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Piperidine GPCR agonists

A technology of CH2 and compounds, applied in the field of G protein-coupled receptor agonists, can solve problems such as dyslipidemia in a high proportion of patients

Inactive Publication Date: 2011-06-08
PROSIDION LIMITED
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Drugs targeting the pathophysiology associated with insulin-dependent type 1 diabetes and non-insulin-dependent type 2 diabetes have many potential side effects and are insufficient to address dyslipidemia and hyperglycemia in a high proportion of patients

Method used

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  • Piperidine GPCR agonists
  • Piperidine GPCR agonists
  • Piperidine GPCR agonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0211] Example 1: 4-{3-[1-(3-isopropyl-[1,2,4]oxadiazol-5-yl)piperidin-4-yl]propoxy}-2-methyl -N-(tetrahydropyran-4-yl)benzamide

[0212]

[0213] HOBt·H 2 O (46.0 mg, 338 micromoles) and EDCI (65.0 mg, 338 micromoles) were added to stirred 4-{3-[1-(3-isopropyl-[1,2,4] oxadiazol-5-yl)piperidin-4-yl]propoxy}-2-methylbenzoic acid (preparation 4, 100 mg, 260 micromoles) in solution. After 15 minutes, tetrahydropyran-4-ylamine (53.0 mg, 520 micromole) was added and the resulting mixture was stirred at ambient temperature for 16 hours. The THF was removed in vacuo and the residue was partitioned with EtOAc and 2M NaOH. The organic phase was separated and washed with 2M NaOH, 1M HCl and brine, then dried (MgSO 4 ). Filtration and solvent evaporation provided the title compound: RT = 3.69 min; m / z (ES + )=471.28[M+H] + (Method A).

[0214] Using a method similar to that outlined in Example 1, the amines listed in Table 1 were synthesized by condensing the appropriate acid ...

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Abstract

Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity.

Description

technical field [0001] The present invention is directed to G protein coupled receptor (GPCR) agonists. In particular, the invention is directed to agonists of GPR119 for use in the treatment of obesity, eg, as a modulator of satiety, metabolic syndrome, and in the treatment of diabetes. Background technique [0002] Obesity is characterized by excess adipose tissue mass relative to body size. Clinically, body fat mass is measured by body mass index (BMI; weight (kg) / height (m) 2 ) or waist circumference. When the BMI is greater than 30, the individual is considered obese, and being overweight has established medical consequences. It has been accepted medical opinion for some time that weight gain, especially as a result of abdominal body fat, is associated with increased diabetes, high blood pressure, heart disease and many other health complications such as arthritis, stroke, gallbladder disease, muscle and respiratory problems , back pain, and even the risk of certain...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D413/14A61K31/445A61P3/00
CPCC07D413/14A61P3/00A61P3/04A61P3/06A61P43/00A61P9/00A61P9/12A61P3/10
Inventor L·S·伯特伦M·C·T·法伊夫R·P·吉瓦兰特纳姆J·凯利
Owner PROSIDION LIMITED