N-Substituted Phthalamic Acids as Sortilin Inhibitors
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Solution Overview
Problem
Current therapies lack specific small molecule modulators to target Sortilin, a receptor implicated in various neurodegenerative and inflammatory disorders, despite its role in mediating pro-apoptotic effects and protein trafficking.
Innovation Solution
Development of N-substituted-5-substituted phthalamic acid compounds that act as Sortilin inhibitors, which can be used in pharmaceutical compositions to treat neurodegenerative diseases, psychiatric disorders, and inflammatory conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current therapies are used to treat neurodegenerative disorders, then treatment is provided, but specific small molecule modulators targeting Sortilin are lacking
Solution Approach 1:
The patent applies parameter changes by systematically varying molecular parameters of phthalamic acid derivatives, including substituent types at different positions, stereochemistry, and molecular size, to optimize Sortilin binding affinity and selectivity. This approach transforms a general therapeutic approach into a targeted therapy with specific molecular parameters tuned for Sortilin inhibition.
Solution Approach 2:
The patent implements local quality by introducing specific substituents at defined positions on the phthalamic acid core structure. Different substituents (R1-R6 groups) provide localized interactions with specific regions of the Sortilin binding site, enabling selective targeting while maintaining overall molecular framework.
2Object-affected harmful factors
If Sortilin-mediated interactions are blocked to treat neurodegenerative diseases, then neurodegenerative processes are alleviated, but potential side effects on other Vps10p family receptors may occur
Solution Approach 1:
The patent uses local quality to achieve selective Sortilin targeting by placing specific functional groups at precise positions on the phthalamic acid core. This localized functional differentiation enables the molecule to distinguish Sortilin from other Vps10p family members (SorLA, SorCS1-3) by forming specific local interactions with Sortilin's unique binding site features.
Solution Approach 2:
The patent applies segmentation by dividing the molecular structure into distinct functional segments (core phthalamic acid, N-substituents, 5-substituents) that can independently contribute to Sortilin binding. This modular design allows optimization of Sortilin specificity while minimizing cross-reactivity with other receptors through selective segment configuration.
Data Source
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AI summary
The present invention is directed to N-substituted-5-substituted phthalamic acids which of formula (A). The compounds are considered useful for the treatment of diseases treatment of a neurodegenerative disease, psychiatric disease, motorneuron disease, peripheral neuropathies, pain, neuroinflammation or atherosclerosis such as Alzheimer's disease and Parkinson's disease.