Inhibitors of metazoan parasite proteases

Details Inhibitors of metazoan parasite proteases Inhibitors of metazoan parasite proteases

A - Human Necessities

61

K

A61K 31/44 (2006.01) A61K 31/00 (2006.01) A61K 31/12 (2006.01) A61K 31/136 (2006.01) A61K 31/415 (2006.01) A61K 31/4164 (2006.01) A61K 31/4178 (2006.01) A61K 31/4402 (2006.01) A61K 31/4406 (2006.01) A61K 31/472 (2006.01)

Patent

CA 2215245

Compositions and methods for treating a patient infected with a metazoan parasite by inhibiting the enzymatic action of the metazoan parasite protease, wherein there is employed at least one compound of general formula (I): A - X - B, wherein A is a substituted or unsubstituted homoaromatic or heteroaromatic ring system comprising one to three rings which binds to at least one of the S2, S1 and S1' subsites; B is a substituted or unsubstituted homoaromatic or heteroaromatic ring system comprising one to three rings which binds to at least one of the S1', S1 and S2 subsites; and X is -C=C-C(=O)-. These compositions and methods have particular utility in the treatment of schistosomiasis, malaria, and other infectious diseases.

La présente invention décrit des compositions et des méthodes de traitement d'un patient infecté par un métazoaire parasite qui inhibent l'action enzymatique de la protéase du métazoaire, et qui utilisent au moins un composant de formule générale (I): A-X-B, dans laquelle A représente un système de cycles homoaromatiques ou hétéroaromatiques avec ou sans substitution comportant un à trois cycles qui se lient à au moins l'un des sous-sites S1, S2 et S1'; B représente un système de cycles homoaromatiques ou hétéroaromatiques comportant un à trois cycles qui se lient à au moins l'un des sous-sites S1', S1 et S2; et X représente -C=C-C(=O)-. Ces compositions et méthodes trouvent tout particulièrement leur utilité dans le traitement de la schistosomiasie, du paludisme et d'autres maladies infectieuses.

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