BCL-2 Inhibitor Compounds Modulating Cell Proliferation
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Solution Overview
Problem
There is a need for compounds that can effectively inhibit the activity of anti-apoptotic BCL-2 proteins to treat various medical conditions, including cancer and other diseases, as existing therapies are inadequate in modulating BCL-2 protein activity.
Innovation Solution
Development of specific compounds with a defined formula and their pharmaceutically acceptable salts, which can modulate BCL-2 protein activity, including inhibition, for use in treating diseases associated with BCL-2, such as cancer and autoimmune diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing therapies are used, then treatment of medical conditions is provided, but BCL-2 protein activity is not adequately inhibited
Solution Approach 1:
The patent employs parameter changes by modifying the chemical structure of BCL-2 inhibitor compounds through various substituents (R1-R6, Cy1-Cy3, E, G, L, X, Y, Z parameters) to optimize inhibition efficacy while maintaining therapeutic versatility across different medical conditions
2Reliability
If BCL-2 protein activity is inhibited, then cell proliferation is reduced, but therapeutic application requires specific compound formulations
Solution Approach 1:
The patent applies parameter changes by systematically varying chemical parameters (R1-R6 substituents, Cy1-Cy3 cyclic groups, E, G, L linkers, X, Y, Z heteroatoms) to develop compound formulations that achieve reliable cell proliferation control while managing formulation complexity through structure-activity relationship optimization
Data Source
AI summary
The disclosure is directed to, in part, to BCL-2 inhibitors, pharmaceutical compositions comprising the same, as well as methods of their use and preparation.