Indole derivatives as steroid 5a-reductase inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 405/06 (2006.01) A61K 31/40 (2006.01) A61K 31/41 (2006.01) C07D 405/14 (2006.01)

Patent

CA 2163778

The present invention provides compounds of formula (I) and the pharmaceutically acceptable base salts thereof, wherein R is -CO2H or tetrazol-5-yl; R1 is C3-C8alkyl optionally substituted by fluoro; and R2 is C2-C4alkyl, together with compositions containing, uses of, processes for the preparation of and intermediates used in the preparation of, such compounds. The compounds have steroid 5.alpha.-reductase inhibitory activity and are useful for treating a disease such as benign prostatic hyperthophy.

La présente invention concerne des composés de la formule (I) et leurs sels de base pharmacutiquement acceptables. Dans cette formule, R représente -CO2H ou tétrazol-5-yle; R1 représente alkyle optionnellement substitué par fluoro; et R2 représente alkyle C2-C4. Cette invention concerne également les compositions contenant de tels composés, les utilisations, les procédés pour leur préparation et les intermédiaires utilisés dans la préparation de ces composés. Les composés ont une activité inhibitrice de la 5alpha-réductase stéroïdienne et ils sont utiles dans le traitement d'une maladie telle que l'hypertrophie bénigne prostatique.

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