Crystalline Form C of Androgen Receptor Modulator
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Solution Overview
Problem
Current androgen receptor modulators used in treating male disorders and hormone replacement therapy often come with undesirable side effects such as acne, weight gain, and adverse lipid changes, necessitating the development of compounds that modulate androgen receptor activity without these side effects.
Innovation Solution
The development of crystalline forms of a compound of Formula (I) or its solvates, which exhibit specific X-ray powder diffraction patterns and melting points, offering improved bioavailability, stability, and processability, thereby providing long-term stability and reduced side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If known androgen receptor modulators are used to treat male disorders and hormone replacement therapy, then therapeutic effects are achieved, but undesirable side effects occur such as acne, weight gain, and adverse lipid changes
Solution Approach 1:
The patent applies parameter changes by developing new chemical compounds with modified molecular structures (Formula I) that alter the interaction with androgen receptor while reducing side effect profile. The crystalline forms with specific X-ray diffraction patterns represent distinct physical parameter states that improve drug properties
Solution Approach 2:
The patent employs local quality by creating specific crystalline forms with defined X-ray powder diffraction patterns (peaks at specific 2θ angles). These localized structural characteristics confer improved stability and bioavailability while maintaining therapeutic activity
2Stability of the object's composition
If crystalline forms of the compound are developed to improve stability and bioavailability, then long-term stability is achieved, but manufacturing complexity increases
Solution Approach 1:
The patent applies preliminary action by pre-characterizing multiple crystalline forms with specific X-ray diffraction patterns and selecting the most stable form for development. This upfront characterization prevents later stability issues and simplifies manufacturing by establishing clear quality criteria
Solution Approach 2:
The patent utilizes solvent-based crystallization methods where solvents are selected and optimized to produce desired crystalline forms. The solvent systems and crystallization conditions are engineered to reliably produce the stable crystalline form during manufacturing
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 crystalline forms of the compound of Formula (I) demonstrate enhanced clinical efficacy as modulators of androgen receptor activity, providing significant improvements in treating diseases and disorders associated with androgen receptor activity while minimizing adverse side effects.
Implementation Method 1
the crystalline form of the compound of Formula (I) may exhibit an X-ray powder diffraction pattern comprising at least one characteristic peak selected from the group consisting of approximately 8.5, 11.8, 12.4, 13.3, 13.7, 15.0, 17.1, 17.5, 18.2, 18.5, 19.5, 21.1, 21.7, 22.1, 22.6, 23.1, 23.7, 24.8, 25.0, 25.5, 26.2, 27.5, and 29.6 degrees 2θ
Implementation Method 2
the crystalline form of the compound of Formula (I) may have a melting point of about 163° C.
Data Source
AI summary
Disclosed herein are methods of crystallizing the compound of Formula (I), as well as crystalline forms thereof. Crystalline forms of Formula (I) disclosed include crystalline Form C, crystalline Form E, and Crystalline form B.