Nalmefene prodrugs
AssigneeJanssen Pharmaceutica NV
InventorsMichel Joseph, Maurice, Andre Guillaume, Tim Gaekens
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Abstract
The present invention relates to ester prodrugs of nalmefene of formula (I), pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of substance abuse disorders such as alcohol abuse and alcohol dependence and impulse control disorders such as pathological gambling and addiction to shopping.
Claims15
A compound of formula (I)
- including any stereochemically isomeric form thereof, wherein
- R1 is C6-16alkyl or C8-12alkylamino;
- or a pharmaceutically acceptable acid addition salt thereof, or a solvate thereof.
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A process for preparing a compound of formula (I-b), defined as compounds of formula (I) wherein R1 represents C8-12alkylamino, comprising reacting nalmefene (II) with an isocyanate of formula (IV),
- or;
- if desired;
- a compound of formula (I-b) is converted into a pharmaceutically acceptable acid addition salt, or conversely, an acid addition salt of a compound of formula (I-b) is converted into a free base form with alkali;
- and, if desired, preparing stereochemically isomeric forms thereof.
Dependencies are inferred from the claim text.