CD73 Inhibitor Compounds for AMP-to-Adenosine Modulation
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Solution Overview
Problem
Current CD73 inhibitors face challenges such as less than ideal metabolic stability, limiting their effectiveness in treating a diverse array of diseases and disorders mediated by CD73, including cancer, fibrosis, neurological disorders, and immune-related conditions.
Innovation Solution
Development of small molecule compounds and compositions that inhibit CD73 activity, modulating the conversion of AMP to adenosine, which can be administered alone or in combination with other therapeutic agents to enhance treatment efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If small molecule CD73 inhibitors are developed to treat diseases mediated by CD73, then therapeutic effectiveness is improved, but metabolic stability deteriorates
Solution Approach 1:
The patent applies parameter changes by systematically modifying chemical structures of small molecule compounds to optimize the balance between CD73 inhibitory activity and metabolic stability. This involves changing molecular parameters such as substituent groups, ring structures, and stereochemistry to achieve compounds that maintain therapeutic effectiveness while improving metabolic stability profiles
Solution Approach 2:
The patent employs composite material principles by designing hybrid molecular structures that combine different chemical moieties with complementary properties. These composite small molecule structures integrate pharmacophores for CD73 binding with structural elements that enhance metabolic stability, creating compounds that achieve both therapeutic effectiveness and improved stability
2Productivity
If CD73 inhibition is used to treat cancer and other diseases, then treatment efficacy is improved, but metabolic stability of inhibitors deteriorates
Solution Approach 1:
The patent utilizes parameter changes to optimize small molecule compounds for enhanced treatment efficacy while addressing metabolic stability issues. By systematically varying chemical parameters including substituent types, molecular weight, and structural rigidity, the invention identifies compounds that achieve superior CD73 inhibition for treating cancer and other diseases while maintaining improved metabolic stability
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
The compounds effectively inhibit CD73 activity, leading to improved treatment outcomes for various diseases and disorders, including increased cancer survival rates, reduced tumor growth, and enhanced immune responses, with potential synergistic effects in combination therapies.
Implementation Method 1
In the next step, AMP is converted to adenosine by 5'-nucleotidase, ecto (NT5E or 5NT), also known as CD73 (Cluster of Differentiation 73)
Data Source
AI summary
Compounds that modulate the conversion of AMP to adenosine by 5′-nucleotidase, ecto, and compositions containing the compounds and methods for synthesizing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by 5′-nucleotidase, ecto is also provided.