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Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto

A compound and hydrate technology, applied in metabolic diseases, active ingredients of heterocyclic compounds, drug combinations, etc., can solve problems such as increased risk of death without taking weight ratio into account

Inactive Publication Date: 2006-09-06
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 proportion of body weight that is muscle (adipose tissue) in relation to fat
[0015] As BMI increases, risk of death increases from multiple causes unrelated to other risk factors

Method used

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  • Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
  • Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
  • Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0958] The activity level 125 The synthetic methods for I binding to the target molecule include:

[0959] A. Sandmeyer and its analogous reactions-this procedure converts aromatic amines or heteroaromatic amines into (for example) the diazonium salt of tetrafluoroborate, and then uses Na 125 I convert it into 125 I-labeled compound. Zhu, D.-G. and their collaborators reported a representative procedure in J. Org. Chem. 2002, 67, 943-948.

[0960] B. Ortho position of phenol 125 Iodination-this program makes 125 I binds to phenol in the ortho position, as reported by Collier, T.L. and his collaborators in J.labelled Compd Radiopharm.1999, 42, S264-S266.

[0961] C. Aryl bromide and heteroaryl bromide and 125 I Interchange-This method is generally a two-step procedure. The first step is to use, for example, Pd to catalyze the reaction [ie Pd(Ph 3 P) 4 ] Or through aryllithium or heteroaryllithium in trihaloalkyl tin or hexaalkyl ditin [e.g. (CH 3 ) 3 SnSn(CH 3 ) 3 ] The presence of...

example

[0967] The examples are provided to further illustrate the present invention in detail without restricting the present invention to the details of these examples.

example 1

[0969] 96-well ring AMP membrane test of RUP3

[0970] material

[0971] 1) Purchasing Perkin Elmer's adenylate cyclase activation scintillation plate test kit-96-well (SMP004B) and the kit provided with the kit 125 I tracer (NEX130), placed in a box and stored in the refrigerator, and do not expose the scintillation plate to light.

[0972] 2) Creatine Phosphate-Sigma P-7936

[0973] 3) Creatine Phosphokinase-Sigma C-3755

[0974] 4) GTP-Sigma G-8877

[0975] 5)ATP-Sigma A-2383

[0976] 6) IBMX-Sigma I-7018

[0977] 7) Hepes-1M distilled water solution-Gibco#15630080

[0978] 8) MgCl 2 -SigmaM-1028-1M solution

[0979] 9) NaCl-Sigma-S6546-5M solution

[0980] 10) Bradford protein test kit-Biorad#5000001

[0981] 11) Proclin 300-Sigma#4-8126

[0982] Binding buffer -Filter through a 45-micron Nalgene filter and store in the refrigerator. All buffers and membranes should be kept cold (in an ice bucket) during testing.

[0983] 20mM Hepes, pH7.41 mM MgCl 2 100mM NaCl

[0984] 2×Reg...

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PUM

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Abstract

The present invention relates to certain fused aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

Description

Technical field [0001] The present invention relates to specific fused aryl and heteroaryl derivatives of glucose metabolism regulators. Therefore, the compounds of the present invention are used to prevent or treat metabolic disorders and their complications, such as diabetes and obesity. Background technique [0002] Diabetes is a serious disease that afflicts more than 100 million people worldwide. In the United States, there are more than 12 million people with diabetes, and 600,000 newly diagnosed cases each year. [0003] Diabetes is a diagnostic term for a class of disorders characterized by abnormal glucose homeostasis leading to hyperglycemia. There are many types of diabetes, but the two most common are type I diabetes (also known as insulin-dependent diabetes or IDDM) and type II diabetes (also known as non-insulin-dependent diabetes or NIDDM). [0004] The pathogens of different types of diabetes are different; however, every diabetic patient has two symptoms the same...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04C07D473/00C07D498/04C07D471/04C07D215/22A61K31/519A61K31/52A61K31/4375A61K31/47A61P3/00A61P3/10
Inventor 罗伯特·M·琼斯格雷姆·森普尔熊易峰辛泳俊任少君伊梅尔达·考尔德伦比阿特丽斯·菲奥拉万蒂金·孙·卡洛琳·蔡卡尔顿·R·塞奇
Owner ARENA PHARMA
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