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Details for Patent: 4,981,842

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Details for Patent: 4,981,842

Title: Method of treating hormonal dependent mammary tumors in female mammals
Abstract:A novel method of treating prostate adenocarcinoma, prostate benign hypertrophia, endometriosis, dysmenorrhea, hirsuitism, hormono-dependant mammary tumors, treatment and prevention of precocious 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, .epsilon.-lauryl-D Lys, .alpha.-dextran-D Lys, (c) Z is HH-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 (bopc), (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 NaMe 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 alkyl of 1 to 3 carbon atoms, Y is Ser (but), Cys, (but), Asp (Obut), Glu (Obut), Orn (box), Lys (bpc) and X is Gly.
Inventor(s): Labrie; Fernand (Quebec, CA), Raynaud; Jean-Pierre (Paris, FR)
Assignee: Roussel Uclaf (Paris, FR)
Filing Date:Apr 05, 1989
Application Number:07/334,088
Claims:1. A method of treating hormono-dependent mammary tumors in female mammals consisting essentially of administering to female 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, D Abu (.alpha.-aminobutyric acid), D Phe, D Ser, D Thr, D Met, D Pgl, D Lys, Leu, Ile, Nle, Val, D 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, .alpha.-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, --NHCH.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.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' wherein Alk' is alkyl of 1 to 3 carbon atoms, Y is Ser (but), Cys (but), Asp (Obut), Glu (Obut), Orn (boc), Lys (boc) and X is Gly sufficient to treat hormomo-dependent mammary tumors.

2. The method of claim 1 wherein 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.

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