Formula 1 Compounds Modulating Biological Activity for Inflammatory Diseases

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Solution Overview

Problem

Current treatments for inflammatory diseases, respiratory complaints, gastrointestinal issues, and other conditions lack effective compounds that can target these conditions specifically and provide significant therapeutic benefits.

Innovation Solution

Development of novel compounds of formula 1 and their derivatives, including pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates, and solvates, which are designed to treat inflammatory diseases and other conditions by modulating biological activity through specific structural features.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments for inflammatory diseases are used, then existing therapies can be administered, but they lack specific targeting and effective therapeutic benefit

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidspecific targeting capability
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies local quality by designing compounds with specific structural features (formula 1) that enable selective binding to particular biological targets involved in inflammatory diseases. The molecular structure includes specific substituents (R1-R6 groups) and functional moieties that confer localized activity against specific disease pathways, thereby achieving both therapeutic efficacy and specific targeting capability simultaneously

Inventive Principle:
Principle #3Local quality

2Reliability

If novel compounds of formula 1 are developed, then specific targeting and therapeutic benefit are achieved, but compound complexity increases

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

Solution Approach 1:

The patent applies segmentation by dividing the complex molecular structure into distinct functional segments: a core scaffold (formula 1) with specific substituents (R1-R6), heteroaryl groups, and functional moieties. This modular approach allows systematic variation of individual segments to optimize therapeutic efficacy while maintaining manageable structural complexity through standardized building blocks

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent applies parameter changes by systematically varying molecular parameters such as substituent types (R1-R6 groups), heteroatom positions, and functional group configurations. These parameter modifications enable tuning of biological activity and target specificity without proportionally increasing overall structural complexity, as changes are made within established molecular frameworks

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS7723381B2Compounds for the treatment of inflammatory diseases
Publication Date: 2010.05.25 BOEHRINGER INGELHEIM INT GMBH
  • US7723381B2 patent drawing
  • US7723381B2 patent drawing
  • US7723381B2 patent drawing

AI summary

Compounds of formula 1 and hetero derivatives thereofand the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.