Rigidified compounds for modulating heparanase activity

Details Rigidified compounds for modulating heparanase activity Rigidified compounds for modulating heparanase activity

C - Chemistry, Metallurgy

07

D

C07D 293/10 (2006.01) A61K 31/41 (2006.01) A61K 31/426 (2006.01) C07D 277/60 (2006.01)

Patent

CA 2592953

Disclosed are novel rigidified compounds having a rhodanine-like residue and at least one aryl or heteroaryl residue linked to the rhodanine-like residue, whereby a core structure of these compounds, as defined in the specification, is characterized as having one or zero free-to-rotate bonds. Also disclosed are pharmaceutical compositions containing these rigidified compounds and uses thereof for modulating the activity of heparanase and hence in the treatment of heparanase-associated diseases and disorders, and uses thereof for modulating the activity of heparin-binding proteins and hence in the treatment of heparin-binding proteins-associated diseases and disorders as well as in the treatment of medical conditions that are at least partially treatable by rhodanine or a rhodanine analog.

L'invention concerne de nouveaux composés rigidifiés comprenant un résidu du type rhodanine et au moins un résidu aryle ou hétéroaryle lié au résidu du type rhodanine. La structure centrale de ces composés, telle qu'elle est définie dans le descriptif, est caractérisée en ce qu'elle comprend une ou zéro liaisons à rotation libre. L'invention concerne également des compositions pharmaceutiques contenant ces composés rigidifiés et leurs utilisations afin de moduler l'activité de l'héparanase et, par conséquent, de traiter des maladies et des troubles associés à l'héparanase et de moduler l'activité de protéines se liant à l'héparine et, par conséquent, de traiter des maladies et des troubles associés aux protéines se liant à l'héparine et permettant également de traiter des états pathologiques qui peuvent être traités au moins partiellement à l'aide de la rhodanine ou d'un analogue de la rhodanine.

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