Benzimidazole derivative

Details Benzimidazole derivative Benzimidazole derivative

C - Chemistry, Metallurgy

07

D

C07D 209/08 (2006.01) A61K 31/404 (2006.01) A61K 31/4184 (2006.01) A61K 31/4439 (2006.01) A61P 5/24 (2006.01) A61P 5/28 (2006.01) A61P 5/38 (2006.01) A61P 13/08 (2006.01) A61P 15/00 (2006.01) A61P 17/00 (2006.01) A61P 17/08 (2006.01) A61P 17/10 (2006.01) A61P 17/14 (2006.01) A61P 35/00 (2006.01) A61P 43/00 (2006.01) C07D 209/12 (2006.01) C07D 235/06 (2006.01) C07D 235/10 (2006.01) C07D 235/12 (2006.01) C07D 235/26 (2006.01) C07D 401/04 (2006.01) C07D 401/06 (2006.01) C07D 405/04 (2006.01)

Patent

CA 2694216

Disclosed is a novel and excellent therapeutic and/or prophylactic method for prostatomegaly, prostate cancer or the like, which relies on the selective inhibitory activity on 17 .beta. HSD type 5. It is found that an indole or benzimidazole derivative having a phenyl group substituted on the nitrogen atom in an indole or benzimidazole ring wherein the phenyl group has a COOH substituted therein has a potent selective inhibitory activity on 17 .beta. HSD type 5, and that the indole or benzimidazole derivative can be used as a therapeutic and/or prophylactic agent for a disease associated with 17 .beta. HSD type 5 such as prostatomegaly, prostate cancer or the like without any adverse side effect induced by the decrease in the testosterone level.

L'invention porte sur un nouveau procédé thérapeutique et/ou prophylactique nouveau excellent pour la prostatomégalie, le cancer de la prostate ou similaire, et qui repose sur l'activité inhibitrice sélective sur 17âHSD type 5. Il a été découvert qu'un dérivé d'indole ou de benzimidazole muni d'un groupe phényle substitué sur l'atome d'azote dans un noyau indole ou benzimidazole dans lequel le groupe phényle a un COOH substitué a une activité inhibitrice sélective puissante sur le 17ßHSD type 5, et que le dérivé d'indole ou de benzimidazole peut être utilisé comme agent thérapeutique et/ou prophylactique pour une maladie associée au 17ßHSD type 5 telle que la prostatomégalie, le cancer de la prostate ou similaire sans que la diminution du taux de testostérone n'induise aucun effet secondaire défavorable.

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