Novel effectors of dipeptidyl peptidase IV

a technology of dipeptidyl peptidase and effectors, which is applied in the field of new effectors of dipeptidyl peptidase iv, can solve the problems of serious vascular changes, high cost, and distinct impairment of the quality of life of patients, and achieve the effect of simple treatment methods

Inactive Publication Date: 2005-09-15
PROSIDION LIMITED
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Benefits of technology

[0012] The aim of the invention is therefore to provide new (especially activity-reducing) effectors for the treatment of e.g. impaired glucose tolerance, glycosuria, hyperlipidae

Problems solved by technology

All methods known hitherto, including more modern procedures, are distinguished by the requirement of a large amount of material, by high costs and often by a distinct impairment of the quality of life of the patients.
The conventional method (daily i.v. insulin injection, customary since the 1930s) treats the acute symptoms of the disease, but after prolonged use leads inter alia to serious vascular changes (arteriosclerosis) and nerve damage.
Such transplants require a high level of technical resources.
Furthermore, they involve a surgical intervention into the recipient organism, which is associated with

Method used

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  • Novel effectors of dipeptidyl peptidase IV
  • Novel effectors of dipeptidyl peptidase IV

Examples

Experimental program
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Effect test

Embodiment Construction

[0018] On administration, preferably oral administration, of these effectors to a mammalian organism, the endogenous (or additionally exogenously administered) insulinotropic peptides GIP1-42 and GLP-17-36 (or alternatively GLP-17-37 or analogues thereof) are broken down to a reduced extent by DP IV or DP IV-like enzymes and therefore the decrease in the concentration of those peptide hormones or their analogues is reduced or delayed. The invention is therefore based on the finding that a reduction in the DP IV or DP IV-like enzymatic activity acting in the blood circulation has an effect on the blood sugar level. It has been found that [0019] 1. the reduction in DP IV or DP IV-analogous activity leads to an increase in the relative stability of the glucose-stimulated or externally introduced incretins (or analogues thereof), that is to say by administration of effectors of DP IV or DP IV-analogous proteins it is possible to control the breakdown of incretin in the blood; [0020] 2. ...

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Abstract

Dipeptide compounds and compounds analogous to dipeptide compounds that are formed from an amino acid and a thiazolidine or pyrrolidine group, and salts thereof used in the treatment of impaired glucose tolerance, glycosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy and also of sequelae of diabetes mellitus in mammals.

Description

CROSS REFERENCE TO OTHER APPLICATIONS [0001] The present application is a continuation of application U.S. Ser. No. 10 / 361,956, filed on Feb. 10, 2003, which is a continuation of application U.S. Ser. No. 09 / 723,638, filed on Nov. 28, 2000, which claims priority of DE 198 / 23831.2 filed on May 28, 1998 and subsequent PCT EP 99 / 03712 application filed on May 28, 1999.BACKGROUND OF THE INVENTION [0002] According to the current state of the art, hyperglycaemia and associated causes and sequelae (including diabetes mellitus) are treated by the administration of insulin (e.g. material isolated from bovine pancreas or obtained by genetic engineering techniques) to the diseased organisms in various forms of administration. All methods known hitherto, including more modern procedures, are distinguished by the requirement of a large amount of material, by high costs and often by a distinct impairment of the quality of life of the patients. The conventional method (daily i.v. insulin injection...

Claims

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Application Information

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IPC IPC(8): A61K31/40A61K31/425C07D295/18A61K31/426A61K31/427A61K31/495A61K38/00A61K45/06A61P3/06A61P3/10A61P13/12A61P43/00C07D207/34C07D277/04C07D295/185C07D417/00C07D417/12C07K5/06
CPCA61K31/40A61K31/425A61K31/426A61K31/427A61K45/06C07D277/04C07D295/185A61K2300/00A61P1/00A61P13/12A61P3/10A61P3/06A61P43/00A61K38/05
Inventor DEMUTH, HANS-ULRICHGLUND, KONRADSCHLENZIG, DAGMARKRUBER, SUSANNE
Owner PROSIDION LIMITED
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