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Details for Patent: 7,049,284

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Details for Patent: 7,049,284

Title:Glucagon-like peptide-2 and its therapeutic use
Abstract: Glucagon-like peptide 2, a product of glucagon gene expression, and analogs of glucagon-like peptide 2, have been identified as gastrointestinal tissue growth factors. Their effects on the growth of small bowel and pancreatic islets are described. Their formulation as a pharmaceutical, and their therapeutic use in treating disorders of the bowel, are described.
Inventor(s): Drucker; Daniel J. (Toronto, CA)
Assignee: 1149336 Ontario Inc. (Toronto, CA)
Filing Date:Nov 20, 2002
Application Number:10/042,746
Claims:1. A method for improving the function of gastrointestinal tissue in a patient in need thereof, comprising the step of administering to the patient an effective amount of a pharmaceutical composition comprising GLP-2 to enhance the nutritional absorption of the small intestine.

2. A method for improving the function of gastrointestinal tissue in a patient in need thereof, comprising the step of administering to the patient an effective amount of a pharmaceutical composition to enhance the nutritional absorption of the small intestine, wherein said pharmaceutical composition comprises a GLP-2, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, which has the formula (SEQ ID NO. 1): R1-(Y)m-His-Ala-Asp-Gly-Ser-Phe-Ser-Asp-Glu-Met-Asn-Thr-aa1-Leu-Asp-aa2-L- eu-Ala-aa3-aa4-Asp-Phe-Ile-Asn-Trp-Leu-aa5-aa6-Thr-Lys-Ile-Thr-Asp-(X) n-R2 wherein: aa1 is Met, Leu, Ile, Val or Cys; aa2 is Ala, Ser, Thr, Pro, Gly, Asn, Asp, Glu or Gln; aa3 is Ala, Ser, Thr, Pro or Gly; aa4 is His or Arg; aa5 is Met, Leu, Ile, Val or Cys; aa6 is Asn, Asp, Glu, Gln, His, Arg or Lys; X is His, Arg, Lys, His-His, His-Arg, His-Lys, Arg-His, Arg-Lys, Lys-His, or Lys-Lys; Y is one or two amino acids selected from the group consisting of His, Arg and Lys; m is 0 or 1; n is 0 or 1; R1 is H or an N-terminal blocking group; and R2 is OH or a C-terminal blocking group, wherein the GLP-2 or salt thereof is comprised of a naturally occurring GLP-2, and when aa1 is Ile, aa2 is Asn, aa3 is Ala, aa4 is Arg, aa5 is Ile, aa6 is Gln, and n is 1, then X is not Arg.

3. A method for improving the function of gastrointestinal tissue in a patient in need thereof, comprising the step of administering to the patient an effective amount of a pharmaceutical composition to enhance the nutritional absorption of the small intestine, wherein said pharmaceutical composition comprises a pharmaceutically acceptable salt of GLP-2, and a pharmaceutically acceptable carrier wherein the GLP-2 has the amino acid sequence (SEQ ID NO. 2): R1-(Y)m-His-Ala-Asp-Gly-Ser-Phe-Ser-Asp-Glu-Met-Asn-Thr-Ile-Leu-Asp-Asn-L- eu-Ala-aa3-Arg-Asp-Phe-Ile-Asn-Trp-Leu-Ile-Gin-Thr-Lys-Ile-Thr-Asp-(X) n-R2 wherein: aa3 is Ala, Ser, Thr, Pro or Gly; X is His, Arg, Lys, His-His, His-Arg, His-Lys, Arg-His, Arg-Lys, Lys-His, or Lys-Lys; Y is one or two amino acids selected from the group consisting of His, Arg and Lys; m is 0 or 1; n is 0 or 1; R1 is H or an N-terminal blocking group; R2 is OH or a C-terminal blocking group; and when aa3 is Ala and n is 1, then X is not Arg.
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