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US 10,293,021 B2Granted
Conjugates and prodrugs for treating cancer and inflammatory diseases
AssigneesCentre National De La Recherche Scientifique, Universite De Poitiers
InventorsSebastien Papot, Isabelle Opalinski, Brigitte Renoux, Thibaut Legigan
Life of this patent
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Abstract
The present invention relates to the field of cancer and inflammatory diseases. More particularly, it aims to provide, for these purposes, novel conjugated forms of active ingredients belonging to the dolastatin family and having the formula as follows: It is also directed towards prodrug forms of these conjugates.
Claims17
A conjugate of general formula (I):
- in which:
- A represents a radical of the dolastatin family or a derivative thereof,
- L represents a radical capable of reacting with an amino, hydroxyl or thiol function,
- G comprises a glucuronyl radical or a derivative thereof,
- Y represents H, or an electron-withdrawing radical chosen from NO2, CF3 and a halogen,
- R1 and R2 represent, independently of one another, H or a linear or branched, saturated or unsaturated C1 to C10 alkyl radical,
- Z represents a hydrocarbon-based spacer radical comprising, at each of its ends, covalent bond functions,
- X represents —O— or —NR3COO—, with R3 representing a hydrogen atom or a linear or branched, saturated or unsaturated C1 to C10 alkyl radical, the bond with the G radical being provided by the oxygen atom (—O),
- an isomer thereof and/or a pharmaceutically acceptable salt thereof.
6 more elements
Dependencies are inferred from the claim text.