US4504414A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Synthetic pyridyl-alanyl decapeptides having antiovulatory activity
Assignee: The University of Texas System
•
Filing: 1983-03-28
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Granted: 1985-03-12
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Expires: 2003-03-28
Abstract
Abstract Pyridyl-alanyl decapeptides have been effectively synthesized and found to have antiovulatory activity. The exemplary [N-Ac-D-2-Nal 1 ,pCl-D-Phe 2 , D-3-Pal 3 ,D-Arg 6 ,D-Ala 10 ]-LHRH has very high potency to inhibit ovulation, both parenterally and orally. Also, this exemplary pyridyl-alanyl-decapeptide showed an unexpected prolonged duration of antiovulatory activity. Such pyridyl-alanyl-decapeptides are useful to control reproduction.
Inventors
- 👤 Karl Folkers
- 👤 Cyril Y. Bowers
- 👤 Teresa M. Kubiak
- 👤 Janusz Stepinski
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 09:17
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: 12
Claim 1
Independent Claim
11 words
[N-Ac-D-2-Nal 1 ,pCl-D-Phe 2 ,D-3-Pal 3 ,D-Arg 6 ,D-Ala 10 ]-LHRH.
Claim 2
Dependent Claim
11 words
[N-Ac-D-2-Nal 1 ,pCl-D-Phe 2 ,D-3-Pal 3 ,D-Arg 6 ,D-Ala 10 ]-LHRH.
Claim 3
Dependent Claim
56 words
Analogs of LHRH wherein position 1 is N-Ac-pCl-D-Phe, N-Ac-D-2-Nal, or N-Ac-3,4-diCl-D-Phe; position 2 is pCl-D-Phe; position 3 is D-2-Pal, D-3-Pal, D-4-Pal, or D-Trp; position 6 is D-2-Pal, D-3-Pal, D-4-Pal, or D-Arg, with at least one of position 3 or 6 being D-2-Pal, D-3-Pal, or D-4-Pal; and position 10 is D-Ala or the unsubstituted normally occuring Gly.
Claim 4
Dependent Claim
56 words
Analogs of LHRH wherein position 1 is N-Ac-pCl-D-Phe, N-Ac-D-2-Nal, or N-Ac-3,4-diCl-D-Phe; position 2 is pCl-D-Phe; position 3 is D-2-Pal, D-3-Pal, D-4-Pal, or D-Trp; position 6 is D-2-Pal, D-3-Pal, D-4-Pal, or D-Arg, with at least one of position 3 or 6 being D-2-Pal, D-3-Pal, or D-4-Pal; and position 10 is D-Ala or the unsubstituted normally occuring Gly.
Claim 5
Dependent Claim
20 words
The LHRH analog of claim 2 which is [N-Ac-(pCl-D-Phe) 1 ,2, D-3-Pal 3 , D-Arg 6 , D-Ala 10 ]-LHRH.
Claim 6
Dependent Claim
20 words
The LHRH analog of claim 2 which is [N-Ac-(pCl-D-Phe) 1 ,2, D-2-Pal 3 , D-Arg 6 , D-Ala 10 ]-LHRH.
Claim 7
Dependent Claim
20 words
The LHRH analog of claim 2 which is [N-Ac-(pCl-D-Phe) 1 ,2, D-4-Pal 3 , D-Arg 6 , D-Ala 10 ]-LHRH.
Claim 8
Dependent Claim
20 words
The LHRH analog of claim 2 which is [N-Ac-(pCl-D-Phe) 1 ,2, D-Trp 3 , D-3-Pal 6 , D-Ala 10 ]-LHRH.
Claim 9
Dependent Claim
17 words
The LHRH analog of claim 2 which is [N-Ac-(pCl-D-Phe) 1 ,2, D-3-Pal 3 ,6, D-Ala 10 ]-LHRH.
Claim 10
Dependent Claim
17 words
The LHRH analog of claim 2 which is [N-Ac-(pCl-D-Phe) 1 ,2, D-4-Pal 3 ,6, D-Ala 10 ]-LHRH.
Claim 11
Dependent Claim
15 words
The LHRH analog of claim 2 which is [N-Ac-(pCl-D-Phe) 1 ,2, D-3-Pal 3 ,6 ]-LHRH.
Claim 12
Dependent Claim
23 words
The LHRH analog of claim 2 which is [N-Ac-3,4-diCl-D-Phe 1 , pCl-D-Phe 2 , D-3-Pal 3 , D-Arg 6 , D-Ala 10 ]-LHRH.
References Cited (Backward Citations)
US3655636A
Cited
US4310517A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1988-03-11 | 1988-09-10 | 1989-03-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-03-11 | 1992-09-10 | 1993-03-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-03-11 | 1996-09-10 | 1997-03-12 | $7700.00 | Window Closed / Lapsed |