US4028319A
Expired / Lapsed
US
⏱️ 0.0 years remaining
2 and 3-substituted enkephalins
Assignee: GD Searle LLC
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Filing: 1976-05-07
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Granted: 1977-06-07
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Expires: 1996-05-07
Abstract
Abstract Analogs of enkephalin having agonist activity at opiate receptors are disclosed herein. These analogs are useful as analgesics, non-addicting narcotic antagonists and anti-diarrheal agents.
Inventors
- 👤 David A. Jones, Jr.
- 👤 James M. Schlatter
- 👤 Richard A. Mikulec
- 👤 Judith A. Reuter
- 👤 Robert H. Mazur
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 05:02
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06017; C07K5/06026; A; A61; A61P; A61P1/00; A61P1/12; A61P25/00; A61P25/04; A61P25/30; C07K14/00; C07K14/435; C07K14/665; C07K14/70; C07K14/702; A61K; A61K38/00
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
46 words
A compound of the formula H--Tyr--W--Phe--Y--OH (I) wherein Y is Leu or Met; W is selected from the group consisting of --Aib--Gly--, --Ala--Gly--, --Sar--Gly--, --Gly--Aib--, --Gly--Ala--, --Gly--Sar--, ##STR9## and the stereochemical configuration of each of the optically active amino acid residues is D, L or DL.
Claim 2
Dependent Claim
46 words
A compound of the formula H--Tyr--W--Phe--Y--OH (I) wherein Y is Leu or Met; W is selected from the group consisting of --Aib--Gly--, --Ala--Gly--, --Sar--Gly--, --Gly--Aib--, --Gly--Ala--, --Gly--Sar--, ##STR9## and the stereochemical configuration of each of the optically active amino acid residues is D, L or DL.
Claim 3
Dependent Claim
47 words
A compound according to claim 1 of the formula H--Tyr--W--Phe--Y--OH (II) wherein Y is Leu or Met; W is selected from the group consisting of --Aib--Gly--, --Ala--Gly--, --Sar--Gly--, --Gly--Aib--, --Gly--Ala--, --Gly--Sar--, ##STR10## and the stereochemical configuration of each of the optically active amino acid residues is L.
Claim 4
Dependent Claim
37 words
A compound according to claim 1 of the formula H--Tyr--Z--Gly--Phe--Y--OH wherein Z is Aib, Ala or Sar; Y is Leu or Met; and the stereochemical configuration of each of the optically active amino acid residues is L.
Claim 5
Dependent Claim
37 words
A compound according to claim 1 of the formula H--Tyr--Gly--Z--Phe--Y--OH wherein Z is Aib, Ala or Sar; Y is Leu or Met; and the stereochemical configuration of each of the optically active amino acid residues is L.
Claim 6
Dependent Claim
34 words
A compound according to claim 1 of the formula H--Tyr--W--Phe--Y--OH wherein Y is Leu or Met; W is ##STR11## and the stereochemical configuration of each of the optically active amino acid residues is L.
Claim 7
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosyl-L-alanylglycyl-L-phenylalanyl-L-methionine.
Claim 8
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosyl-L-alanylglycyl-L-phenylalanyl-L-leucine.
Claim 9
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosylsarcosylglycyl-L-phenylalanyl-L-methionine.
Claim 10
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosylsarcosylglycyl-L-phenylalanyl-L-leucine.
Claim 11
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosylglycyl-L-alanyl-L-phenylalanyl-L-methionine.
Claim 12
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosylglycyl-L-alanyl-L-phenylalanyl-L-leucine.
Claim 13
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosylglycylsarcosyl-L-phenylalanyl-L-methionine.
Claim 14
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosylglycylsarcosyl-L-phenylalanyl-L-leucine.
Claim 15
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosyl-5-aminopentanoyl-L-phenylalanyl-L-methionine.
Claim 16
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosyl-5-aminopentanoyl-L-phenylalanyl-L-leucine.
Claim 17
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosyl-p-aminobenzoyl-L-phenylalanyl-L-methionine.
Claim 18
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosyl-p-aminobenzoyl-L-phenylalanyl-L-leucine.
Claim 19
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosyl-α-aminoisobutyrylglycyl-L-phenylalanyl-L-methionine.
Claim 20
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosyl-α-aminoisobutyrylglycyl-L-phenylalanyl-L-leucine.
Claim 21
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosylglycyl-α-aminoisobutyryl-L-phenylalanyl-L-methionine.
Claim 22
Dependent Claim
9 words
The compound according to claim 1 which is L-tyrosylglycyl-α-aminoisobutyryl-L-phenylalanyl-L-leucine.
Claim 23
Dependent Claim
9 words
The compound according to claim 1 which is D-tyrosylglycyl-D-alanyl-D-phenylalanyl-D-leucine.
Claim 24
Dependent Claim
9 words
The compound according to claim 1 which is DL-tyrosylglycyl-DL-alanyl-DL-phenylalanyl-DL-leucine.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-06-06 | 1980-12-06 | 1981-06-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-06-06 | 1984-12-06 | 1985-06-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-06-06 | 1988-12-06 | 1989-06-07 | $7700.00 | Window Closed / Lapsed |