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Details for Patent: 5,189,021

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Details for Patent: 5,189,021

Title: Method of treating precocious puberty
Abstract:A novel method of treating prostate adenocarcinoma, prostate benign hypertrophia, endometriosis, dysmenorrhea, hirsiutism, hormono-dependant mammary tumors, treatment and prevention of precociuos puberty, induction of a retardation of the appearance of puberty and treatment of acne of mammals comprising administering to warm-blooded animals an effective amount of a peptide of the formula wherein (a) Z is Gly-NH.sub.2, Y is Leu and X is Gly, (b) Z is Gly-NH.sub.2, Y is Leu, X is DN Leu, DN Val, D Abu (.alpha.-aminobutyric acid), D Phe, D Ser, D Thr, D Met, D Pgl, D Lys, Leu, Ile, Nle, Val, N Val, Met, Phe, D Leu, D Arg, D Ser (tbu), D Thr (tbu), D Cys (tbu), D Asp (O tbu), D Glu (Otbu), D Orn (boc), D Lys (boc), D Trp, Trp, 2-methyl Ala, D Tyr, s-lauryl-D Lys, a-dextran-D Lys, (c) Z is NH-cyclopropyl-or NH-Alk wherein Alk is alkyl of 1 to 3 carbon atoms, Y is Leu and X is D Ser (tbu), D Thr (tbu), D Asp (Otbu), D Glu (Otbu), D Orn (boc), D Lys (boc), (d) Z is --NH--CH.sub.3, --NH--CH.sub.2 --CH.sub.3, NH--CH.sub.2 --CH.sub.2 --CH.sub.3, --NH--CH.sub.2 -- CH.sub.2 --OH, ##STR1## Y is Leu and X is Gly, (e) Z is --NH--CH.sub.2 --CH.sub.3, Y is Leu and X is D Trp, D Leu, D Ala, D Ser (tbu), D Tyr, D Lys, Ala, (f) Z is Gly-NH.sub.2 or --NH--CH.sub.2 --CH.sub.3, Y is M.alpha.Me Leu and X is Gly, (g) Z is -NH-cyclopropyl, Y is Leu and X is D Leu or (h) Z is Gly-NH.sub.2, -NH-cyclopropyl or -NHAlk' where Alk' is alky lof 1 to 3 carbon atoms, Y is Ser (but), Cys (but), Asp (Obut), Glu (Obut), Orn (boc), Lys (boc) and X is Gly.
Inventor(s): Labrie; Fernand (Quebec, CA), Raynaud; Jean-Pierre (Paris, FR)
Assignee: Roussel Uclaf (Paris, FR)
Filing Date:Oct 10, 1990
Application Number:07/595,297
Claims:1. A method of treating or preventing precocious puberty in mammals consisting essentially of administering to mammals an amount of a peptide of the formula

wherein (a) Z is Gly-NH.sub.2, Y is Leu and X is Gly, (b) Z is Gly-NH.sub.2, Y is Leu, X is DL Leu, DL Val, D Abu (.alpha.-aminobutyric acid), D Phe, D Ser, D Thr, D Met, D Pgl, D Lys, Leu, Ile, Nle, Val, Met, Phe, D Leu, D Arg, D Ser (tbu), D Thr (tbu), D Cys (tbu), D Asp (O tbu), D Glu (O tbu), D Orn (boc), D Lys (boc), D Trp, Trp, 2-methyl Ala, D Tyr, lauryl-D Lys, dextran-D Lys, (c) Z is NH-cyclopropyl or NH-Alk- wherein Alk is alkyl of 1 to 3 carbon atoms, Y is Leu and X is D Ser (tbu), D Thr (tbu), D Asp (Otbu), D Glu (Otbu), D Orn (boc), D Lys (boc), (d) Z is --NH--CH.sub.3, --NH--CH.sub.2 --CH.sub.3 --NH--CH.sub.2 --CH.sub.2 --CH.sub.3 --NH--CH.sub.2 --CH.sub.2 --OH, ##STR3## Y is Leu and X is Gly, (e) Z is --NH--CH.sub.2 --CH.sub.3, Y is Leu and X is D Trp, D Leu, D Ala, D Ser (tbu), D Tyr, D Lys, Ala, (f) Z is Gly-NH.sub.2 or --NH--CH.sub.2 --CH.sub.3, Y is N Me Leu and X is Gly, (g) Z is -NH-cyclopropyl, Y is Leu and X is D Leu or (h) Z is Gly-NH.sub.2, -NH-cyclopropyl or -NHAlk' wherein Alk' is alkyl of 1 to 3 carbon atoms, Y is Ser (but), Cys (but), Asp (Obut), Glu (Obut), Orn (box), Lys (boc) and X is Gly sufficient to treat or prevent precocious puberty.

2. The method of claim 1 wherein the peptide is administered in association with an antiandrogen.

3. The method of claim 1 wherein the peptide is [D Ser (Tbu).sup.6 des Gly NH.sub.2.sup.10 ] LH-RH ethylamide.

4. The method of claim 1 wherein the peptide is administered to male warm-blooded animals in an amount sufficient for the treatment or prevention of precocious puberty.

5. The method of claim 4 wherein the peptide is adminstered in association with an antiandrogen.

6. The method of claim 1 wherein the peptide is administered to female warm-blooded animals in an amount sufficient for the treatment or prevention of precocious puberty.
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