Patent US4128638A successfully refreshed from Google Patents.
US4128638A
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Nona- and deca-peptide amide derivatives demonstrating high ovulation inducing activity
Assignee: Orica Ltd
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Filing: 1976-04-05
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Granted: 1978-12-05
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Expires: 1996-04-05
Abstract
Abstract A peptide amide derivative of general formula (I) wherein when X is Gly, Y is Leu and Z is β-Ala-NH 2 or Sar-NH 2 ; when X is D-Ala, Y is Leu, Ile, Nle, Val, Nval, or Met and Z is Gly-NH 2 , β-Ala-NH 2 or Sar-NH 2 , provided that when X is D-Ala and Y is Leu Z is not Gly-NH 2 ; and when X is β-Ala, Y is Leu, Ile, Nle, Val, Nval or Met and Z is Gly-NH 2 , β-Ala-NH 2 , Sar-NH 2 or -NRR' wherein R and R', which may be the same or different, are H, lower alkyl containing from 1 to 6 carbon atoms, substituted lower alkyl containing from 1 to 6 carbon atoms, or together may form a ring; or a pharmaceutically acceptable acid-addition salt or metal-ion complex thereof; and an inert carrier therefor. pGlu-His-Trp-Ser-Tyr-X-Y-Arg-Pro-Z (I)
Inventors
- 👤 Keith Moody
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 19:20
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/04; C07K7/23; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/13
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
23 words
A peptide amide derivative selected from the group consisting of: L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-prolyl-glycinamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-glycyl-L-leucyl-L-arginyl-L-prolyl-62 -alaninamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-glycyl-L-leucyl-L-arginyl-L-prolyl-sarcosinamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-methylamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-ethylamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-n-propylamide; and L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline pyrrolidide.
Claim 2
Dependent Claim
23 words
A peptide amide derivative selected from the group consisting of: L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-prolyl-glycinamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-glycyl-L-leucyl-L-arginyl-L-prolyl-62 -alaninamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-glycyl-L-leucyl-L-arginyl-L-prolyl-sarcosinamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-methylamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-ethylamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-n-propylamide; and L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline pyrrolidide.
Claim 3
Dependent Claim
7 words
The peptide amide L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-prolyl-glycinamide. (β-Ala 6 -LHRH).
Claim 4
Dependent Claim
7 words
The peptide amide L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-prolyl-glycinamide. (β-Ala 6 -LHRH).
Claim 5
Dependent Claim
7 words
The peptide amide L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-glycyl-L-leucyl-L-arginyl-L-prolyl-β-alaninamide. (β-Ala 10 -LHRH).
Claim 6
Dependent Claim
7 words
The peptide amide L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-glycyl-L-leucyl-L-arginyl-L-prolyl-β-alaninamide. (β-Ala 10 -LHRH).
Claim 7
Dependent Claim
7 words
The peptide amide L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-glycyl-L-leucyl-L-arginyl-L-prolyl-sarcosinamide. (Sar 10 -LHRH).
Claim 8
Dependent Claim
7 words
The peptide amide L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-glycyl-L-leucyl-L-arginyl-L-prolyl-sarcosinamide. (Sar 10 -LHRH).
Claim 9
Dependent Claim
11 words
The peptide amide L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-methylamide. (β-Ala 6 -des-Gly 10 -LHRH methylamide).
Claim 10
Dependent Claim
11 words
The peptide amide L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-methylamide. (β-Ala 6 -des-Gly 10 -LHRH methylamide).
Claim 11
Dependent Claim
11 words
The peptide amide L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-ethylamide. (β-Ala 6 -des-Gly 10 -LHRH ethylamide).
Claim 12
Dependent Claim
11 words
The peptide amide L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-ethylamide. (β-Ala 6 -des-Gly 10 -LHRH ethylamide).
Claim 13
Dependent Claim
11 words
The peptide amide L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-n-propylamide. (β-Ala 6 -des-Gly 10 -LHRH n-propylamide).
Claim 14
Dependent Claim
11 words
The peptide amide L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-n-propylamide. (β-Ala 6 -des-Gly 10 -LHRH n-propylamide).
Claim 15
Dependent Claim
10 words
The peptide amide L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline pyrrolidide. (β-Ala 6 -des-Gly 10 -LHRH-pyrrolidide).
Claim 16
Dependent Claim
10 words
The peptide amide L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline pyrrolidide. (β-Ala 6 -des-Gly 10 -LHRH-pyrrolidide).
Claim 17
Dependent Claim
44 words
A composition of matter for the treatment of mammals to induce ovulation comprising an effective amount of a peptide amide derivative selected from the group consisting of: L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-prolyl-glycinamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-glycyl-L-leucyl-L-arginyl-L-prolyl-β-alaninamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-glycyl-L-leucyl-L-arginyl-L-prolyl-sarcosinamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-methylamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-ethylamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-n-propylamide; and L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline pyrrolidide and an inert carrier therefor.
Claim 18
Dependent Claim
44 words
A composition of matter for the treatment of mammals to induce ovulation comprising an effective amount of a peptide amide derivative selected from the group consisting of: L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-prolyl-glycinamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-glycyl-L-leucyl-L-arginyl-L-prolyl-β-alaninamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-glycyl-L-leucyl-L-arginyl-L-prolyl-sarcosinamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-methylamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-ethylamide; L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline N-n-propylamide; and L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-β-alanyl-L-leucyl-L-arginyl-L-proline pyrrolidide and an inert carrier therefor.
Claim 19
Dependent Claim
21 words
A composition according to claim 1 suitable for administration by injection comprising a sterile saline solution of said peptide amide derivative.
Claim 20
Dependent Claim
29 words
A method of treating mammals to promote maturation of egg follicles and induce ovulation by administering to the mammal a therapeutic dose of a composition according to claim 1.
Claim 21
Dependent Claim
15 words
A method according to claim 11 wherein the composition is administered in a single dose.
Claim 22
Dependent Claim
13 words
A method according to claim 11 wherein the composition is administered by infusion.
Claim 23
Dependent Claim
14 words
A method according to claim 11 wherein the composition is administered by intravenous injection.
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) | 1981-12-04 | 1982-06-05 | 1982-12-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-12-04 | 1986-06-05 | 1986-12-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-12-04 | 1990-06-05 | 1990-12-05 | $7700.00 | Window Closed / Lapsed |