Patent US4198398A successfully refreshed from Google Patents.
US4198398A
Expired / Lapsed
US
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Enkephalin analogues
Assignee: Individual
•
Filing: 1978-07-10
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Granted: 1980-04-15
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Expires: 1998-07-10
Abstract
Abstract Compounds corresponding in structure to enkephalin or polypeptide analogues thereof, wherein one or more peptide links of the enkephalin or analogue is represented by a group or groups the same or different selected from dimethylene, methylene-imino and keto-methylene groups.
Inventors
- 👤 Derek Hudson
- 👤 Robert Sharpe
- 👤 Michael Szelke
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 18:33
CPC Classifications
C; C07; C07C; C07C271/00; C07C271/06; C07C271/08; C07C271/10; C07C271/22; C07K; C07K14/00; C07K14/435; C07K14/665; C07K14/70; C07K14/702; C07K5/00; C07K5/02; C07K5/0207; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 35
Claim 1
Independent Claim
110 words
Compounds having the general formula R--Tyr--X--Gly--B--Y--Z where (a) --X is a Gly or any D-amino acid residue --B is a Phe or N-methyl Phe residue --Y is Leu, Met (as such or in the form of its sulphoxide), Pro, or Hypro, or formal derivatives thereof in which the carbonyl oxygen of the terminal carboxyl group is replaced by hydrogen atoms --Z is NHR or OR (b) The peptide link between one or more of the residues is represented by a group or groups the same or different selected from dimethylene, methylene-imino and ketomethylene groups. (c) R is hydrogen or methyl, ethyl, propyl, cyclopropyl, butyl, allyl or other protective aliphatic group.
Claim 2
Dependent Claim
110 words
Compounds having the general formula R--Tyr--X--Gly--B--Y--Z where (a) --X is a Gly or any D-amino acid residue --B is a Phe or N-methyl Phe residue --Y is Leu, Met (as such or in the form of its sulphoxide), Pro, or Hypro, or formal derivatives thereof in which the carbonyl oxygen of the terminal carboxyl group is replaced by hydrogen atoms --Z is NHR or OR (b) The peptide link between one or more of the residues is represented by a group or groups the same or different selected from dimethylene, methylene-imino and ketomethylene groups. (c) R is hydrogen or methyl, ethyl, propyl, cyclopropyl, butyl, allyl or other protective aliphatic group.
Claim 3
Dependent Claim
12 words
Compounds according to claim 1, wherein X is Gly, D-Ala or D-Met.
Claim 4
Dependent Claim
28 words
Compounds according to claim 1 or 2, wherein the Phe or N-methyl Phe residue representing B is substituted with a hydroxy group or halogen in the aromatic ring.
Claim 5
Dependent Claim
43 words
Compounds according to claim 1 or 2, wherein Y is Leu, Met (as such or in the form of its sulphoxide), Pro, or Hypro, or formal derivatives thereof in which the carbonyl oxygen of the terminal carboxyl group is replaced by hydrogen atoms.
Claim 6
Dependent Claim
36 words
Compounds according to claim 1, wherein one or more of the remaining peptide links and/or any methylene-imino group(s) present is in N-substituted form carrying a methyl, ethyl, propyl, cyclopropyl, butyl, allyl or other protective aliphatic group.
Claim 7
Dependent Claim
19 words
The compound NH 2 --CH(CH 2 C 6 H 4 OH)--CH 2 --CH 2 --CH 2 --CO--Gly--Phe--Met--NH 2 .
Claim 8
Dependent Claim
19 words
The compound NH 2 --CH(CH 2 C 6 H 4 OH)--CH 2 --CH 2 --CH 2 --CO--Gly--Phe--Met--NH 2 .
Claim 9
Dependent Claim
14 words
The compound H-Tyr--NH--CH 2 --CH 2 --CH 2 --CH 2 --CO--Phe--Met-- NH 2 .
Claim 10
Dependent Claim
14 words
The compound H-Tyr--NH--CH 2 --CH 2 --CH 2 --CH 2 --CO--Phe--Met-- NH 2 .
Claim 11
Dependent Claim
17 words
The compound NH 2 --CH(CH 2 C 6 H 4 OH)--CH 2 --NH--CH 2 --CO--Gly--Phe--Met--NH 2 .
Claim 12
Dependent Claim
17 words
The compound NH 2 --CH(CH 2 C 6 H 4 OH)--CH 2 --NH--CH 2 --CO--Gly--Phe--Met--NH 2 .
Claim 13
Dependent Claim
15 words
The compound NH 2 --CH(CH 2 C 6 H 4 OH)--CH 2 --NH--CH 2 --CO--Gly--Phe--Metol.
Claim 14
Dependent Claim
15 words
The compound NH 2 --CH(CH 2 C 6 H 4 OH)--CH 2 --NH--CH 2 --CO--Gly--Phe--Metol.
