US4425269A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Metabolically protected analogs of neurotensin
Assignee: Merck and Co Inc
•
Filing: 1982-06-07
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Granted: 1984-01-10
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Expires: 2002-06-07
Abstract
Abstract There are disclosed metabolically protected linear analogs of the carboxy terminal pentapeptide fragment of the tridecapeptide, neurotensin.
Inventors
- 👤 Marcia E. Christy
- 👤 Kenneth L. Shepard
- 👤 Robert G. Strachan
- 👤 Sandor L. Varga
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 03:25
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/04; C07K7/08; C07K7/083; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
68 words
A blocked pentapeptide derivative compound of neurotensin having the formula: α-A-B-Pro-Tyr-C-D-Y (I) wherein: A is another blocked amino acid selected from the group alkoxycarbonyl-4-aminobutyric acid; alkoxycarbonyl-β-alanine; and, alkoxycarbonyl; B is a basic amino acid residue selected from the group 2,4-diaminobutyric acid, lysine, arginine, ornithine, and homoarginine; C is a member of the group: isoleucine, norleucine, or valine; D is a member of the group: leucine or norleucine; and,
Claim 2
Dependent Claim
68 words
A blocked pentapeptide derivative compound of neurotensin having the formula: α-A-B-Pro-Tyr-C-D-Y (I) wherein: A is another blocked amino acid selected from the group alkoxycarbonyl-4-aminobutyric acid; alkoxycarbonyl-β-alanine; and, alkoxycarbonyl; B is a basic amino acid residue selected from the group 2,4-diaminobutyric acid, lysine, arginine, ornithine, and homoarginine; C is a member of the group: isoleucine, norleucine, or valine; D is a member of the group: leucine or norleucine; and,
Claim 3
Dependent Claim
17 words
Y is OH,OCH 3 ,OCH 2 ,C 6 H 5 , NH 2 ,NH(lower alkyl),NH(aralkyl) or NH(dimethylaminoethyl).
Claim 4
Dependent Claim
17 words
Y is OH,OCH 3 ,OCH 2 ,C 6 H 5 , NH 2 ,NH(lower alkyl),NH(aralkyl) or NH(dimethylaminoethyl).
Claim 5
Dependent Claim
17 words
A compound of claim 1 wherein said ester is a member of the group: loweralkyl and aralkyl.
Claim 6
Dependent Claim
15 words
A compound of claim 1 wherein said amide is an unsubstituted amide, aminoaralkyl, and dimethylaminoethyl.
Claim 7
Dependent Claim
42 words
A blocked pentapeptide derivative compound of neurotensin having the formula: α-A-B-Pro-Tyr-C-D-Y (I) wherein: A is t-butyloxycarbonyl; B is lysine or 2,4-diaminobutyric acid; C is isoleucine; D is leucine; and, Y is OH, OCH 3 or OCH 2 C 6 H 5 .
Claim 8
Dependent Claim
42 words
A blocked pentapeptide derivative compound of neurotensin having the formula: α-A-B-Pro-Tyr-C-D-Y (I) wherein: A is t-butyloxycarbonyl; B is lysine or 2,4-diaminobutyric acid; C is isoleucine; D is leucine; and, Y is OH, OCH 3 or OCH 2 C 6 H 5 .
Claim 9
Dependent Claim
33 words
A blocked pentapeptide derivative compound of neurotensin having the formula: α-A-B-Pro-Tyr-C-D-Y (I) wherein: A is t-butyloxycarbonyl; B is lysine; C is isoleucine; D is leucine; and, Y is OH or OCH 3 .
Claim 10
Dependent Claim
33 words
A blocked pentapeptide derivative compound of neurotensin having the formula: α-A-B-Pro-Tyr-C-D-Y (I) wherein: A is t-butyloxycarbonyl; B is lysine; C is isoleucine; D is leucine; and, Y is OH or OCH 3 .
Claim 11
Dependent Claim
29 words
A blocked pentapeptide derivative compound of neurotensin having the formula: α-A-B-Pro-Tyr-C-D-Y (I) wherein: A is t-butyloxycarbonyl; B is lysine; C is isoleucine; D is leucine; and, Y is OH.
Claim 12
Dependent Claim
29 words
A blocked pentapeptide derivative compound of neurotensin having the formula: α-A-B-Pro-Tyr-C-D-Y (I) wherein: A is t-butyloxycarbonyl; B is lysine; C is isoleucine; D is leucine; and, Y is OH.
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) | 1987-01-09 | 1987-07-11 | 1988-01-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-01-09 | 1991-07-11 | 1992-01-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-01-09 | 1995-07-11 | 1996-01-10 | $7700.00 | Window Closed / Lapsed |