Decalin Derivatives Inhibit Cell Adhesion in Sickle Cell Anemia

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for sickle cell anemia lack effective cell adhesion inhibitors, which are crucial for managing the disease's complications such as vaso-occlusion, where defective red blood cells adhere to vascular endothelium, restricting blood flow and causing organ issues.

Innovation Solution

Development of decalin derivatives, specifically compounds of formula (I), and their pharmaceutical compositions, which act as cell adhesion inhibitors, are synthesized and used to treat sickle cell anemia by reducing the adhesivity of sickle red blood cells to vascular endothelium.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for sickle cell anemia are used, then existing therapeutic options are available, but effective cell adhesion inhibition is lacking

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidcell adhesion inhibition capability
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of decalin derivatives through systematic variation of substituents at different positions (R1-R10 groups). This structural parameter optimization enables the compounds to achieve potent cell adhesion inhibition activity, directly addressing the lack of effective adhesion inhibitors in current sickle cell treatments

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention employs composite material principles by creating decalin derivative compounds with multiple functional groups and complex molecular architectures. These composite molecular structures combine hydrophobic decalin core with various polar and non-polar substituents, enabling simultaneous interaction with multiple targets involved in cell adhesion processes

Inventive Principle:
Principle #40Composite materials

2Reliability

If decalin derivatives are developed as new cell adhesion inhibitors, then effective treatment for vaso-occlusion is achieved, but the complexity of drug development increases

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoiddrug development complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the decalin derivative development into systematic stages: core structure identification, substituent optimization at specific positions (R1-R10), and structure-activity relationship analysis. This segmented approach manages development complexity while achieving therapeutic efficacy through iterative optimization of molecular parameters

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention demonstrates universality by designing decalin derivatives with multiple functional groups that can simultaneously target different aspects of cell adhesion. The compounds exhibit multi-functionality by potentially interfering with multiple adhesion molecules and pathways, providing robust therapeutic efficacy across different sickle cell complications

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

Data Source

PatentUS11724995B2Decalin derivatives, a process for the preparation and pharmaceutical composition thereof
Publication Date: 2023.08.15 COUNCIL OF SCI & IND RES
  • US11724995B2 patent drawing
  • US11724995B2 patent drawing
  • US11724995B2 patent drawing

AI summary

Decalin derivative compounds of formula (I) are provided, including processes for preparation thereof, and pharmaceutical compositions including the decalin derivative compounds. Methods are provided for treating blood related disorders, such as sickle cell anemia, in a subject in need thereof using a compound of formula (I).