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1,3-thiazol-2-yl substituted benzamides for the treatment of diseases associated with nerve fiber sensitization

An alkyl-based, multi-purpose technology, applied in the direction of nervous system diseases, respiratory system diseases, cardiovascular system diseases, etc., can solve the problems of inability to chemically reflect hypersensitivity and abnormal taste

Pending Publication Date: 2021-02-19
BAYER AG +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These shortcomings include the inability to directly target chemoreflex hypersensitivity and taste abnormalities associated with dual P2X2 / 3 blockade

Method used

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  • 1,3-thiazol-2-yl substituted benzamides for the treatment of diseases associated with nerve fiber sensitization
  • 1,3-thiazol-2-yl substituted benzamides for the treatment of diseases associated with nerve fiber sensitization
  • 1,3-thiazol-2-yl substituted benzamides for the treatment of diseases associated with nerve fiber sensitization

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Embodiment Construction

[0058] The terms mentioned herein preferably have the following meanings:

[0059] The terms "halogen atom", "halo-" or "halo-" are understood to mean fluorine, chlorine, bromine or iodine atoms, preferably fluorine or chlorine atoms.

[0060] The term "alkyl" is understood to mean a linear or branched saturated monovalent hydrocarbon radical having the indicated number of carbon atoms, usually in the R 2 2 to 6 carbon atoms in the case of , and 1 to 4, preferably 1-3 carbon atoms in the case of all other alkyl substituents, for example and preferably methyl, ethyl, propyl, butyl, pentyl, Hexyl, isopropyl, isobutyl, sec-butyl, tert-butyl, isopentyl, 2-methylbutyl, 1-methylbutyl, 1-ethylpropyl, 1,2-dimethyl Propyl, neopentyl, 1,1-dimethylpropyl, 4-methylpentyl, 3-methylpentyl, 2-methylpentyl, 1-methylpentyl, 2-ethylbutyl base, 1-ethylbutyl, 3,3-dimethylbutyl, 2,2-dimethylbutyl, 1,1-dimethylbutyl, 2,3-dimethylbutyl, 1 ,3-Dimethylbutyl or 1,2-dimethylbutyl or isomers thereof. ...

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Abstract

The present invention relates to use 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprisingsaid compounds for the treatment or prophylaxis of diseases which are associated with nerve fiber sensitization, and / or other pathological conditions associated with autonomic imbalance caused by increased chemoreceptor sensitivity, in particular for the treatment of breathing disorders, Cheyne Stokes respiration, central and obstructive sleep apnea, cardiovascular disease, hypertension, resistant hypertension, and heart failure, which are related to increased activity of P2X3 receptors.

Description

[0001] The present invention relates to the use of 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as a single agent or in combination with other active ingredients, as well as pharmaceutical compositions and combinations comprising said compounds Use of a substance for the treatment or prevention of diseases related to nerve fiber sensitization and / or autonomic nervous disorders, especially cardiovascular diseases, heart failure and hypertension. Background technique [0002] The present invention relates to the use of chemical compounds inhibiting P2X3 receptors in treating diseases related to nerve fiber sensitization. P2X purinoceptor 3 is a human protein encoded by the P2RX3 gene (Garcia-Guzman M, Stuehmer W, Soto F, 1997, Brain Res Mol Brain Res 47(1-2):59-66). The product of this gene belongs to the ATP purinoceptor family. This receptor acts as a ligand-gated ion channel and transduces ATP-induced nociceptor activation. [0003] P2X purinergic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/427A61P9/10A61P9/04A61P25/28A61P9/12
CPCA61K31/427A61P9/04A61P9/10A61P9/12A61P25/28A61K31/506A61K31/5377A61K9/0053A61P11/00
Inventor L·H·霍夫梅斯特O·M·费舍尔
Owner BAYER AG
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