Pyrazole Compounds as Oral FSHR Modulators
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Solution Overview
Problem
Current treatments for infertility and male hypogonadism using FSH are limited by high cost, lack of oral dosing options, and the need for extensive monitoring, highlighting the need for low molecular weight FSH mimetics that can selectively activate the follicle-stimulating hormone receptor (FSHR) for oral administration.
Innovation Solution
Development of pyrazole compounds that act as positive allosteric modulators of FSHR, represented by specific chemical formulas, which can be administered orally and effectively modulate FSHR activity to treat various disorders associated with abnormal cellular responses triggered by follicle-stimulating hormone events.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If FSH (follicle stimulating hormone) is used to treat infertility and male hypogonadism, then the therapeutic effect is achieved through activation of FSHR, but the treatment is limited by high cost, lack of oral dosing capability, and need for extensive monitoring
Solution Approach 1:
The patent changes the molecular parameters of the FSH molecule by creating small molecule pyrazole compounds that mimic FSH activity. These compounds have fundamentally different molecular characteristics from the native FSH protein, enabling oral bioavailability while maintaining FSHR activation capability. The parameter change transforms the drug from a large protein hormone to a small organic molecule suitable for oral administration.
Solution Approach 2:
The invention creates simplified copies of FSH's biological activity through small molecule pyrazole compounds. Rather than using the complete FSH protein structure, the patent develops molecular copies that retain the essential receptor-binding and activating properties while eliminating the limitations of protein-based therapy, such as poor oral absorption and high cost of production.
2Reliability
If FSH protein product is administered parenterally to achieve ovulation induction, then the therapeutic effect is achieved, but the treatment requires extensive monitoring by specialist physicians and cannot be self-administered
Solution Approach 1:
The small molecule pyrazole compounds enable patients to self-administer treatment orally without requiring specialist monitoring. The improved pharmacokinetic properties and oral bioavailability allow for self-managed therapy, eliminating the need for complex clinical monitoring protocols and specialist physician involvement that are currently required for parenteral FSH administration.
Solution Approach 2:
The patent develops small molecule compounds that can be manufactured more cost-effectively than recombinant FSH proteins. These molecules have simpler synthesis routes and do not require complex biomanufacturing processes, cell culture systems, or purification infrastructure, thereby reducing treatment cost and eliminating the need for expensive ongoing monitoring.
3Ease of operation
If low molecular weight FSH mimetics are developed to enable oral administration, then the ease of administration is improved, but the selectivity and potency for FSHR activation must be maintained
Solution Approach 1:
The pyrazole compounds exhibit local quality optimization by designing specific molecular regions that selectively interact with FSHR binding sites. The molecules contain localized functional groups and structural features (such as the pyrazole core with specific substituents) that are optimized for high-affinity binding to FSHR, ensuring selective activation of the target receptor while maintaining oral bioavailability.
Data Source
AI summary
The present invention relates to pyrazole compounds, and pharmaceutically acceptable compositions thereof, useful as positive allosteric modulators of follicle stimulating hormone receptor (FSHR).