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US 2025/0197416 A1Published application
Parthenolide derivatives and use thereof
AssigneeUniversity of Rochester
InventorsRudi Fasan, Andrew R. Bortz, John M. Bennett
Life of this patent
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Abstract
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Claims25
A compound of the general formula selected from the group consisting of A1 through A45:
- wherein
- A is ═CH2 or —CH2R* wherein R* is an amino acid residue banded to the A methylene via a nitrogen or sulfur atom;
- or R* is —NR1R2, —NR1C(O)R2, —NR1CO2R2, or —SR1, wherein R1 and R2 are independently selected from the group consisting of H and an optionally substituted alkyl, alkenyl, or alkynyl group, an optionally substituted heteroalkyl, heteroalkenyl, or heteroalkynyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, or an optionally substituted heterocyclic group;
- or R* is —NR1R2, wherein R1 and R2 optionally together with the nitrogen atom form a an optionally substituted 5-12 membered ring, the ring optionally comprising at least one heteroatom or group selected from the group consisting of —CO—, —SO—, —SO2—, and —PO—;
- L is —O—, —NH—, —NHC(O)—, —OC(O)—, —OC(O)NH—, —S—, —SO—, —SO2—, —PO—, —OCH2—, or a chemical bond connecting the carbon atom to Y;
- Y represents a hydrogen atom, an optionally substituted alkyl, alkenyl, or alkynyl group, an optionally substituted heteroalkyl, heteroalkenyl, or heteroalkynyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, or an optionally substituted heterocyclic group with the proviso that when -L-Y is hydrogen, -M-X is not hydroxyl, nor —C(O)CH2CH3 and A is not —CH2—N(CH3)2, wherein -L-Y together with the carbon atom at position C2 optionally forms carbonyl;
- or
- Y is absent and L represents a halogen atom, an azido group (—N3), an optionally substituted triazole group, or a group —NR3R4, where R3 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, or alkynyl group;
- R4 represents an optionally substituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl group;
- or where R3 and R4 are connected together to form an optionally substituted heterocyclic group;
- and
- M is —O— or —OC(O)— and X represents a hydrogen atom, an optionally substituted alkyl, alkenyl, or alkynyl group, an optionally substituted heteroalkyl, heteroalkenyl, or heteroalkynyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, or an optionally substituted heterocyclic group.
9 more elements
(canceled)
(canceled)
(canceled)
(canceled)
Dependencies are inferred from the claim text.