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Details for Patent: 7,700,549

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Details for Patent: 7,700,549

Title:Exendin agonist analogs to treat diabetes
Abstract: Methods for treating conditions or disorders which can be alleviated by reducing food intake are disclosed which comprise administration of an effective amount of an exendin or an exendin agonist, alone or in conjunction with other compounds or compositions that affect satiety. The methods are useful for treating conditions or disorders, including obesity, Type II diabetes, eating disorders, and insulin-resistance syndrome. The methods are also useful for lowering the plasma glucose level, lowering the plasma lipid level, reducing the cardiac risk, reducing the appetite, and reducing the weight of subjects. Pharmaceutical compositions for use in the methods of the invention are also disclosed.
Inventor(s): Beeley; Nigel Robert Arnold (Solana Beach, CA), Prickett; Kathryn S. (San Diego, CA), Bhavsar; Sunil (San Diego, CA), Young; Andrew (La Jolla, CA)
Assignee: Amylin Pharmaceuticals, Inc. (San Diego, CA)
Filing Date:Aug 29, 2008
Application Number:12/201,918
Claims:1. A method of treating diabetes in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an exendin agonist peptide analog comprising the amino acid sequence of SEQ ID NO: 3 or a pharmaceutically acceptable salt thereof: TABLE-US-00154 (SEQ ID NO:3) X.sub.aa1 X.sub.aa2 X.sub.aa3 Gly Thr X.sub.aa4 X.sub.aa5 X.sub.aa6 X.sub.aa7 X.sub.aa8 Ser Lys Gln X.sub.aa9 Glu Glu Glu Ala Val Arg Leu X.sub.aa10 X.sub.aa11 X.sub.aa12 X.sub.aa13 Leu Lys Asn Gly Gly X.sub.aa14 Ser Ser Gly Ala X.sub.aa15 X.sub.aa16 X.sub.aa17 X.sub.aa18-Z;

Wherein X.sub.aa1 is His, Arg or Tyr; X.sub.aa2 is Ser, Gly, Ala or Thr; X.sub.aa3 is Asp or Glu; X.sub.aa4 is Phe, Tyr or naphthylalanine; X.sub.aa5 is Thr or Ser; X.sub.aa6 is Ser or Thr; X.sub.aa7 is Asp or Glu; X.sub.aa8 is Leu, lle, Val, pentylglycine or Met; X.sub.aa9 is Leu, Ile, pentylglycine, Val or Met; X.sub.aa10 is Phe, Tyr or naphthylalanine; X.sub.aa11 is Ile, Val, Leu, pentylglycine, tert-butylglycine or Met; X.sub.aa12 is Glu or Asp; X.sub.aa13 is Trp, Phe, Tyr or naphthylalanine; X.sub.aa14, X.sub.aa15, X.sub.aa16 and X.sub.aa17 are independently Pro, homoproline, 3Hyp, 4Hyp, thioproline, N-alkylglycine, N-alkylpentylglycine or N-alkylalanine; X.sub.aa18 is Ser, Thr or Tyr; and Z is --OH or --NH.sub.2; with the proviso that the compound is not exendin-3 or exendin-4.

2. The method of claim 1, wherein the exendin agonist peptide analog of SEQ ID NO: 3 is HGEGTFTSDLSKQLEEEAVRLFIEFLKNGGPSSGAPPPS-NH.sub.2 (SEQ 1D NO:9).

3. The method of claim 1, wherein the exendin agonist peptide analog of SEQ 1D NO:3 is HGEGTFTSDLSKQLEEEAVRLFPIEWLKNGGPSSGAPPPS-NH.sub.2 (SEQ ID NO: 10).

4. The method of claim 1, wherein the exendin agonist peptide analog of SEQ ID NO: 3 is SEQ ID NO: 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, or 36.

5. The method of claim 1, wherein the diabetes is Type II diabetes.

6. The method of claim 1, further comprising administering a therapeutically effective amount of amylin, an amylin agonist, a calcitonin, a leptin, a cholecystokinin, or a combination of two or more thereof.

7. A method of treating diabetes in a human in need thereof comprising administering to the human a therapeutically effective amount of an exendin agonist peptide analog comprising the amino acid sequence of SEQ ID NO: 5 or a pharmaceutically acceptable salt thereof: TABLE-US-00155 (SEQ ID NO:5) X.sub.aa.sub.1 X.sub.aa2 X.sub.aa3 Gly X.sub.aa5 X.sub.aa6 X.sub.aa7 X.sub.aa8 X.sub.aa9 X.sub.aa10 X.sub.aa11 X.sub.aa12 X.sub.aa13 X.sub.aa14 X.sub.aa15 X.sub.aa16 X.sub.aa17 Ala X.sub.aa19 X.sub.aa20 X.sub.aa21 X.sub.aa22 X.sub.aa23 X.sub.aa24 X.sub.aa25 X.sub.aa26 X.sub.aa27 X.sub.aa28-Z.sub.1;

