Nitrooxy Cycloalkane Derivatives for Sustained Hypertension Treatment

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Solution Overview

Problem

Current treatments for hypertension, Pulmonary Arterial Hypertension, congestive heart failure, and related conditions often fail to provide sustained and controlled delivery of therapeutic agents, leading to inadequate management of excessive water retention, cardiovascular diseases, and oxidative stress.

Innovation Solution

Development of nitrooxy cycloalkane derivatives, including pharmaceutically acceptable salts and hydrates, for controlled and sustained delivery, which are administered to treat hypertension, PAH, congestive heart failure, and other conditions by acting as antihypertensive agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If conventional treatments for hypertension and cardiovascular conditions are administered, then therapeutic effects are achieved, but sustained and controlled delivery is not provided

Engineering Contradiction:
Improveduration of therapeutic actionVSAvoidcontrolled delivery reliability
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of nitrate esters to create novel compounds with optimized pharmacokinetic properties. The invention introduces specific molecular modifications to achieve sustained release and controlled delivery, transforming the duration and reliability parameters of drug action through chemical parameter optimization

Inventive Principle:
Principle #35Parameter changes

2Stress or pressure

If existing antihypertensive agents are used, then blood pressure is reduced, but inadequate management of water retention and oxidative stress occurs

Engineering Contradiction:
Improveblood pressureVSAvoidmulti-condition management capability
Core Design Contradiction:
Stress or pressureVSAdaptability or versatility

Solution Approach 1:

The patent implements universality by designing nitrooxy cycloalkane derivatives that simultaneously address multiple pathological conditions. The compounds are engineered to provide broad-spectrum therapeutic effects including blood pressure reduction, water retention management, and oxidative stress protection, enabling one agent to perform multiple functions that were previously requiring separate medications

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentEP2369924B1Nitrooxy cycloalkane derivatives
Publication Date: 2014.11.26 MERCK SHARP & DOHME CORP
  • EP2369924B1 patent drawing
  • EP2369924B1 patent drawing
  • EP2369924B1 patent drawing

AI summary

A compound having the structure wherein Y is selected from the group consisting of -C(O)OR2, -C(O)NHR8, -C(CH2)1-2OR3, OH, and or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.