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Modulators of metabolism and the treatment of disorders related thereto

A related disease, effective dose technology, applied in the direction of metabolic diseases, medical preparations containing active ingredients, diseases, etc., can solve the problems of increased risk of death, failure to consider the proportion of muscle constitution, etc.

Inactive Publication Date: 2009-07-15
ARENA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The problem with this definition is that it does not take into account the body mass ratio of muscle to fat (adipose tissue)
[0016] Risk of death from multiple causes increases with increasing BMI independent of other risk factors

Method used

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  • Modulators of metabolism and the treatment of disorders related thereto
  • Modulators of metabolism and the treatment of disorders related thereto
  • Modulators of metabolism and the treatment of disorders related thereto

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0138] Example 1: In vivo effects of RUP3 agonists on glucose homeostasis in rats

[0139] General Procedure-Oral Glucose Tolerance Test (oGTT)

[0140] Male Sprague Dawley rats (Harlan, San Diego, California (CA)) weighing about 350-375g were fasted for 16 hours and randomly divided into groups (n=6) To receive 0.3mg / kg, 3mg / kg or 30mg / kg RUP3 agonist. The compound was delivered orally via a gavage needle (oral, volume 2 mL / kg). At the beginning of the test, a blood glucose meter (Accu-Chek Advantage, Roche Diagnostics) was used to assess blood glucose levels, and a vehicle (20% hydroxypropyl-β-cyclodextrin) was administered to rats Or test compound. Thirty minutes after the test compound was administered, the blood glucose level was evaluated again, and the rats were orally administered with 3 g / kg dextrose. Then blood glucose measurements were taken 30 minutes, 60 minutes, and 120 minutes after this time. RUP3 agonist 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methyl...

example 2

[0141] Example 2: Receptor binding assay

[0142] In addition to the methods described herein, another method of evaluating test compounds is by determining their binding affinity to the RUP3 receptor. This type of assay usually requires a radiolabeled ligand for the RUP3 receptor. Without using the known ligands of the RUP3 receptor and its radiolabel, the compound of formula (I) can be labeled with a radioisotope and used in the assay to evaluate the affinity of the test compound with the RUP3 receptor.

[0143] The radiolabeled RUP3 compound of formula (I) can be used in screening assays to identify / evaluate compounds. In general, the ability of newly synthesized or newly identified compounds (ie, test compounds) to reduce the ability of the "radiolabeled compound of formula (I)" to bind to the RUP3 receptor can be evaluated. Therefore, the ability of the test compound to compete with the "radiolabeled compound of formula (I)" or the radiolabeled RUP3 ligand for binding to the ...

example 3

[0155] The following examples further illustrate the compounds of the present invention and their synthesis. The following examples are provided to further illustrate the present invention, without restricting the present invention to the details of these examples. The compounds described in this article are named according to CS ChemDrawUltra version 7.0.1. In some cases, common names are used and those skilled in the art should recognize these common names.

[0156] Chemistry: Proton Nuclear Magnetic Resonance ( 1 H NMR spectrum is on Varian Mercury Vx-400 equipped with 4-core automatic switchable probe and z-gradient field or equipped with QNP (Quad Nucleus Probe) or BBI (Broad Band Inverse) probe and z-gradient field on Bruker Avance-400 (Bruker Avance-400). The chemical shift is expressed in parts per million (ppm), where the residual solvent signal is used as a reference. NMR abbreviations are used as follows: s = singlet, d = doublet, t = triplet, q = quartet, m = multiplet...

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Abstract

The present invention relates to 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methyl-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester, pharmaceutically acceptable salts, solvates and hydrates thereof that are modulators of glucose metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.

Description

Technical field [0001] The present invention relates to 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methyl-pyrimidin-4-yloxy]-piperidine as a glucose metabolism regulator Isopropyl-1-carboxylate and its pharmaceutically acceptable salts, solvates and hydrates. Therefore, the compounds of the present invention can be used to treat metabolic-related disorders and their complications, such as diabetes and obesity. Background technique [0002] Diabetes is a serious disease that affects more than 100 million people worldwide. In the United States, there are more than 12 million people with diabetes, of which 600,000 are newly diagnosed each year. [0003] Diabetes is a diagnostic term for a group of disorders characterized by abnormal glucose homeostasis leading to elevated blood sugar. There are many types of diabetes, but the two most common ones are type I diabetes (also known as insulin-dependent diabetes or IDDM) and type II diabetes (also known as non-insulin dependen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/14A61K31/506A61P3/00
CPCC07D401/14A61P13/12A61P15/00A61P15/10A61P17/00A61P19/02A61P19/10A61P25/00A61P27/02A61P27/12A61P3/00A61P3/04A61P35/00A61P3/06A61P3/08A61P9/00A61P9/04A61P9/10A61P9/12A61P3/10A61K31/506
Inventor 罗伯特·M·琼斯于尔格·莱曼
Owner ARENA PHARMA
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