharmaceuticals. These polymers are characterized in that they comprise repeating units that are represented by the following formula &mdash[N(R1)&mdash(CHR2)m]- wherein R1 is R3&mdash(CHR4)n-CONH&mdashR5 R2 is selected from H and optionally substituted C1-5alkyl R3 is CH2CO, C(O)O, C(O)NH OR C(S)NH R4 is selected from H and optionally substituted C1-5alkyl R5 is H an C1-5alkyl aryl or a moiety comprising a functional group that can be used for conjugation m is 2 or 3 and n is 1-5 or n is 0 and R3 is CH2. The invention relates further to a conjugate of these polyoxazoline polymers with at least one active moiety, such as a therapeutic moiety, a targeting moiety and/or diagnostic moiety, and to the use of these conjugates in the therapeutic treatment or prophylactic treatment or diagnosis of a disease or disorder.
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