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Novel glucagon antagonists/inverse agonists

a technology of glucagon antagonists and inverse agonists, which is applied in the direction of drug compositions, peptide/protein ingredients, metabolic disorders, etc., can solve the problem of general knowledge that is not orally availabl

Inactive Publication Date: 2005-11-17
LAU JESPER +6
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, they are generally known not to be orally available because of degradation by physiological enzymes, and poor distribution in vivo.

Method used

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  • Novel glucagon antagonists/inverse agonists
  • Novel glucagon antagonists/inverse agonists
  • Novel glucagon antagonists/inverse agonists

Examples

Experimental program
Comparison scheme
Effect test

example 1

General Procedure (A)

3-(4-[(4-Cyclohex-1-enylphenyl)-(4-phenylthiazol-2-yl)amino]methyl}benzoylamino)propionic acid

[0154]

[0155] Fmoc-β-Ala-Wang resin (0.57 mmol / g, 50 μmol) was treated with piperidine (20% in NMP, 1000 μL) for 10 min and the resin was drained. This was repeated once. The resin was washed with NMP (6×1000 μL). 4-Carboxybenzaldehyde (0.5 M in NMP, 500 μL), HOBt (0.5 M in NMP, 500 μL) and DIC (0.5 M in toluene, 500 μL) were added and the resulting mixture was shaken for 15 hours at room temperature. The resin was drained and washed with DMF (3×1000 μL). The resulting resin-bound aldehyde was added the appropriate amine, in this case 4-(cyclohex-1-enyl)aniline, prepared as described in WO 00 / 69810 (1.0 M in NMP, 600 μL), NaCNBH3 (1.0 M in NMP:methanol (7:3), 600 μL) and acetic acid (140 μL). The resulting mixture was shaken for 9 hours at room temperature, drained and washed with MeOH (1000 μL) for 1 hour, followed by washing with with 5% DIPEA in methanol (1×) and NM...

example 2

General Procedure (A)

3-(4-{[(4-Cyclohexylphenyl)-(4-phenylthiazol-2-yl)amino]methyl}benzoylamino)propionic acid

[0158]

example 3

General Procedure (A)

3-(4{[(4-Cyclohexylphenyl)-(5-methyl-4-phenylthiazol-2-yl)amino]methyl}benzoylamino)propionic acid

[0159]

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Abstract

Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS [0001] This application is a continuation of U.S. application Ser. No. 10 / 448,529 filed on May 30, 2003 claims priority under 35 U.S.C. 119 of Danish application no. PA 2001 01789 filed Dec. 3, 2001, Danish application no. PA 2002 01006 filed on Jun. 27, 2002 and Danish application no. PA 2002 01927 filed on Dec. 17, 2002 and U.S. application Ser. No. 60 / 394,145 filed on Jul. 3, 2002 and U.S. provisional application No. 60 / 434,255 filed on Dec. 18, 2002, the contents of which are fully incorporated herein by reference.FIELD OF THE INVENTION [0002] The present invention relates to agents that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists. BACKGROUND OF THE INVENTION [0003] Glucagon is a key hormonal agent that, in co-operation with insulin, mediates homeostatic regulation of the amount of glucose in the blood. Glucagon primarily ac...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/195A61K31/198A61K31/41A61K31/4439A61K45/06
CPCA61K31/195A61K31/198A61K31/41A61K31/4439A61K45/06A61P3/00A61K2300/00
Inventor LAU, JESPERCHRISTENSEN, INGERMADSEN, PETERBLOCH, PAWBEHRENS, CARSTENKODRA, JANOSNIELSEN, POUL
Owner LAU JESPER
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