Substituted acyl derivatives of octahydro-1h-indole-2-...

C - Chemistry – Metallurgy – 07 – D

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C07D 209/42 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1205476

ABSTRACT . An octahydro-1-(.omega.-mercaptoalkanoyl)-1H-indole-2- carboxylic acid and derivatives thereof, and an octahydro- lH-indole-2-carboxylic acid and derivatives thereof having the general formula: Image (i) and Image (xiv) wherein R and R4 are hydrogen, straight and branched chain alkyl of from 1 to 4 carbon atoms, R1 is hydrogen, benzyl, straight and branched chain alkyl of from 1 to 4 carbon atoms, R2 is hydrogen and R3-CO-, wherein R3 is phenyl, straight and branched alkyl of from 1 to 4 carbon atoms, R5 is hydrogen, benzyl, straight and branched chain alkyl of from 1 to 4 carbon atoms, R6 is hydrogen, straight and branched chain alkyl of from 1 to 4 carbon atoms, Ar is phenyl, mono- and di-substituted phenyl, wherein the substituents are fluorine, chlorine, bromine, hydroxy, amino, straight and branched chain alkyl and alkoxy of from 1 to 4 carbon atoms, m is 0, 1, 2 or 3, and n is 0 or 1, and pharmaceutically acceptable salts thereof; and methods for their preparation. The compounds of the invention are useful as antihypertensive agents.

372381

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