.

Deeper Knowledge, Faster

  • Analyze global market entry opportunities
  • Uncover prior art in expired and abandoned patents
  • Obtain formulation and manufacturing information

► See Plans & Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

Serving 500+ biopharmaceutical companies globally:

Farmers Insurance
Deloitte
Mallinckrodt
McKinsey
Merck
Fish and Richardson
Fuji
Moodys
Boehringer Ingelheim
Johnson and Johnson

Generated: July 21, 2017

DrugPatentWatch Database Preview

Claims for Patent: 4,472,382

« Back to Dashboard

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.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Serving 500+ biopharmaceutical companies globally:

Chubb
Chinese Patent Office
Johnson and Johnson
US Army
US Department of Justice
Deloitte
Citi
Novartis
Cipla
UBS

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

Copyright 2002-2017 thinkBiotech LLC
ISSN: 2162-2639

Secure SSL Encrypted Heap | Mobile and Web Analytics

Follow DrugPatentWatch:



Google
Twitter
Google Plus
botpot