114359-43-2Relevant articles and documents
Peptidyl difluorodiol renin inhibitors
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, (2008/06/13)
A renin inhibiting compound of the formula: wherein A is a functional group; W is (1)-C(O)-,(2)-CH(OH)-or(3)-N(R?)-wherein R? is hydrogen or loweralkyl; U is (1)-C(O)-,(2)-CH?-or(3)-N(R?)-wherein R? is hydrogen or lower alkyl, with the proviso that when W is-CH(OH)-then U is-CH?-and with the proviso that U is-C(O)-or-CH?-when W is-N(R?)-; V is (1)-CH-,(2)-C(OH)-or(3)-C(halogen)-with the proviso that v is-CH--when U is-N(R?)-; Q is-CH(R?)-or-C(=CHR1a)-wherein R? is (1) loweralkyl,(2) cycloalkylalkyl,(3) arylalkyl,(4) (heterocyclic) alkyl,(5) 1-benzyloxyethyl,(6) phenoxy,(7) thiophenoxy or(8) anilino, provided that B is-CH?-or-CH(OH)-or A is hydrogen when R? is phenoxy, thiophenoxy or anilino and R1a is aryl or heterocyclic; R? is a functional group; R? is (1) loweralkyl,(2) cycloalkylmethyl or(3) benzyl; R? is-CH(OH)-or-C(O)-; R? 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 pharmaceutically acceptable salt, ester or prodrug thereof.
RENIN INHIBITING COMPOUNDS
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, (2008/06/13)
The invention relates to renin inhibiting compounds of the formula STR1 wherein A is hydrogen; loweralkyl; arylalkyl; Or 10 wherein R 10 is hydrogen or loweralkyl; NR 11 R 12 wherein R. sub.11 and R 12 are independently selected from hydrogen and loweralkyl; or R 13--CO--B wherein B is NH, O, CH 2, HNCH 2 and R 13 is loweralkyl, alkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, aminoalkyl, N-protected aminoalkyl, hydroxylated dialkylamino, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic, carboxyalkyl, or lower alkyl carboxyalkyl esters; W is N or CH: U,V may be the following combinations H,OH; OH,H; H, H; or when taken together as O represents a carbonyl with the provisos that if U,V=H, OH, then W=CH, and if U,V=O then W=N; R 1 , R 3 and R 5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R 2, R 4, R 7, R 8 and R 9 are hydrogen or loweralkyl and may be the same or different; X is NH, O, S, SO, SO 2, or CH 2 ; and R 6 is loweralkyl cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protecting group, with the proviso that R 6 may be an N-protecting group when X is NH.