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New compounds as adenosine a1 receptor antagonists

The technology of a compound, -R1, is applied in the field of new compounds as adenosine A1 receptor antagonists, which can solve the problems of limited potency and selectivity disclosed

Active Publication Date: 2010-09-15
PALOBIOFARMA SL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A report (Ijzerman P, et al., J. Med. Chem. 2001, 44, 749-762) describes the selective A 1 Antagonist, but disclosed limited potency and selectivity, and results were obtained using rat adenosine receptors instead of human adenosine receptors

Method used

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  • New compounds as adenosine a1 receptor antagonists
  • New compounds as adenosine a1 receptor antagonists
  • New compounds as adenosine a1 receptor antagonists

Examples

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Embodiment 1

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Embodiment 3

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Abstract

This compounds correspond to the formula (I), where: R1 represents and aryl or heteroaryl group optionally substituted by one or more substituents selected from the group consisting of halogen atoms, straight or branched optionally substituted lower alkyl, cycloalkyl, hydroxy, straight or branched, optionally substituted lower alkoxy, cyano, or -CO2R', wherein R' represents a hydrogen atom or a straight or branched, optionally substituted lower alkyl group; R2 represents a group selected from: a) a straight or branched lower alkyl group substituted by one or more carboxylic groups (-COOH) andoptionally substituted by one or more halogen atoms; b) a cycloalkyl group substituted by one or more carboxylic groups (-COOH) and optionally substituted by one or more halogen atoms; c) a straight or branched alkylcycloalkyl or cycloalkylalkyl group substituted by one or more carboxylic groups (-COOH) and optionally substituted by one or more halogen atoms.

Description

field of invention The present invention relates to novel antagonists of adenosine receptors, in particular A 1 Antagonists of adenosine receptor subtypes, relating to the use of said compounds in the treatment of diseases susceptible to amelioration by antagonism of adenosine receptors, in particular in the treatment of cardiovascular, renal and respiratory diseases , these diseases are known by using A 1 Antagonists of adenosine receptors are improved, more specifically diseases such as congestive heart failure, renal failure, hypertension, hypotension during dialysis, ischemia, supraventricular arrhythmias, myocardial reperfusion injury, asthma, COPD and Allergic rhinitis, also relates to pharmaceutical composition comprising said compound. Background of the invention The effects of adenosine are via at least four receptors hitherto known as belonging to the G protein-coupled receptor family A 1 、A 2A 、A 2B and A 3 It is mediated by specific cell membrane receptors ...

Claims

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Application Information

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IPC IPC(8): C07D277/56C07D417/04A61K31/426A61P9/00
CPCC07D277/56C07D417/04A61P11/02A61P11/06A61P11/08A61P13/12A61P17/00A61P17/04A61P19/02A61P25/22A61P25/28A61P37/08A61P43/00A61P9/00A61P9/06A61P9/10A61P9/12A61K31/426
Inventor L·冈扎雷兹利奥J·A·卡马乔高梅兹
Owner PALOBIOFARMA SL
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