Modulators of metabolism and the treatment of disorders related thereto

A related disease, effective dose technology, applied in the fields of metabolic diseases, medical preparations containing active ingredients, organic chemistry, 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

[0139] Example 1: In vivo effects of RUP3 agonists on glucose homeostasis in rats

[0140] General Procedures - Oral Glucose Tolerance Test (oGTT)

[0141] Male Sprague Dawley rats (Harlan, San Diego, CA) weighing approximately 350-375 g were fasted for 16 hours and randomized into groups (n=6) to receive 0.3 mg / kg, 3 mg / kg or 30 mg / kg of RUP3 agonist. Compounds were delivered orally (po, volume 2 mL / kg) via gavage needle. At the beginning of the test, blood glucose levels were assessed using a blood glucose meter (Accu-Chek Advantage, Roche Diagnostics), and vehicle (20% hydroxypropyl-β-cyclodextrin) was administered to the rats or test compounds. Thirty minutes after administration of the test compound, blood glucose levels were assessed again, and the rats were orally administered a dose of 3 g / kg dextrose. Blood glucose measurements were then taken 30 minutes, 60 minutes and 120 minutes after this point. RUP3 agonist 4-[5-methoxy-6-(2-methyl-6-[1,2,4]triazol-1-yl-pyri...

example 2

[0142] Example 2: Receptor Binding Assay

[0143] In addition to the methods described herein, another way to evaluate a test compound is by determining its binding affinity to the RUP3 receptor. Assays of this type typically require radiolabeled ligands for the RUP3 receptor. Without the use of known ligands for the RUP3 receptor and their radiolabelling, compounds of formula (I) can be labeled with a radioisotope and used in assays to assess the affinity of test compounds for the RUP3 receptor.

[0144] Radiolabeled RUP3 compounds of formula (I) can be used in screening assays to identify / evaluate compounds. In general, newly synthesized or newly identified compounds (ie, test compounds) can be assessed for their ability to reduce the binding of a "radiolabeled compound of formula (I)" to the RUP3 receptor. Thus, the ability of a test compound to compete with a "radiolabeled compound of formula (I)" or a radiolabeled RUP3 ligand for binding to the RUP3 receptor is directly...

example 3

[0156] The following examples further illustrate the compounds of the invention and their synthesis. The following examples are provided to further illustrate the invention without limiting the invention to the details of these examples. Compounds described herein are named according to CS ChemDrawUltra version 7.0.1. In certain instances, common names are used with the understanding that those skilled in the art will recognize such common names.

[0157] Chemistry: Proton NMR ( 1 H NMR) spectra were performed on a Varian Mercury Vx-400 equipped with 4-nuclei auto-switchable probes and a z-gradient field or equipped with QNP (Quad Nucleus Probe) or BBI (Broad Band Inverse) probe and z-gradient fields recorded on a Bruker Avance-400. Chemical shifts are expressed in parts per million (ppm) using the residual solvent signal as a reference. NMR abbreviations are used as follows: s = singlet, d = doublet, t = triplet, q = quartet, m = multiplet, br = broad. Microwave irradiat...

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Abstract

The present invention relates to 4-[5-Methoxy-6-(2-methyl-6-[1,2,4]triazol-1-yl-pyridin-3-ylamino)-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-[5-methoxy-6-(2-methyl-6-[1,2,4]triazol-1-yl-pyridin-3-ylamino)- Pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester and pharmaceutically acceptable salts, solvates and hydrates thereof. Accordingly, the compounds of the present invention are useful in the treatment of 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, with 600,000 new diagnoses each year. [0003] Diabetes mellitus is a diagnostic term for a group of disorders characterized by abnormal glucose homeostasis resulting in elevated blood sugar. There are many types of diabetes, but the two most common are type 1 diabetes (also known as insulin-dependent diabetes or IDDM) and type 2 diabetes (also known as non-insulin-depende...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/14A61P3/00A61K31/506
CPCC07D401/14A61P3/00A61P3/04A61P3/06A61P3/10A61K31/506
Inventor 罗伯特·M·琼斯于尔格·莱曼埃米·旭婷·汪
Owner ARENA PHARMA
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