3-benzoylindole derivatives and drugs containing the same

C - Chemistry – Metallurgy – 07 – D

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C07D 209/12 (2006.01) A61K 31/495 (2006.01)

Patent

CA 2294772

3-Benzoylindole derivatives represented by general formula (I) wherein R1 represents lower alkyl; n is an integer of from 1 to 5; R2 and R3 represent each hydrogen, lower alkyl or optionally substituted phenyl; and R4 represents hydrogen or lower alkyl. Because of having a potent .alpha.1-adrenergic receptor blocking effect and a testosterone 5.alpha.-reductase inhibitory effect and showing a high safety, these compounds are useful as preventives and/or remedies for prostatic hypertrophy, urinary disorders in association with prostatic hypertrophy, baldness or acne.

L'invention concerne des dérivés de 3-benzoylindole de la formule générale (I) dans laquelle R?1¿ est alkyle inférieur; n est un entier compris entre 1 et 5; R?2¿ et R?3¿ sont chacun hydrogène, alkyle inférieur ou phényle éventuellement substitué; et R?4¿ est hydrogène ou alkyle inférieur. Ces composés ont un puissant effet d'inhibition du récepteur .alpha.¿1?-adrénergique et de la 5-.alpha.-réductase de la testostérone, et offrent un niveau de sécurité élevé, ce qui en fait des composés efficaces en tant que médicaments préventifs et/ou thérapeutiques contre l'hypertrophie prostatique, les troubles urinaires, la calvitie ou l'acné.

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