Conjugates
AssigneeTransfection Holdings Limited
InventorsAlan Lawson SEWELL, Ezequiel Silva NIGENDA, Sean Niall O'BYRNE, Ricardo LOPEZ-GONZALEZ, Rodolfo MARQUEZ
Life of this patent
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Abstract
The present invention provides a conjugate of formula (I) and its use in methods of treatment, and also methods for delivering an active agent into a cell. The methods may be used to deliver an active agent into a nematode, flatworm, parasite or bacterium. The conjugate of formula (I) is: (formula (I)), wherein -D- is C1-4 alkylene or C2-4 alkenylene, preferably C2-4 alkenylene, where the alkylene or alkenylene is optionally substituted with alkyl or halo; A- is an active agent for delivery; and —RA, —RB, —RT1, —RT2, —R1, —R2, —R3, —X— and -L- are as defined herein.
Claims23
A conjugate of formula (I), or a pharmaceutical composition comprising the conjugate of formula (I):
- wherein:
- —RA and —RB are each independently selected from hydrogen, alkyl, alkenyl, alkynyl, aralkyl, cycloalkylalkyl, alkanoyl and aralkanoyl;
- or —RA and —RB together with —C(RC1)(RC2) form a 6-membered ring, where
- —RC1 is independently selected from hydrogen, alkyl, alkenyl, alkynyl, aralkyl and cycloalkylalkyl, and
- —RC2 is independently selected from hydrogen, alkyl, alkenyl, alkynyl, aralkyl, cycloalkylalkyl, alkoxy, alkenoxy, alkynoxy, aralkoxy and cycloalkylalkoxy, or
- —RC1 and —RC2 are together oxo (═O);
- —RT1 and —RT2 are each independently hydrogen or alkyl;
- —R1 and —R2 are each independently selected from hydrogen, alkyl, alkenyl, alkynyl, aralkyl and cycloalkylalkyl;
- —R3 is hydrogen or alkyl;
- -D- is C2-4 alkenylene or C1-4 alkylene, where the alkenylene or alkylene is optionally substituted with alkyl or halo;
- —X— is a covalent bond, —N(R4)—, —O—, —S—, or —Se—, where —R4 is hydrogen or alkyl;
- -L- is a linker or a covalent bond;
- and
- A- is an active agent for delivery, and comprises a dye, a small drug, a polypeptide, a polynucleotide or a polysaccharide;
- and salts, solvates and protected forms thereof.
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Dependencies are inferred from the claim text.