Back to results
US 6,667,371 B2Granted
Block copolymers based on poly(ortho esters) containing amine groups
AssigneeA.P. Pharma, Inc.
InventorsSteven Y. Ng, Jorge Heller
Life of this patent
Estimating the term…
Abstract
Block copolymers based on poly(ortho esters) containing amine groups. These block copolymers have both hydrophilic and hydrophobic blocks. They form micelles in aqueous solution, making them suitable for encapsulation or solubilization of hydrophobic or water-insoluble materials; and they also form bioerodible matrices for the sustained release of active agents.
Claims9
A block copolymer of formula X, formula Y, or formula Z:
- RA—[OCH2CH2]f—[POE]g—H (X),
- RA—[OCH2CH2]f—[POE]g—[OCH2CH2]h—ORB (Y),
- H—A—[POE]g—[OCH2CH2]h—[POE]j—H (Z),
- where:
- RA is C1-C4 alkyl;
- RB is C1-C4 alkyl;
- f and h are independently an integer from 2 to 1000;
- g and j are independently an integer from 2 to 200;
- POE is a poly(ortho ester) unit of formula IA or formula IIA:
- where
- R* is a C1-C4 alkyl;
- R is a bond, —(CH2)—, or —(CH2)b—O—(CH2)c—;
- where a is an integer of 1 to 10, and b and c are independently integers of 1 to 5;
- and
- each A is independently selected from R1, R2, R3, and R4, where
- R1 is:
- where:
- p is an integer of 1 to 20;
- R5 is hydrogen or C1-C4 alkyl;
- and
- where:
- s is an integer of 0 to 30;
- t is an integer of 2 to 200;
- and
- R7 is hydrogen or C1-C4 alkyl;
- where:
- x is an integer of 0 to 30;
- y is an integer of 2 to 200;
- R8 is hydrogen or C1-C4 alkyl;
- R9 and R10 are independently C1-C12 alkylene;
- R11 is hydrogen or C1-C6 alkyl and R12 is C1-C6 alkyl;
- or R11 and R12 together are C3-C10 alkylene;
- and
- R4 is the residue of a diol containing at least one amine functionality incorporated therein;
- in which at least 0.1 mol % of the A units are R1, and at least 0.1 mol % of the A units are R4.
32 more elements
Dependencies are inferred from the claim text.