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US5574008A Expired / Lapsed US ⏱️ 0.0 years remaining

Biologically active fragments of glucagon-like insulinotropic peptide

Assignee: Eli Lilly and Co
•
Filing: 1994-08-30
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Granted: 1996-11-12
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Expires: 2014-08-30
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Abstract

Abstract N-terminal truncated forms of glucagon like insulinotropic peptide (GLP-1) and analogs thereof are provided. The claimed polypeptides promote glucose uptake by cells but do not stimulate insulin expression or secretion. The invention also provides methods for treating diabetes and pharmaceutical formulations comprising the claimed polypeptides.

Inventors

  • 👤 William T. Johnson
  • 👤 Fatima E. Yakubu-Madas

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 14:26
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/605; A; A61; A61K; A61K38/00

Claims Analysis

Total Claims: 24
Claim 1
Independent Claim 89 words
A GLP- 1 fragment of the formula: R.sup.1 -Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-TrP-Leu-Val-X-Gly-Arg-R.sup.2 (SEQ ID NO:1) wherein R 1 is selected from the group consisting of: a) H 2 N-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser (SEQ ID NO:7); and, b) H 2 N-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser (SEQ ID NO:8); X is selected from the group consisting of Lys and Arg; and wherein R 2 is selected from the group consisting of NH 2 , OH, Gly-NH 2 , and Gly-OH, with the proviso that when R 1 is b) and R 2 is Gly-NH 2 or Gly-OH, X must be Arg.
Claim 2
Dependent Claim 89 words
A GLP- 1 fragment of the formula: R.sup.1 -Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-TrP-Leu-Val-X-Gly-Arg-R.sup.2 (SEQ ID NO:1) wherein R 1 is selected from the group consisting of: a) H 2 N-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser (SEQ ID NO:7); and, b) H 2 N-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser (SEQ ID NO:8); X is selected from the group consisting of Lys and Arg; and wherein R 2 is selected from the group consisting of NH 2 , OH, Gly-NH 2 , and Gly-OH, with the proviso that when R 1 is b) and R 2 is Gly-NH 2 or Gly-OH, X must be Arg.
Claim 3
Dependent Claim 19 words
The GLP-1 fragment of claim 1 that has the amino acid sequence: H 2 N-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-NH 2 (SEQ ID NO:9).
Claim 4
Dependent Claim 20 words
A pharmaceutical composition comprising the GLP-1 fragment of claim 2 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.
Claim 5
Dependent Claim 34 words
A method of treating diabetes in a mammal comprising administering to a mammal in need of such treatment an effective amount of the GLP-1 fragment of claim 2, or a pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim 12 words
The method of claim 4 wherein the mammal is a human being.
Claim 7
Dependent Claim 34 words
A method of treating diabetes in a mammal comprising administering to a mammal in need of such treatment an effective amount of a GLP-1 fragment of claim 1, or a pharmaceutically acceptable salt thereof.
Claim 8
Dependent Claim 12 words
The method of claim 6 wherein the mammal is a human being.
Claim 9
Dependent Claim 19 words
The GLP-1 fragment of claim 1 that has the amino acid sequence: H 2 N-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-NH 2 (SEQ ID NO:13).
Claim 10
Dependent Claim 20 words
A pharmaceutical composition comprising the GLP-1 fragment of claim 8 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.
Claim 11
Dependent Claim 34 words
A method of treating diabetes in a mammal comprising administering to a mammal in need of such treatment an effective amount of the GLP-1 fragment of claim 8, or a pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim 12 words
The method of claim 10 wherein the mammal is a human being.
Claim 13
Dependent Claim 18 words
The GLP-1 fragment of claim 1 that has the amino acid sequence: H 2 N-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-Gly-OH (SEQ ID NO:10).
Claim 14
Dependent Claim 20 words
A pharmaceutical composition comprising the GLP-1 fragment of claim 12 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.
Claim 15
Dependent Claim 34 words
A method of treating diabetes in a mammal comprising administering to a mammal in need of such treatment an effective amount of the GLP-1 fragment of claim 12, or a pharmaceutically acceptable salt thereof.
Claim 16
Dependent Claim 12 words
The method of claim 14 wherein the mammal is a human being.
Claim 17
Dependent Claim 19 words
The GLP-1 fragment of claim 1 that has the amino acid sequence: H 2 N-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-NH 2 (SEQ ID NO:11).
Claim 18
Dependent Claim 20 words
A pharmaceutical composition comprising the GLP-1 fragment of claim 16 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.
Claim 19
Dependent Claim 34 words
A method of treating diabetes in a mammal comprising administering to a mammal in need of such treatment an effective amount of the GLP-1 fragment of claim 16, or a pharmaceutically acceptable salt thereof.
Claim 20
Dependent Claim 12 words
The method of claim 18 wherein the mammal is a human being.
Claim 21
Dependent Claim 20 words
A pharmaceutical composition comprising a GLP-1 fragment of claim 1 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.
Claim 22
Independent Claim 31 words
A method of treating diabetes in a mammal comprising administering to a mammal in need of such treatment an effective amount of a GLP-1 fragment having the amino acid sequence: ##STR1##
Claim 23
Independent Claim 31 words
A method of treating diabetes in a mammal comprising administering to a mammal in need of such treatment an effective amount of a GLP-1 fragment having the amino acid sequence: ##STR1##
Claim 24
Dependent Claim 12 words
The method of claim 21 wherein the mammal is a human being.

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3.5 Years (Year 4) 1999-11-12 2000-05-13 2000-11-12 $2000.00 Window Closed / Lapsed
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