Stable Chiral Boron Compounds for Cancer Therapy
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Solution Overview
Problem
Peptide boronic acid compounds used in cancer therapy and amyloidosis treatment are not stable at ambient conditions, requiring specific storage and administration methods, limiting their effectiveness and convenience.
Innovation Solution
Development of stable boron-containing compounds such as boronate, boronate esters, boranamines, boranediamines, and boronic mono/di-thioesters that can be formulated as both liquid and solid drugs, allowing for broader distribution and longer circulation in the body.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If peptide boronic acid compounds are used for cancer therapy, then anti-cancer effectiveness is improved, but stability at ambient conditions deteriorates
Solution Approach 1:
The patent changes the chemical parameters of the boronic acid compounds by developing stereoselective synthesis methods that produce specific enantiomers and diastereomers. This parameter change in molecular configuration improves both the stability at ambient conditions and the anti-cancer effectiveness, resolving the contradiction between these two properties.
2Reliability
If peptide boronic acid compounds are formulated for injection, then bioactivity is maintained, but administration convenience deteriorates
Solution Approach 1:
The patent changes the physical and chemical parameters of the compounds by stabilizing them at ambient conditions and developing new formulations. This allows the drugs to be administered through multiple routes (oral, parenteral, rectal) rather than requiring specialized injection formulations, thereby improving administration convenience while maintaining bioactivity.
3Duration of action of moving object
If stable boron-containing compounds are developed, then circulation time in body is improved, but formulation complexity increases
Solution Approach 1:
The patent changes the chemical stability parameters of the boron-containing compounds, enabling them to remain stable at ambient conditions and in various formulations. This inherent stability allows for simpler formulation approaches while achieving extended circulation time in the body, thus resolving the contradiction between circulation duration and formulation complexity.
Data Source
AI summary
Useful chiral specific boron-containing compounds, such as boronate, boronate esters, boranamines, borane diamines, boranamine thioesters, and boronic mono/di-thioesters, have been prepared. These compounds and compositions containing them are useful as anti-cancer or anti-amyloidosis agents.