Claim 15
Dependent Claim
9 words
The compound H-Tyr--NH--CH 2 --CO--CH 2 --CH 2 CO--Phe--Met--OH.
Claim 16
Dependent Claim
9 words
The compound H-Tyr--NH--CH 2 --CO--CH 2 --CH 2 CO--Phe--Met--OH.
Claim 17
Dependent Claim
9 words
The compound H-Tyr--NH--CH 2 --CH 2 --NH--CH 2 --CO--Phe--Met--OH.
Claim 18
Dependent Claim
9 words
The compound H-Tyr--NH--CH 2 --CH 2 --NH--CH 2 --CO--Phe--Met--OH.
Claim 19
Dependent Claim
9 words
The compound H--Tyr--NH--CH 2 --CH 2 --NH--CH 2 --CO--Phe--Metol.
Claim 20
Dependent Claim
9 words
The compound H--Tyr--NH--CH 2 --CH 2 --NH--CH 2 --CO--Phe--Metol.
Claim 21
Dependent Claim
11 words
The Compound H--Tyr--NH-CH 2 --CH 2 --NH--CH 2 --CO--Phe--Met--NH 2 .
Claim 22
Dependent Claim
11 words
The Compound H--Tyr--NH-CH 2 --CH 2 --NH--CH 2 --CO--Phe--Met--NH 2 .
Claim 23
Dependent Claim
27 words
A pharmaceutical composition comprising as the active ingredient compounds of claim 1 or pharmaceutically acceptable N-protected or salt forms thereof in a pharmaceutically acceptable diluent or carrier.
Claim 24
Dependent Claim
21 words
A pharmaceutical composition according to claim 14 wherein the active ingredient is a compound wherein X is gly D-ala or D-met.
Claim 25
Dependent Claim
36 words
A pharmaceutically active composition according to claim 14 wherein the active ingredients is a compound wherein the Phe or N-methyl Phe residue representing B is substituted with a hydroxy group or halogen in the aromatic ring.
Claim 26
Dependent Claim
50 words
A pharmaceutical composition according to claim 14 wherein the active ingredient is a compound wherein Y is Leu, Met (as such or in the form of its sulphoxide), Pro, or Hypro, or formal derivatives thereof in which the carbonyl oxygen of the terminal carboxyl group is replaced by hydrogen atoms.
Claim 27
Dependent Claim
45 words
A pharmaceutical composition according to claim 14 wherein the active ingredient is a compound wherein one or more of the remaining peptide links and/or any methylene-imino group(s) present is in N-substituted form carrying a methyl, ethyl, propyl, cyclopropyl, butyl, allyl or other protective aliphatic group.
Claim 28
Dependent Claim
29 words
A pharmaceutical composition according to claim 14 wherein the active ingredient is NH 2 --CH(CH 2 C 6 H 4 OH)--CH 2 --CH 2 --CH 2 --CO--Gly--Phe--Met--NH 2 .
Claim 29
Dependent Claim
21 words
A pharmaceutical composition according to claim 14 wherein the active ingredient is H-Tyr--NH--CH 2 --CH 2 --CH 2 --CO--Phe--Met--NH 2 .
Claim 30
Dependent Claim
27 words
A pharmaceutical composition according to claim 14 wherein the active ingredient is NH 2 --CH(CH 2 C 6 H 4 OH)--CH 2 --NH--CH 2 --CO--Gly--Phe--Met--NH 2 .
Claim 31
Dependent Claim
25 words
A pharmaceutical composition according to claim 14 wherein the active ingredient is NH 2 --CH(CH 2 C 6 H 4 OH)--CH 2 --NH--CH 2 CO--Gly--Phe--Metol.
Claim 32
Dependent Claim
19 words
A pharmaceutical composition according to claim 14 wherein the active ingredient is H--Try--NH--CH 2 --CO--CH 2 --CH 2 --CO--Phe--Met--OH.
Claim 33
Dependent Claim
19 words
A pharmaceutical composition according to claim 14 wherein the active ingredient is H-Tyr--NH--CH 2 --CO--CH 2 --CH 2 --CO--Phe--Met--OH.
Claim 34
Dependent Claim
19 words
A pharmaceutical composition according to claim 14 wherein the active ingredient is H-Tyr--NH--CH 2 --CH 2 --NH--CH 2 --CO--Phe--Metol.
Claim 35
Dependent Claim
21 words
A pharmaceutical composition according to claim 14 wherein the active ingredient is H--Tyr--NH--CH 2 --CH 2 --NH--CH 2 --CO--Phe--Met--NH 2 .
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) | 1983-04-15 | 1983-10-15 | 1984-04-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-04-15 | 1987-10-15 | 1988-04-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-04-15 | 1991-10-15 | 1992-04-15 | $7700.00 | Window Closed / Lapsed |