PATENTSCOPE will be unavailable a few hours for maintenance reason on Tuesday 19.11.2019 at 4:00 PM CET
Search International and National Patent Collections
Some content of this application is unavailable at the moment.
If this situation persists, please contact us atFeedback&Contact
1. (WO1999034833) DEGRADABLE HETEROBIFUNCTIONAL POLY(ETHYLENE GLYCOL) ACRYLATES AND GELS AND CONJUGATES DERIVED THEREFROM
Note: Text based on automatic Optical Character Recognition processes. Please use the PDF version for legal matters

THAT WHICH IS CLAIMED IS:
1. A heterobifunctional polymer comprising:
a poly(alkylene oxide) backbone;
a first terminus comprising an acrylate group;
a second terminus comprising a target or a reactive moiety capable of coupling to a target; and
a hydrolytically degradable linkage for releasing said target upon hydrolysis.

2. A compound represented by the formula:
CH2=CZ-C02-POLY-W-POLY'-Q
where
Z represents H or alkyl;
POLY and POLY' are poly(alkylene oxide) groups that can be the same or different and are represented by the formula -(CH2CHRO)n-CH2CHR- in which R is H or alkyl, and n ranges from about 10 to about 4000;
Q represents a functional group; and
W represents a hydrolytically unstable linkage.

3. A compound represented by the formula:
CH2=CZ-CO2-POLY-W-Q
where
Z represents H or alkyl;
POLY is poly(alkylene oxide), represented by the formula
-(CH2CHRO)n-CH2CHR- in which R is H or alkyl, and n ranges from about 10 to about 4000;
Q represents a functional group; and
W represents a hydrolytically unstable linkage.

4. The compound of either of Claims 2 or 3 , wherein POLY and POLY' are poly(ethylene glycol).
5. The compound of either of Claims 2 or 3, wherein W comprises a hydrolyzable covalent bond selected from the group consisting of esters, orthoesters, imines, acetals, peptide bonds, and disulfides.

6. The compound of either of Claims 2 or 3 , wherein W has a structure of:
-0(CH2)m-CO2Rι-C02-where m ranges from 1 to 10, and Ri is -CH2-, -CH2CH2- or -CH(CH3)CH2-, or W has the structure -O-(CH2)m-CO2-.

7. The compound of either of Claims 2 or 3, wherein Q is selected from the group consisting of aldehydes, carboxylic acids, active esters, active carbonates, sulfonate esters, amines, hydrazides, orthopyridyl disulfides, and thiols.

8. A conjugate having a formula of:
(CH2=CZ-C02-POLY-W-POLY'-L)x-T
where
Z is H or an alkyl group;
POLY and POLY' are poly(alkylene oxides) comprising groups that can be the same or different and are represented by the formula
-(CH2CHRO)n-CH2CHR- in which R is H or alkyl, and n ranges from about 10 to about 4000;
W represents a hydrolytically unstable linkage;
L is hydrolytically stable linkage;
x is an integer of 1-10; and
T is a target molecule.

9. The conjugate of Claim 7, wherein R is H.

10. The conjugate of Claim 7, wherein W has the structure of:
-O(CH2)m-CO2RrC02-where m ranges from 1 to 10, Ri is selected from the group consisting of -CH2-, -CH2CH2-, and -CH(CH3)CH2- or W has the structure -O-(CH2)m-CO2-.
11. The conjugate of Claim 7, wherein T is selected from the group consisting of proteins, polysaccharides, oligonucleotides, lipids, vitamins, hormones, or small molecule pharmaceuticals.

12. A compound having the following structure:
CH2=CZC02-POLY-W-Q
where Z represents H or alkyl;
POLY is a poly(alkylene oxide) represented by the formula
-(CH2CHRO)n-CH2CHR- in which R is H or alkyl, and n ranges from about 10 to about 4000;
Q represents a functional group; and
W represents a hydrolytically unstable linkage.

13. The compound of Claim 11 , wherein POLY is poly(ethylene glycol).

14. The compound of Claim 11 , wherein W comprises a hydrolyzable covalent bond selected from the group consisting of esters, orthoesters, imines, acetals, peptide bonds, and disulfides.

15. The compound of Claim 11 , wherein W has the structure of:
-O(CH2)m-CO2R!-C02-where m ranges from 1 to 10 and Rj is -CH2-, -CH2CH2-, or -CH(CH3)CH2- or W has the structure -O-(CH2)m-CO2-.

16. The compound of Claim 11 , wherein Q is selected from the group consisting of aldehydes, carboxylic acids, active esters, active carbonates, sulfonate esters, amines, hydrazides, orthopyridyl disulfides, N-succinimidyl, and thiols.

17. A conjugate having the following structure:
(CH2=CZCO2-POLY-W-L)x-T
where
Z represents H or alkyl;
POLY is a poly(alkylene oxide) comprising a group represented by the formula -(CH2CHRO)n-CH2CHR- in which R is H or alkyl, and n ranges from about 10 to about 4000;
W represents a hydrolytically unstable linkage;
L is a hydrolytically stable linkage;
x is an integer from 1 to 10; and
T is a target molecule.

18. A polymer selected from the group consisting of compounds represented by the formula:
CH2=CZ-C02-POLY-W-POLY'-Q1,
(CH2=CZ-CO2-POLY-W-POLY'-L)x-T,
CH2=CZCO2-POLY-W-Q, and
(CH2=CZCO2-POLY-W-L)x-T,
where
Z is H or an alkyl group;
POLY and POLY' are poly(alkylene oxides) that can be the same or different and are represented by the formula -(CH2CHRO)n-CH2CHR- in which R is H or alkyl, and n ranges from about 10 to about 4000;
W represents a hydrolytically unstable linkage;
Q represents a functional group;
L is hydrolytically stable linkage;
x is an integer of 1 - 10; and
T is a target molecule.

19. The polymer composition of Claim 17, wherein W has the structure of:
-O(CH2)m-CO2R!-CO2-where m ranges from 1 to 10, R\ is selected from the group consisting of -CH2-, -CH2CH2-, and -CH(CH3)CH2- or W has the structure of -O-(CH2)m-CO2-.

20. The polymer composition of Claim 17, wherein T is a protein.
21. The polymer composition of Claim 17, wherein R is H.

22. A hydrogel comprising a co-polymerization product of a multiacrylate and at least one compound selected from the group consisting of compounds represented by the formula:
CH2=CZ-C02-POLY-W-POLY'-Qb
(CH2=CZ-CO2-POLY-W-POLY'-L)x-T,
CH2=CZCO2-POLY-W-Q, and
(CH2=CZCO2-POLY-W-L)x-T,
where
Z is H or an alkyl group;

POLY and POLY' are poly(alkylene oxides) that may be the same or different and are represented by the formula -(CH2CHRO)n-CH2CHR- in which R is H or alkyl, and n ranges from about 10 to about 4000;
W represents a hydrolytically unstable linkage;
Q represents a functional group;
L is hydrolytically stable linkage;
x is an integer of 1-10; and
T is a target molecule.

23. The hydrogel of Claim 21 , wherein said multiacrylate is selected from the group consisting of PEG diacrylates and N-vinylpyrrolidone.

24. The hydrogel of Claim 22, wherein said PEG diacrylate is CH2=CHCO2-PEG-O-CH2C02CH(CH3)CH2CONH-PEGO2CCH=CH2 or
CH2=CHCO2-PEG-O-CH2C02PEG-02CCH=CH2.

25. The hydrogel of Claim 21 , wherein T is a protein.