Sulfonylpyrrole hydrochloride salts as histone deacetylases inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases.

Abstract

The invention relates to N-sulfonylpyrroles as well as salts thereof that are effective HDAC inhibitors. In more detail, this invention refers to salts of a compd. selected from (E)-(E)-N-hydroxy-3-(1-[4-(([2-(1H-indol-2yl)-ethyl]-methyL-amino)-methyl)-benzene sulfonyl]-1H-pyrrol-3-yl)-acrylamide, (E)-3-[1-(4-dimethylaminomethyl-benzenesulfonyl)-1H-pyrrol-3-yl]-N-hydroxy-acrylamide (I), and (E)-N-hydroxy-3-[1-(5-pyridin-2-yl-thiophene-2-sulfonyl)-1H-pyrrol-3-yl]-acrylamide with hydrochloric acid, their hydrates and to cryst. forms of these salts and hydrates. Example compd. I was prepd. by a general procedure (procedure given). All the invention compds. were evaluated for their HDAC inhibitory activity. From the assay, it was detd. that compd. I exhibited an IC50 value in the range of 0.002 to 40 μM for HDAC. [on SciFinder(R)]