New pradimicin derivatives for the treatment of diseases caused by kinetoplastids

The present invention relates to a class of novel pradimicins and analogues and derivatives thereof, including the compounds of formula A, I and 111, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof and their use to treat or prevent kinetoplastid infections and their use to manufacture a medicine to treat or prevent kinetoplastid infections, particularly infections with trypanosoma and leishmania, such as Trypanosoma brucei, Trypanosoma cruzi and Leischmania donovani. wherein Ra, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the claim 1 or as described in detail in the description of the invention. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent kinetoplastid infections. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of kinetoplastid infections and pathologic conditions such as, but not limited to Trypanosomiasis, such as African trypanosomiasis, sleeping sickness, Chagas disease and leishmaniasis.

Octrooi-publicatienummer: EP3054958

Jaar aanvraag: 2020

Jaar toekenning: 2020

Jaar van publicatie: 2020

Status: Toegewezen

Technologiedomeinen: Farmaceutische producten

Gevalideerd voor IOF-sleutel: Ja

Toegewezen aan: Associatie KULeuven