Back to results
US 7,745,392 B2Granted
Multi-valent guanidinium compounds for enhancing molecular translocation across cellular membranes and epithelial tissues
AssigneeNitto Denko Corporation
InventorsZheng Hou, Jian Liu, Lei Yu
Life of this patent
Estimating the term…
Abstract
Disclosed herein are guanidinium containing compounds consisting of a core moiety with a plurality of side chains containing guanidinium groups. Such compounds have enhanced translocation across cellular membranes and epithelial tissues. The compounds may also have a therapeutic or other biologically active moiety attached so that these moieties may be effectively transported into a cell by the guanidinium containing compound.
Claims22
A compound having the formula:
- wherein C is selected from the group consisting of:
- wherein R is selected from the group consisting of hydrogen, optionally substituted C1-12 alkyl, optionally substituted C2-C12 alkenyl, and optionally substituted C2-C12 alkynyl;
- wherein Y is a group of the formula:
- wherein 2 to 6 Y groups are attached to C;
- wherein Z has the formula:
- wherein one Z is attached to C or is absent;
- wherein each L is separately selected to be a linker moiety comprising a molecular fragment having a molecular weight less than 1000;
- wherein each BB is separately selected to be a backbone moiety comprising an organic fragment having a molecular weight less than 5000;
- wherein each G is separately selected to be a guanidinium group covalently attached to BB and has the formula:
- or each G is separately selected from the group consisting of:
- each R1, R2, R3, and R4 is hydrogen;
- wherein each T is a terminal group separately selected from the group consisting of hydrogen, an amine group, a carboxylic group, a N-terminal peptide or group that forms an N-terminal peptide bond with BB, a C-terminal peptide or group that forms a C-terminal peptide bond with BB, a reporting moiety, a targeting moiety, and a therapeutic moiety, or each T is separately absent;
- and
- wherein each n is separately selected to be an integer from 1 to 8.
11 more elements
A compound selected from the group consisting of:
- wherein Z has the formula:
- wherein each T is a terminal group separately selected from the group consisting of hydrogen, an amine group, a carboxylic group, a N-terminal peptide or group that forms an N-terminal peptide bond with BB, a C-terminal peptide or group that forms a C-terminal peptide bond with BB, a reporting moiety, a targeting moiety, and a therapeutic moiety, or each T is separately absent;
- and
- wherein each L is separately selected to be a linker moiety comprising a molecular fragment having a molecular weight less than 1000.
1 more element
Dependencies are inferred from the claim text.