US4172130A
Expired / Lapsed
US
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α-AMINOACYL CONTAINING NEW PEPTIDES WITH GASTRIN EFFECTS AND A PROCESS FOR THE PREPARATION THEREOF
Assignee: Richter Gedeon Vegyeszeti Gyar Nyrt
•
Filing: 1977-12-29
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Granted: 1979-10-23
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Expires: 1997-12-29
Abstract
Abstract Peptides of the formula:
Inventors
- 👤 Lajos Kisfaludy
- 👤 Istvan Schon
- 👤 Vince Varro
- 👤 Laszlo Varga
- 👤 Jozsef Nafradi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 03:14
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/30; C07D207/34; C07D207/36; C07D207/40; C07D207/404; A; A61; A61P; A61P1/00; C07C; C07C291/00; C07C291/02; C07C291/04; C07C53/00; C07C53/15; C07K; C07K5/00; C07K5/04; C07K5/10; C07K5/1024; A61K; A61K38/00
Claims Analysis
Total Claims: 34
Claim 1
Independent Claim
49 words
A peptide of the formula: A--Trp--B--Asp--Phe--NH--Y wherein A is tert.-butoxycarbonyl-aminooxy-acyl , benzyloxycarbonyl-aminooxy-acyl, (aminooxy)-acyl or E-aminooxy-acyl, wherein E is benzoyl or straight-chain or branched C 1-5 aliphatic acyl, B is methionyl, leucyl, norleucyl, norvalyl or 2-amino-decanoyl, and Y is hydrogen or carboxymethoxy, a pharmaceutically acceptable acid-addition salt or complex thereof.
Claim 2
Dependent Claim
49 words
A peptide of the formula: A--Trp--B--Asp--Phe--NH--Y wherein A is tert.-butoxycarbonyl-aminooxy-acyl , benzyloxycarbonyl-aminooxy-acyl, (aminooxy)-acyl or E-aminooxy-acyl, wherein E is benzoyl or straight-chain or branched C 1-5 aliphatic acyl, B is methionyl, leucyl, norleucyl, norvalyl or 2-amino-decanoyl, and Y is hydrogen or carboxymethoxy, a pharmaceutically acceptable acid-addition salt or complex thereof.
Claim 3
Dependent Claim
1 words
(tert.-Butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanine-amide.
Claim 4
Dependent Claim
1 words
(tert.-Butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanine-amide.
Claim 5
Dependent Claim
1 words
(Aminooxy)-acetyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanine-amide.
Claim 6
Dependent Claim
1 words
(Aminooxy)-acetyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanine-amide.
Claim 7
Dependent Claim
1 words
2-(tert.-Butoxycarbonyl-aminooxy)-L-propionyl-L-tryptophyl-L-methyionyl-L-aspartyl-L-phenylalanine-amide.
Claim 8
Dependent Claim
1 words
2-(tert.-Butoxycarbonyl-aminooxy)-L-propionyl-L-tryptophyl-L-methyionyl-L-aspartyl-L-phenylalanine-amide.
Claim 9
Dependent Claim
1 words
2-(tert.-Butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-L-leucyl-L-aspartyl-L-phenylalanine-amide.
Claim 10
Dependent Claim
1 words
2-(tert.-Butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-L-leucyl-L-aspartyl-L-phenylalanine-amide.
Claim 11
Dependent Claim
1 words
2-D-(tert.-Butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-leucyl-L-aspartyl-L-phenylalanine-amide.
Claim 12
Dependent Claim
1 words
2-D-(tert.-Butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-leucyl-L-aspartyl-L-phenylalanine-amide.
Claim 13
Dependent Claim
2 words
2-[3-(tert.-Butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid.
Claim 14
Dependent Claim
2 words
2-[3-(tert.-Butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid.
Claim 15
Dependent Claim
1 words
2-D-(tert.-Butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-norleucyl-L-aspartyl-L-phenylalanine-amide.
Claim 16
Dependent Claim
1 words
2-D-(tert.-Butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-norleucyl-L-aspartyl-L-phenylalanine-amide.
Claim 17
Dependent Claim
1 words
2-(D-tert.Butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-norvalyl-L-aspartyl-L-phenylalanine-amide.
Claim 18
Dependent Claim
1 words
2-(D-tert.Butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-norvalyl-L-aspartyl-L-phenylalanine-amide.
