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Last Updated: March 28, 2024

Details for Patent: 6,858,576


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Title: Methods for regulating gastrointestinal motility
Abstract:Methods for reducing gastric motility and delaying gastric emptying for therapeutic and diagnostic purposes are disclosed which comprise administration of an effective amount of an exendin or an exendin agonist. Methods for treating conditions associated with elevated, inappropriate, or undesired post-prandial blood glucose levels are disclosed which comprise administration of an effective amount of an exendin or an exendin agonist alone or in conjunction with other anti-gastric emptying agents.
Inventor(s): Young; Andrew A. (San Diego, CA), Gedulin; Bronislava (San Diego, CA), Beeley; Nigel Robert Arnold (Solana Beach, CA), Prickett; Kathryn S. (San Diego, CA)
Assignee: Amylin Pharmaceuticals, Inc. (San Diego, CA)
Filing Date:Aug 08, 1997
Application Number:08/908,867
Claims:1. A method of reducing gastric motility in a subject in need thereof comprising administering to said subject an amount of an exendin effective for reducing gastric motility.

2. A method of delaying gastric emptying in a subject in need thereof comprising administering to said subject an amount of an exendin effective for delaying gastric emptying.

3. The method according to claim 1 or 2 wherein said exendin is exendin-3.

4. The method according to claim 1 or 2 wherein said exendin is exendin-4.

5. The method according to claim 1 or 2 wherein said subject is undergoing a gastrointestinal diagnostic procedure.

6. The method according to claim 5 wherein said gastrointestinal diagnostic procedure is a radiological examination.

7. The method according to claim 6 wherein said gastric gastrointestinal diagnostic procedure is magnetic resonance imaging.

8. The method according to claim 1 or 2 wherein said subject is suffering from a gastrointestinal disorder.

9. A method of reducing gastric motility in a subject in need thereof comprising administering to said subject an amount of an exendin analog effective for reducing gastric motility, wherein said exendin analog is selected from a peptide compound of the formula:

wherein: Xaa.sub.1 is His, Arg or Tyr; Xaa.sub.2 is Ser, Gly, Ala or Thr; Xaa.sub.3 is Asp or Glu; Xaa.sub.4 is Phe, Tyr or naphthylalanine; Xaa.sub.5 is Thr or Ser; Xaa.sub.6 is Ser or Thr; Xaa.sub.7 is Asp or Glu; Xaa.sub.8 is Leu, Ile, Val, pentylglycine or Met; Xaa.sub.9 is Leu, Ile, pentylglycine, Val or Met; Xaa.sub.10 is Phe, Tyr or naphthylalanine; Xaa.sub.11 is Ile, Val, Leu, pentylglycine, tert-butylglycine or Met; Xaa.sub.12 is Glu or Asp; Xaa.sub.13 is Trp, Phe, Tyr, or naphthylalanine; Xaa.sub.14, Xaa.sub.15, Xaa.sub.16 and Xaa.sub.17 are independently Pro, homoproline, 3Hyp, 4Hyp, thioproline, N-alkylglycine, N-alkylpentylglycine or N-alkylalanine; Xaa.sub.18 is Ser, Thr or Tyr; and Z is --OH or --NH.sub.2 ;

with the proviso that the compound does not have the formula of either exendin-3 or exendin-4 and pharmaceutically acceptable salts thereof.

10. A method of reducing gastric motility in a subject in need thereof comprising administering to said subject an amount of an exendin analog effective for reducing gastric motility, wherein said exendin analog is selected from a peptide compound of the formula:

wherein: Xaa.sub.1 is His or Arg; Xaa.sub.2 is Ser or Gly; Xaa.sub.3 is Asp or Glu; Xaa.sub.4 is Phe or naphthylalanine; Xaa.sub.5 is Thr or Ser; Xaa.sub.6 is Ser or Thr; Xaa.sub.7 is Asp or Glu; Xaa.sub.8 is Leu or pentylglycine Xaa.sub.9 is Leu or pentylglycine; Xaa.sub.10 is Phe or naphthylalanine; Xaa.sub.11 is Ile, Val or tert-butylglycine; Xaa.sub.12 is Glu or Asp; Xaa.sub.13 is Trp or Phe; Xaa.sub.14, Xaa.sub.15, Xaa.sub.16 and Xaa.sub.17 are independently selected from Pro, homoproline or N-methylalanine; Xaa.sub.18 is Ser or Tyr; and Z is --OH or --NH.sub.2 ;

with the proviso that the compound does not have the formula of either exendin-3 or exendin-4 and pharmaceutically acceptable salts thereof.

