Formula I Compounds Modulating c-Myc Activity
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Solution Overview
Problem
Current therapies lack effective compounds to modulate Myc activity, particularly c-Myc, which is frequently deregulated in various cancers, leading to uncontrolled cell proliferation and oncogenesis.
Innovation Solution
Development of selective c-Myc inhibitors, represented by compounds of Formula (I), which can down-regulate Myc expression, inhibit Myc activity, and disrupt Myc interactions with DNA, thereby treating proliferative diseases such as cancers and inflammatory conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current therapies are used, then treatment of proliferative diseases is provided, but effective modulation of Myc activity is not achieved
Solution Approach 1:
The patent applies parameter changes by developing compounds with specific molecular structures (Formula I) that alter the biochemical parameters of Myc protein interaction. The compounds modify binding affinity and specificity through structural variations in R1, R2, R3, R4, Y, and Z parameters, enabling effective Myc activity modulation that current therapies cannot achieve.
2Measurement precision
If selective c-Myc inhibitors are developed, then specific targeting of Myc-regulated pathways is achieved, but complexity of compound structure increases
Solution Approach 1:
The patent applies segmentation by dividing the inhibitor compound into distinct functional segments: a core heterocyclic structure (Y and Z positions) and variable substituent groups (R1, R2, R3, R4). This modular segmentation allows optimization of Myc-binding specificity through targeted modification of individual segments while maintaining overall structural manageability.
Solution Approach 2:
The patent applies local quality by assigning specific functional properties to different parts of the molecule. The core heterocyclic structure (positions Y and Z) provides the essential Myc-binding interface with specific geometric and electronic properties, while the R1-R4 substituents provide localized interactions that fine-tune specificity and affinity for Myc-regulated pathways.
Data Source
AI summary
The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases, e.g., cancers (e.g., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angiogenesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject.