Small Molecule IL-17 Modulators for Oral Autoimmune Therapy
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Solution Overview
Problem
Current therapies lack orally available, highly efficacious small molecule modulators of IL-17 for treating autoimmune diseases, with existing treatments relying on monoclonal antibodies that have limitations in convenience and safety.
Innovation Solution
Development of novel amino-acid anilides and derivatives with high metabolic stability and membrane permeability for oral administration, and compounds with high skin permeability for topical therapy, specifically designed to modulate the IL-17 signaling pathway.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If monoclonal antibodies are used to treat IL-17 mediated autoimmune diseases, then therapeutic efficacy is improved, but patient convenience and safety are worsened due to injection requirements and long half-life
Solution Approach 1:
The patent replaces the mechanical injection system (monoclonal antibodies requiring parenteral administration) with a chemical system (small molecule compounds that can be orally administered). This substitution eliminates the need for injections while maintaining therapeutic efficacy through oral bioavailability of the small molecule compounds.
2Reliability
If monoclonal antibodies are used to treat IL-17 mediated autoimmune diseases, then therapeutic efficacy is improved, but safety is worsened due to difficulty in withdrawing treatment
Solution Approach 1:
The patent introduces dynamic control of treatment through small molecule compounds with appropriate pharmacokinetic profiles. Unlike monoclonal antibodies with long half-lives that are difficult to withdraw, the small molecule compounds allow for rapid adjustment and withdrawal of treatment, providing dynamic safety control while maintaining therapeutic efficacy.
3Ease of operation
If small molecule modulators are developed for oral administration, then patient convenience is improved, but metabolic stability and membrane permeability must be optimized
Solution Approach 1:
The patent applies parameter optimization to the chemical structure of small molecule compounds, specifically adjusting metabolic stability and membrane permeability parameters. This allows the compounds to achieve oral bioavailability while maintaining simplicity in administration, resolving the contradiction between convenience and structural complexity.
Data Source
AI summary
The present disclosure relates to a compound according to formula Iand pharmaceutically acceptable salts, hydrates, or solvates thereof. The disclosure further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.