Novel indole derivatives exhibiting chymase-inhibitory...

C - Chemistry – Metallurgy – 07 – D

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C07D 401/06 (2006.01) A61K 31/4045 (2006.01) A61K 31/437 (2006.01) A61K 31/4709 (2006.01) A61K 31/5377 (2006.01) A61P 9/00 (2006.01) A61P 9/04 (2006.01) A61P 9/10 (2006.01) A61P 9/12 (2006.01) A61P 11/00 (2006.01) A61P 11/06 (2006.01) A61P 13/12 (2006.01) A61P 17/00 (2006.01) A61P 29/00 (2006.01) A61P 37/08 (2006.01) A61P 43/00 (2006.01) C07D 405/06 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 471/04 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2411165

Novel indole derivatives of the general formula (I) exhibiting useful chymase- inhibitory activities are prepared by a novel chemical synthesis method. In said formula (I), wherein A is oxygen or nitrogen which may be substituted with alkyl; R1 and R2 are each independently hydrogen or alkyl, or may be united to form cycloalkyl, an aromatic ring, or a heterocycle; R3 is hydrogen, C1-10 alkyl, or the like; R4 is substituted alkyl; and R5 is hydrogen, halogeno, alkyl, or alkoxy.

L'invention concerne de nouveaux dérivés indoliques de la formule générale (I) à activités inhibitrices de chymase, préparés suivant un nouveau procédé de synthèse chimique. A représente l'oxygène ou l'azote, que l'on peut substituer par l'alkyle. R?1¿ et R?2¿ représentent chacun individuellement l'hydrogène ou l'alkyle. Ils peuvent également s'unir pour former un cycloalkyle, un noyau aromatique ou un hétérocycle. R?3¿ représente l'hydrogène, C¿1-10? alkyle, ou analogue. R?4¿ représente l'alkyle substitué et R?5¿ l'hydrogène, l'halogène, l'alkyle ou l'alcoxy.

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