US6593295B2
Expired / Lapsed
US
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Long lasting insulinotropic peptides
Assignee: Conjuchem LLC
•
Filing: 2001-06-06
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Granted: 2003-07-15
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Expires: 2021-06-06
Abstract
Abstract Modified insulinotropic peptides are disclosed. The modified insulinotropic peptides are capable of forming a peptidase stabilized insulinotropic peptide. The modified insulinotropic peptides are capable of forming covalent bonds with one or more blood components to form a conjugate. The conjugates may be formed in vivo or ex vivo. The modified peptides are administered to treat humans with diabetes and other related diseases.
Inventors
- 👤 Dominique P. Bridon
- 👤 Benoit L'Archeveque
- 👤 Alan M. Ezrin
- 👤 Darren L. Holmes
- 👤 Anouk Leblanc
- 👤 Serge St. Pierre
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 10:13
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/005; A; A61; A61P; A61P25/00; A61P25/08; A61P25/14; A61P25/18; A61P25/20; A61P25/22; A61P25/24; A61P25/28; A61P3/00; A61P3/04; A61P3/08; A61P3/10; A61P35/00; A61P41/00; C07K14/435; C07K14/575; C07K14/605; A61K; A61K38/00; C12; C12N; C12N2740/00; C12N2740/00011; C12N2740/10011; C12N2740/16011; C12N2740/16111; C12N2740/16122
Claims Analysis
Total Claims: 31
Claim 1
Independent Claim
27 words
A modified insulinotropic peptide comprising an insulinotropic peptide provided with a maleimide group which reacts with thiol groups on blood components to form a stable covalent bond.
Claim 2
Dependent Claim
27 words
A modified insulinotropic peptide comprising an insulinotropic peptide provided with a maleimide group which reacts with thiol groups on blood components to form a stable covalent bond.
Claim 3
Dependent Claim
26 words
A modified peptide as claimed in claim 1 wherein the insulinotropic peptide is selected from the group consisting of GLP-1, exendin-3, exendin-4, or a derivative thereof.
Claim 4
Dependent Claim
19 words
A modified insulinotropic peptide as claimed in claim 1 , wherein the peptide is GLP-1 or a derivative thereof.
Claim 5
Dependent Claim
70 words
A modified insulinotropic peptide as claimed in claim 1 , selected from the group consisting of GLP-1(1-36)-Lys 37 (ε-(AEEA) n -MPA)-NH 2 ; GLP-1 (7-36)-Lys 37 (ε-(AEEA) n MPA)-NH 2 ; exendin-4 (1-39)-Lys40 (ε-(AEEA) n -MPA)-NH 2 ; exendin-3 (1-39)-Lys 40 (ε-(AEEA) n -MPA)-NH 2 ; exendin-4 (1-39)-Lys40 (ε-(AEEA) n -MPA)-NH 2 ; Lys 26 ε-(AEEA) n -MPA GLP-1 (7-36)-NH 2 ; GLP-1 (7-36)-EDA-MPA; and exendin 4 (1-39)-EDA-MPA, wherein n=0-2.
Claim 6
Dependent Claim
59 words
A modified insulinotropic peptide as claimed in claim 4 , selected from the group consisting of GLP-1 (1-36)-Lys 37 (ε-MPA)-NH 2 , GLP-1 (1-36)-Lys 37 (ε-AEEA-AEEA-MPA)-NH 2 , GLP-1 (7-36)-Lys 37 (ε-MPA)-NH 2 , GLP-1 (7-36)-Lys 37 (ε-AEEA-AEEA-MPA)-NH 2 exendin-4 (1-39)-Lys 40 (ε-MPA)-NH 2 , exendin-4 (1-39)-Lys 40 (ε-AEEA-AEEA-MPA)-NH 2 , exendin-3(1-39)-Lys 40 (ε-MPA)-NH 2 and exendin-3(1-39)-Lys 40 (ε-AEEA-AEEA-MPA).
Claim 7
Dependent Claim
27 words
A method for treating diabetes in a patient, comprising administering to the patient an effective amount of a modified insulinotropic peptide as claimed in claim 1 .
Claim 8
Dependent Claim
27 words
A method for treating diabetes in a patient, comprising administering to the patient an effective amount of a modified insulinotropic peptide as claimed in claim 3 .
