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Peptide for treating obesity

The technology of a compound, x1-x2-x3-arg-x4-x5, is applied in the field of application of the compound in the preparation of medicines, and can solve problems such as obesity

Inactive Publication Date: 2007-10-10
NOVO NORDISK AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Furthermore, studies on ectopic central expression of agouti proteins (MC1, MC3 and MC4 antagonists) or overexpression of endogenously produced MC3 and MC4 antagonists (agouti gene-related peptide, AGRP) in the mouse brain Studies have shown that overexpression of these two antagonists leads to the development of obesity [Kleibig et al., PNAS 92, 4728-4732 (1995)]

Method used

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  • Peptide for treating obesity
  • Peptide for treating obesity
  • Peptide for treating obesity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0260] 2-[2-(Hexadecanoylamino)ethoxy]ethoxyacetyl-His-Ser-Nle-c[Glu-Asn-D-Phe-Arg-Trp-Lys]-NH 2

[0261]

[0262] Step A of Example 1: Protected Peptide Resin Fmoc-Nle-c[Glu-Asn(Trt)-D-Phe-Arg(Pbf)-Trp-Lys]-NH-Rink Linker-Polystyrene

[0263] Fmoc-Rink resin (4-(2′,4′-dimethoxyphenyl-Fmoc-aminomethyl)-phenoxy polystyrene resin, Bachem D-2080, Lot 514460; 0.47mmol / g) Charge into two 60 ml Teflon reactors with glaze (each reactor: 3.55 g, 1.67 mmol). The resin in each reactor was washed with DCM (30ml).

[0264] Branching of Fmoc: The resin was shaken with 20% piperidine in NMP (25 ml) for 20 min, then washed with NMP / DCM 1:1 (5 x 30 ml).

[0265] Acylation with Fmoc-Lys(Mtt)-OH: In a separate glass vial, Fmoc-amino acid (10.0 mmol) was mixed with NMP (12.5 ml), DCM (22.5 ml) and 1M 1-hydroxybenzotriazole ( HOBt) in NMP (10.0 ml, 10.0 mmol) were mixed. To the resulting clear solution was added DIC (1.56ml, 10.0mmol) rapidly and the solution was shaken immediately. The ...

Embodiment 2

[0286] 2-[2-(Hexadecanoylamino)ethoxy]ethoxyacetyl-Gln-Ser-Nle-c[Glu-Asn-D-Phe-Arg-Trp-Lys]-NH 2

[0287]

[0288] LCMS (system 1): Rt = 4.49 min; ((m+2) / 2) = 787.

Embodiment 3

[0290] 2-[2-(2-{2-[2-(tetradecanoylamino)ethoxy]ethoxy}acetylamino)ethoxy]ethoxyacetyl-Nle-c[Glu-Asn -D-Phe-Arg-Trp-Lys]-NH 2

[0291]

[0292] LCMS (system 1): Rt = 4.30 min; ((m+2) / 2) = 738.

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Abstract

The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity.

Description

field of invention [0001] The present invention relates to novel peptide compounds which are ligands for one or more melanocortin receptors and which can exert prolonged activity, to the use of said compounds in therapy, to the administration of said compounds to The method of treatment of patients also relates to the use of said compound in the preparation of medicaments. Background of the invention [0002] Obesity is a well-known risk factor for the development of many common diseases such as atherosclerosis, hypertension, type II diabetes (non-insulin-dependent diabetes mellitus (NIDDM)), dyslipidemia, coronary heart disease, osteoarthritis, and various malignancies . It can also cause significant problems through reduced mobility and reduced quality of life. The incidence of obesity and the resulting diseases is increasing in all industrialized countries. To date, only a few pharmacological treatments are available, namely sibutramine (Abbot; acts via serotonergic an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/68A61K38/34C07K7/50C07K7/64A61K38/12A61K47/48
CPCC07K7/56A61K38/00C07K14/68C07K14/72A61P1/16A61P15/10A61P19/02A61P3/10A61P35/00A61P3/04A61P3/06A61P39/00A61P43/00A61P9/00A61P9/10A61P9/12
Inventor U·森斯富斯L·克里斯滕森
Owner NOVO NORDISK AS