11. A method of delaying gastric emptying in a subject in need thereof comprising administering to said subject an amount of an exendin analog effective for delaying gastric emptying, wherein said exendin analog is selected from a peptide compound of the formula:

wherein: Xaa.sub.1 is His, Arg or Tyr; Xaa.sub.2 is Ser, Gly, Ala or Thr; Xaa.sub.3 is Asp or Glu; Xaa.sub.4 is Phe, Tyr or naphthylalanine; Xaa.sub.5 is Thr or Ser; Xaa.sub.6 is Ser or Thr; Xaa.sub.7 is Asp or Glu; Xaa.sub.8 is Leu, Ile, Val, pentylglycine or Met; Xaa.sub.9 is Leu, Ile, pentylglycine, Val or Met; Xaa.sub.10 is Phe, Tyr or naphthylalanine; Xaa.sub.11 is Ile, Val, Leu, pentylglycine, tert-butylglycine or Met; Xaa.sub.12 is Glu or Asp; Xaa.sub.13 is Trp, Phe, Tyr, or naphthylalanine; Xaa.sub.14, Xaa.sub.15, Xaa.sub.16 and Xaa.sub.17 are independently Pro, homoproline, 3Hyp, 4Hyp, thioproline, N-alkylglycine, N-alkylpentylglycine or N-alkylalanine; Xaa.sub.18 is Ser, Thr or Tyr; and Z is --OH or --NH.sub.2 ;

with the proviso that the compound does not have the formula of either exendin-3 or exendin-4 and pharmaceutically acceptable salts thereof.

12. A method of delaying gastric emptying in a subject in need thereof comprising administering to said subject an amount of an exendin analog effective for delaying gastric emptying, wherein said exendin analog is selected from a peptide compound of the formula:

wherein: Xaa.sub.1 is His or Arg; Xaa.sub.2 is Ser or Gly; Xaa.sub.3 is Asp or Glu; Xaa.sub.4 is Phe or naphthylalanine; Xaa.sub.5 is Thr or Ser; Xaa.sub.6 is Ser or Thr; Xaa.sub.7 is Asp or Glu; Xaa.sub.8 is Leu or pentylglycine Xaa.sub.9 is Leu or pentylglycine; Xaa.sub.10 is Phe or naphthylalanine; Xaa.sub.11 is Ile, Val or tert-butylglycine; Xaa.sub.12 is Glu or Asp; Xaa.sub.13 is Trp or Phe; Xaa.sub.14, Xaa.sub.15, Xaa.sub.16 and Xaa.sub.17 are independently selected from Pro, homoproline or N-methylalanine; Xaa.sub.18 is Ser or Tyr; and Z is --OH or --NH.sub.2 ;

with the proviso that the compound does not have the formula of either exendin-3 or exendin-4 and pharmaceutically acceptable salts thereof.

13. The method according to claim 9, 10, 11, or 12 wherein said subject is undergoing a gastrointestinal diagnostic procedure.

14. The method according to claim 13 wherein said gastrointestinal diagnostic procedure is a radiological examination.

15. The method according to claim 14 wherein said gastric gastrointestinal diagnostic procedure is magnetic resonance imaging.

16. The method according to claim 9, 10, 11, or 12 wherein said subject is suffering from a gastrointestinal disorder.

17. A method of reducing gastric motility in a subject in need thereof comprising administering to said subject an amount of exendin-4 effective for reducing gastric motility.

18. A method of delaying gastric emptying in a subject in need thereof comprising administering to said subject an amount of exendin-4 effective for delaying gastric emptying.

19. The method according to claim 17 or 18 wherein said subject is undergoing a gastrointestinal diagnostic procedure.

20. The method according to claim 19 wherein said gastrointestinal diagnostic procedure is a radiological examination.

21. The method according to claim 20 wherein said gastric gastrointestinal diagnostic procedure is magnetic resonance imaging.

22. The method according to claim 17 or 18 wherein said subject is suffering from a gastrointestinal disorder.

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