Formula I Compounds for Systemic Autophagy Induction
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Solution Overview
Problem
Current treatments for autophagy-related diseases such as cancer, age-related diseases, and infections lack effective and selective autophagy inducers that can be administered systemically.
Innovation Solution
Development of compounds according to Formula (I) or their salts, solvates, and hydrates, which act as potent autophagy inducers, achieving higher systemic concentrations compared to the brain, thereby facilitating systemic treatment.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments for autophagy-related diseases are used, then disease management is attempted, but effective and selective autophagy induction cannot be achieved
Solution Approach 1:
The patent modifies chemical parameters of existing compounds (such as tamoxifen and toremifene) by introducing specific substituents at defined positions in the molecular structure. This creates analogs with enhanced autophagy-inducing activity and improved pharmacokinetic properties for systemic administration, resolving the contradiction between reliable autophagy induction and systemic treatment capability
2Reliability
If autophagy is induced in disease cells, then therapeutic efficacy is improved, but selective induction in target tissues remains challenging
Solution Approach 1:
The patent introduces specific substituents at defined positions (R1, R2, R3) in the core molecular structure to create local chemical modifications that enhance target tissue selectivity. These localized structural changes allow the compounds to preferentially induce autophagy in disease-affected tissues while maintaining systemic administration capability, thereby achieving both therapeutic efficacy and selectivity
Data Source
AI summary
The invention relates to pharmaceutical compositions and methods of treating autophagy related diseases and disorders, in particular for a systemic treatment thereof. The present invention relates to compounds according to Formula (I) or salts, solvates and/or hydrates thereof, wherein said compounds induce and/or stimulate the process of autophagy, as well as uses of the compounds in the treatment and prevention of autophagy related diseases and disorders. Examples are cancer, age-related diseases, and viral infection that can be effectively treated with compounds that are effective when provided systemically.