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US4178284A Expired / Lapsed US ⏱️ 0.0 years remaining

Octapeptides

Assignee: Wyeth LLC
•
Filing: 1978-12-11
•
Granted: 1979-12-11
•
Expires: 1998-12-11
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Abstract

Abstract Octapeptide derivatives of Met- and Leu-enkephalin C-terminally modified by addition of L-Lys-Gly-L-Glu-OH or L-Lys-Gly-L-Gln-OH release endogenous growth hormone without analgesia or side effects elicited by the enkephalins or morphine.

Inventors

  • 👤 Dimitrios Sarantakis

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-30 04:07
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/665; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/28

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 38 words
A compound of the formula H-Tyr-X.sub.1 -Gly-Phe-X.sub.2 -Lys-Gly-X.sub.3 -OH in which X 1 is Gly or D-Ala X 2 is Met, Leu, D-Met or D-Leu, and X 3 is Glu or Gln or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim 38 words
A compound of the formula H-Tyr-X.sub.1 -Gly-Phe-X.sub.2 -Lys-Gly-X.sub.3 -OH in which X 1 is Gly or D-Ala X 2 is Met, Leu, D-Met or D-Leu, and X 3 is Glu or Gln or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim 14 words
The compound of claim 1 which is H-Tyr-Gly-Gly-Phe-Met-Lys-Gly-Gln-OH or a pharmaceutically acceptable salt thereof.
Claim 4
Dependent Claim 14 words
The compound of claim 1 which is H-Tyr-D-Ala-Gly-Phe-Met-Lys-Gly-Gln-OH or a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim 14 words
The compound of claim 1 which is H-Tyr-D-Ala-Gly-Phe-Met-Lys-Gly-Glu-OH or a pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim 14 words
The compound of claim 1 which is H-Tyr-Gly-Gly-Phe-Leu-Lys-Gly-Gln-OH or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim 14 words
The compound of claim 1 which is H-Tyr-D-Ala-Gly-Phe-Leu-Lys-Gly-Glu-OH or a pharmaceutically acceptable salt thereof.
Claim 8
Dependent Claim 14 words
The compound of claim 1 which is H-Tyr-D-Ala-Gly-Phe-D-Met-Lys-Gly-Glu-OH or a pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim 14 words
The compound of claim 1 which is H-Tyr-D-Ala-Gly-Phe-D-Leu-Lys-Gly-Gln-OH or a pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim 66 words
A compound of the formula R-Tyr(R.sup.1)-X.sub.1 -Gly-Phe-X.sub.2 -Lys(R.sup.2)-Gly-Glu(α-R.sup.3)-Z in which R is an α-amino protecting group; R 1 is a hydroxy protecting group; R 2 is an amino protecting group; R 3 is a carboxy protecting group; X 1 is Gly or D-Ala; X 2 is Met, Leu, D-Met or D-Leu; and Z is a benzhydrylamine modified, a hydroxymethyl or a chloromethyl modified polystyrene resin support.
Claim 11
Dependent Claim 66 words
A compound of the formula R-Tyr(R.sup.1)-X.sub.1 -Gly-Phe-X.sub.2 -Lys(R.sup.2)-Gly-Glu(α-R.sup.3)-Z in which R is an α-amino protecting group; R 1 is a hydroxy protecting group; R 2 is an amino protecting group; R 3 is a carboxy protecting group; X 1 is Gly or D-Ala; X 2 is Met, Leu, D-Met or D-Leu; and Z is a benzhydrylamine modified, a hydroxymethyl or a chloromethyl modified polystyrene resin support.
Claim 12
Dependent Claim 29 words
A compound of claim 9 in which R is tert-butyloxycarbonyl, R 1 is 2,6-dichlorobenzyl, R 2 is 2-chlorobenzyloxycarbonyl, R 3 is benzyl and Z is a benzhydrylamine polystyrene resin.

References Cited (Backward Citations)

US4127533A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1982-12-10 1983-06-11 1983-12-11 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1986-12-10 1987-06-11 1987-12-11 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1990-12-10 1991-06-11 1991-12-11 $7700.00 Window Closed / Lapsed

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