Formula I Mineralocorticoid Receptor Antagonists for Cardiovascular Treatment

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Solution Overview

Problem

Current therapeutic options for hypertension and heart failure are suboptimal, and there is a need for additional pharmacological interventions that effectively target aldosterone-mediated disorders, including cardiovascular diseases.

Innovation Solution

Development of compounds with Mineralocorticoid Receptor (MR) antagonist activity, specifically represented by Formula I, which are designed to treat aldosterone-mediated disorders by antagonizing the MR, thereby addressing hypertension, heart failure, and other cardiovascular disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing therapeutic options are used for hypertension and heart failure, then current treatment protocols are maintained, but therapeutic effectiveness is suboptimal

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidtreatment options
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by developing new chemical compounds with modified molecular structures (Formula I) that exhibit enhanced MR antagonist activity. The structural variations in the compounds allow for optimized binding affinity and selectivity, thereby improving therapeutic effectiveness while providing novel treatment options beyond existing therapies

Inventive Principle:
Principle #35Parameter changes

2Reliability

If new MR antagonist compounds are developed, then therapeutic effectiveness is improved, but device complexity increases

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidcompound structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the complex molecular structure into distinct functional domains (Formula I components) that can be independently optimized. This modular approach allows for systematic development of compounds with improved efficacy while maintaining manageable structural complexity through defined substituent patterns

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP2765860B1Mineralocorticoid receptor antagonists
Publication Date: 2016.08.17 MERCK SHARP & DOHME CORP
  • EP2765860B1 patent drawing
  • EP2765860B1 patent drawing
  • EP2765860B1 patent drawing

AI summary

The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, that are aldosterone receptor antagonists which might be useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).