ERR-α Inverse Agonists for Metabolic and Inflammatory Disease Treatment
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
There is a need for new Estrogen Related Receptor alpha (ERR-α) inverse agonists to treat various conditions such as cancer, arthritis, inflammatory airway disease, and metabolic disorders, as existing treatments are inadequate for conditions mediated by ERR-α activity.
Innovation Solution
Development of novel compounds, specifically ERR-α modulators represented by Formula (I), which can act as inverse agonists to regulate ERR-α activity, thereby treating or inhibiting the progression of associated diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing treatments are used for ERR-α mediated conditions, then current standard therapies are applied, but they are inadequate for treating conditions like cancer, arthritis, and metabolic disorders
Solution Approach 1:
The patent develops novel chemical compounds with specific molecular structures (Formula I) that bind to ERR-α receptors, changing the pharmacological parameters of treatment. These compounds represent a new class of inverse agonists with distinct binding characteristics compared to existing therapies, enabling effective treatment of ERR-α mediated conditions where prior treatments failed
Solution Approach 2:
The patent introduces intermediary compounds that act as inverse agonists at the ERR-α receptor level. These compounds serve as mediators between the therapeutic goal and the biological target, providing a mechanism to modulate ERR-α activity that was not available through existing treatments
2Reliability
If novel ERR-α modulators are developed, then therapeutic benefits are achieved for various diseases, but the complexity of drug development and validation increases
Solution Approach 1:
The patent segments the therapeutic approach by developing a series of related compounds with systematic structural variations (different R groups in Formula I). This segmentation allows for modular optimization of therapeutic properties while maintaining the core inverse agonist mechanism, making the development process more manageable despite the novelty of the approach
Data Source
AI summary
The present invention relates to compounds of Formula (I),methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.