The use of cd4-binding small molecules to inhibit hiv infection

Details The use of cd4-binding small molecules to inhibit hiv infection The use of cd4-binding small molecules to inhibit hiv infection

A - Human Necessities

61

K

A61K 31/41 (2006.01) A61K 31/00 (2006.01) A61K 31/4196 (2006.01) A61K 31/427 (2006.01) A61K 31/429 (2006.01) A61K 31/4439 (2006.01)

Patent

CA 2338329

A method of inhibiting HIV-I infection is provided that comprises adminitering to a subject an effective amount of an active compound having a molecular weight of between 200 daltons and 650 daltons. At a concentration of not more than 100 µM, compounds useful in the practice of the invention inhibit greater than 50% of the binding of gp120 to CD4. Prefered compounds are further characterized in that they inhibit less than 10 % of the binding of human CD4- expressing, CD4-transfected COS cells to Raji cells.

On décrit un procédé qui permet d'inhiber l'infection par le VIH-1 qui consiste à administrer à un individu une quantité efficace d'un composé actif don't le poids moléculaire se situe entre 200 et 650 daltons. A une concentration ne dépassant pas 100 mu M, les composés utilisés dans le cadre de la présente invention inhibent plus de 50 % de la liaison de gp120 à CD4. Des composés préférés se caractérisent en outre par le fait qu'ils inhibent moins de 10 % de la liaison de cellules COS transfectées par CD4, exprimant le CD4 humain aux cellules Raji.

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