申请人:——
公开号:US20020009426A1
公开(公告)日:2002-01-24
The present invention includes polymeric transport systems corresponding to the formula:
1
wherein:
R
31
is a linear or branched polymer residue; Y
10
and Y
11
are independently O, S, or NR
40
; X
2
is O, S or NR
41
; R
32
-
35
, R
37
-
41
, R
50
and R
51
are independently selected from among hydrogen, C
1-6
alkyls, C
3-12
branched alkyls, C
3-8
cycloalkyls, C
1-6
substituted alkyls, C
3-8
substituted cycloalkyls, aryls, substituted aryls, aralkyls, C
1-6
heteroalkyls and substituted C
1-6
heteroalkyls; a, b and e are each independently selected positive integers; L is an amino acid residue or a bifunctional linker; X
3
is
2
wherein Y
12
and Y
13
are independently O, S, or NR
41
; Z is a bond, a moiety that is actively transported into a target cell, a hydrophobic moiety or combinations thereof;, D
1
and D
2
are OH, a residue of a hydroxyl, a residue of an amine-containing moiety or a leaving group; and y
1
and y
2
are independently selected positive integers.
本发明涉及与以下公式对应的聚合物转运系统:1其中:R31是线性或支链聚合物残基;Y10和Y11独立地为O、S或NR40;X2为O、S或NR41;R32-35、R37-41、R50和R51独立地选自氢、C1-6烷基、C3-12支链烷基、C3-8环烷基、C1-6取代烷基、C3-8取代环烷基、芳基、取代芳基、芳基烷基、C1-6杂原子烷基和取代C1-6杂原子烷基;a、b和e各自独立地选自正整数;L是氨基酸残基或双功能链接剂;X3为2,其中Y12和Y13独立地为O、S或NR41;Z是键合、主动转运到目标细胞的基团、亲水性基团或其组合;D1和D2为OH、含氨基基团的残基或离去基团;y1和y2独立地选自正整数。