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Fluorinated aminotriazole derivatives

A compound, trifluoromethyl technology, applied in the field of ALX receptor activator, can solve neuron toxicity and other problems

Inactive Publication Date: 2015-09-30
IDORSIA PHARM LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

While the accumulation of leukocytes at sites of tissue injury can be considered an innate host response to clearance of noxious agents, activated mononuclear phagocytes also release substances such as superoxide anion, which can be harmful to neurons. poisonous

Method used

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  • Fluorinated aminotriazole derivatives
  • Fluorinated aminotriazole derivatives
  • Fluorinated aminotriazole derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0576] 2-Methyl-5-m-tolyl-oxazole-4-carboxylic acid {2-[5-(1,1-difluoro-ethyl)-furan-2-ylmethyl]-2H-[1 ,2,3]triazol-4-yl}-amide:

[0577] Following general procedure A, from 2-[5-(1,1-difluoro-ethyl)-furan-2-ylmethyl]-2H-[1,2,3]triazol-4-ylamine with 2 -Methyl-5-m-tolyl-oxazole-4-carboxylic acid begins.

[0578] LC-MS-Conditions 02:t R =1.12 minutes; [M+H] + =427.83.

Embodiment 2

[0580]5-Phenyl-oxazole-4-carboxylic acid {2-[4-(1,1-difluoro-ethyl)-thiazol-2-ylmethyl]-2H-[1,2,3]triazole -4-yl}-amide:

[0581] Following general procedure A, from 2-[4-(1,1-difluoro-ethyl)-thiazol-2-ylmethyl]-2H-[1,2,3]triazol-4-ylamine with 5 -Phenyl-oxazole-4-carboxylic acid to start.

[0582] LC-MS-Conditions 01:t R =1.01 minutes; [M+H] + =416.90.

Embodiment 3

[0584] 2-Methyl-5-m-tolyl-oxazole-4-carboxylic acid {2-[4-(1,1-difluoro-ethyl)-thiazol-2-ylmethyl]-2H-[1 ,2,3]triazol-4-yl}-amide:

[0585] Following general procedure A, from 2-[4-(1,1-difluoro-ethyl)-thiazol-2-ylmethyl]-2H-[1,2,3]triazol-4-ylamine with 2 -Methyl-5-m-tolyl-oxazole-4-carboxylic acid begins.

[0586] LC-MS-Conditions 02:t R =1.10 minutes; [M+H] + =445.09.

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Abstract

The invention relates to fluorinated aminotriazole derivatives of formula (I), wherein A, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.

Description

technical field [0001] The present invention relates to fluorinated aminotriazole derivatives of formula (I) and their use as medicine. The invention also relates to related aspects, including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of formula (I), and especially their use as activators of the ALX receptor. Background technique [0002] ALXR (alias lipoxin A4 receptor, FPRL1, FPR2; disclosed in WO2003 / 082314 as nucleotide sequence SEQ ID NO: 1 and amino acid sequence SEQ ID NO: 2) is a member of the G-protein coupled receptor group. ALXR has been found to mediate calcium mobilization in response to high concentrations of formyl-methionine-leucyl-phenylalanine polypeptides. Furthermore, it has been found that a lipid metabolism product, lipoxin A4 (LXA4), and its analogs, bind ALXR with high affinity and increase arachidonic acid production and G-protein activation in ALXR-transfected cells ( Chiang et al....

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D413/14C07D417/14A61K31/4192A61P9/00
CPCC07D413/14C07D417/14A61P1/00A61P1/02A61P1/16A61P11/00A61P11/02A61P11/06A61P13/12A61P17/00A61P17/06A61P19/02A61P21/04A61P25/00A61P25/02A61P25/04A61P25/28A61P27/02A61P27/04A61P29/00A61P31/18A61P37/00A61P37/02A61P37/06A61P37/08A61P43/00A61P5/16A61P9/00A61P9/10A61P3/10C07D413/12A61K31/42
Inventor 丹尼尔·布尔奥利维尔·考米波夫塞尔文·库恩科琳娜·格里索斯托米泽维尔·莱罗尔西尔维娅·里卡德-比尔德斯滕
Owner IDORSIA PHARM LTD
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