Therapeutic conjugates
AssigneeAriel Scientific Innovations Ltd.
InventorsGary GELLERMAN, Andrii BAZYLEVICH
Life of this patent
Estimating the term…
Abstract
Provided herein is a class of anti-cancer conjugates designed to cross the blood-brain barrier (BBB) and thereby deliver a methylation agent into cancerous tumor cells, wherein the conjugate comprises a BBB-shuttle moiety that allows the conjugate to cross the BBB, and at least two methylation moieties of the methyltriazene type attached thereto for effecting DNA methylation in the cancerous cells. Also provided are uses of the conjugates in the treatment of brain cancer.
Claims16
A compound comprising:
- a blood-brain barrier shuttle moiety, and
- at least two methylation moieties, each independently represented by general Formula I:
- wherein R is selected from the group consisting of hydrogen, a C1-4 alkyl, a labeling moiety, and a bioactive agent.
A compound comprising an amino acid and a methylation moiety attached to a side-chain of the amino acid, represented by general Formula III:
- wherein:
- R is selected from the group consisting of hydrogen, a C1-4 alkyl, a labeling moiety, and a bioactive agent,
- R1 is said side-chain,
- R2 is a hydrogen or a C1-4 alkyl, and
- PG is hydrogen or a protecting group.
Dependencies are inferred from the claim text.