SARM Solid Forms With Polymorph Control for Stable Oral Therapy
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Solution Overview
Problem
Current approaches lack effective solutions for developing compounds that address male contraception, hormone-related conditions such as Androgen Decline in Aging Male (ADAM) and Androgen Decline in Female (ADIF), chronic muscular wasting, and prostate cancer, with existing treatments having limitations in efficacy and stability.
Innovation Solution
Development of solid forms of (R) or (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide, which act as selective androgen receptor modulators (SARMs), including crystalline and paracrystalline forms, for use in male contraception, hormone-related treatments, and prostate cancer management.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing treatments for hormone-related conditions are used, then treatment coverage is provided, but efficacy and stability are limited
Solution Approach 1:
The patent develops multiple polymorphic forms (Forms A, B, C, D) of SARM compounds with different physical and chemical parameters including solubility, dissolution rate, and stability characteristics. Each polymorph is optimized for specific therapeutic applications, allowing the same active ingredient to achieve both high efficacy/stability and broad adaptability across different hormone-related conditions through parameter variation rather than requiring multiple different compounds
2Manufacturing precision
If polymorphic forms are developed to improve drug properties, then solubility and dissolution rate change, but manufacturing complexity increases
Solution Approach 1:
The patent establishes detailed characterization data for each polymorphic form including XRPD patterns, DSC thermograms, and solubility profiles before manufacturing. This preliminary characterization allows manufacturers to select the appropriate polymorph for their specific needs and implement targeted manufacturing protocols, reducing overall complexity by having pre-defined options rather than requiring complex real-time control
Solution Approach 2:
Different polymorphic forms are produced by varying crystallization parameters such as solvent type, temperature, and pH. This allows manufacturers to control which polymorph forms by adjusting these parameters during the manufacturing process, providing a relatively simple method to achieve precise polymorphic form control without complex equipment or procedures
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The solid forms of (R) or (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide demonstrate androgenic and anabolic activity, effectively treating a range of conditions associated with ADAM and ADIF, preventing or halting prostate cancer, and providing oral androgen replacement therapy.
Implementation Method 1
selective androgen receptor modulators (SARMs)... demonstrate androgenic and anabolic activity
Implementation Method 2
Polymorphs, solvates and salts of various drugs have been described in the literature as imparting novel properties to the drugs. Organic small drug molecules have a tendency to self-assemble into various polymorphic forms depending on the environment that drives the self assembly.
Implementation Method 3
Heat and solvent mediated effects can also lead to changes that transform one polymorphic form into another.
Data Source
AI summary
The present invention relates to solid forms of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide and process for producing the same.