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US3975365A Expired / Lapsed US ⏱️ 0.0 years remaining

Inhibitory octapeptides angiotensin II

Assignee: GD Searle LLC
•
Filing: 1975-01-27
•
Granted: 1976-08-17
•
Expires: 1995-01-27
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Abstract

Abstract Octapeptide derivatives characterized by an oxygen or sulfur-containing moiety in the C-terminal position are potent inhibitors of the pharmacological effects of Angiotensin and possess the additional advantage of a favorable antagonist/agonist ratio.

Inventors

  • 👤 Robert H. Mazur

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-04 22:07
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/04; C07K7/14; C07K5/00; C07K5/04; C07K5/08; C07K5/0802; C07K5/0804; C07K5/0808; A; A61; A61K; A61K38/00

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 74 words
A compound of the formula ##EQU24## wherein X represents a sarcosine or aspartic acid residue, Y represents the residue of isoleucine or valine, n is 1, A is O, S, SO, SO 2 , and R is arylalkyl of the formula ##SPC2## wherein m is 1 or 2, w is hydrogen, halo, loweralkyl having 1-7 carbon atoms, or loweralkoxy having 1-7 carbon atoms, and the amino acid residues having L or DL stereochemical configuration.
Claim 2
Dependent Claim 74 words
A compound of the formula ##EQU24## wherein X represents a sarcosine or aspartic acid residue, Y represents the residue of isoleucine or valine, n is 1, A is O, S, SO, SO 2 , and R is arylalkyl of the formula ##SPC2## wherein m is 1 or 2, w is hydrogen, halo, loweralkyl having 1-7 carbon atoms, or loweralkoxy having 1-7 carbon atoms, and the amino acid residues having L or DL stereochemical configuration.
Claim 3
Dependent Claim 63 words
As in claim 1, a compound of the formula ##EQU25## wherein X represents a sarcosine or aspartic acid residue, Y represents the residue of isoleucine or valine, A represents O, S, SO, or SO 2 , w is hydrogen, halo, loweralkyl having 1-7 carbon atoms or loweralkoxy having 1-7 carbon atoms and the amino acid residues having the L or DL stereochemical configuration.
Claim 4
Dependent Claim 35 words
As in claim 1, a compound of the formula ##EQU26## wherein A represents O, S, SO, or SO 2 and w represents hydrogen, halo, loweralkyl having 1-7 carbon atoms or loweralkoxy having 1-7 carbon atoms.
Claim 5
Dependent Claim 15 words
The compound according to claim 1 wherein A represents S, w represents hydrogen or halo.
Claim 6
Dependent Claim 24 words
The compound according to claim 1 wherein R is loweralkyl having 1-7 carbon atoms and the amino acids having L or DL stereochemical configuration.
Claim 7
Dependent Claim 15 words
A compound according to claim 1, wherein the amino acids have the L stereochemical configuration.
Claim 8
Dependent Claim 13 words
A compound according to claim 1, wherein X represents an aspartic acid residue.
Claim 9
Dependent Claim 12 words
A compound according to claim 1, wherein X represents a sarcosine residue.
Claim 10
Dependent Claim 12 words
A compound according to claim 1, wherein Y represents an isoleucine residue.
Claim 11
Dependent Claim 12 words
A compound according to claim 1, wherein Y represents a valine residue.
Claim 12
Dependent Claim 9 words
The compound according to claim 1 which is L-aspartyl-L-arginyl-L-valyl-L-tyrosyl-L-isoleucyl-L-histidyl-L-prolyl-S-benzyl-L-cysteine.
Claim 13
Dependent Claim 9 words
The compound according to claim 1 which is sarcosyl-L-arginyl-L-valyl-L-tyrosyl-L-isoleucyl-L-histidyl-L-prolyl-S-benzyl-L-cysteine.
Claim 14
Dependent Claim 9 words
The compound according to claim 1 which is L-aspartyl-L-arginyl-L-valyl-L-tyrosyl-L-isoleucyl-L-histidyl-L-prolyl-S-(p-chlorobenzyl)-L-cysteine.
Claim 15
Dependent Claim 9 words
The compound according to claim 1 which is L-aspartyl-L-arginyl-L-valyl-L-tyrosyl-L-isoleucyl-L-histidyl-L-prolyl-L-O-(2-phenethyl)-serine.

References Cited (Backward Citations)

US3886134A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1979-08-17 1980-02-16 1980-08-17 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1983-08-17 1984-02-16 1984-08-17 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1987-08-17 1988-02-16 1988-08-17 $7700.00 Window Closed / Lapsed

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