Claim 19
Dependent Claim
1 words
tert.-Butoxycarbonyl-aminooxy-acetyl-L-tryptophyl-2-L-amino-decanoyl-L-aspartyl-L-phenylalanine-amide.
Claim 20
Dependent Claim
1 words
tert.-Butoxycarbonyl-aminooxy-acetyl-L-tryptophyl-2-L-amino-decanoyl-L-aspartyl-L-phenylalanine-amide.
Claim 21
Dependent Claim
1 words
tert.-Butoxycarbonyl-aminooxy-acetyl-L-tryptophyl-2-D-amino-decanoyl-L-aspartyl-L-phenylalanine-amide.
Claim 22
Dependent Claim
1 words
tert.-Butoxycarbonyl-aminooxy-acetyl-L-tryptophyl-2-D-amino-decanoyl-L-aspartyl-L-phenylalanine-amide.
Claim 23
Dependent Claim
3 words
2- [2-tert.-Butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid.
Claim 24
Dependent Claim
3 words
2- [2-tert.-Butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid.
Claim 25
Dependent Claim
2 words
2-[2-D-(tert.-Butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid.
Claim 26
Dependent Claim
2 words
2-[2-D-(tert.-Butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid.
Claim 27
Dependent Claim
2 words
2-[2-L-(tert.-Butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid.
Claim 28
Dependent Claim
2 words
2-[2-L-(tert.-Butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid.
Claim 29
Dependent Claim
23 words
A method for increasing gastric acid secretions which comprises the step of administering an effective amount of a compound according to claim 1.
Claim 30
Dependent Claim
12 words
The method according to claim 15 wherein the compound is enterally administered.
Claim 31
Dependent Claim
23 words
A composition for increasing gastric acid secretion consists essentially of at least one compound according to claim 1 in a pharmaceutically acceptable vehicle.
Claim 32
Dependent Claim
16 words
A composition according to claim 17 wherein said vehicle is selected from enterally administerable compatible vehicles.
Claim 33
Dependent Claim
33 words
A compound selected from the group consisting of: (tert.-butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanine-amide; (aminooxy)-acetyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanine-amide 2-(tert.-butoxycarbonyl-aminooxy)-L-propionyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanine-amide; 2-(tert.-butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-L-leucyl-L-aspartyl-L-phenylalanine-amide; 2-D-(tert.-butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-leucyl-L-aspartyl-L-phenylalanine-amide; 2-[3-(tert.-butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid; 2-D-(tert.-butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-norleucy-L-aspartyl-L-phenylalanine-amide; 2-D-(tert.-butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-norvalyl-L-aspartyl-L-phenylalanine-amide; (tert.-butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-2-L-amino-decanoyl-L-aspartyl-L-phenylalanine-amide; (tert.butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-2-D-amino-decanoyl-L-aspartyl-L-phenylalanine-amide; 2-[2-(tert.-butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid; 2-[2-D-(tert.-butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid; and 2-[2-L-(tert.butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid and the acid-addition salts and complexes thereof.
Claim 34
Dependent Claim
33 words
A compound selected from the group consisting of: (tert.-butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanine-amide; (aminooxy)-acetyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanine-amide 2-(tert.-butoxycarbonyl-aminooxy)-L-propionyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanine-amide; 2-(tert.-butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-L-leucyl-L-aspartyl-L-phenylalanine-amide; 2-D-(tert.-butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-leucyl-L-aspartyl-L-phenylalanine-amide; 2-[3-(tert.-butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid; 2-D-(tert.-butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-norleucy-L-aspartyl-L-phenylalanine-amide; 2-D-(tert.-butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-norvalyl-L-aspartyl-L-phenylalanine-amide; (tert.-butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-2-L-amino-decanoyl-L-aspartyl-L-phenylalanine-amide; (tert.butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-2-D-amino-decanoyl-L-aspartyl-L-phenylalanine-amide; 2-[2-(tert.-butoxycarbonyl-aminooxy)-acetyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid; 2-[2-D-(tert.-butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid; and 2-[2-L-(tert.butoxycarbonyl-aminooxy)-propionyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanyl-aminooxy]-acetic acid and the acid-addition salts and complexes thereof.
References Cited (Backward Citations)
US3896103A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-10-22 | 1983-04-23 | 1983-10-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-10-22 | 1987-04-23 | 1987-10-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-10-22 | 1991-04-23 | 1991-10-23 | $7700.00 | Window Closed / Lapsed |