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Claims for Patent: 4,244,946

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Claims for Patent: 4,244,946

Title: Water-soluble peptides affecting gonadal function
Abstract:[im-Bzl D-His.sup.6 ]LRF and [D-His.sup.6 (im-Bzl), Pro.sup.9 -NEt]LRF exhibit hydrophillicity comparable to that of LRF and act as superagonists exhibiting potencies, respectively, about 12 and more than 200 times that of LRF. The peptides or their nontoxic salts can be administered by intravenous subcutaneous, sublingual, oral, intravaginal, intranasal or rectal routes. The peptides can be used to regulate fertility in male and female mammals, including human beings.
Inventor(s): Rivier; Jean E. F. (La Jolla, CA), Vale, Jr.; Wylie W. (La Jolla, CA)
Assignee: The Salk Institute for Biological Studies (San Diego, CA)
Application Number:06/047,026
Patent Claims: 1. A compound selected from the class defined by the formulae:

p-Glu-His-Trp-Ser-Tyr-D-His(im-Bzl)-Leu-Arg-R and its nontoxic salts, and

X.sup.1 -p-Glu-His(X.sup.2)-Trp-Ser(X.sup.3)-Tyr(X.sup.4)-D-His(im-Bzl)-Leu-Arg(X. sup.5)-Pro-X.sup.6

wherein R is selected from the group consisting of Pro-Gly-NH.sub.2 and Pro-NH-CH.sub.2 -CH.sub.3 ;

X.sup.1 is either hydrogen or an .alpha.-amino protecting group;

X.sup.2 is a protecting group for the imidazole nitrogen atom selected from the group consisting of Tos, benzyl, trityl, 2,2,2-trifluoro-1-benzyloxycarbonylaminoethyl, 2,2,2-trifluoro-1tert-butyloxycarbonylaminoethyl and 2,4-dinitrothiophenyl;

X.sup.3 is a protecting group for the alcoholic hydroxyl group of Ser selected from the group consisting of acetyl, benzoyl, tetrahydropyranyl, tert-butyl, trityl, benzyl and 2,6-dichlorobenzyl;

X.sup.4 is a protecting group for the phenolic hydroxyl group of Tyr selected from the group consisting of tetrahydropyranyl, tert-butyl, trityl, benzyl, benzyloxycarbonyl, 4-bromobenzyloxycarbonyl and 2,6-dichlorobenzyl;

X.sup.5 is protecting group for the nitrogen atoms of Arg selected from the group consisting of nitro, Tos, benzyloxycarbonyl, adamantyloxycarbonyl, and BOC, or is hydrogen; and

X.sup.6 is selected from the group consisting of dimethylamine, alkylamine of 1 to 5 carbon atoms, phenethylamine, O-CH.sub.2 -[resin support], Gly-O-CH.sub.2 -[resin support], and Gly-NH [resin support].

2. A compound in accordance with claim 1 wherein R is Pro-Gly-NH.sub.2.

3. A compound in accordance with claim 1 wherein R is Pro-NH-CH.sub.2 -CH.sub.3.

4. A method for regulating fertility and the production of gonadotropins and sex steroids in male and female mammalians comprising administering an effective amount of a peptide having the formula:

p-Glu-His-Trp-Ser-Tyr-D-His(im-Bzl)-Leu-Arg-R, wherein

R is selected from the group consisting of Pro-Gly-NH.sub.2 and Pro-NH-CH.sub.2 -CH.sub.3, or a nontoxic salt thereof.

5. A method in accordance with claim 4 wherein R is Pro-Gly-NH.sub.2.

6. A method in accordance with claim 4 wherein R is Pro-NH-CH.sub.2 -CH.sub.3.
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