Patent number: 4857507
Abstract: The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; OR.sub.10 or SR.sub.10 wherein R.sub.10 is hydrogen, loweralkyl or aminoalkyl; NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; ##STR2## wherein B is NH, alkylamino, S, O, CH.sub.2 or CHOH and R.sub.13 is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, aminoalkyl, alkoxycarbonylalkyl, carboxyalkyl, N-protected aminoalkyl, alkylaminoalkyl, (N-protected)(alkyl)aminoalkyl, dialkylaminoalkyl, (heterocyclic) alkyl or a substituted or unsubstituted heterocyclic; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloaklylmethyl, benzyl, .alpha.,.alpha.
Type:
Grant
Filed:
January 9, 1987
Date of Patent:
August 15, 1989
Assignee:
Abbott Laboratories
Inventors:
Saul H. Rosenberg, Joseph Dellaria, Anthony K, L. Fung, Dale J. Kempf, Jay R. Luly, Jacob J. Plattner
Patent number: 4853371
Abstract: An octapeptide of the formula: ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl, R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H; A.sub.3 is CH.sub.2 -A.sub.6 (where A.sub.6 is pentafluorophenyl, naphthyl, pyridyl, or phenyl); A.sub.4 is o- m- or p-substituted X-Phe (where X is a halogen, H, NO.sub.2, OH, NH.sub.2, or C.sub.1-3 alkyl), pentafluoro-Phe, or .alpha.-Nal; A.sub.5 is Thr, Ser, Phe, Val, .alpha.-aminobutyric acid, or Ile, provided that when A.sub.3 is phenyl, A.sub.1 is H, and A.sub.2 is H, A.sub.5 cannot be Val; and A.sub.7 is Thr, Trp, or .beta.-Nal; or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
June 22, 1988
Date of Patent:
August 1, 1989
Assignee:
The Administrators of the Tulane Educational Fund
Inventors:
David H. Coy, William A. Murphy, Mark L. Heiman