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US 2025/0144078 A1Published application
Thiostrepton-inspired compounds for treatment of cancer and preparation thereof
AssigneeRS Oncology, LLC
InventorsGeorge N. Naumov, Jarrett B. Duncan, Paul R. Werkhoven, Bart DeCorte, Brian Cunniff, Johannes W.G. Meissner
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Abstract
Disclosed herein are structures, compositions and syntheses of pharmaceutically relevant compounds inspired by thiostrepton, as well as methods of treating cancer with such compounds.
Claims85
A compound having the structure of Formula (IA):
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is —NH2, —NH(CH3), —O—CH3, or —NH—CH2—C(O)—NH2;
- R2 is —H, —CH3, ═CH2, or ═CH(alkyl);
- R3 is —H, —CH3, ═CH2, or ═CH(alkyl);
- R5 is —C(O)—R1 or —CN;
- Ring A is aryl, heteroaryl, cycloalkyl, or heterocyclyl;
- Ring B is absent or present and, when present, is aryl, heteroaryl, cycloalkyl, or heterocyclyl;
- R4 is hydrogen, a protecting group, —C(O)—CH3, -L′, or -L-Y;
- L′, when present, is a reactive linker moiety;
- L, when present, is a linker moiety;
- Y, when present, is a mitochondrial targeting moiety;
- each is independently a single bond or a double bond;
- and
- any hydrogen atom is optionally replaced with a deuterium.
11 more elements
A composition comprising a compound of Formula (IA), wherein R4 is hydrogen, a protecting group, or —C(O)—CH3,
- wherein the compound is contained within a nanoparticle, liposome or micelle, wherein the nanoparticle, liposome, or micelle is conjugated to a mitochondrial targeting moiety.
A composition comprising a compound of Formula (IB), wherein R4 is hydrogen, a protecting group, or —C(O)—CH3,
- wherein the compound is contained within a nanoparticle, liposome or micelle, wherein the nanoparticle, liposome, or micelle is conjugated to a mitochondrial targeting moiety.
Dependencies are inferred from the claim text.