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1. (WO2019063638) FUNCTIONALIZED POLYMERS FOR THE INTRACELLULAR RELEASE OF BIOACTIVE MOLECULES
注意: このテキストは、OCR 処理によってテキスト化されたものです。法的な用途には PDF 版をご利用ください。

CLAIMS

1. A bioactive molecule delivery system comprising:

a) a bioactive molecule; and

b) a biocompatible and/or biodegradable polymer covalently derivatized with a radical of formula R


R

optionally via linker, and wherein:

^ is the point of attachment to the polymer, or, when a linker is present, to the linker;

Ra, Rb and Rc can be the same or different and are selected from methyl and ethyl;

G is a d-C5 linear, branched or cyclic alkyl, optionally substituted with one or more groups selected from hydroxy, carboxyl, carboxylate, 1-pyrrolidinyl, 1-azetidinyl, 1-aziridinyl, sulfhydryl, -NRdRe and -N=NRf;

Rd, Re and Rf are independently selected from hydrogen, methyl, ethyl and propyl; m can be zero or 1;

-X- is selected form the list of -C(O)-, -NRg-, -S- and -S02-,

Rg is selected from hydrogen, methyl, ethyl and propyl;

Z is a pharmaceutically acceptable anion;

n can be zero or 1, and it can only be zero when G bears a carboxylate;

with the proviso that R cannot be

z- + O

2. System according to claim 1, wherein the radical R is selected from radicals of formula A, B and C


A B C

where ^ , Ra, Rib, Rc, G, Z and n are as defined in claim 1.

3. System according to claim 2, wherein the radical R is selected from


wherein a wavy bond indicates that the radical's carbon atom attached through it be in either of the R and the S configuration;

and wherein ^ and Z are as defined in claim 2.

System according to claim 2, wherein the radical R is selected from



wherein a wavy bond indicates that the radical's carbon atom attached through it may be in either of the R and the S configuration;

and wherein ^ and Z are as defined in claim 2.

5. System according to claims 1-2, wherein Ra, Rb and Rc each are methyl.

6. System according to claims 1 -5, wherein the polymer is in the form of nanoparticles.

7. System according to claim 6, wherein the nanoparticles have an average size of about 100 nm.

8. System according to claims 1-7, wherein the polymer is selected form the list of a polyhydroxyalkanoate and a polyester.

9. System according to claim 8, wherein the polymer is a polyhydroxyalkanoate selected from poly(3-hydroxyproprionate), poly(3-hydroxybutyrate), poly(3-hydroxyvalerate) and copolymers of the same.

10. System according to claim 8, wherein the polymer is a polyester selected from polycaprolactone, polylactic acid, polyglycolic acid and copolymers of the same.

11. System according to claims 1-10, for use in transporting the bioactive molecule inside cells that express an organic cationic transporter.

12. System according to claim 11, wherein the bioactive molecule is selected from indomethacin, curcumin, acyclovir, coumarin-6, and (R)-3-(3-tetradecylureido)-4- (trimethylammonium)butanoate

13. System according to claims 11 or 12, wherein the organic cationic transporter is selected from SLC22A4, SLC6A14 and SLC6A16.