Pharmaceutical composition comprising oxyntomodulin derivatives and a method for reducing body weight using the composition

View Patent ↗

Loading inventors, assignments & file history…

Monitor This Case

Get email alerts when status or documents change.

Order Certified Copies

Most orders are placed with the USPTO same day — all within 24 business hours.

Order via The Patent Place →

Pre-filled with this patent's details

Quick Facts

Patent No.: US 7,928,058
App. No.: 12/223,942
Granted: Apr 19, 2011
Kind: B2

External Links

USPTO Patent Center↗ Full Patent PDF↗

Abstract

Modified oxyntomodulin derivatives. Such derivatives can be used for the treatment of metabolic diseases such as diabetes and obesity.

Claims (46)

1. A polypeptide comprising the amino acid sequence of SEQ ID NO:4, further comprising a substitution of Asp, Glu, Ile, Val, D-Ser, Met, D-Ala, Trp, Asn, Leu, or α-aminoisobutyric acid for the Ser at position 2 and a pharmaceutically acceptable salt thereof.

2. The polypeptide of claim 1 , wherein the polypeptide further comprises one or more amino acid substitutions selected from

(a) Asp, Glu, Pro, Leu or L-norleucine for the Gln at position 3;

(b) Ala, Cys, Cys(mPEG), or Cys(cholesteryl) for the Ser at position 11;

(d) Ala for the Ser at position 16;

(e) Cys, Cys(mPEG), or Cys(cholesteryl) for the Arg at position 17;

(f) Cys, Cys(mPEG), or Cys(cholesteryl) for the Arg at position 18;

(g) Cys, Cys(mPEG), or Cys(cholesteryl) for the Gln at position 20;

(h) Cys, Cys(mPEG), or Cys(cholesteryl) for the Asp at position 21;

(i) Cys, Cys(mPEG), or Cys(cholesteryl) for the Gln at position 24;

(j) Met(O), Val, norleucine, alanine, α-aminoisobutyric acid or O-methyl-homoserine for the Met at position 27;

(k) Cys, Cys(mPEG), or Cys(cholesteryl) for the Asn at position 28;

(l) Cys, Cys(mPEG), or Cys(cholesteryl) for the Thr at position 29;

(m) Cys, Cys(mPEG), or Cys(cholesteryl) for the Ile at position 36; or

(n) Cys, Cys(mPEG), or Cys(cholesteryl) for the Ala at position 37.

3. The polypeptide of claim 1 , wherein the polypeptide further comprises a deletion of amino acids 31-37.

4. The polypeptide of claim 1 , wherein the polypeptide further comprises a Lys(Palmitoyl), Cys, Cys(mPEG), or Cys(cholesteryl) at the carboxy terminus.

5. The polypeptide of claim 1 , wherein the polypeptide comprises α-aminoisobutyric acid for the Ser at position 2, Asp for the Gln at position 3, Met(O) for the Met at position 27, and a Cys(mPEG) at the carboxy terminus.

6. The polypeptide of claim 1 , wherein the polypeptide comprises α-aminoisobutyric acid for the Ser at position 2, Asp for the Gln at position 3, Met(O) for the Met at position 27, and a Cys(cholesteryl) at the carboxy terminus.

7. The polypeptide of claim 1 , wherein the polypeptide comprises D-Ser for the Ser at position 2 and a Lys(palmitoyl) at the carboxy terminus.

8. The polypeptide of claim 1 , wherein the polypeptide is selected from a polypeptide comprising the amino acid sequence of SEQ ID NO:114, SEQ ID NO:120, or SEQ ID NO:121.

9. A pharmaceutical composition comprising the polypeptide of claim 1 and a pharmaceutically suitable carrier.

10. A method for reducing body weight in a subject in need thereof comprising the step of administering to the subject a polypeptide comprising the amino acid sequence of SEQ ID NO:4, further comprising a substitution of Asp, Glu, lie, Val, D-Ser, Met, D-Ala, Trp, Asn, Leu, or α-aminoisobutyric acid for the Ser at position 2 and a pharmaceutically acceptable salt thereof.

11. The method of claim 10 , wherein the polypeptide further comprises one or more amino acid substitutions selected from