Steroidal Contraceptive Compounds Preventing Bone Density Loss
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current male contraceptive agents lack estrogenic properties, leading to decreased circulating estrogen and negative impacts on bone density, such as osteoporosis, and do not provide dual roles like steroidal receptor activation/deactivation and therapeutic activity against diseases.
Innovation Solution
Development of monomeric and oligomeric compounds with androgenic, progestogenic, and estrogenic activities, capable of aromatization to mitigate bone density loss, comprising specific structural features for receptor binding and therapeutic efficacy, including steroidal-based compounds covalently coupled with linker groups for controlled activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If male contraceptive agents are used to achieve contraception, then contraceptive efficacy is improved, but bone density is reduced leading to osteoporosis
Solution Approach 1:
The patent combines multiple steroidal functionalities (androgenic, progestogenic, and estrogenic activities) into a single contraceptive agent. The compound of Formula I integrates androgen receptor binding capability with progestogenic activity and estrogenic properties, thereby providing contraceptive efficacy while simultaneously preventing bone density loss through estrogenic activity.
Solution Approach 2:
The contraceptive agent is designed to perform multiple functions simultaneously: (1) androgenic activity for contraceptive effect, (2) progestogenic activity for additional contraceptive mechanism, and (3) estrogenic activity for bone density protection. This multi-functional design allows a single compound to address both contraception and bone health concerns.
2Reliability
If conventional male contraceptive agents are used, then contraceptive function is provided, but dual therapeutic roles are not achieved
Solution Approach 1:
The patent designs the contraceptive agent to serve dual purposes: primary contraceptive function through androgenic and progestogenic activities, and secondary therapeutic function through estrogenic activity that prevents bone density loss. This allows the same compound to function both as a contraceptive and as a protective agent against osteoporosis.
Solution Approach 2:
The compound exhibits dynamic functionality by undergoing aromatization in vivo to produce estrogenic activity. The molecular structure of Formula I can be converted to estrogenic metabolites within the body, enabling the agent to adapt its functionality based on physiological conditions and provide both contraceptive and bone-protective effects at different times or locations.
Data Source
AI summary
Disclosed herein are monomeric and oligomeric compound embodiments for use as contraceptive agents. Monomeric compound embodiments disclosed herein comprise substituents that facilitate the ability of the compounds to exhibit progestogenic, androgenic, and estrogenic activity, which can prevent or inhibit bone density loss in subjects. Oligomeric compound embodiments disclosed herein provide the ability to control receptor activation and/or treatment by incorporating a tunable linker group which couples steroidal-based compounds to one another or with therapeutic agents and facilitates selective cleavage of the monomeric components of the oligomeric compound.