Peptidyl diflurodiol renin inhibitors

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 5/06 (2006.01) A61K 31/00 (2006.01) A61K 38/05 (2006.01) C07C 215/20 (2006.01) C07C 233/36 (2006.01) C07C 233/47 (2006.01) C07C 259/20 (2006.01) C07C 265/08 (2006.01) C07C 271/16 (2006.01) C07C 271/22 (2006.01) C07C 275/24 (2006.01) C07C 309/24 (2006.01) C07C 309/82 (2006.01) C07C 317/28 (2006.01) C07C 317/44 (2006.01) C07C 323/52 (2006.01) C07C 323/60 (2006.01) C07D 205/04 (2006.01) C07D 207/12 (2006.01) C07D 213/40 (2006.01) C07D 231/12 (2006.01) C07D 263/20 (2006.01) C07D 263/24 (2006.01) C07D 277/3

Patent

CA 2024698

PEPTIDYL DIFLUORODIOL RENIN INHIBITORS ABSTRACT OF THE DISCLOSURE A renin inhibiting compound of the formula: Image wherein A is a functional group; W is (1) C(O)-, (2) -CH(OH)- or (3) -N(R2)- wherein R2 is hydrogen or loweralkyl; U is (1) -C(O)-, (2) -CH2- or (3) -N(R2)- wherein R2 is hydrogen or lower alkyl, with the proviso that when W is -CH(OH)- then U is -CH2- and with the proviso that U is -C(O)- or -CH2- when W is -N(R2)-; V is (1) -CH-, (2) -C(OH)- or (3) -C(halogen)- with the proviso that V is -CH- when U is -N(R2)-; Q is -CH(R1)- or -C(=CHR1a)- wherein R1 is (1) loweralkyl, (2) cycloalkylalkyl, (3) arylalkyl, (4) (heterocyclic)alkyl, (5) 1-benzyloxyethyl, (6) phenoxy, (7) thiophenoxy or (8) anilino, provided that B is -CH2- or -CH(OH)- or A is hydrogen when R1 is phenoxy, thiophenoxy or anilino and R1a is aryl or heterocyclic; R3 is a functional group; R4 is (1) loweralkyl, (2) cycloalkylmethyl or (3) benzyl; R5 is -CH(OH)- or -C(O)-; R6 is -CH(OH)- or -C(O)-; and Z is (1) lower alkyl, (2) aryl, (3) arylalkyl, (4) cycloalkyl, (5) cycloalkylalkyl, (6) heterocyclic or (7) (heterocyclic)alkyl; or a pharmaceutlcally acceptable salt, ester or prodrug thereof.

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