C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 295/00 (2006.01) A61K 31/495 (2006.01) C07D 241/08 (2006.01) C07D 295/13 (2006.01) C07D 295/185 (2006.01) C07D 295/26 (2006.01) C07D 487/08 (2006.01)
Patent
CA 2138521
Compounds characterized generally as ethynyl alanine amino diol compounds having a piperazinyl-terminated or a piper- azinyl-alkylamino-terminated group and derivatives thereof are useful as renin inhibitors for the treatment of hypertension. Com- pounds of particular interest are those of formula (I), wherein A is selected from CO and SO2; wherein X is selected from oxy- gen atom and methylene; wherein G is a piperazinyl group or is a piperazinyl-containing group of formula (II), wherein B is a piperazinyl group or a alkylen-bridged-piperazinyl group; wherein R1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R2 is phenylmethyl; wherein each of R3 and R5 is hydrido; wherein R4 is selected from formula (III), wherein V is selected from hydrido and methyl; wherein R6 is cyclohexylmethyl; wherein R7 is selected from isobutyl, cyc- lopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a num- ber selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
G.d. Searle & Co.
Osler Hoskin & Harcourt Llp
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