LSD1 Inhibitor Compounds Modulating Enzyme Activity
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Solution Overview
Problem
Current treatments for cancers involving LSD1, such as prostate, bladder, neuroblastomas, lung cancers, and sarcomas, lack effective pharmacological inhibitors that specifically target LSD1 activity, limiting therapeutic options.
Innovation Solution
Development of compounds with specific structural formulas that modulate LSD1 activity, including structural Formula I and its pharmaceutically acceptable salts, which can be used to treat various diseases associated with LSD1 overexpression or misregulation, including cancers.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current cancer treatments are used, then existing therapeutic options are available, but effective pharmacological inhibitors specifically targeting LSD1 activity are lacking
Solution Approach 1:
The patent applies parameter changes by developing a series of chemical compounds with modified molecular structures (Formula I with various R1-R5 substituents) to optimize LSD1 inhibition. The compounds represent systematic variations in chemical parameters such as aromatic ring substitutions, side chain lengths, and functional groups to achieve effective and selective LSD1 inhibition for cancer treatment
2Object-affected harmful factors
If LSD1 inhibitors are developed to treat cancers, then therapeutic benefits are achieved, but specificity and selectivity of the inhibitors must be ensured
Solution Approach 1:
The patent applies local quality by designing compounds where specific local structural features (such as the aromatic ring system with particular substituent patterns at R1-R5 positions) provide selective binding to LSD1. The modular substitution patterns allow optimization of local molecular properties to enhance selectivity for LSD1 over other enzymes while maintaining cancer treatment efficacy
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
These compounds effectively modulate LSD1 activity, providing therapeutic benefits for treating cancers and other diseases associated with LSD1 overexpression or misregulation, offering a targeted approach to cancer treatment.
Implementation Method 1
LSD1 also known as lysine (K)-specific demethylase 1A (LSD1) is a protein in humans that in encoded by the KDM1A gene and specifically demethylates mono- or dimethylated dimethylated histone H3 lysine4 (H3K4) and H3 lysine 9 (H3K9) via a redox process
Data Source
AI summary
Provided are novel compounds of Formula (I):and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with LSD1. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with LSD1.