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11. 发明申请

US20160083415A1 Crystalline Anhydrate Forms Of A Pharmaceutical 有权
标题翻译：一种药物的结晶无水形式
公开(公告)号：US20160083415A1
公开(公告)日：2016-03-24
申请号：US14459528
申请日：2014-08-14
申请人： Steven K. White , Igor Ivanisevic , Kyle Stephens , Mark Andres , Brenton Skylar Wolfe
发明人： Steven K. White , Igor Ivanisevic , Kyle Stephens , Mark Andres , Brenton Skylar Wolfe
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。

12. 发明申请

US20140018337A1 Steroids Having 7-Oxygen and 17-Heteroaryl Substitution-3 有权
标题翻译：具有7-氧和17-杂芳基取代的类固醇-3
公开(公告)号：US20140018337A1
公开(公告)日：2014-01-16
申请号：US14027842
申请日：2013-09-16
申请人： Harbor Therapeutics, Inc.
发明人： James M. Frincke
IPC分类号： C07J43/00
CPC分类号： C07J43/003 , C07J13/005 , C07J41/0011
摘要： The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3β-hydroxy-17β-aminoandrost-5-ene, 3β-hydroxy-16α-fluoro-17β-aminoandrost-5-ene, 3α-hydroxy-16α-fluoro-17β-aminoandrost-5-ene, 3β-hydroxy-16β-fluoro-17β-aminoandrost-5-ene, 1α,3β-dihydroxy-4α-fluoroandrost-5-ene-17-one, 1α,3β,17β-trihydroxy-4α-fluoroandrost-5-ene, 1β,3β-dihydroxy-6α-bromoandrost-5-ene, 1α-fluoro-3β,12α-dihydroxyandrost-5-ene-17-one, 1α-fluoro-3β,4α-dihydroxyandrost-5-ene and 4α-fluoro-3β,6α,17β-trihydroxyandrostane.
摘要翻译：本发明涉及化合物用于改善或治疗诸如囊性纤维化，中性白细胞减少症或其他示例性病症的病症的用途。可使用的示例性化合物包括3β-羟基-17β-氨基雄甾-5-烯，3β-羟基-16α-氟-17β-氨基雄甾-5-烯，3α-羟基-16α-氟-17β-氨基雄甾-5-烯，3β-羟基-16β-氟-17β-氨基雄甾-5-烯，1α，3β-二羟基-4α-氟代雄甾-5-烯-17-酮，1α，3β，17β-三羟基-4α-氟代雄甾-5-烯，1beta，3β-二羟基-6α-溴代雄甾-5-烯，1α-氟-3β，12α-二羟基雄甾-5-烯-17-酮，1α-氟-3β，4α-二羟基雄甾-5-烯和4α-氟 -3β，6α，17β-三羟基雄甾烷。

13. 发明申请

US20130066087A1 METHODS FOR PREPARING 17-ALKYNYL-7-HYDROXY STEROIDS AND RELATED COMPOUNDS-2 有权
标题翻译：制备17-烷基-7-羟基甾体和相关化合物-2的方法
公开(公告)号：US20130066087A1
公开(公告)日：2013-03-14
申请号：US13664304
申请日：2012-10-30
申请人： Steven K. White , Yu Ge , Yujin Huang
发明人： Steven K. White , Yu Ge , Yujin Huang
IPC分类号： C07J75/00
CPC分类号： C07J1/0048 , C07J71/00 , C07J75/00
摘要： The invention relates to processes for preparing 17-alkynyl-7-hydroxy-steroids, such as 17-Ethynyl-10R,13S-dimethyl 2,3,4,7,8R,9S,10,11,12,13,14S,15,16,17-hexadecahydro-1H-cyclopenta[a]phenanthrene-3R,7R,17S-triol (also referred to as 17α-ethynyl-androst-5-ene-3β,7β,17β-triol), that are essentially free of process impurities having binding activity at nuclear estrogen receptors.
摘要翻译：本发明涉及制备17-炔基-7-羟基甾族化合物的方法，例如17-乙炔基-10R，13S-二甲基2,3,4,7,8R，9S，10,11,12,13,14S， 15,16,17-十六氢-1H-环戊二烯并[a]菲-3R，7R，17S-三醇（也称为17α-乙炔基 - 雄甾-5-烯-3＆bgr，7＆bgr，17＆bgr三醇）其基本上不含在核雌激素受体上具有结合活性的工艺杂质。

14. 发明授权

US08367646B2 Steroid compounds and treatment methods 失效
标题翻译：类固醇化合物和治疗方法
公开(公告)号：US08367646B2
公开(公告)日：2013-02-05
申请号：US13306141
申请日：2011-11-29
申请人： James M. Frincke
发明人： James M. Frincke
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： A61K31/568 , A61K31/565 , A61K31/567 , A61K31/5685 , A61K45/06 , C07J1/00 , C07J1/0011 , C07J1/0022 , C07J1/0025 , C07J1/0048 , C07J31/00 , C07J41/00
摘要： The invention provides methods to treating conditions such as prostate cancer, or for ameliorating one or more symptoms associated with prostate cancer, or for agents that modulate the biological activity of the androgen receptor. The invention also provides methods and compositions suitable for therapeutic applications.
摘要翻译：本发明提供了治疗诸如前列腺癌或改善与前列腺癌相关的一种或多种症状的病症或调节雄激素受体生物学活性的药物的方法。本发明还提供适用于治疗应用的方法和组合物。

15. 发明授权

US08252947B2 Solid state forms of a pharmaceutical 有权
标题翻译：固体形式的药物
公开(公告)号：US08252947B2
公开(公告)日：2012-08-28
申请号：US12418559
申请日：2009-04-03
申请人： Steven K. White , Igor Ivanisevic , Kyle Stephens , Mark Andres , Brenton Skylar Wolfe
发明人： Steven K. White , Igor Ivanisevic , Kyle Stephens , Mark Andres , Brenton Skylar Wolfe
IPC分类号： C07J5/00 , C07J7/00 , A61K31/56
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。

