Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Tripeptides – e.g. – tripeptide thyroliberin – etc.
Patent
1988-07-01
1989-05-02
Kight, John
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
Tripeptides, e.g., tripeptide thyroliberin , etc.
530300, 530330, C07C10352, A61K 3702
Patent
active
048269581
ABSTRACT:
The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is ##STR2## wherein B is thiomorpholino, morpholino, 4-sulfonylmorpholino, 3,4-dihydroxypyrrolidino, alkoxy or loweralkyl and C is NH or CH.sub.2 ; R.sub.1, R.sub.3 and R.sub.7 are independently selected from loweralkyl or lipophilic or aromatic amino acid side chains; R.sub.2, R.sub.4, and R.sub.6 are independently selected from hydrogen or loweralkyl; R.sub.5 is phenyl, isopropyl, cyclohexyl, 1,3-dioxan-2-yl; 1,3-dioxolan-2-yl, loweralkyl, 1,3-dithiolan-2-yl or 1,3-dithian-2-yl; X is hydrogen, loweralkyl or --CH.sub.2 OR.sub.8, wherein R.sub.8 is hydrogen, loweralkyl or alkaryl; and R.sub.9 is hydrogen, loweralkyl, hydroxy, hydroxyalkyl, difluoro, alkoxy, allyl, alkaryloxy or thioalkyl and pharmaceutically acceptable salts thereof.
REFERENCES:
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Boger et al., "Novel Renin Inhibitors Containing the Amino Acid Statine", Nature, vol. 303, May 5, 1983, pp. 81-84.
Chemical Abstract, vol 96: 30586v, "New Renin Inhibitors Homologous with Pepstatin", Eid et al.
Chemical Abstract, vol 99: 195414n, "Renin Inhibiting Peptides having Phe Deletion", Boger et al.
Chemical Abstract, vol. 101: 7653c, "Enzyme Inhibitors", Szelke et al.
Abbott Laboratories
Crowley Steven R.
Katz Martin L.
Kight John
Nutter Nathan M.
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