Novel derivatives of mesalazine, process of their preparation and their use in the treatment of intestinal inflammatory diseases
AssigneeSofar SPA
InventorCarla LABRUZZO
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AssigneeSofar SPA
InventorCarla LABRUZZO
Estimating the term…
The present invention refers to the compounds corresponding to the following general formula (I): wherein: R═C4-C8 alkanoyl; and X═NH—R1 where R1═H, or an amine protecting group; and/or the pharmaceutically acceptable salts thereof. Preferred compounds according to the present invention are represented by the following formula (Ia): wherein: R═C4-C8 alkanoyl; and/or the pharmaceutically acceptable salts thereof. In a preferred embodiment, an object of the present invention is to provide 5-amino-2-(butyryloxy)benzoic acid and/or the pharmaceutically acceptable salts thereof, preferably hydrochloride salt. A further object of the present invention is represented by the use of the compounds of formula (Ia), in particular 5-amino-2-(butyryloxy)benzoic acid and/or pharmaceutically acceptable salts thereof, as a medicament and by the use thereof for the treatment of intestinal inflammatory diseases. The present invention also regards the synthesis processes to obtain such compounds and some intermediate compounds of said synthesis processes.
Compound of formula (I):
5-amino-2-(butyryloxy)benzoic acid and/or pharmaceutically acceptable salts thereof, preferably hydrochloride salt.
Process for the preparation of the compound of formula (Ia) comprising the following steps:
Process for the preparation of 5-amino-2-(butyryloxy)benzoic acid hydrochloride comprising the following steps:
Process for the preparation of the compound of formula (Ia) comprising the following steps:
Process for the synthesis of 5-amino-2-(butyryloxy)benzoic acid comprising the following steps:
Compound of formula (Ib):
Dependencies are inferred from the claim text.