Synthetic pyridyl-alanyl decapeptides having antiovulatory activity

DETAILED DESCRIPTION What is claimed: 1.
[N-Ac-D-2-Nal .
sup.
1,pCl-D-Phe.
sup.
2,D-3-Pal.
sup.
3,D-Arg.
sup.
6,D-Ala.
sup.
10 ]-LHRH.
2.
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.
3.
The LHRH analog of claim 2 which is [N-Ac-(pCl-D-Phe).
sup.
1,2, D-3-Pal.
sup.
3, D-Arg.
sup.
6, D-Ala.
sup.
10 ]-LHRH.
4.
The LHRH analog of claim 2 which is [N-Ac-(pCl-D-Phe).
sup.
1,2, D-2-Pal.
sup.
3, D-Arg.
sup.
6, D-Ala.
sup.
10 ]-LHRH.
5.
The LHRH analog of claim 2 which is [N-Ac-(pCl-D-Phe).
sup.
1,2, D-4-Pal.
sup.
3, D-Arg.
sup.
6, D-Ala.
sup.
10 ]-LHRH.
6.
The LHRH analog of claim 2 which is [N-Ac-(pCl-D-Phe).
sup.
1,2, D-Trp.
sup.
3, D-3-Pal.
sup.
6, D-Ala.
sup.
10 ]-LHRH.
7.
The LHRH analog of claim 2 which is [N-Ac-(pCl-D-Phe).
sup.
1,2, D-3-Pal.
sup.
3,6, D-Ala.
sup.
10 ]-LHRH.
8.
The LHRH analog of claim 2 which is [N-Ac-(pCl-D-Phe).
sup.
1,2, D-4-Pal.
sup.
3,6, D-Ala.
sup.
10 ]-LHRH.
9.
The LHRH analog of claim 2 which is [N-Ac-(pCl-D-Phe).
sup.
1,2, D-3-Pal.
sup.
3,6 ]-LHRH.
10.
The LHRH analog of claim 2 which is [N-Ac-3,4-diCl-D-Phe.
sup.
1, pCl-D-Phe.
sup.
2, D-3-Pal.
sup.
3, D-Arg.
sup.
6, D-Ala.
sup.
10 ]-LHRH.




Description:
BACKGROUND OF THE INVENTION During the decade, over a thousand analogs of the luteinizing hormone releasing hormone (LHRH) have been internationally synthesized, some of which were significant agonists, "super-agonists" or antagonists.
The biological goal of antagonists of LHRH is effective and potent antiovulatory activity toward control of conception.
Folkers, Humphries and Bowers [Z.
Naturforsch.
37b, 246-249 (1982)] critiqued the evolution of design and achievement of inhibitors of LHRH as inhibitors of ovulation, based on the research of many investigators.
A recent significant advance in sequence changes to increase antiovulatory potency was reported by Coy et al