Claim 9
Dependent Claim
27 words
A method for treating diabetes in a patient, comprising administering to the patient an effective amount of a modified insulinotropic peptide as claimed in claim 4 .
Claim 10
Dependent Claim
30 words
A method for enhancing the expression of insulin in a patient, comprising administering to the patient an effective amount of a modified insulinotropic peptide as claimed in claim 1 .
Claim 11
Dependent Claim
30 words
A method for enhancing the expression of insulin in a patient, comprising administering to the patient an effective amount of a modified insulinotropic peptide as claimed in claim 3 .
Claim 12
Dependent Claim
30 words
A method for enhancing the expression of insulin in a patient, comprising administering to the patient an effective amount of a modified insulinotropic peptide as claimed in claim 4 .
Claim 13
Dependent Claim
18 words
A conjugate comprising a modified insulinotropic peptide as claimed in claim 1 covalently bonded to a blood component.
Claim 14
Dependent Claim
18 words
A conjugate comprising a modified insulinotropic peptide as claimed in claim 3 covalently bonded to a blood component.
Claim 15
Dependent Claim
18 words
A conjugate comprising a modified insulinotropic peptide as claimed in claim 4 covalently bonded to a blood component.
Claim 16
Dependent Claim
14 words
A conjugate as claimed in claim 12 wherein the blood component is serum albumin.
Claim 17
Dependent Claim
14 words
A conjugate as claimed in claim 13 wherein the blood component is serum albumin.
Claim 18
Dependent Claim
14 words
A conjugate as claimed in claim 14 wherein the blood component is serum albumin.
Claim 19
Independent Claim
52 words
A method for extending the in vivo half-life of an insulinotropic peptide comprising coupling to the peptide a maleimide group that forms a covalent bond with a blood component in vivo, thereby forming a modified insulinotropic peptide having an in vivo half-life longer than the in vivo half-life of the insulinotropic peptide.
Claim 20
Independent Claim
52 words
A method for extending the in vivo half-life of an insulinotropic peptide comprising coupling to the peptide a maleimide group that forms a covalent bond with a blood component in vivo, thereby forming a modified insulinotropic peptide having an in vivo half-life longer than the in vivo half-life of the insulinotropic peptide.
Claim 21
Dependent Claim
25 words
A method as claimed in claim 18 wherein the insulinotropic peptide is selected from the group consisting of GLP-1, exendin-3, exendin-4 or a derivative thereof.
Claim 22
Dependent Claim
37 words
A method as claimed in claim 19 wherein the GLP-1 peptide is selected from the group consisting of GLP-1 (1-36)-Lys 37 , GLP-1(7-36)-Lys 37 and D-Ala 8 GLP-1(7-36)-Lys 37 , exendin-4 (1-39)-Lys 40 and exendin-3(1-39)-Lys 40 .
Claim 23
Dependent Claim
20 words
A pharmaceutical composition comprising a modified insulinotropic peptide as claimed in claim 1 in association with a pharmaceutically acceptable carrier.
Claim 24
Dependent Claim
20 words
A pharmaceutical composition comprising a modified insulinotropic peptide as claimed in claim 3 in association with a pharmaceutically acceptable carrier.
Claim 25
Dependent Claim
20 words
A pharmaceutical composition comprising a modified insulinotropic peptide as claimed in claim 4 in association with a pharmaceutically acceptable carrier.
Claim 26
Dependent Claim
18 words
A pharmaceutical composition comprising a conjugate as claimed in claim 12 in association with a pharmaceutically acceptable carrier.
Claim 27
Dependent Claim
18 words
A pharmaceutical composition comprising a conjugate as claimed in claim 13 in association with a pharmaceutically acceptable carrier.
Claim 28
Dependent Claim
18 words
A pharmaceutical composition comprising a conjugate as claimed in claim 14 in association with a pharmaceutically acceptable carrier.
Claim 29
Dependent Claim
18 words
A pharmaceutical composition comprising a conjugate as claimed in claim 15 in association with a pharmaceutically acceptable carrier.
Claim 30
Dependent Claim
18 words
A pharmaceutical composition comprising a conjugate as claimed in claim 16 in association with a pharmaceutically acceptable carrier.
Claim 31
Dependent Claim
18 words
A pharmaceutical composition comprising a conjugate as claimed in claim 17 in association with a pharmaceutically acceptable carrier.
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