Patent US4162248A successfully refreshed from Google Patents.
US4162248A
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Somatostatin analogs
Assignee: Merck and Co Inc
•
Filing: 1978-04-07
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Granted: 1979-07-24
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Expires: 1998-04-07
Abstract
Abstract Somatostatin analogs having the structural formula:
Inventors
- 👤 Robert G. Strachan
- 👤 William J. Paleveda
- 👤 Daniel F. Veber
- 👤 Frederick W. Holly
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 15:53
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/655; C07K14/6555; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/16
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
81 words
Compounds of the formula: cyclo[(X).sub.j -(A).sub.k -(B).sub.1 -Phe-Phe-(D- or L-)Trp-Lys-Thr-Phe-Thr-(C).sub.m ] wherein X is ##STR24## and n= 0 to 4; A is Lys, ε-INOC-Lysine; B is Asn, Ala, α-aminobutyric acid; C is Ser, Gly; j, k, l and m are 0 or 1, with the proviso that j, k, l, and m are not all 1 and not all 0; wherein the ring formed by the peptide backbone contains 24 to 33 atoms and pharmaceutically acceptable non-toxic acid addition salts thereof.
Claim 2
Dependent Claim
81 words
Compounds of the formula: cyclo[(X).sub.j -(A).sub.k -(B).sub.1 -Phe-Phe-(D- or L-)Trp-Lys-Thr-Phe-Thr-(C).sub.m ] wherein X is ##STR24## and n= 0 to 4; A is Lys, ε-INOC-Lysine; B is Asn, Ala, α-aminobutyric acid; C is Ser, Gly; j, k, l and m are 0 or 1, with the proviso that j, k, l, and m are not all 1 and not all 0; wherein the ring formed by the peptide backbone contains 24 to 33 atoms and pharmaceutically acceptable non-toxic acid addition salts thereof.
Claim 3
Dependent Claim
53 words
The compound according to claim 1 wherein X is ##STR25## and n= 0 to 4; A is Lys; B is Asn or α-aminobutyric acid; C is Ser; j, k, l and m are 0 or 1, with the proviso that j, k, l, and m are not all 1 and not all 0.
Claim 4
Dependent Claim
10 words
The compound according to claim 2 wherein j is zero.
Claim 5
Dependent Claim
10 words
The compound according to claim 3 wherein k is zero.
Claim 6
Dependent Claim
10 words
The compound according to claim 4 wherein 1 is zero.
Claim 7
Dependent Claim
10 words
The compound according to claim 4 wherein m is zero.
Claim 8
Dependent Claim
10 words
The compound according to claim 3 having the formula: cyclo(Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser).
Claim 9
Dependent Claim
10 words
The compound according to claim 4 having the formula: cyclo(Asn-Phe-Phe-D-Trp-Lys-Thr-Phe-Thr-Ser).
Claim 10
Dependent Claim
10 words
The compound according to claim 5 having the formula: cyclo(Phe-Phe-D-Trp-Lys-Thr-Phe-Thr-Ser).
Claim 11
Dependent Claim
10 words
The compound according to claim 6 having the formula: cyclo(Asn-Phe-Phe-D-Trp-Lys-Thr-Phe-Thr).
Claim 12
Dependent Claim
81 words
A composition comprising a therapeutically effective amount of the peptides having the structure: cyclo[(X).sub.j -(A).sub.k -(B).sub.1 -Phe-Phe-(D-or L-)Trp-Lys-Phe-Thr-(C).sub.m ] wherein X is ##STR26## and n= 0 to 4; A is Lys, ε-INOC-Lysine; B is Asn, Ala, α-aminobutyric acid; C is Ser, Gly; j, k, l and m are 0 or 1, with the provisio that j, k, l and m are not all 1 and not all 0; and pharmaceutically acceptable non-toxic acid addition salts thereof and a pharmaceutically acceptable carrier.
Claim 13
Dependent Claim
81 words
A composition comprising a therapeutically effective amount of the peptides having the structure: cyclo[(X).sub.j -(A).sub.k -(B).sub.1 -Phe-Phe-(D-or L-)Trp-Lys-Phe-Thr-(C).sub.m ] wherein X is ##STR26## and n= 0 to 4; A is Lys, ε-INOC-Lysine; B is Asn, Ala, α-aminobutyric acid; C is Ser, Gly; j, k, l and m are 0 or 1, with the provisio that j, k, l and m are not all 1 and not all 0; and pharmaceutically acceptable non-toxic acid addition salts thereof and a pharmaceutically acceptable carrier.
Claim 14
Dependent Claim
79 words
A composition comprising a therapeutically effective amount of the peptides having the structure: cyclo[(X).sub.j -(A).sub.k -(B).sub.1 -Phe-Phe-(D- or L-)Trp-Lys-Thr-Phe-Thr-(C).sub.m ] wherein X is ##STR27## and n=0 to 4; A is Lys; B is Asn or α-aminobutyric acid; C is Ser; j, k, l and m are 0 or 1, with the proviso that j, k, l and m are not all 1 and not all 0; and pharmaceutically acceptable non-toxic acid addition salts thereof and a pharmaceutically acceptable carrier.
Claim 15
Dependent Claim
79 words
A composition comprising a therapeutically effective amount of the peptides having the structure: cyclo[(X).sub.j -(A).sub.k -(B).sub.1 -Phe-Phe-(D- or L-)Trp-Lys-Thr-Phe-Thr-(C).sub.m ] wherein X is ##STR27## and n=0 to 4; A is Lys; B is Asn or α-aminobutyric acid; C is Ser; j, k, l and m are 0 or 1, with the proviso that j, k, l and m are not all 1 and not all 0; and pharmaceutically acceptable non-toxic acid addition salts thereof and a pharmaceutically acceptable carrier.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-07-23 | 1983-01-22 | 1983-07-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-07-23 | 1987-01-22 | 1987-07-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-07-23 | 1991-01-22 | 1991-07-24 | $7700.00 | Window Closed / Lapsed |