C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 295/13 (2006.01) A61K 31/395 (2006.01) C07D 265/06 (2006.01) C07D 265/30 (2006.01) C07D 265/32 (2006.01) C07D 267/00 (2006.01) C07D 267/10 (2006.01) C07D 269/02 (2006.01) C07D 277/04 (2006.01) C07D 281/00 (2006.01) C07D 285/00 (2006.01) C07D 491/08 (2006.01) C07D 498/08 (2006.01)
Patent
CA 2136842
2136842 9404518 PCTABScor01 Compounds characterized generally as morpholino/thiomorpholino-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of formula (I), wherein A is selected from CO and SO2; wherein X is selected from oxygen atom and methylene; wherein B is selected from morpholino group, thiomorpholino group, four-, five- and seven-member heterocyclic homologue groups of morpholino and thiomorpholino groups, and oxo-, alkyl- and alkylene-bridged derivatives of said groups; 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 .alpha., wherein V is selected from hydrido and methyl; wherein R6 is cyclohexylmethyl; wherein R7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
Hanson Gunnar J.
Manning Robert E.
G.d. Searle & Co.
Osler Hoskin & Harcourt Llp
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