Amino acid derivatives, a process for the preparation...

C - Chemistry – Metallurgy – 07 – K

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C07K 5/065 (2006.01) A61K 31/395 (2006.01) A61K 38/05 (2006.01) C07D 233/54 (2006.01) C07D 233/64 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2051455

ABSTRACT Compound of the formula: Image wherein R1 is morpholinocarbonyl, thiomorpholinocarbonyl, hexahydro-1H-azepin-1-ylcarbonyl, octahydroazocin-1-ylcarbonyl, piperidinocarbonyl, lower alkanoyl, dipropylcarbamoyl, tetrahydroisoquinolylcarbonyl or a heterocyclic group, R2 is lower alkyl, R3 is lower alkyl which may be substituted with substituent(s) selected from the group consisting of aryl and cyclo(lower)alkyl, R4 is lower alkyl, X is lower alkylene, Y1 is a single bond or Image , in which R5 is lower alkyl, and Y2 is -NH- or -O-, provided that R3 is isobutyl, 2-ethylbutyl or lower alkyl substituted with substituent(s) selected from the group consisting of aryl and cyclo(lower)alkyl, 1) when R1 is morpholinocarbonyl and Y1 iS Image ; 2) when R1 is morpholinocarbonyl or thiomorpholinocarbonyl, Y1 is a single bond and Y2 is -O-; or 3) when R1 is lower alkanoyl and Y2 is -O-; and their pharmaceutically acceptable salts. The preparation of these compounds, pharmaceutical compositions containing them and their uses for therapeutic treatment and the pre- vention of hypertension, heart failure, renal diseases or glaucoma in humans and animals, are also disclosed.

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