Sanofi

Claire Trecant

Alain Dlubala

Isabelle Ripoche

The disclosure relates to derivatives of morphine-6-glucuronide of formula (I) wherein R1 is as defined in the disclosure, or an acid addition salt thereof, as well as in hydrate or solvate form. The disclosure also relates to the preparation method thereof and to the use of same in therapeutics.

Derivatives of morphine-6-glucuronide, preparation method thereof and use of same in therapeutics

The disclosure relates to compounds of formula (I): wherein R1, R2, and n are as defined in the disclosure, and addition salts solvates and hydrates thereof. The disclosure also relates to the preparation method of said compounds and to the use of the same in therapeutics.

Bicyclic derivatives of morphine-6-glucuronide, preparation method thereof and use of same in therapeutics

The disclosure relates to a method for preparing morphine-6-glucuronide or one of the deritives thereof comprising reacting a compound of formula (I): wherein Ris as defined in the disclosure,with a glucuronic acid derivative of formula (II): wherein PG, X, and Rare as defined in the disclosure,in the presence of an aromatic solvent and trimethylsilyl trifluoromethanesulfonate;(ii) reacting the product obtained in step (i) with a strong basic agent; and then (iii) recovering the product obtained in step (ii).

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Strasbourg, France

Claire Trecant