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    • 7. 发明授权
    • Crystalline anhydrate forms of a pharmaceutical
    • 晶体无水物形式的药物
    • US09555046B2
    • 2017-01-31
    • US14459528
    • 2014-08-14
    • NeurMedix, Inc.
    • Steven K WhiteIgor IvanisevicKyle StephensMark AndresBrenton Skylar Wolfe
    • C07J5/00C07J7/00A61K31/57
    • C07J1/00A61K31/57C07B2200/13C07J5/00C07J7/0005
    • The invention provides and describes solid state 17α-ethynyl-androst-5-ene-3β,7β,17β-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17α-ethynyl-androst-5-ene-3β,7β,17β-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol and uses of such formulations in treating the described conditions.
    • 本发明提供并描述了包括无定形和结晶形式及其特定多态形式的固态17α-乙炔基 - 雄甾-5-烯-3β,7β,17β-三醇。 17α-乙炔基 - 雄甾-5-烯-3β,7β,17β-三醇的水合物和溶剂合物包括I型无水物和IV型和V型溶剂合物。 本发明还涉及含有所述固态形式的17α-乙炔基 - 雄甾-5-烯-3β,7β,17β-三醇的固体和悬浮液制剂,并且该制剂用于治疗高血糖病症如2型糖尿病和代谢 综合征和自身免疫病症,例如类风湿性关节炎,溃疡性结肠炎和1型糖尿病以及受试者或人类患者的其它炎症相关病症。 本发明还涉及从17α-乙炔基 - 雄甾-5-烯-3β,7β,17β-三醇的固体形式制备液体制剂的方法以及这些制剂在治疗所述病症中的用途。