Isoindoline-dione Compound for Hematological Malignancies

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Solution Overview

Problem

Current cancer therapies for hematological malignancies, such as surgery, chemotherapy, and radiation therapy, are associated with significant drawbacks including toxicity, side effects, and drug resistance, making them ineffective for many patients, particularly those with relapsed or refractory cases.

Innovation Solution

The use of 2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione, its enantiomers, tautomers, isotopologs, or pharmaceutically acceptable salts, for treating, preventing, or managing hematological malignancies, including leukemia, lymphoma, and multiple myeloma, by administering a therapeutically effective amount to subjects in need.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional chemotherapeutic agents are used to treat hematological malignancies, then tumor cells may be eradicated in some cases, but the treatment causes severe toxicity and significant side effects including bone marrow depression and immunosuppression

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidtoxicity and side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of conventional chemotherapeutic agents through the development of novel compounds with altered molecular properties. These structural modifications aim to change the pharmacokinetic and pharmacodynamic parameters of the drugs, thereby improving therapeutic effectiveness while reducing toxicity and side effects associated with conventional chemotherapy regimens

Inventive Principle:
Principle #35Parameter changes

2Reliability

If combinations of chemotherapeutic agents are administered to overcome drug resistance, then treatment coverage may be expanded, but the complexity of the treatment protocol increases and multidrug resistance may still develop

Engineering Contradiction:
Improveovercoming drug resistanceVSAvoidtreatment protocol complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies merging by combining multiple therapeutic functions into a single novel chemotherapeutic compound. The designed molecules integrate multiple pharmacophores or functional groups that can simultaneously target different mechanisms of cancer cell death, thereby overcoming drug resistance without requiring complex combination protocols. This consolidation reduces treatment complexity while maintaining effectiveness against resistant tumor cells

Inventive Principle:
Principle #5Merging (Combining)

3Reliability

If surgery is used to remove neoplastic tissue, then immediate reduction in tumor burden may be achieved, but surgery may be contraindicated due to patient health or may not completely remove neoplastic tissue

Engineering Contradiction:
Improvetumor removal effectivenessVSAvoidapplicability to all patients
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies mechanics substitution by replacing the mechanical approach of surgical removal with a chemical therapy approach using novel chemotherapeutic agents. These compounds are designed to selectively target and destroy neoplastic cells through biochemical mechanisms, providing a non-mechanical alternative that can reach tumor cells throughout the body without the limitations of surgical accessibility and patient physical condition

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

Data Source

PatentUS12178822B2Methods of treating hematological malignancies using 2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dion
Publication Date: 2024.12.31 CELGENE CORP
  • US12178822B2 patent drawing
  • US12178822B2 patent drawing
  • US12178822B2 patent drawing

AI summary

Provided herein are methods of using 2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione, or an enantiomer, a mixture of enantiomers, a tautomer, an isotopolog, or a pharmaceutically acceptable salt thereof, for treating, preventing or managing hematological malignancies.