Selective Androgen Receptor Modulators for Prostate-Sparing Anabolic Effects
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Solution Overview
Problem
Current androgen replacement therapies (ARTs) for treating androgen deficiency in males have limitations, including side effects such as prostate issues, and lack of long-term safety data, necessitating the development of selective androgen receptor modulators (SARMs) that can provide anabolic effects without stimulating the prostate.
Innovation Solution
Development of compounds that modulate the androgen receptor, acting as selective agonists, partial agonists, or antagonists to mimic the effects of testosterone while sparing the prostate, offering potential treatments for conditions like hypogonadism, osteoporosis, and benign prostatic hyperplasia.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Strength
If traditional androgen replacement therapies are used, then anabolic effects (muscle and bone density improvement) are achieved, but prostate-related side effects occur
Solution Approach 1:
The patent applies the local quality principle by designing SARM compounds that exhibit tissue-selective androgenic activity. Different compounds within the patent demonstrate preferential binding affinity to androgen receptors in specific tissues (muscle, bone, brain) versus the prostate. This is achieved through structural modifications to the androgen core that enhance selectivity for certain AR isoforms or receptor conformations prevalent in anabolic tissues while having reduced affinity for prostatic AR, thereby providing anabolic benefits with minimal prostate stimulation
Solution Approach 2:
The patent segments the androgenic effect by creating multiple compound variants with differentiated tissue selectivity profiles. Each compound in the series can be optimized for specific indications (e.g., muscle wasting, osteoporosis, cognitive function) by adjusting molecular substituents. This segmentation allows clinicians to select compounds that target specific anabolic needs while avoiding prostate-related adverse effects
2Ease of operation
If androgen replacement therapy is administered, then libido and mood improvement are achieved, but long-term safety concerns arise
Solution Approach 1:
The SARM compounds act as intermediaries that selectively activate androgen receptors in the central nervous system (brain, hypothalamus, hippocampus) and peripheral tissues (muscle, bone) while deliberately avoiding activation in the prostate. This intermediary action provides the desired libido and mood benefits through CNS androgenic activity without the long-term safety concerns associated with prostatic androgen stimulation, such as prostate cancer risk and benign prostatic hyperplasia
3Object-affected harmful factors
If selective androgen receptor modulators are developed, then prostate-sparing effects are achieved, but compound selectivity and specificity must be precisely controlled
Solution Approach 1:
The patent systematically varies molecular parameters (substituent types, positions, and configurations on the androgen core) to fine-tune the selectivity profile of each SARM compound. By adjusting these chemical parameters, the inventors optimize the ratio of anabolic activity to prostatic activity for each compound variant, achieving the desired prostate-sparing effects while maintaining precise control over compound selectivity through structure-activity relationship optimization
Data Source
AI summary
This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.