06303569 is referenced by 61 patents and cites 14 patents.

The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric compounds comprise the formula:

wherein:

B is H, OH, OSiR

13

, a residue of an amine-containing target moiety or a residue of a hydroxyl-containing moiety;

L

1

and L

2

are bifunctional linking moieties;

Y

2

is O or S;

R

2

is selected from the group consisting of 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, substituted C

1-6

heteroalkyls, C

1-6

alkoxy, phenoxy, and C

1-6

heteroalkoxy;

R

9

, R

10

, R

13

are independently one of hydrogen, C

1-6

alkyls, C

3-12

branched alkyls, C

3-8

cycloalkyls, C

1-6

substituted alkyls, C

3

S substituted cycloalkyls, aryls, substituted aryls, aralkyls, C

1-6

heteroalkyls, substituted C

1-6

heteroalkyls, C

1-6

alkoxy, phenoxy, and C

1-6

heteroalkoxy;

Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group;

(m) is zero or one; and

R

11

is a polymer residue.

The first prodrug is generated when the polymeric portion of the double prodrug is cleaved and the parent molecule is generated rapidly thereafter in vivo, as a result of a trialkyl lock type lactonization-type reaction.

Title
Trialkyl-lock-facilitated polymeric prodrugs of amino-containing bioactive agents
Application Number
9/137430
Publication Number
6303569 (B1)
Application Date
August 21, 1998
Publication Date
October 16, 2001
Inventor
Annapurna Pendri
Matawan
NJ, US
Yun H Choe
Piscatway
NJ, US
Richard B Greenwald
Somerset
NJ, US
Agent
Roberts & Mercanti L
US
Assignee
Enzon
NJ, US
IPC
A61K 31/215
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