Affinity medicant conjugate
AssigneeAF Chemicals, LLC
InventorMichael Kelner
Life of this patent
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Abstract
In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The medicant moiety can be a toxin including an acylfulvene or a drug moiety. The affinity moiety can be an antibody, a binding protein, a steroid, a lipid, a growth factor, a protein, a peptide or non peptidic. The affinity moiety can be covalently bound to the medicant via a linker. Novel linkers that can be directed to cysteine, arginine or lysine residues based on solution pH allow greater flexibility in preserving and/or generating specific epitopes in the AMC.
Claims15
A compound of the formula:
- or a pharmaceutically acceptable salt thereof, wherein X and R1 are connected through a Linker Unit and X is selected from the group consisting of —NH—, —NR8—, —S—, —O—, —CH2—, —CHR8—, —CHR8R9—, —OC(═O)—, —N(R3)S(═O)—, and —N(═N)—;
- R1 represents an Affinity Moiety selected from the group consisting of an antibody, an antibody fragment, a receptor protein, a peptidic growth factor, an anti-angiogenic protein, a specific binding peptide, a protease cleavable peptide, a glycopeptide, a peptide, a natural peptidic toxin, a protein toxin and an oligonucleotide;
- R3, R4, R5, R6, and R7 each independently represent —H, -, —OH, —OCH3, —OC(═O)CH3 —CH3, —CH2—CH3, —CH—(CH3)2, —C(CH3)3, —CH2—CH2—CH3, —CH2—CH—(CH3)2, —CH—C—(CH3)3, —C(═O)CH3,—CH2OH, and —(C1-C4)alkyl;
- R8, and R9 each independently represent —CH2—, -, —CH2—CH2—, —CH(CH3)—CH2—, —C(CH3)2—CH2—, —CH2—CH2—CH2—, —CH2—CH(CH3)—CH2—, —CH—C(CH3)2—CH2—, —C(═O)CH2—, —CH2O—;
- where the Linker Unit is selected from the group consisting of 4-fluorosulfonyl benzoyl, 3-fluorosulfonyl benzoyl and 2-fluorosulfonyl benzoyl.
A compound of the formula:
- or a pharmaceutically acceptable salt thereof, wherein X and R1 are connected through a Linker Unit;
- where X is selected from the group consisting of a secondary amino group, a carbonyl group, an ester, and an alcohol;
- R1 represents an Affinity Moiety selected from the group consisting of an antibody, an antibody fragment, a receptor protein, a peptidic growth factor, an anti-angiogenic protein, a specific binding peptide, protease cleavable peptide, a glycopeptide, a peptide, a natural peptidic toxin, a protein toxin and an oligonucleotide;
- R3, R4, R5, R6, R7 each independently represent —H, -, —CH3, —CH2—CH3, —CH—(CH3)2, —C(CH3)3, —CH2—CH2—CH3, —CH2—CH—(CH3)2, —CH—C—(CH3)3, —C(═O)CH3, —CH2OH, and —(C1-C4)alkyl;
- where the Linker Unit is selected from the group consisting of 4-fluorosulfonyl benzoyl, 3-fluorosulfonyl benzoyl and 2-fluorosulfonyl benzoyl.
Dependencies are inferred from the claim text.