Crystalline solvate forms of a pharmaceutical
Inventors
White, Steven K. • Ivanisevic, Igor • Stephens, Kyle • Andres, Mark • Wolfe, Brenton Skylar
Assignees
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Publication Number
US-10995112-B2
Publication Date
2021-05-04
Expiration Date
Abstract
Described herein are solid state 17α-ethynylandrost-5-ene-3β,7β,17β-triol including amorphous and crystalline forms and specific polymorphic forms thereof, and use of solid state 17α-ethynylandrost-5-ene-3β,7β,17β-triol in treating numerous diseases and disorders, including hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions, and neurodegenerative conditions in subjects or human patients.
Core Innovation
The invention relates to solid state forms of 17α-ethynylandrost-5-ene-3β,7β,17β-triol, including amorphous and crystalline forms. The solid state forms include crystalline polymorph and pseudopolymorph forms identified by labeled forms such as Form I-IV, Form III, Form IV, and Form V, and the solid state forms can be substantially free of other solid state forms, including substantially free of amorphous form.
The crystalline forms include crystalline solvate forms of 17α-ethynylandrost-5-ene-3β,7β,17β-triol, including crystalline methanolate, crystalline ethanolate, and solvates with alcohol or water. The disclosure also describes crystalline anhydrates characterized by X-ray crystallography space group and unit-cell parameters, and amorphous forms described as substantially free of crystalline.
The document further characterizes the solid state forms using analytical techniques including XRPD, DSC, DTA, TGA, Raman spectroscopy, vibrational spectroscopy, and solid-state NMR. These solid state forms are connected to pharmaceutical composition use, wherein the pharmaceutical composition comprises the solid state form and at least one pharmaceutically acceptable excipient.
Claims Coverage
The document provides one independent method claim, supported by dependent claims that specify the treated neurodegenerative conditions and further narrow the crystalline solvate and labeled solid-state form.
Treating a neurodegenerative condition with a crystalline solvate pharmaceutical composition
Administering to a human or mammal in need thereof an effective amount of a pharmaceutical composition comprising a solid state form of 17α-ethynylandrost-5-ene-3β,7β,17β-triol, wherein the solid state form is crystalline solvate 17α-ethynylandrost-5-ene-3β,7β,17β-triol, and at least one pharmaceutically acceptable excipient.
Coverage centers on a method of treating a neurodegenerative condition by administering an effective amount of a pharmaceutical composition that contains a crystalline solvate of 17α-ethynylandrost-5-ene-3β,7β,17β-triol with a pharmaceutically acceptable excipient, with dependent claims narrowing the neurodegenerative indication and specifying particular crystalline solvate types and labeled crystalline forms.
Stated Advantages
Documented Applications
Treating neurodegenerative conditions by administering an effective amount of a pharmaceutical composition comprising a crystalline solvate of 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
Treating neurodegenerative conditions including Alzheimer’s disease, Parkinson’s disease, or Amyotrophic Lateral Sclerosis.
Treating hyperglycemic/metabolic conditions and autoimmune/inflammatory conditions.
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