Malaria is caused by unicellular Plasmodium parasites which are transmitted by the bite of mosquitoes. Although several medicines are available for prophylaxis and treatment of acute infection, their application is severely hampered by emerging resistances of the parasites. Novel drugs displaying a low risk of cross-resistance with established medicines are urgently needed.
With hundreds of millions infected patients worldwide and hundreds of thousands fatal outcomes annually, Malaria is one of the most dangerous infective diseases worldwide.
Inhibition of the growth of erythrocytic stages of Plasmodium para-sites
Low risk of cross-resistance with established antimalarial drugs
The invented compound class against malaria inhibits the growth erythrocytic (human red blood cell) stages of plasmodium para- sites. Since the compounds are structurally unrelated to existing anti-malaria drugs, the risk of cross-resistance is low.
Fig. 1:N-Unsubstituted 3,4-bis(indol-3-yl)cyclobut-3- ene-1,2-diones“
In fig. 1 the claimed Markush structure „N- Unsubstituted 3,4-bis(indol-3-yl) cyclobut-3- ene-1,2-diones as antimalarial drugs“ is de- picted, in which A(n), X, E, L, R, Y, and M(p) embody defined atoms or atom groups.
Granted US 10,287,271