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US4253997A Expired / Lapsed US ⏱️ 0.0 years remaining

Anti-ovulatory decapeptides

Assignee: Wyeth LLC
•
Filing: 1979-12-17
•
Granted: 1981-03-03
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Expires: 1999-12-17
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Abstract

Abstract The compounds D-p-Glu-D-Phe-D-Nal(1)-L-Ser-L-Tyr-X-L-Leu-L-Arg-L-Pro-Gly-NH2 where X is D-Nal(1), D-Trp, D-Phe, D-Tyr, D-Lys, D-Met, D-Ala or D-Pgl and pharmaceutically acceptable salts thereof exhibit antiovulatory activity in female mammals and are useful contraceptive agents.

Inventors

  • 👤 Dimitrios Sarantakis

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-04 23:33
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; Y10S930/28

Claims Analysis

Total Claims: 13
Claim 1
Independent Claim 24 words
A compound of the formula: D-p-Glu-D-Phe-D-Nal(1)-Ser-Tyr-X-Leu-Arg-Pro-Gly-NH.sub.2 in which X is D-Nal(1), D-Trp, D-Phe, D-Tyr, D-Lys, D-Met, D-Ala or D-Pgl and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim 24 words
A compound of the formula: D-p-Glu-D-Phe-D-Nal(1)-Ser-Tyr-X-Leu-Arg-Pro-Gly-NH.sub.2 in which X is D-Nal(1), D-Trp, D-Phe, D-Tyr, D-Lys, D-Met, D-Ala or D-Pgl and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim 16 words
A compound of claim 1 which is D-(5-oxoprolyl)-D- phenylalanyl-D-3-(1-naphthyl)-alanyl-L-seryl-L-tyrosyl-D-3-(1-naphthyl)-alanyl-L-leucyl-L-arginyl-L-prolyl-glycine amide or a pharmaceutically acceptable salt thereof.
Claim 4
Dependent Claim 15 words
A compound of claim 1 which is D-(5-oxoprolyl)-D-phenylalanyl-D-3-(1-naphthyl)-alanyl-L-seryl-L-tyrosyl-D-tryptophyl-L-leucyl-L-arginyl-L-prolyl-glycine amide or a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim 15 words
A compound of claim 1 which is D-(5-oxoprolyl)-D-phenylalanyl-D-3-(1-naphthyl)-alanyl-L-seryl-L-tyrosyl-D-phenylalanyl-L-leucyl-L-arginyl-L-prolyl-glycine amide or a pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim 15 words
A compound of claim 1 which is D-(5-oxoprolyl)-D-phenylalanyl-D-3-(1-naphthyl)alanyl-L-seryl-L-tyrosyl-D-tyrosyl-L-leucyl-L-arginyl-L-prolyl-glycine amide or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim 15 words
A compound of claim 1 which is D-(5-oxoprolyl)-D-phenylalanyl-D-3-(1-naphthyl)alanyl-L-seryl-L-tyrosyl-D-lysyl-L-leucyl-L-arginyl-L-prolyl-glycine amide or a pharmaceutically acceptable salt thereof.
Claim 8
Dependent Claim 15 words
A compound of claim 1 which is D-(5-oxoprolyl)-D-phenylalanyl-D-3-(1-naphthyl)alanyl-L-seryl-L-tyrosyl-D-methionyl-L-leucyl-L-arginyl-L-prolyl-glycine amide or a pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim 15 words
A compound of claim 1 which is D-(5-oxoprolyl)-D-phenylalanyl-D-3-(1-naphthyl)-alanyl-L-seryl-L-tyrosyl-D-alanyl-L-leucyl-L-arginyl-L-prolyl-glycine amide or a pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim 15 words
A compound of claim 1 which is D-(5-oxoprolyl-D-phenylalanyl-D-3-(1-naphthyl)alanyl-L-seryl-L-tyrosyl-D-phenyl-glycyl-L-leucyl-L-arginyl-L-prolyl-glycine amide or a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim 55 words
A compound of the formula: (R)D-p-Glu-D-Phe-D-Nal(1)-Ser(R.sup.4)-Tyr(R.sup.5)-X-Leu-Arg(R.sup.8)-Pro-Gly-Z in which R is hydrogen or an alpha amino protecting group; R 4 is a hydroxyl protecting group; R 5 is a phenolic hydroxy protecting group; R 8 is a nitrogen protecting group for the guanyl side chain of arginine; and Z is a benzhydrylamine modified polystyrene resin support.
Claim 12
Dependent Claim 55 words
A compound of the formula: (R)D-p-Glu-D-Phe-D-Nal(1)-Ser(R.sup.4)-Tyr(R.sup.5)-X-Leu-Arg(R.sup.8)-Pro-Gly-Z in which R is hydrogen or an alpha amino protecting group; R 4 is a hydroxyl protecting group; R 5 is a phenolic hydroxy protecting group; R 8 is a nitrogen protecting group for the guanyl side chain of arginine; and Z is a benzhydrylamine modified polystyrene resin support.
Claim 13
Dependent Claim 11 words
The compound of claim 10 which is N-benzyloxycarbonyl-D-(5-oxoprolyl)-D-phenylalanyl-D-3-(1-naphthyl)alanyl-O-benzyl-L-seryl-O-2,6-dichlorobenzyl-L-tyrosyl-D-3-(1-naphthyl)alanyl-L-leucyl-N g -tosyl-L-arginyl-L-prolyl-glycyl-benzhydrylamine polystyrene.

References Cited (Backward Citations)

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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) 1984-03-02 1984-09-01 1985-03-03 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1988-03-02 1988-09-01 1989-03-03 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1992-03-02 1992-09-01 1993-03-03 $7700.00 Window Closed / Lapsed

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