Multi-Armed Forms of Activated Polyoxazoline and Methods of Synthesis Thereof
AssigneeSerina Therapeutics, Inc.
InventorsJ. Milton Harris, Michael David Bentley, Kunsang Yoon, Zhihao Fang
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Abstract
The present disclosure provides novel POZ-2 derivatives, methods for synthesizing POZ-2 derivatives and intermediates useful in such methods. In one embodiment, the POZ-2 derivative comprises two linear POZ chains of the present disclosure linked directly or indirectly to a branching moiety that contains a functional group for linking the POZ-2 derivative to the target molecule. Target molecule-POZ-2 conjugates are also described. In certain embodiment, the POZ-2 derivatives have low polydispersity values and a decreased amount of impurities produced by unwanted side reactions, such as, but not limited to, chain transfer.
Claims37
An activated polyoxazoline-2 (POZ-2) derivative of the general structure
- Wherein
- POZa is a polyoxazoline of formula —[N(COR2)CH2CH2]n—;
- POZb is a polyoxazoline of formula —[N(COR2)CH2CH2]x—;
- L(I), L(II) and L(III) are linking groups;
- Br is a branching moiety that is linked with or without a linking group to POZa, POZb and is selected from the group consisting of a nitrogen atom, a substituted or unsubstituted aryl group or a carbon atom, provided that when Br is a carbon atom, at least one of c or d is 1 and the corresponding linking group contains a substituted or unsubstituted aryl group;
- X is a functional group which is capable of forming a linkage with a target molecule or being converted to a group that is capable of forming a linkage with a target molecule;
- A is a non-reactive group;
- R1 is independently selected for each of POZa and POZb from hydrogen, alkyl, substituted alkyl, aralkyl, or substituted aralkyl group;
- R2 is independently selected for each repeating unit of POZ from an unsubstituted or substituted alkyl, alkenyl, alkyl, aralkyl or aryl group;
- c, d and e are independently selected from 1 or zero;
- f is zero when Br is a nitrogen atom or substituted or unsubstituted aryl group and is 1 when Br is a carbon atom;
- and
- n and x are independently selected for each of POZa and POZb from 3 to 1000.
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17-85. (canceled)
A POZ-2 derivative having the structure
- wherein
- POZa is a polyoxazoline of formula —[N(COR2)CH2CH2]n—;
- POZb is a polyoxazoline of formula —[N(COR2)CH2CH2]n—;
- VI and VII are each a linking group;
- R1 is independently selected for each POZ chain from hydrogen, an alkyl, substituted alkyl, aralkyl, or substituted aralkyl group;
- R2 is independently selected for each repeating unit of POZa and POZb from an unsubstituted or substituted alkyl, alkenyl, alkyl, aralkyl or aryl group;
- x is 1 to 20;
- and
- n and m are independently selected from 3 to 1000.
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97-105. (canceled)
107-113. (canceled)
115-118. (canceled)
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Dependencies are inferred from the claim text.