Methods for the identification of compounds capable of...

A - Human Necessities – 61 – K

Patent

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A61K 31/565 (2006.01) A61K 38/21 (2006.01) A61K 45/00 (2006.01) C07K 14/16 (2006.01) C07K 16/10 (2006.01) C12Q 1/70 (2006.01) G01N 33/569 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2190613

A method for treating an individual exposed to or infected with HIV is disclosed which comprises administering to said individual a therapeutically effective amount of one or more compounds which inhibit or prevent replication of said HIV by interfering with the replicative or other essential functions of vpr expressed by said HIV, by interactively blocking the vpr target in human cells, and thereby preventing translocation of the vpr/target complex from the cytosol of said human cells to the nuclei of said cells, where vpr carries on activities essential to replication of HIV. In preferred embodiments, the compound or compounds which interactively block the target are steroid hormone receptor antagonists, glucocorticoid receptor antagonists, or glucocorticoid receptor Type II antagonists, especially mifepristone (RU-486). Pharmaceutical compositions comprising there compounds, as well as a method for identifying them and a kit for use therein, are also disclosed.

Procédé de traitement d'un individu atteint de VIH ou exposé à celui-ci et consistant à administrer audit individu une dose thérapeutiquement efficace d'un ou de plusieurs composés inhibant ou empêchant la réplication dudit VIH en agissant sur les fonctions de réplication ou sur d'autres fonctions essentielles de vpr exprimée par ledit VIH, par blocage interactif de la cible de vpr dans les cellules de l'homme, ce qui empêche la translocation du complexe vpr/cible depuis le cytosol desdites cellules vers les noyaux desdites cellules, où vpr exerce des activités essentielles à la réplication du VIH. Dans des modes de réalisation préférés, le(s) composé(s) bloquant la cible de façon interactive sont des antagonistes de récepteurs d'hormones stéroïdes, des antagonistes de récepteurs de glucocorticoïdes ou des antagonistes de type II de récepteurs de glucocorticoïdes, en particulier mifepristone (RU-486). L'invention concerne également des compositions pharmaceutiques comprenant lesdits composés, ainsi qu'un procédé servant à les identifier et un matériel de mise en application dudit procédé.

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