Crystalline Forms of Compound 1 for Angiogenic Disease Treatment
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Solution Overview
Problem
There is a need for new therapeutic compositions to treat diseases associated with aberrant signaling of growth factors and angiogenesis, such as cancer, macular degeneration, and diabetic retinopathy, as existing treatments are inadequate in effectively inhibiting pathological angiogenesis.
Innovation Solution
The development of crystalline forms of Compound 1, specifically crystalline forms E and C, which are prepared through mixing with methanol and ethyl acetate, respectively, and used in pharmaceutical compositions to treat angiogenic ocular diseases by inhibiting abnormal angiogenesis.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing therapeutic compositions are used to treat angiogenic ocular diseases, then treatment is provided, but the compositions are inadequate in effectively inhibiting pathological angiogenesis
Solution Approach 1:
The patent introduces new crystalline forms of Compound 1 with distinct crystal structures (different XRPD patterns, densities, and physical properties) to improve the effectiveness of inhibiting pathological angiogenesis. The crystalline forms are prepared through specific processes involving different solvents (methanol, ethyl acetate) and conditions, resulting in enhanced therapeutic reliability for treating angiogenic ocular diseases compared to existing compositions
2Reliability
If new crystalline forms of Compound 1 are developed to improve treatment effectiveness, then reliability of inhibiting angiogenesis is improved, but the complexity of the pharmaceutical composition increases
Solution Approach 1:
The patent develops multiple crystalline forms (including Form E and Form C) of Compound 1 with distinct physical parameters such as XRPD patterns, densities, and solubility characteristics. Each crystalline form is prepared through specific processes using different solvents and conditions, providing reliable treatment options while systematically characterizing each form to manage the complexity through structured classification and preparation protocols
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 Compound 1 effectively treat proliferative diseases associated with angiogenesis, including cancer and macular degeneration, by administering a therapeutically effective amount, providing a viable solution for conditions like diabetic retinopathy and age-related macular degeneration.
Implementation Method 1
Some embodiments include a process for preparing a crystalline form E described herein, comprising mixing Compound 1 and methanol. Some embodiments include a process for preparing a crystalline form C described herein, comprising mixing Compound 1 and ethyl acetate.
Implementation Method 2
This disclosure relates to crystalline forms of Compound 1. Some embodiments include the crystalline form has an X-ray powder diffraction (XRPD) pattern with a largest peak at about 10-11 degrees 2θ. Some embodiments include a crystalline form of Compound 1 having an X-ray powder diffraction (XRPD) pattern with a largest peak at about 8-9 degrees 2θ.
Data Source
AI summary
Described herein are crystalline forms of Compound 1 useful for the prevention and treatment of angiogenic ocular conditions; methods of treating a disease comprising; processes for preparing; and kits comprising, the same.