Peptidylaminodiols

C - Chemistry – Metallurgy – 07 – D

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C07D 233/64 (2006.01) C07K 5/02 (2006.01) C07K 5/04 (2006.01) C07K 5/06 (2006.01) C07K 5/065 (2006.01) C07K 5/078 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1287445

PEPTIDYLAMINODIOLS Abstract of the Disclosure The invention relates to renin inhibiting compounds of the formula: Image wherein R10 is Image , Image , Image , Image or Image ; A is hydrogen or an N-protecting group; w is 0 or 1; B is hydrogen, hydroxy, NH, N-alkyl, loweralkyl or arylalkyl; with the proviso that when w is 1, B is NH and when w is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R1 is loweralkyl or lipophilic or aromatic or hydrophilic amino acid side chains; m is 1-3; n is 1-3; p is 1-3; q is 1-3; s is 1-3; t is 0-2; R2 is hydrogen or loweralkyl; R3 and R4 are independently selected from loweralkyl, lipophilic or aromatic amino acid side chains; R5 and R7 are independently selected from hydrogen or loweralkyl; and R6 is hydrogen, loweralkyl, vinyl, arylalkyl or wherein R8 is hydrogen or loweralkyl, X is 0, NH or S and R9 is hydrogen, loweralkyl or alkanoyl or XR9 together can be loweralkylsulfonyl, N3 or Cl.

500188

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