Releasable polymeric conjugates based on aliphatic biodegradable linkers
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Abstract
Activated polymeric bicine derivatives such as Formula (I), as well as conjugates made therewith are disclosed. Methods of making and using the bicine derivatives are also disclosed.
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34 Claims
- 1. A compound comprising the Formula (I):
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31. A method of preparing a polymer conjugate, comprising reacting a compound of the formula:
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32. A method of preparing a bicine-based polymer transport system, comprising:
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a) reacting a blocked bifunctional linker with an anhydride to form an extended blocked bifunctional spacer of the formula;
b) attaching the blocked bifunctional spacer to each hydroxyl of an acid protected bicine molecule;
c) deblocking the resultant intermediate and reacting it with an activated polymer under basic coupling conditions, and d) deprotecting the bicine acid and thereafter activating the acid with a suitable activating group under coupling conditions.
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Specification