Wherein X.sub.aa1 is His, Arg, Tyr, Ala, Norval, Val or Norleu; X.sub.aa2 is Ser, Gly, Ala or Thr; X.sub.aa3 is Ala, Asp or Glu; X.sub.aa4 is Ala, Norval, Val, Norleu or Gly; X.sub.aa5 is Ala or The; X.sub.aa6 is Phe, Tyr or naphthylalanine; X.sub.aa7 is Thr or Ser; X.sub.aa8 is Ala, Ser or Thr; X.sub.aa9 is Ala, Norval, Val, Norleu, Asp or Gly; X.sub.aa10 is Ala, Leu, Ile, Val, pentylglycine or Met; X.sub.aa11 is Ala or Ser; X.sub.aa12 is Ala or Lys; X.sub.aa13 is Ala or Gln; X.sub.aa14 is Ala, Leu, Ile, pentylglycine, Val or Met; X.sub.aa15 is Ala or Glu; X.sub.aa16 is Ala or Glu; X.sub.aa17 is Ala or Glu; X.sub.aa19 is Ala or Val; X.sub.aa20 is Ala or Arg; X.sub.aa21 is Ala or Leu; X.sub.aa22 is Phe, Tyr or naphthylalanine; X.sub.aa23 is Ile, Val, Leu, pentylglycine, tert-butylglycine or Met; X.sub.aa24 is Ala, Glu or Asp; X.sub.aa25 is Ala, Trp, Phe, Tyr or naphthylalanine; X.sub.aa26 is Ala or Leu; X.sub.aa17 is Ala or Lys; X.sub.aa28 is Ala or Asn; Z.sub.1 is --OH, --NH.sub.2, Gly-Z.sub.2, Gly Gly-Z.sub.2, Gly Gly X.sub.aa31--Z.sub.2, Gly Gly X.sub.aa31 Ser-Z.sub.2, Gly Gly X.sub.aa31 Ser Ser-Z.sub.2, Gly Gly X.sub.aa31 Ser Ser Gly-Z.sub.2, Gly Gly X.sub.aa31 Ser Ser Gly Ala-Z.sub.2, Gly Gly X.sub.aa31 Ser Ser Gly Ala-Xaa.sub.36-Z.sub.2; Gly Gly X.sub.aa31 Ser Ser Gly Ala-Xaa.sub.36 Xaa.sub.37-Z.sub.2; Gly Gly X.sub.aa31 Ser Ser Gly Ala-Xaa.sub.36 Xaa.sub.37 Xaa.sub.38-Z.sub.2 or Gly Gly X.sub.aa31 Ser Ser Gly Ala-Xaa.sub.36 Xaa.sub.37 Xaa.sub.38-X.sub.aa39-Z.sub.2; X.sub.aa31, X.sub.aa36, X.sub.aa37 and X.sub.aa38 are independently Pro, homoproline, 3Hyp, 4Hyp, thioproline, N-alkylglycine, N-alkylpentylglycine or N-alkylalanine; X.sub.aa39 is Ser or Tyr; and Z.sub.2 is --OH or --NH.sub.2; provided that no more than three of X.sub.aa3, X.sub.aa4, X.sub.aa5, X.sub.aa6, X.sub.aa8, X.sub.aa9, X.sub.aa10, X.sub.aa11, X.sub.aa12, X.sub.aa13, X.sub.aa14, X.sub.aa15, X.sub.aa16, X.sub.aa17, X.sub.aa19, X.sub.aa20, X.sub.aa21, X.sub.aa24, X.sub.aa25, X.sub.aa26, X.sub.aa27 and X.sub.aa28 are Ala; and provided also that, if X.sub.aa1 is His, Arg or Tyr, then at least one of X.sub.aa3, X.sub.aa4, and X.sub.aa9 is Ala.

8. The method of claim 7, wherein the exendin agonist peptide analog of SEQ ID NO:5 comprises the amino acid sequence of any one of SEQ ID NOs: 104-172.

9. The method of claim 7, further comprising administering a therapeutically effective amount of amylin, an amylin agonist, a calcitonin, a leptin, a cholecystokinin, or a combination of two or more thereof.

10. The method of claim 7, wherein the diabetes is Type II diabetes.

11. The method of claim 7, wherein the exendin agonist peptide analog is administered at a dose of from about 0.1 .mu.g/kg/day to about 1 .mu.g/kg/day.

12. A method of treating diabetes in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an exendin agonist peptide analog comprising the amino acid sequence of SEQ ID NO: 9: HGEGTFTSDLSKQLEEEAVRLFI EFLKNGGPSSGAPPPS-NH.sub.2 or SEQ ID NO:10 HGEGTFTSDLSKQLEEEAVRLFPIEWLKNGGPSSGAPPPS-NH.sub.2 to treat diabetes in the subject.

13. The method of claim 12, wherein the exendin agonist peptide analog comprises the amino acid sequence of SEQ ID NO: 9.

14. The method of claim 12, wherein the exendin agonist peptide analog comprises the amino acid sequence of SEQ ID NO: 10.

15. The method of claim 12, wherein the exendin agonist peptide analog is administered at a dose of from about 0.1 .mu.g/kg/day to about 1 .mu.g/kg/day.

16. The method of claim 12, wherein the diabetes is Type II diabetes.

17. The method of claim 12, further comprising administering a therapeutically effective amount of amylin, an amylin agonist, a calcitonin, a leptin, a cholecystokinin, or a combination of two or more thereof.

18. The method of claim 12, wherein the exendin agonist peptide analog is in the form of a pharmaceutically acceptable salt.
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