US6703365B2
Expired / Lapsed
US
⏱️ 0.0 years remaining
Glucagon-like insulinotropic peptides, compositions and methods
Assignee: Eli Lilly and Co
•
Filing: 2002-04-17
•
Granted: 2004-03-09
•
Expires: 2022-04-17
Abstract
Abstract The present invention provides novel complexes consisting of certain GLP-1 molecules associated with a divalent metal cation that is capable of co-precipitating with a GLP-1 molecule. Pharmaceutical compositions and methods of using such complexes for enhancing the expression of insulin in B-type islet cells is claimed, as is a method for treating maturity onset diabetes mellitus in mammals, particularly humans.
Inventors
- 👤 John A. Galloway
- 👤 James A. Hoffmann
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 10:13
CPC Classifications
C; C07; C07K; C07K17/00; C07K17/14; C07K14/00; C07K14/435; C07K14/575; C07K14/605; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/62; A61P; A61P3/00; A61P3/08; A61P3/10; A61P43/00; A61K38/00; Y; Y10; Y10S; Y10S977/00; Y10S977/70; Y10S977/773; Y10S977/902; Y10S977/904; Y10S977/915
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
116 words
A pharmaceutical composition comprising a compound of the formula: R 1 -X-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-SerTyr-Leu-Y-Gly-Gln-Ala-Ala-Lys-Z-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-R 2 wherein: R 1 is selected from the group consisting of L-histidine, D-histidine, desamino-histidine, 2-amino-histidine, β-hydroxy-histidine, homohistidine, alpha-fluoromethyl-histidine, and alpha-methyl-histidine; X is selected from the group consisting of Gly, Val, Thr, Ile, and alpha-methyl-Ala; Y is selected from the group consisting of Glu, Gln, Ala, Thr, Ser, and Gly; Z is selected from the group consisting of Glu, Gln, Ala, Thr, Ser, and Gly; R 2 is selected from the group consisting of NH 2 , and Gly-OH; wherein the compound is complexed with a macromolecule selected from the group consisting of: a polyester, a polyamino acid, polyvinylpyrrolidone, methyl cellulose, carboxymethylcellulose and protamine sulfate.
Claim 2
Dependent Claim
116 words
A pharmaceutical composition comprising a compound of the formula: R 1 -X-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-SerTyr-Leu-Y-Gly-Gln-Ala-Ala-Lys-Z-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-R 2 wherein: R 1 is selected from the group consisting of L-histidine, D-histidine, desamino-histidine, 2-amino-histidine, β-hydroxy-histidine, homohistidine, alpha-fluoromethyl-histidine, and alpha-methyl-histidine; X is selected from the group consisting of Gly, Val, Thr, Ile, and alpha-methyl-Ala; Y is selected from the group consisting of Glu, Gln, Ala, Thr, Ser, and Gly; Z is selected from the group consisting of Glu, Gln, Ala, Thr, Ser, and Gly; R 2 is selected from the group consisting of NH 2 , and Gly-OH; wherein the compound is complexed with a macromolecule selected from the group consisting of: a polyester, a polyamino acid, polyvinylpyrrolidone, methyl cellulose, carboxymethylcellulose and protamine sulfate.
Claim 3
Dependent Claim
13 words
The pharmaceutical composition of claim 1 , wherein the macromolecule is protamine sulfate.
Claim 4
Dependent Claim
98 words
A pharmaceutical composition comprising a compound of the formula: R 1 -X-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Y-Gly-Gln-Ala-Ala-Lys-Z-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-R 2 wherein: R 1 is selected from the group consisting of L-histidine, D-histidine, desamino-histidine, 2-amino-histidine, β-hydroxy-histidine, homohistidine, alpha-fluoromethyl-histidine, and alpha-methyl-histidine; X is selected from the group consisting of Gly, Val, Thr, Ile, and alpha-methyl-Ala; Y is selected from the group consisting of Glu, Gln, Ala, Thr, Ser, and Gly; Z is selected from the group consisting of Glu, Gln, Ala, Thr, Ser, and Gly; R 2 is selected from the group consisting of NH 2 , and Gly-OH; wherein the compound is entrapped in a microcapsule.
Claim 5
Dependent Claim
98 words
A pharmaceutical composition comprising a compound of the formula: R 1 -X-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Y-Gly-Gln-Ala-Ala-Lys-Z-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-R 2 wherein: R 1 is selected from the group consisting of L-histidine, D-histidine, desamino-histidine, 2-amino-histidine, β-hydroxy-histidine, homohistidine, alpha-fluoromethyl-histidine, and alpha-methyl-histidine; X is selected from the group consisting of Gly, Val, Thr, Ile, and alpha-methyl-Ala; Y is selected from the group consisting of Glu, Gln, Ala, Thr, Ser, and Gly; Z is selected from the group consisting of Glu, Gln, Ala, Thr, Ser, and Gly; R 2 is selected from the group consisting of NH 2 , and Gly-OH; wherein the compound is entrapped in a microcapsule.
Claim 6
Dependent Claim
23 words
The pharmaceutical composition of claim 1 wherein R1 is L-histidine; X is Val; Y is Glu; Z is Glu; and R2 is Gly-OH.
Claim 7
Dependent Claim
24 words
The pharmaceutical composition of claim 2 , wherein R1 is L-histidine; X is Val; Y is Glu; Z is Glu; and R2 is Gly-OH.
Claim 8
Dependent Claim
23 words
The pharmaceutical composition of claim 3 , wherein R1 L-histidine; X is Val; Y is Glu; Z is Glu; and R2 is Gly-OH.
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