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Claims for Patent: 4,472,382

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Claims for Patent: 4,472,382

Title: Treatment method
Abstract:A novel method of treating prostate adenocarcinoma, prostate benign hypertrophia, endometriosis, dysmenorrhea, hirsuitism, hormono-dependent 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, D Met, .epsilon.-lauryl -D Lys, .epsilon.-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 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' where 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.
Inventor(s): Labrie; Fernand (Quebec, CA), Raynaud; Jean-Pierre (Paris, FR)
Assignee: Roussel Uclaf (Paris, FR)
Application Number:06/468,932
Patent Claims: 1. A method for the treatment of prostate adenocarcinoma and prostate benign hypertrophaia comprising administering to male warm-blooded animals an effective amount of an association of an antiandrogen and 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 (Otbu), D Glu (Otbu), D Orn (boc), D Lys (boc), D Trp, Trp, 2-methyl Ala, D Tyr, D Met, .epsilon.-lauryl-D Lys, .epsilon.-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.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 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 prostate adenocarcinoma and prostate benign hypertrophia.

2. The method of claim 1 wherein the antiandrogen is 5,5-dimethyl-3-[4-nitro-3-trifluoromethyl-phenyl]-2,4-imidazolidine dione.

3. The method of claim 1 wherein the antiandrogen is 2-methyl-N-[4-nitro-3-trifluoromethyl-phenyl]-propanamide.

4. 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.

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

6. The method of claim 1 wherein the daily dose of the peptide is 10 to 100,000 .mu.g.

7. The method of claim 1 wherein the peptide is administered intranasally at a daily dose of 100 to 100,000 .mu.g.

8. The method of claim 1 wherein the peptide is administered parenterally at a daily dose of 10 to 10,000 .mu.g.

9. The method of claim 1 wherein the peptide is [D Ser (Tbu).sup.6, des Gly NH.sub.2.sup.10 ] LH--RH ethylamide and is administered parenterally at a daily dose of 10 to 200 .mu.g.

10. The method of claim 1 wherein the peptide is [D Ser (Tbu).sup.6, des Gly NH.sub.2.sup.10 ] LH--RH ethylamide and is administered intranasally at a daily dose of 100 to 2000 .mu.g.

11. The method of claim 9 wherein the peptide is administered once or twice a day each day.

12. The method of claim 10 wherein the peptide is administered once or twice a day each day.

13. The method of claim 9 wherein the peptide is administered once or twice a day with intervals of several days.

14. The method of claim 10 wherein the peptide is administered once or twice a day with intervals of several days.

15. The method of claim 1 wherein the daily dose of the antiandrogen is 10 mg to 1 g per day.

16. The method of claim 6 wherein the daily dose of the antiandrogen is 10 mg to 1 g per day.

17. A method for the treatment of prostate adenocarcenoma and prostate benign hypertrophial comprising administering to male humans an effective amount of an association of [D-Ser (TBu).sup.6,des-Gly-NH.sub.2.sup.10 ]-LH--RH ethylamide and 5,5-dimethyl-3-[4-nitro-3-trifluoromethyl-phenyl]-2,4-imidazolidine-dione sufficient to treat prostate adenocarcenoma and prostate benign hypertrophia.

18. The method of claim 17 wherein the daily dose of 5,5-dimethyl-3-[4-nitro-3-trifluoromethyl-phenyl]-2,4-imidazolidine-dione is 10 mg to 1 g per day and the daily dose of the said peptide is 10 to 100,000 mg per day.
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