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Glucagon analogues

A compound and residue technology, applied in glucagon, hormone peptides, drug combinations, etc., can solve the problem that the mechanism of action of oxyntomodulin is not very clear.

Inactive Publication Date: 2013-04-24
ZEALAND PHARM AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The mechanism of action of oxyntomodulin is not well understood

Method used

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preparation example Construction

[0387] The peptide components of the compounds of the invention may be prepared by standard synthetic methods, by using recombinant expression systems, or any other suitable method. Thus, the peptides can be synthesized in a variety of ways including, for example, methods comprising:

[0388] (a) peptide synthesis by stepwise synthesis or by fragment assembly, using solid or liquid phase methods, and isolation and purification of the final peptide product; or

[0389] (b) expressing the nucleic acid construct encoding the peptide in a host cell and recovering the expression product from the host cell culture; or

[0390](c) performing cell-free in vitro expression of the nucleic acid construct encoding the peptide, and recovering the expression product;

[0391] Or use any combination of methods (a), (b) and (c) to obtain peptide fragments, which are subsequently ligated to obtain complete peptides, and the peptides are recovered.

[0392] Compounds of the invention may ofte...

Embodiment 1

[0482] Example 1: Efficacy on GLP-1 and Glucagon Receptors

[0483] The potency of the compounds of the invention was assessed by exposing cells expressing human glucagon-R and human GLP-1R to increasing concentrations of the compounds listed in Table 1 below and measuring the cAMP formed as described in the Methods section above .

[0484] The EC of the compound of the present invention is shown in table 1 50 Results, and corresponding values ​​for human glucagon and human GLP-1 as reference compounds:

[0485] Table 1. Effects of compounds of the invention on GLP-1 and glucagon receptors (EC 50 )

[0486]

[0487]

[0488]

[0489] a Regarding the re-measurement relative to the earlier determination value of 23.

[0490] b Re-determination relative to an earlier determination of 3.0.

[0491] c Re-assay relative to earlier determination of 0.89.

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Abstract

The invention provides materials and methods for promoting weight loss or preventing weight gain and for treating diabetes and associated metabolic disorders. In particular, the invention provides novel glucagon analogue peptide compounds effective in such methods. The compounds may mediate their effect by having, for example, increased selectivity for the GLP-1 receptor compared to human glucagon.

Description

technical field [0001] The present invention relates to glucagon analogs and their medical use, for example in the treatment of obesity and diabetes. Background technique [0002] Obesity and diabetes are growing global health problems and they are associated with a variety of diseases, notably cardiovascular disease (CVD), obstructive sleep apnea, stroke, peripheral arterial disease, microvascular complications and osteoarthritis. [0003] About 250 million people worldwide suffer from diabetes, and it is estimated that 380 million people will suffer from diabetes by 2025. Many had additional cardiovascular risk factors, including high / abnormal LDL and triglycerides and low HDL. [0004] Cardiovascular disease accounts for approximately 50% of deaths in people with diabetes, and the morbidity and mortality associated with obesity and diabetes underscores the medical need for effective treatment options. [0005] Preproglucagon is a 158 amino acid precursor polypeptide tha...

Claims

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Application Information

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IPC IPC(8): C07K14/605A61K38/26A61P5/48
CPCC07K14/605A61P3/04A61P3/06A61P43/00A61P5/48A61P9/00A61P9/10A61P9/12A61P3/10A61K38/26A61K45/06A61K38/00
Inventor 迪特·里贝尔埃迪·迈尔
Owner ZEALAND PHARM AS
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