Spliceosome-Interfering Compounds for Solid Tumor Cancer Treatment
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Solution Overview
Problem
Current cancer treatments are inadequate in effectively addressing the rapid growth and metastasis of cancer cells, particularly in solid tumor cancers such as breast, lung, cervical, prostate, ovarian, pancreatic, and renal cell cancers, due to limitations in disrupting transcription pathways.
Innovation Solution
Development of compounds, including those with Formulae I, Ia, and their stereoisomers, pharmaceutically acceptable salts, prodrugs, and antibody conjugates, which interfere with spliceosomes to disrupt the transcription pathways of cancer cells, thereby limiting their growth and metastasis.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If compounds that disrupt transcription pathways are used to treat cancer, then cancer cell proliferation is limited, but the effectiveness in addressing rapid growth and metastasis is insufficient
Solution Approach 1:
The patent modifies the chemical structure of transcription pathway disruptors by changing parameters such as molecular weight, functional groups, and stereochemistry to enhance their effectiveness against rapidly dividing cancer cells while reducing resistance development
Solution Approach 2:
The invention creates composite therapeutic agents combining multiple transcription pathway disruptors with different mechanisms of action to achieve synergistic effects, thereby improving reliability in limiting cancer cell proliferation and addressing the insufficiency of single-agent therapies
2Reliability
If spliceosome-interfering compounds are developed to disrupt transcription pathways, then cancer cell growth is slowed, but the complexity of the compound structures increases
Solution Approach 1:
The patent divides the complex spliceosome-interfering compound into modular components with distinct functional regions, allowing each segment to target specific spliceosome elements while simplifying the overall synthesis and reducing structural complexity
Solution Approach 2:
The invention introduces intermediary molecules that facilitate the interaction between the compound and spliceosome components, acting as bridges that enhance transcription pathway disruption without requiring overly complex direct binding structures
3Reliability
If existing cancer treatments are used, then some therapeutic effect is achieved, but the high social and economic costs indicate inadequate effectiveness
Solution Approach 1:
The patent develops compounds that exploit the cancer cell's own transcription pathways and spliceosome machinery against them, allowing the treatment to achieve therapeutic effect through the cell's inherent biological processes rather than requiring external intervention, thereby improving cost-effectiveness
Solution Approach 2:
The invention converts the cancer cell's rapid transcription and splicing activities, which are harmful for tumor growth, into a vulnerability by designing compounds that specifically target and disrupt these processes, achieving therapeutic effect while reducing treatment costs through more effective disease control
Data Source
AI summary
Embodiments provide, among other compounds, a family of compounds that can be used as therapeutic anti-cancer agents, methods for using such compounds to treat cancer, and methods of making such compounds.