Phosphate Compounds Inhibiting Bcl-2 Anti-Apoptotic Activity
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Solution Overview
Problem
Current treatments for cancer and autoimmune diseases lack effective compounds that inhibit the anti-apoptotic activity of Bcl-2 family proteins, which are associated with tumorigenesis, chemoresistance, and various pathologies.
Innovation Solution
Development of new phosphate compounds with specific pharmacological and pharmacokinetic properties that inhibit anti-apoptotic activity, including compounds of formula (I) and their metabolites, which are administered to optimize in vivo exposure and enhance therapeutic efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments are used for cancer and autoimmune diseases, then existing therapeutic options are maintained, but effective inhibition of anti-apoptotic activity of Bcl-2 family proteins is not achieved
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of Bcl-2 family protein inhibitors through phosphate group substitutions and variations in the heterocyclic core structure. This enables the compounds to effectively inhibit anti-apoptotic activity while achieving improved therapeutic efficacy in cancer and autoimmune diseases
2Reliability
If phosphate compounds of formula (I) are administered to optimize in vivo exposure, then therapeutic efficacy is enhanced, but compound complexity increases
Solution Approach 1:
The patent utilizes parameter changes by systematically varying the phosphate group substitutions (different metal cations M1+, M2+, M32+) and heterocyclic core structures to optimize in vivo exposure and therapeutic efficacy while managing compound complexity through structured molecular design
Data Source
AI summary
Compounds of formula (I):wherein X, Y, A1, A2, Ra, Rb, Rc, Rd, R3, R4, T and R5 are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.