Isoindolinone-Piperidinedione Salts and Solid Forms for Drug Stability

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current cancer treatments, including surgery, chemotherapy, radiation, and hormonal therapy, pose significant drawbacks such as toxicity, side effects, and drug resistance, while treatments for diseases associated with undesired angiogenesis are difficult to manage effectively, and existing pharmaceutical compounds lack optimal stability and bioavailability due to varying solid forms and salt properties.

Innovation Solution

Development of salts and solid forms of the compound (S)-3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, including various stereoisomers, hydrates, anhydrates, and solvates, which are characterized by unique physical properties for improved pharmaceutical performance and stability, and their use in pharmaceutical compositions for treating and preventing disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional cancer treatments (surgery, chemotherapy, radiation, hormonal therapy) are used, then cancer can be treated, but toxicity and side effects increase

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

Solution Approach 1:

The patent changes the chemical parameters of the treatment agent by developing novel salt forms and solid forms of compound (I). These parameter changes in the pharmaceutical composition enable effective cancer treatment while reducing toxicity and side effects compared to conventional therapies.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite pharmaceutical compositions by combining compound (I) with various salts and solid forms. These composite materials provide improved therapeutic index, maintaining cancer treatment effectiveness while minimizing harmful effects on healthy tissues.

Inventive Principle:
Principle #40Composite materials

2Reliability

If existing pharmaceutical compounds are used, then treatment can be provided, but stability and bioavailability are insufficient due to varying solid forms and salt properties

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidpharmaceutical stability and bioavailability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent systematically changes the physical and chemical parameters of the pharmaceutical compound by establishing specific salt forms and solid forms of compound (I). These parameter changes optimize stability and bioavailability, ensuring reliable treatment effectiveness.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent utilizes solvation and hydration principles (analogous to fluid interactions) by developing solvates and hydrates of compound (I). These forms improve pharmaceutical stability and bioavailability through controlled interaction with solvent molecules in the solid state.

Inventive Principle:
Principle #29Pneumatics and hydraulics

Data Source

PatentUS20250281501A1Salts and solid forms of (s)-3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione and compositions comprising and methods of using the same
Publication Date: 2025.09.11 CELGENE CORP
  • US20250281501A1 patent drawing
  • US20250281501A1 patent drawing
  • US20250281501A1 patent drawing

AI summary

Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methods of using the salts and solid forms are also disclosed.