Patent EP0742616A1 successfully refreshed from Google Patents.
US4143133A
Expired / Lapsed
US
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Claudogenic-interceptive nonapeptides
Assignee: Wyeth LLC
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Filing: 1977-10-03
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Granted: 1979-03-06
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Expires: 1997-10-03
Abstract
Abstract Compounds of the formula: L-p-Glu-L-His-L-Trp-L-Ser-L-Tyr-D-2-(cyclohexyl)Gly-Y-L-Arg-L-Pro-NHC.sub.2 H 5 in which Y is L-Leu or L-(N-methyl)-Leu or a non-toxic acid addition salt thereof, are potent ovulation inducers and claudogenic-interceptive agents useful in preventing or terminating pregnancy in mammals.
Inventors
- 👤 Theodore J. Foell
- 👤 Richard W. A. Rees
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 22:05
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/04; C07K7/23; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/28
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
21 words
A compound of the formula: L-p-Glu-L-His-L-Trp-L-Ser-L-Tyr-D-2-(cyclohexyl)Gly-Y-L-Arg-L-Pro-NHC.sub.2 H.sub.5 in which Y is L-Leu or L-(N-methyl)-Leu or a non-toxic acid addition salt thereof.
Claim 2
Dependent Claim
21 words
A compound of the formula: L-p-Glu-L-His-L-Trp-L-Ser-L-Tyr-D-2-(cyclohexyl)Gly-Y-L-Arg-L-Pro-NHC.sub.2 H.sub.5 in which Y is L-Leu or L-(N-methyl)-Leu or a non-toxic acid addition salt thereof.
Claim 3
Dependent Claim
17 words
A compound of claim 1 of the formula: L-p-Glu-L-His-L-Trp-L-Ser-L-Tyr-D-2-(cyclohexyl)Gly-L-(N-methyl)Leu-L-arg-L-Pro-NHC.sub.2 H.sub.5, or a non-toxic acid addition salt thereof.
Claim 4
Dependent Claim
18 words
A compound of claim 1 of the formula: L-p-Glu-L-His-L-Trp-L-Ser-L-Tyr-D-2-(cyclohexyl)Gly-L-Leu-L-Arg-L-Pro-NHC.sub.2 H.sub.5 , or a non-toxic acid addition salt thereof.
Claim 5
Dependent Claim
68 words
A compound of the formula: L-p-Glu-L-His(R)-L-Trp-L-Ser(R.sup.1)-L-Tyr(R.sup.2)-D-2-(cyclohexyl)Gly-Y-L-Arg(R.sup.3)-L-Pro-Z in which Y is L-Leu or L-(N-methyl)Leu; Z is --O--CH.sub.2 -[polystyrene resin support] or --NHC.sub.2 H.sub.5 ; r and R 3 are independently selected from the group consisting of tosyl, acetyl, benzoyl, tert-butyl, trityl, benzyl, benzyloxycarbonyl, adamantyloxycarbonyl and nitro; and R 1 and R 2 are independently selected from the group consisting of acetyl, tosyl, benzoyl, tert-butyl, trityl, benzyl, benzyloxycarbonyl and 2,6-dichlorobenzyl.
Claim 6
Dependent Claim
68 words
A compound of the formula: L-p-Glu-L-His(R)-L-Trp-L-Ser(R.sup.1)-L-Tyr(R.sup.2)-D-2-(cyclohexyl)Gly-Y-L-Arg(R.sup.3)-L-Pro-Z in which Y is L-Leu or L-(N-methyl)Leu; Z is --O--CH.sub.2 -[polystyrene resin support] or --NHC.sub.2 H.sub.5 ; r and R 3 are independently selected from the group consisting of tosyl, acetyl, benzoyl, tert-butyl, trityl, benzyl, benzyloxycarbonyl, adamantyloxycarbonyl and nitro; and R 1 and R 2 are independently selected from the group consisting of acetyl, tosyl, benzoyl, tert-butyl, trityl, benzyl, benzyloxycarbonyl and 2,6-dichlorobenzyl.
Claim 7
Dependent Claim
32 words
The compound of claim 4 in which Y is L-(N-methyl)Leu, Z is --NHC 2 H 5 , R and R 3 are tosyl; R 1 is benzyl and R 2 is 2,6-dichlorobenzyl.
Claim 8
Dependent Claim
32 words
The compound of claim 4 in which Y is L-Leu, Z is --NHC 2 H 5 , R and R 3 are tosyl; R 1 is benzyl and R 2 is 2,6-dichlorobenzyl.
Claim 9
Independent Claim
61 words
A method for terminating pregnancy in a female mammal which comprises administering a nonapeptide of the formula: L-p-Glu-L-His-L-Trp-L-Ser-L-Tyr-D-2-(cyclohexyl)Gly-Y-L-Arg-L-Pro-NHC.sub.2 H.sub.5, in which Y is L-Leu or L-(N-methyl)Leu; or a pharmaceutically acceptable acid addition salt therof, to said ammmal, post coitally, in a daily regimen containing at least about 30 micrograms per kilogram host body weight for a time sufficient to terminate pregnancy.
Claim 10
Independent Claim
61 words
A method for terminating pregnancy in a female mammal which comprises administering a nonapeptide of the formula: L-p-Glu-L-His-L-Trp-L-Ser-L-Tyr-D-2-(cyclohexyl)Gly-Y-L-Arg-L-Pro-NHC.sub.2 H.sub.5, in which Y is L-Leu or L-(N-methyl)Leu; or a pharmaceutically acceptable acid addition salt therof, to said ammmal, post coitally, in a daily regimen containing at least about 30 micrograms per kilogram host body weight for a time sufficient to terminate pregnancy.
Claim 11
Dependent Claim
12 words
The method of claim 7 in which said nonapeptide is L-P-Glu-L-His-L-Trp-L-Ser-L-Tyr-D-2-(cyclohexyl)Gly-L-Lue-L-Arg-L-Pro-NHC.sub.2 H.sub.5.
Claim 12
Dependent Claim
12 words
The method of claim 7 in which said nonapeptide is L-p-Glu-L-His-L-Trp-L-Ser-L-Tyr-D-2(cyclohexyl)Gly-L-(N-methyl)Leu-L-Arg-L-Pro-NHC.sub.2 H.sub.5.
Claim 13
Dependent Claim
37 words
The method of claim 7 in which said nonapeptide is administered, orally or parenterally, to said mammal following a daily regimen beginning on day 1 after coitus and extending through about the first 8 days post implantation.
Claim 14
Dependent Claim
32 words
The method of claim 7 in which said nonapeptide is administered, orally or parenterally, following a daily regimen beginning on day 1 after coitus and extending through about day 7 post coitus.
References Cited (Backward Citations)
US3992530A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-03-05 | 1982-09-04 | 1983-03-06 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-03-05 | 1986-09-04 | 1987-03-06 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-03-05 | 1990-09-04 | 1991-03-06 | $7700.00 | Window Closed / Lapsed |