Peptidylaminodiols

Details Peptidylaminodiols Peptidylaminodiols

1987-12-18

1991-07-16

Lee, Lester L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530331, 530332, 546141, 546146, 548225, 548344, 548537, 564153, 564157, A61K 3702, C07K 506, C07K 508

Patent

active

050325779

ABSTRACT:
A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is C.dbd.O or CHOH; U is CH.sub.2 or NR.sub.2, provided that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, (alpha,alpha)-dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkenyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, lowerakenyl, benzyl or heterocyclic ring substituted methyl; R.sub.4 is loweralkyl, cycloalkylmethyl or benzyl; R.sub.5 is vinyl, formyl, hydroxymethyl or hydrogen; R.sub.7 is hydrogen or loweralkyl; R.sub.8 and R.sub.9 are independently selected from OH and NH.sub.2 ; and R.sub.6 is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R.sub.5 and R.sub.7 are both hydrogen and R.sub.8 and R.sub.9 are OH, the carbon bearing R.sub.5 is of the "R" configuration and the carbon bearing R.sub.6 is of the "S" configuration, or pharmaceutically acceptable salts or esters thereof. Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.

REFERENCES:
patent: 4548926 (1985-10-01), Matsueda et al.
patent: 4609643 (1986-09-01), Szelke et al.
patent: 4616088 (1986-10-01), Ryono et al.
patent: 4645759 (1987-02-01), Luly et al.
patent: 4652551 (1987-03-01), Luly et al.
patent: 4657931 (1987-04-01), Baran et al.
patent: 4680284 (1987-07-01), Luly et al.
patent: 4698329 (1987-10-01), Matsueda et al.
patent: 4845079 (1989-07-01), Luly et al.
patent: 4877785 (1989-10-01), Hanson et al.
patent: 4900746 (1990-02-01), Hanson et al.
patent: 4902706 (1990-02-01), Hanson et al.
Burger, Medicinal Chemistry, 1960, pp. 565-571, 578-581, 600-601.
Denkewalter et al., Progress in Drug Research, vol. 10, 1966, pp. 510-512.
Plattner et al, J. Med. Chem. 31(12) 2277-2288, 1988.
Thaisrivongs et al., J. Med. Chem. 1987, 30(6) 976-982.
Hanson et al., Biochem. Biophys. Res. Comm. 1985, 132(1) 155-161.
Matsueda et al., Chem. Lett., 1044, (1985).
T. Kokubu et al., Hypertension 8(6) (Suppl. II), II-I, (1986).
S. Thaisrivongs, et al., J. Med. Chem. 28 1555, (1985).
G. Hanson et al., Biochem. Biophys. Res. Commun. 132, 155, (1985).
Weber et al., Renin Inhibition in Hypertension, vol. 81, No. 6, Jun. 1990, pp. 1768-1774.

Affiliated with

Also associated with

Rating

Peptidylaminodiols does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Peptidylaminodiols, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Peptidylaminodiols will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-131867