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公开(公告)号：US20090291932A1
公开(公告)日：2009-11-26
申请号：US12370510
申请日：2009-02-12
CPC分类号： A61K31/569 , A61K31/337 , C07J1/0048 , C07J7/0005
摘要： The invention provides and describes solid state 17α-ethynyl-5α-androstane-3α,17β-diol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-5α-androstane-3α,17β-diol include Form III anhydrate and Form I solvate. The invention further relates to solid and suspension formulations containing 17α-ethynyl-5α-androstane-3α,17β-diol in a described solid state form and use of the formulations to treat cancers or precancers such as prostate cancer or breast cancer in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-5α-androstane-3α,17β-diol and uses of such formulations in treating the described conditions.
摘要翻译： 本发明提供并描述了固态17α-乙炔基-5α-雄甾烷-3α，17β-二醇，其包括无定形和结晶形式及其特定的多态形式。 17α-乙炔基-5α-雄甾烷-3α，17β-二醇的水合物和溶剂化物包括III型无水物和I型溶剂合物。 本发明还涉及含有所述固体形式的17α-乙炔基-5α-雄甾烷-3α，17β-二醇的固体和悬浮液制剂，并且该制剂用于治疗受试者或人类中的癌症或前列腺癌如前列腺癌或乳腺癌 耐心。 本发明还涉及从17α-乙炔基-5α-雄甾烷-3α，17β-二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。
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公开(公告)号：US20160083415A1
公开(公告)日：2016-03-24
申请号：US14459528
申请日：2014-08-14
IPC分类号： C07J7/00
CPC分类号： C07J1/00 , A61K31/57 , C07B2200/13 , C07J5/00 , C07J7/0005
摘要： 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.
摘要翻译： 本发明提供并描述了固态17α-乙炔基 - 雄甾-5-烯-3β，其中包括无定形和结晶形式及其特定多态形式的17β-三醇。 17α-乙炔基 - 雄甾-5-烯-3＆bgr; 7＆bgr，17＆bgr三醇的水合物和溶剂化物包括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，17α，17β-三醇的固体和悬浮液制剂，以及该制剂用于治疗高血糖病症如2型 糖尿病和代谢综合征以及自身免疫病症，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他炎症相关病症。 本发明还涉及从17α-乙炔基 - 雄甾-5-烯-3β，7α，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。
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公开(公告)号：US20160175322A9
公开(公告)日：2016-06-23
申请号：US14459493
申请日：2014-08-14
IPC分类号： A61K31/57
CPC分类号： C07J1/00 , A61K31/57 , C07B2200/13 , C07J5/00 , C07J7/0005
摘要： 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.
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公开(公告)号：US20120302537A1
公开(公告)日：2012-11-29
申请号：US13563996
申请日：2012-08-01
IPC分类号： A61K31/57 , A61P3/00 , A61P3/10 , A61P3/04 , A61P3/06 , A61P25/28 , A61P25/16 , A61P25/00 , A61P27/02 , A61P9/10 , A61P7/04 , A61P37/00 , A61P1/00 , A61P1/04 , A61P29/00
CPC分类号： C07J1/00 , A61K31/57 , C07B2200/13 , C07J5/00 , C07J7/0005
摘要： 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.
摘要翻译： 本发明提供并描述了固态17α-乙炔基 - 雄甾-5-烯-3β，其中包括无定形和结晶形式及其特定多态形式的17β-三醇。 17α-乙炔基 - 雄甾-5-烯-3＆bgr; 7＆bgr，17＆bgr三醇的水合物和溶剂化物包括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，17α，17β-三醇的固体和悬浮液制剂，以及该制剂用于治疗高血糖病症如2型 糖尿病和代谢综合征以及自身免疫病症，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他炎症相关病症。 本发明还涉及从17α-乙炔基 - 雄甾-5-烯-3β，7α，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。
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公开(公告)号：US20130345455A1
公开(公告)日：2013-12-26
申请号：US13919593
申请日：2013-06-17
申请人： Keith Lorimer , Brenton Skylar Wolfe , Erin E. Jansen , Steven K. White , Harbor Therapeutics, Inc.
IPC分类号： C07J7/00
CPC分类号： A61K31/569 , A61K31/337 , C07J1/0048 , C07J7/0005
摘要： The invention provides and describes solid state 17α-ethynyl-5α-androstane-3α,17β-diol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-5α-androstane-3α,17β-diol include Form III anhydrate and Form I solvate. The invention further relates to solid and suspension formulations containing 17α-ethynyl-5α-androstane-3α,17β-diol in a described solid state form and use of the formulations to treat cancers or precancers such as prostate cancer or breast cancer in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-5α-androstane-3α,17β-diol and uses of such formulations in treating the described conditions.
摘要翻译： 本发明提供并描述了固态17α-乙炔基-5α-雄甾烷-3α，17β-二醇，其包括无定形和结晶形式及其特定的多态形式。 17α-乙炔基-5α-雄甾烷-3α，17β-二醇的水合物和溶剂化物包括III型无水物和I型溶剂合物。 本发明还涉及含有所述固体形式的17α-乙炔基-5α-雄甾烷-3α，17β-二醇的固体和悬浮液制剂，并且该制剂用于治疗受试者或人类中的癌症或前列腺癌如前列腺癌或乳腺癌 耐心。 本发明还涉及从17α-乙炔基-5α-雄甾烷-3α，17β-二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。
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公开(公告)号：US08252947B2
公开(公告)日：2012-08-28
申请号：US12418559
申请日：2009-04-03
CPC分类号： C07J1/00 , A61K31/57 , C07B2200/13 , C07J5/00 , C07J7/0005
摘要： 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, β,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.