16. 发明授权

US08569275B2 Steroids having 7-oxgen and 17-heteroaryl substitution 有权
标题翻译：类固醇具有7-氧基和17-杂芳基取代基
公开(公告)号：US08569275B2
公开(公告)日：2013-10-29
申请号：US13095528
申请日：2011-04-27
申请人： James M. Frincke
发明人： James M. Frincke
IPC分类号： A61K31/58 , C07J43/00
CPC分类号： C07J43/003 , C07J13/005 , C07J41/0011
摘要： The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3β-hydroxy-17β-aminoandrost-5-ene, 3β-hydroxy-16α-fluoro-17β-aminoandrost-5-ene, 3α-hydroxy-16α-fluoro-17β-aminoandrost-5-ene, 3β-hydroxy-16β-fluoro-17β-aminoandrost-5-ene, 1α,3β-dihydroxy-4α-fluoroandrost-5-ene-17-one, 1α,3β,17β-trihydroxy-4α-fluoroandrost-5-ene, 1β,3β-dihydroxy-6α-bromoandrost-5-ene, 1α-fluoro-3β,12α-dihydroxyandrost-5-ene-17-one, 1α-fluoro-3β,4α-dihydroxyandrost-5-ene and 4α-fluoro-3β,6α,17β-trihydroxyandrostane.
摘要翻译：本发明涉及化合物用于改善或治疗诸如囊性纤维化，中性白细胞减少症或其他示例性病症的病症的用途。可以使用的示例性化合物包括3β-羟基-17β-氨基雄甾-5-烯，3β-羟基-16α-氟-17β-氨基雄甾-5-烯，3α-羟基-16α-氟-17β-氨基雄甾-5-烯，3β-羟基-16β-氟-17β-氨基雄甾-5-烯，1α，3β-二羟基-4α-氟代雄甾-5-烯-17-酮，1α，3β，17β-三羟基-4α-氟代雄甾-5-烯，1beta，3β-二羟基-6α-溴代雄甾-5-烯，1α-氟-3β，12α-二羟基雄甾-5-烯-17-酮，1α-氟-3β，4α-二羟基雄甾-5-烯和4α-氟 -3β，6α，17β-三羟基雄甾烷。

17. 发明申请

US20120296105A1 CRYSTALLINE ANHYDRATE FORMS OF A PHARMACEUTICAL 审中-公开
标题翻译：药物的结晶形式
公开(公告)号：US20120296105A1
公开(公告)日：2012-11-22
申请号：US13563982
申请日：2012-08-01
申请人： Steven K. White , Igor Ivanisevic , Kyle Stephens , Mark Andres , Brenton Skylar Wolfe
发明人： Steven K. White , Igor Ivanisevic , Kyle Stephens , Mark Andres , Brenton Skylar Wolfe
IPC分类号： C07J75/00 , C07J1/00
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。

18. 发明授权

US08309746B2 Methods for preparing 17-alkynyl-7-hydroxy steroids and related compounds 有权
标题翻译：制备17-炔基-7-羟基类固醇及相关化合物的方法
公开(公告)号：US08309746B2
公开(公告)日：2012-11-13
申请号：US12479626
申请日：2009-06-05
申请人： Steven K. White , Yu Ge , Yujin Huang
发明人： Steven K. White , Yu Ge , Yujin Huang
IPC分类号： C07J1/00
CPC分类号： C07J1/0048 , C07J71/00 , C07J75/00
摘要： The invention relates to processes for preparing 17-alkynyl-7-hydroxy-steroids, such as 17-Ethynyl-10R,13S-dimethyl 2,3,4,7,8R,9S, 10,11,12,13,14S,15,16,17-hexadecahydro-1H-cyclopenta[a]phenanthrene-3R, 7R,17S-triol (also referred to as 17α-ethynyl-androst-5-ene-3β,7β,17β-triol), that are essentially free of process impurities having binding activity at nuclear estrogen receptors.
摘要翻译：本发明涉及制备17-炔基-7-羟基甾族化合物的方法，例如17-乙炔基-10R，13S-二甲基2,3,4,7,8R，9S，10,11,12,13,14S， 15,16,17-十六氢-1H-环戊二烯并[a]菲-3R，7R，17S-三醇（也称为17α-乙炔基 - 雄甾-5-烯-3＆bgr，7＆bgr，17＆bgr三醇）其基本上不含在核雌激素受体上具有结合活性的工艺杂质。

19. 发明申请

US20160045516A1 Treatment Methods Using Pharmaceutical Solid State Forms 有权
标题翻译：使用药物固体形式的治疗方法
公开(公告)号：US20160045516A1
公开(公告)日：2016-02-18
申请号：US14459493
申请日：2014-08-14
申请人： Steven K. White , Igor Ivanisevic , Kyle Stephens , Mark Andres , Brenton Skylar Wolfe
发明人： Steven K. White , Igor Ivanisevic , Kyle Stephens , Mark Andres , Brenton Skylar Wolfe
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。

20. 发明授权

US08518922B2 Pharmaceutical solid state forms 有权
标题翻译：药物固体形式
公开(公告)号：US08518922B2
公开(公告)日：2013-08-27
申请号：US12370510
申请日：2009-02-12
申请人： Steven White , Erin Olson , Keith Lorimer , Brenton Skylar Wolfe
发明人： Steven White , Erin Olson , Keith Lorimer , Brenton Skylar Wolfe
IPC分类号： A61K31/567 , C07J1/00
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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