Non-peptidic Proline Modulators for Orexin Receptor Specificity
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Solution Overview
Problem
Current treatments for conditions related to orexin receptor dysfunction, such as eating disorders, obesity, and addiction, lack effective modulators that can specifically target and modulate orexin receptors OX1 and OX2 to achieve therapeutic benefits.
Innovation Solution
Development of non-peptidic small molecules that can activate or inhibit orexin receptors OX1 and OX2, including compounds of a specific formula that can be used in pharmaceutical compositions to modulate these receptors, thereby treating a range of malconditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments are used for orexin receptor dysfunction, then existing therapeutic approaches are available, but they lack effective modulators that can specifically target orexin receptors OX1 and OX2
Solution Approach 1:
The patent applies parameter changes by developing non-peptidic small molecules with specific molecular structures (formula I) that differ fundamentally from existing peptidic approaches. This structural parameter change enables the compounds to specifically bind to and modulate orexin receptors OX1 and OX2, achieving reliable receptor targeting that was not possible with conventional treatments.
Solution Approach 2:
The patent substitutes peptidic molecules with non-peptidic small molecules. This replacement changes the fundamental nature of the therapeutic agent from peptide-based to small molecule-based, enabling new mechanisms of receptor interaction and providing effective modulators that specifically target orexin receptors, thereby resolving the lack of available effective treatments.
2Reliability
If non-peptidic small molecules are developed to target orexin receptors, then specific modulation of OX1 and OX2 is achieved, but the complexity of compound synthesis and formulation increases
Solution Approach 1:
The patent applies segmentation by dividing the complex task of creating orexin receptor modulators into specific molecular components defined by formula (I). The compound structure is segmented into distinct elements (A, B, D, J, R1, R2, Z) that can be independently optimized and synthesized, then assembled to achieve the desired receptor modulation efficacy while managing synthesis complexity.
3Ease of manufacture
If selective orexin receptor modulators are used, then therapeutic benefits for specific malconditions are achieved, but the scope of applicability across different conditions requires extensive validation
Solution Approach 1:
The patent applies universality by designing non-peptidic small molecules that can serve multiple therapeutic functions. The compounds of formula (I) are developed to modulate orexin receptors OX1 and OX2, which are involved in various physiological processes including sleep-wake regulation, food intake, and stress response. This multi-functionality allows the same compound class to potentially treat diverse malconditions such as sleep disorders, eating disorders, obesity, and addiction, expanding adaptability across different conditions.
Data Source
AI summary
The present invention is directed to compounds that can modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.