Molecules comprising a bis(heteroaryl)maleimide backbone,...

Details Molecules comprising a bis(heteroaryl)maleimide backbone,... Molecules comprising a bis(heteroaryl)maleimide backbone,...

C - Chemistry, Metallurgy

07

D

C07D 405/14 (2006.01) A61K 31/4025 (2006.01) A61P 31/18 (2006.01)

Patent

CA 2715483

The invention relates to molecules having a bis(heteroaryl)maleimide structure and exhibiting inhibitory characteristics with respect to enzymes which have a catalytic pocket comprising invariant D, D and E or D, D and D amino acids, such as transposases, RAG recombinases or retroviral integrases. The invention also relates to the use of these molecules for the in vitro, ex vivo or in vivo inhibition of transposases, of RAG recombinases and of retroviral integrases, such as the HIV virus integrase, and also the use of these molecules in the treatment of pathological conditions associated with these enzymes in an animal or human host, in particular in the treatment of AIDS.

L'invention concerne des molécules possédant une structure bis- (hétéroaryl)maléimide, et présentant des caractéristiques inhibitrices d'enzymes à poche catalytique comprenant des acides aminés invariants D, D et E ou D, D et D, telles que les transposases, les recombinases RAG ou les intégrases rétrovirales. L'invention concerne également l'utilisation de ces molécules pour l'inhibition in vitro, ex vivo ou in vivo de transposases, de recombinases RAG et d'intégrases rétrovirales, telles que l'intégrase du virus VIH, ainsi que l'utilisation de ces molécules dans le traitement des pathologies associées à ces enzymes chez un hôte animal ou humain, en particulier dans le traitement du SIDA.

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