Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1987-01-09
1989-05-02
Phillips, Delbert R.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
514 18, 530331, 530338, 530800, 564170, 564174, 564180, A61K 3702, C07K 508
Patent
active
048268151
ABSTRACT:
The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; Or.sub.10 wherein R.sub.10 is hydrogen or loweralkyl; NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are independently selected from hydrogen and loweralkyl; or R.sub.13 --CO--B wherein B is NH, O, CH.sub.2, HNCH.sub.2 and R.sub.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.dbd.H,OH, then W=CH, and if U,V.dbd.O then W.dbd.N; R.sub.1 , R.sub.3 and R.sub.5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R.sub.2, R.sub.4, R.sub.7, R.sub.8 and R.sub.9 are hydrogen or loweralkyl and may be the same or different; X is NH, O, S, SO, SO.sub.2, or CH.sub.2 ; and R.sub.6 is loweralkyl cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protecting group, with the proviso that R.sub.6 may be an N-protecting group when X is NH.
REFERENCES:
patent: 4609641 (1986-09-01), Evans et al.
patent: 4645759 (1987-02-01), Luly et al.
Dellaria Joseph
Fung Anthony K. L.
Kempf Dale J.
Luly Jay R.
Plattner Jacob J.
Abbott Laboratories
Crowley Steven R.
Katz Martin L.
Phillips Delbert R.
Weinstock Steven F.
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