US4215038A
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Peptides which inhibit gonadal function
Assignee: Salk Institute for Biological Studies
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Filing: 1978-10-16
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Granted: 1980-07-29
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Expires: 1998-10-16
Abstract
Abstract Peptides which inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. The peptides have the structure: R1-R2-R3-Ser-Tyr-R4-R5-Arg-R6 wherein R1 is selected from the group consisting of D-pGlu, D-Pro, D-Trp, D-His, D-Arg, D-Leu, Formyl D-Pro, Acetyl D-Pro, Benzoyl D-Pro and beta -Ala; R2 is selected from the group consisting of D-Phe, Phe, N alpha Me-Phe, His, D-His, D-Trp, Trp and N alpha Me-Leu; R3 is selected from the group consisting of D-Trp, Trp; D-Phe, Phe, Pro and D-His; R4 is selected from the group consisting of Gly, D-Trp, D-Phe and D-Tyr; R5 is selected from the group consisting of Leu and N alpha Me Leu; and R6 is selected from the group consisting of Pro-Gly-NH2 and Pro-NH-CH2-CH3.
Inventors
- 👤 Jean E. F. Rivier
- 👤 Catherine L. Rivier
- 👤 Wylie W. Vale, Jr.
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 00:49
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/04; C07K7/23; C07K7/16; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/13
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
121 words
A peptide which is effective to inhibit release of steroids by the gonadotropins of mammalians, said peptide having the formula: R.sub.1 -R.sub.2 -R.sub.3 -Ser-Tyr-R.sub.4 -R.sub.5 -Arg-R.sub.6 wherein R 1 is selected from the group consisting of D-pGlu, D-Pro, D-Trp, D-His, D-Arg, D-Leu, formyl D-Pro, acetyl D-Pro, benzoyl D-Pro and β-Ala, R 2 is selected from the group consisting of D-Phe, D-His and D-Trp; R 3 is selected from the group consisting of D-Trp, D-Phe, and D-His; R 4 is selected from the group consisting of D-Trp, D-Phe and D-Tyr; R 5 is selected from the group consisting of Leu and N a Me-Leu; and R 6 is selected from the group consisting of Pro--Gly--NH 2 and Pro--NH--CH 2 --CH 3 .
Claim 2
Dependent Claim
121 words
A peptide which is effective to inhibit release of steroids by the gonadotropins of mammalians, said peptide having the formula: R.sub.1 -R.sub.2 -R.sub.3 -Ser-Tyr-R.sub.4 -R.sub.5 -Arg-R.sub.6 wherein R 1 is selected from the group consisting of D-pGlu, D-Pro, D-Trp, D-His, D-Arg, D-Leu, formyl D-Pro, acetyl D-Pro, benzoyl D-Pro and β-Ala, R 2 is selected from the group consisting of D-Phe, D-His and D-Trp; R 3 is selected from the group consisting of D-Trp, D-Phe, and D-His; R 4 is selected from the group consisting of D-Trp, D-Phe and D-Tyr; R 5 is selected from the group consisting of Leu and N a Me-Leu; and R 6 is selected from the group consisting of Pro--Gly--NH 2 and Pro--NH--CH 2 --CH 3 .
Claim 3
Dependent Claim
35 words
A peptide in accordance with claim 1 wherein R 1 is D-pGlu, R 2 is D-Phe, R 3 is D-Trp, R 4 is D-Trp, R 5 is Leu and R 6 is Pro--Gly--NH 2 .
Claim 4
Dependent Claim
37 words
A peptide in accordance with claim 1 wherein R 1 is D-pGlu, R 2 is D-Phe, R 3 is D-Trp, R 4 is D-Trp, R 5 is N a Me-Leu and R 6 is Pro--Gly--NH 2 .
Claim 5
Dependent Claim
37 words
A peptide in accordance with claim 1 wherein R 1 is D-pGlu, R 2 is D-Phe, R 3 is D-Trp, R 4 is D-Trp, R 5 is Leu and R 6 is Pro--NH--CH 2 --CH 3 .
Claim 6
Dependent Claim
39 words
A peptide in accordance with claim 1 wherein R 1 is D-pGlu, R 2 is D-Phe, R 3 is D-Trp, R 4 is D-Trp, R 5 is N a Me-Leu and R 6 is Pro--NH--CH 2 --CH 3 .
Claim 7
Dependent Claim
35 words
A peptide in accordance with claim 1 wherein R 1 is D-Trp, R 2 is D-Phe, R 3 is D-Trp, R 4 is D-Trp, R 5 is Leu and R 6 is Pro--Gly--NH 2 .
Claim 8
Dependent Claim
35 words
A peptide in accordance with claim 1 wherein R 1 is D-Arg, R 2 is D-Phe, R 3 is D-Trp, R 4 is D-Trp, R 5 is Leu and R 6 is Pro--Gly--NH 2 .
Claim 9
Dependent Claim
35 words
A peptide in accordance with claim 1 wherein R 1 is D-Leu, R 2 is D-Phe, R 3 is D-Trp, R 4 is D-Trp, R 5 is Leu and R 6 is Pro--Gly--NH 2 .
Claim 10
Dependent Claim
35 words
A peptide in accordance with claim 1 wherein R 1 is D-His, R 2 is D-Phe, R 3 is D-Trp, R 4 is D-Trp, R 5 is Leu and R 6 is Pro--Gly--NH 2 .
Claim 11
Dependent Claim
35 words
A peptide in accordance with claim 1 wherein R 1 is D-Pro, R 2 is D-Phe, R 3 is D-Trp, R 4 is D-Trp, R 5 is Leu and R 6 is Pro--Gly--NH 2 .
Claim 12
Dependent Claim
35 words
A peptide in accordance with claim 1 wherein R 1 is D-pGlu, R 2 is D-Phe, R 3 is D-Phe, R 4 is D-Trp, R 5 is Leu and R 6 is Pro--Gly--NH 2 .
Claim 13
Dependent Claim
36 words
A peptide in accordance with claim 1 wherein R 1 is formyl D-Pro, R 2 is D-Phe, R 3 is D-Trp, R 4 is D-Trp, R 5 is Leu and R 6 is Pro--Gly--NH 2 .
Claim 14
Dependent Claim
36 words
A peptide in accordance with claim 1 wherein R 1 is acetyl D-Pro, R 2 is D-Phe, R 3 is D-Trp, R 4 is D-Trp, R 5 is Leu and R 6 is Pro--Gly--NH 2 .
Claim 15
Dependent Claim
36 words
A peptide in accordance with claim 1 wherein R 1 is benzoyl D-Pro, R 2 is D-Phe, R 3 is D-Trp, R 4 is D-Trp, R 5 is Leu and R 6 is Pro--Gly--NH 2 .
Claim 16
Dependent Claim
35 words
A peptide in accordance with claim 1 wherein R 1 is β-Ala, R 2 is D-Phe, R 3 is D-Trp, R 4 is D-Trp, R 5 is Leu and R 6 is Pro--Gly--NH 2 .
Claim 17
Dependent Claim
35 words
A peptide in accordance with claim 1 wherein R 1 is D-pGlu, R 2 is D-Trp, R 3 is D-Trp, R 4 is D-Trp, R 5 is Leu and R 6 is Pro--Gly--NH 2 .
References Cited (Backward Citations)
US4008209A
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US3928307A
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US4010125A
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-07-29 | 1984-01-28 | 1984-07-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-07-29 | 1988-01-28 | 1988-07-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-07-29 | 1992-01-28 | 1992-07-29 | $7700.00 | Window Closed / Lapsed |