US4130554A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Process for preparing somatostatin analog
Assignee: Merck and Co Inc
•
Filing: 1975-04-08
•
Granted: 1978-12-19
•
Expires: 1995-04-08
Abstract
Abstract Somatostatin analog, hereinafter designated des(Ala1-Gly2)desaminocys3-somatostatin, having the structure: <IMAGE> <IMAGE> is prepared by controlled stepwise procedures starting with individual amino acid components. This peptide has the property of lowering blood glucose, inhibiting gastric secretion and inhibiting growth hormone release in humans and animals.
Inventors
- 👤 Frederick W. Holly
- 👤 William J. Paleveda
- 👤 Robert G. Strachan
- 👤 Daniel F. Veber
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 13:28
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/655; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/16
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
6 words
The peptide having the structure: S-Acm-β-mercaptopropionyl-(ε-INOC)Lys-Asn-Phe-Phe-Trp-(.epsilon.-INOC)Lys-Thr-Phe-Thr-Ser-(Acm)Cys-OH.
Claim 2
Dependent Claim
6 words
The peptide having the structure: S-Acm-β-mercaptopropionyl-(ε-INOC)Lys-Asn-Phe-Phe-Trp-(.epsilon.-INOC)Lys-Thr-Phe-Thr-Ser-(Acm)Cys-OH.
Claim 3
Dependent Claim
6 words
The peptide having the structure: S-Acm-β-mercaptopropionyl-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-(Acm)Cys-OH.
Claim 4
Dependent Claim
6 words
The peptide having the structure: S-Acm-β-mercaptopropionyl-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-(Acm)Cys-OH.
Claim 5
Dependent Claim
23 words
The process of preparing the peptide having the structure β-mercaptopropionyl-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH which comprises treating the peptide having the amino acid sequence S-Acm-β-mercaptopropionyl-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-(Acm)Cys-OH with iodine.
Claim 6
Dependent Claim
23 words
The process of preparing the peptide having the structure β-mercaptopropionyl-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH which comprises treating the peptide having the amino acid sequence S-Acm-β-mercaptopropionyl-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-(Acm)Cys-OH with iodine.
Claim 7
Dependent Claim
37 words
The process of preparing the peptide having the structure β-mercaptopropionyl-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH which comprises treating the peptide having the amino acid sequence β-mercaptopropionyl-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH by stirring a solution containing said peptide in the presence of atmospheric oxygen and copper ion.
Claim 8
Dependent Claim
37 words
The process of preparing the peptide having the structure β-mercaptopropionyl-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH which comprises treating the peptide having the amino acid sequence β-mercaptopropionyl-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH by stirring a solution containing said peptide in the presence of atmospheric oxygen and copper ion.
Claim 9
Dependent Claim
48 words
The process of preparing the peptide of claim 1 wherein the process comprises forming the active ester of the peptide having the amino acid sequence S-Acm-β-mercaptopropionyl-(ε-INOC)Lys-Asn-Phe-Phe-OH and reacting said active ester with the amino group of the tryptophan residue of the peptide having the amino acid sequence Trp-(ε-INOC)Lys-Thr-Phe-Thr-Ser-(Acm)Cys.
Claim 10
Dependent Claim
46 words
The process of preparing the peptide of claim 1 wherein the process comprises forming the azide of the peptide having the amino acid sequence S-Acm-β-mercaptopropionyl-(ε-INOC)Lys-Asn-Phe-Phe-OMe and reacting said azide with the amino group of the tryptophan residue of the peptide having the amino acid sequence Trp-(ε-INOC)Lys-Thr-Phe-Thr-Ser-(Acm)Cys.
Claim 11
Dependent Claim
21 words
The process of preparing the peptide having the structure: S-Acm-β-mercaptopropionyl-(ε-INOC)Lys-Asn-Phe-Phe-OMe wherein the process comprises treating the peptide (ε-INOC)Lys-Asn-Phe-Phe-OMe with S-Acm-β-mercaptopropionyl NPE.
Claim 12
Dependent Claim
21 words
The process of preparing the peptide having the structure: S-Acm-β-mercaptopropionyl-(ε-INOC)Lys-Asn-Phe-Phe-OMe wherein the process comprises treating the peptide (ε-INOC)Lys-Asn-Phe-Phe-OMe with S-Acm-β-mercaptopropionyl NPE.
Claim 13
Dependent Claim
25 words
The process of preparing the peptide of claim 2 wherein the process comprises treating the peptide having the amino acid sequence Acm-β-mercaptopropionyl-(ε-INOC)Lys-Asn-Phe-Phe-Trp-(.epsilon.-INOC)Lys-Thr-Phe-Thr-Ser-(Acm)Cys-OH with zinc dust.
Claim 14
Dependent Claim
26 words
The process for preparing the peptide having the structure: β-mercaptopropionyl-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH wherein the process comprises treating the peptide having the amino acid structure: S-Acm-β-mercaptopropionyl-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-(Acm)Cys-OH with mercuric ion.
Claim 15
Dependent Claim
26 words
The process for preparing the peptide having the structure: β-mercaptopropionyl-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH wherein the process comprises treating the peptide having the amino acid structure: S-Acm-β-mercaptopropionyl-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-(Acm)Cys-OH with mercuric ion.
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) | 1981-12-18 | 1982-06-19 | 1982-12-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-12-18 | 1986-06-19 | 1986-12-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-12-18 | 1990-06-19 | 1990-12-19 | $7700.00 | Window Closed / Lapsed |