摘要翻译： 本发明提供并描述了固态17α-乙炔基 - 雄甾-5-烯-3和bgr，17和b-三醇，包括无定形和结晶形式及其特定的多晶型物。 17α-乙炔基 - 雄甾-5-烯-3＆bgr;，17β-三醇的水合物和溶剂化物包括Form I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，17α，17β-三醇的固体和悬浮液制剂，以及该制剂用于治疗高血糖病症如2型 糖尿病和代谢综合征以及自身免疫病症，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他炎症相关病症。 本发明还涉及从固体形式的17α-乙炔基 - 雄甾-5-烯-3β，7α，17β-三醇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。
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公开(公告)号：US20130345184A1
公开(公告)日：2013-12-26
申请号：US13919386
申请日：2013-06-17
申请人： Brenton Skylar Wolfe , Steven K. White , Erin E. Jansen , Keith Lorimer , Harbor Therapeutics, Inc.
IPC分类号： C07J1/00 , A61K31/337 , A61K31/569
CPC分类号： A61K31/569 , A61K31/337 , C07J1/0048 , C07J7/0005
摘要： The invention provides and describes solid state 17α-ethynyl-5α-androstane-3α,17β-diol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-5α-androstane-3α,17β-diol include Form III anhydrate and Form I solvate. The invention further relates to solid and suspension formulations containing 17α-ethynyl-5α-androstane-3α,17β-diol in a described solid state form and use of the formulations to treat cancers or precancers such as prostate cancer or breast cancer in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-5α-androstane-3α,17β-diol and uses of such formulations in treating the described conditions.
摘要翻译： 本发明提供并描述了固态17α-乙炔基-5α-雄甾烷-3α，17β-二醇，其包括无定形和结晶形式及其特定的多态形式。 17α-乙炔基-5α-雄甾烷-3α，17β-二醇的水合物和溶剂化物包括III型无水物和I型溶剂合物。 本发明还涉及含有所述固体形式的17α-乙炔基-5α-雄甾烷-3α，17β-二醇的固体和悬浮液制剂，并且该制剂用于治疗受试者或人类中的癌症或前列腺癌如前列腺癌或乳腺癌 耐心。 本发明还涉及从17α-乙炔基-5α-雄甾烷-3α，17β-二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。
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公开(公告)号：US20120296105A1
公开(公告)日：2012-11-22
申请号：US13563982
申请日：2012-08-01
CPC分类号： C07J1/00 , A61K31/57 , C07B2200/13 , C07J5/00 , C07J7/0005
摘要： 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.
摘要翻译： 本发明提供并描述了固态17α-乙炔基 - 雄甾-5-烯-3β，其中包括无定形和结晶形式及其特定多态形式的17β-三醇。 17α-乙炔基 - 雄甾-5-烯-3＆bgr; 7＆bgr，17＆bgr三醇的水合物和溶剂化物包括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，17α，17β-三醇的固体和悬浮液制剂，以及该制剂用于治疗高血糖病症如2型 糖尿病和代谢综合征以及自身免疫病症，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他炎症相关病症。 本发明还涉及从17α-乙炔基 - 雄甾-5-烯-3β，7α，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。
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公开(公告)号：US20090291933A1
公开(公告)日：2009-11-26
申请号：US12418559
申请日：2009-04-03
IPC分类号： A61K31/567 , C07J5/00 , A61P25/28 , A61P9/10
CPC分类号： C07J1/00 , A61K31/57 , C07B2200/13 , C07J5/00 , C07J7/0005
摘要： 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.
摘要翻译： 本发明提供并描述了固态17α-乙炔基 - 雄甾-5-烯-3β，7beta，17β-三醇，其包括无定形和结晶形式及其特定的多态形式。 17α-乙炔基 - 雄甾-5-烯-3β，7beta，17β-三醇的水合物和溶剂化物包括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，7beta，17β-三醇的固体和悬浮液制剂，以及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，7beta，17β-三醇的固态形式制备液体制剂的方法以及这些制剂在治疗所述条件中的用途。
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公开(公告)号：US20160045516A1
公开(公告)日：2016-02-18
申请号：US14459493
申请日：2014-08-14
IPC分类号： A61K31/57
CPC分类号： C07J1/00 , A61K31/57 , C07B2200/13 , C07J5/00 , C07J7/0005
摘要： 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.
摘要翻译： 本发明提供并描述了固态17α-乙炔基 - 雄甾-5-烯-3β，其中包括无定形和结晶形式及其特定多态形式的17β-三醇。 17α-乙炔基 - 雄甾-5-烯-3＆bgr; 7＆bgr，17＆bgr三醇的水合物和溶剂化物包括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，17α，17β-三醇的固体和悬浮液制剂，以及该制剂用于治疗高血糖病症如2型 糖尿病和代谢综合征以及自身免疫病症，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他炎症相关病症。 本发明还涉及从17α-乙炔基 - 雄甾-5-烯-3β，7α，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。
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