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US 11,230,710 B2Granted
Compounds and methods for trans-membrane delivery of molecules
AssigneeAposense Ltd.
InventorsIlan Ziv, Joseph Dubrovsky, Hagit Grimberg
Life of this patent
Estimating the term…
Abstract
A system for delivery of drugs, and especially genetic drugs such as siRNA or antisense oligonucleotides (ASO) across biological membranes is provided. It comprises a trans-membrane delivery moiety, energized by the membrane internal electrical field, and a redox-sensitive disulfide moiety, designed to be reduced at the cytoplasm, thus releasing the cargo drug to exert its pharmaceutical effects at its target sites.
Claims8
A Conjugate, having the structure as set forth in Formula (I):
- including pharmaceutically-acceptable salts, hydrates, solvates and metal chelates of the compound represented by the structure as set forth in Formula (I), and solvates and hydrates of the salts, wherein:
- D is the drug to be delivered across biological membranes, selected from a group consisting of a small-molecule drug, a peptide, a protein, and a native or modified, single-stranded or double-stranded DNA or RNA, siRNA or ASO;
- y, z and w are each an integer, independently selected from 0, 1, 2, 3, 4, 5 or 6, wherein whenever the integer is 0, it means that the respective E moiety is null;
- at least one of y, z or w is different from 0;
- wherein at least one of E, E′ or E″ has the structure as set forth in Formulae (IV) or (IVa):
- including pharmaceutically acceptable salts, hydrates, solvates and metal chelates of the compound represented by the structure as set forth in Formulae (IV) and (IVa), and solvates and hydrates of the salts.
3 more elements
A Conjugate, having the structure as set forth in Formula (I):
- including pharmaceutically-acceptable salts, hydrates, solvates and metal chelates of the compound represented by the structure as set forth in Formula (I), and solvates and hydrates of the salts, wherein:
- D is the drug to be delivered across biological membranes, selected from a group consisting of a small-molecule drug, a peptide, a protein, and a native or modified, single-stranded or double-stranded DNA or RNA, siRNA or ASO;
- y, z and w are each an integer, independently selected from 0, 1, 2, 3, 4, 5 or 6, wherein whenever the integer is 0, it means that the respective E moiety is null;
- at least one of y, z or w is different from 0;
- wherein at least one of E, E′ or E″ has the structure as set forth in Formulae (V) or (Va):
- including pharmaceutically acceptable salts, hydrates, solvates and metal chelates of the compound represented by the structure as set forth in Formulae (V) or (Va), and solvates and hydrates of the salts.
3 more elements
Dependencies are inferred from the claim text.