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21. 发明申请

US20130345455A1 METHODS OF PREPARING PHARMACEUTICAL SOLID STATE FORMS 有权
标题翻译：制备药物固体状态的方法
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.
发明人： Steven K. White , Erin E. Jansen , Keith Lorimer , Brenton Skylar Wolfe
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。

22. 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。

23. 发明授权

US07547687B2 Therapeutic treatment methods 失效
公开(公告)号：US07547687B2
公开(公告)日：2009-06-16
申请号：US11674128
申请日：2007-02-12
申请人： Christopher L. Reading , Clarence N. Ahlem , Dominick L. Auci , Charles Dowding , James M. Frincke , Mei Li , Theodore M. Page , Dwight R. Stickney , Richard J. Trauger , Steven K. White
发明人： Christopher L. Reading , Clarence N. Ahlem , Dominick L. Auci , Charles Dowding , James M. Frincke , Mei Li , Theodore M. Page , Dwight R. Stickney , Richard J. Trauger , Steven K. White
IPC分类号： A61K31/568
CPC分类号： A61K31/56 , A61K31/58
摘要： The invention relates to the use of compounds to ameliorate or treat a 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.

24. 发明申请

US20080090791A1 Cystic fibrosis treatment methods 失效
标题翻译：囊性纤维化治疗方法
公开(公告)号：US20080090791A1
公开(公告)日：2008-04-17
申请号：US11549580
申请日：2006-10-13
申请人： Christopher L. Reading , Clarence N. Ahlem , Dominick L. Auci , Charles Dowding , James M. Frincke , Mei Li , Theodore Page , Dwight R. Stickney , Richard J. Trauger , Steven K. White
发明人： Christopher L. Reading , Clarence N. Ahlem , Dominick L. Auci , Charles Dowding , James M. Frincke , Mei Li , Theodore Page , Dwight R. Stickney , Richard J. Trauger , Steven K. White
IPC分类号： A61K31/58 , A61K31/56 , A61P43/00
CPC分类号： A61K31/58 , A61K31/56 , Y02A50/411
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。

25. 发明申请

US20080085873A1 Disease treatment methods 审中-公开
标题翻译：疾病治疗方法
公开(公告)号：US20080085873A1
公开(公告)日：2008-04-10
申请号：US11549615
申请日：2006-10-13
申请人： Christopher L. Reading , Clarence N. Ahlem , Dominick L. Auci , Charles Dowding , James M. Frincke , Mei Li , Theodore M. Page , Dwight R. Stickney , Richard J. Trauger , Steven K. White
发明人： Christopher L. Reading , Clarence N. Ahlem , Dominick L. Auci , Charles Dowding , James M. Frincke , Mei Li , Theodore M. Page , Dwight R. Stickney , Richard J. Trauger , Steven K. White
IPC分类号： A61K31/58 , A61P17/06 , A61P3/10 , A61P43/00
CPC分类号： A61K31/58 , A61K31/56 , Y02A50/411
摘要： The invention relates to the use of compounds to ameliorate or treat a 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，中性粒细胞减少症或其它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。

26. 发明授权

US5817845A Methods for stereospecific synthesis of 11,13-cis polyene esters 失效
标题翻译：立体特异性合成11,13-顺式多烯酯的方法
公开(公告)号：US5817845A
公开(公告)日：1998-10-06
申请号：US731069
申请日：1996-10-09
申请人： Steven K. White , Chan Kou Hwang , David T. Winn
发明人： Steven K. White , Chan Kou Hwang , David T. Winn
IPC分类号： C07C45/47 , C07C45/60 , C07C47/225 , C07C51/00
CPC分类号： C07C403/20 , C07C403/14 , C07C45/60 , C07B2200/09 , C07C2101/16
摘要： Methods for stereospecific synthesis of 9-cis olefins and retinoids. In one particular aspect, a cis olefin is generated via a lactol ring opening with complete retention of double bond configuration.
摘要翻译：立体特异性合成9-顺式烯烃和类视色素的方法。在一个特定的方面，通过具有完全保留双键构型的内酯醇环开口产生顺式烯烃。

27. 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。

28. 发明申请

US20130338125A1 TREATMENT METHODS USING PHARMACEUTICAL SOLID STATE FORMS 审中-公开
标题翻译：使用药物固体状态的治疗方法
公开(公告)号：US20130338125A1
公开(公告)日：2013-12-19
申请号：US13919728
申请日：2013-06-17
申请人： Steven K. White , Dwight Stickney , Harbor Therapeutics, Inc.
发明人： Steven K. White , Dwight Stickney
IPC分类号： A61K31/569 , A61K31/337
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。

29. 发明申请

US20120220560A1 STEROID TETROL SOLID STATE FORMS 审中-公开
标题翻译： STEROID TETROL固体状态
公开(公告)号：US20120220560A1
公开(公告)日：2012-08-30
申请号：US13328374
申请日：2011-12-16
申请人： Steven K. White , Erin E. Jansen
发明人： Steven K. White , Erin E. Jansen
IPC分类号： A61K31/565 , A61P29/00 , A61P3/08 , A61P3/00 , A61P3/10 , A61P3/04 , C07J1/00 , A61P37/00
CPC分类号： A61K31/56 , C07J1/0022
摘要： The invention relates to solid state forms of androst-5-ene-3β,7β,16α,17β-tetrol, formulations containing or prepared from such solid state forms and use of these materials for modulating unwanted inflammation including acute and chronic non-productive inflammation. The formulations can be used to prevent, treat or slow the progression of conditions related to autoimmunity and metabolic disorders such as arthritis, multiple sclerosis, ulcerative colitis, Type 1 diabetes and Type 2 diabetes.
摘要翻译：本发明涉及固体形式的雄甾-5-烯-3β，17β，16α，17β-四烯，含有或由这些固态形式制备的制剂，以及这些材料用于调节不希望的炎症，包括急性和慢性非 - 生殖炎。制剂可用于预防，治疗或减缓与自身免疫和代谢紊乱如关节炎，多发性硬化，溃疡性结肠炎，1型糖尿病和2型糖尿病有关的病症的进展。

30. 发明申请

US20090291932A1 PHARMACEUTICAL SOLID STATE FORMS 有权
标题翻译：药物固体状态
公开(公告)号：US20090291932A1
公开(公告)日：2009-11-26
申请号：US12370510
申请日：2009-02-12
申请人： Steven K. White , Dwight Stickney , Erin Olson , Keith Richard Lorimer , Brenton Skylar Wolfe
发明人： Steven K. White , Dwight Stickney , Erin Olson , Keith Richard Lorimer , Brenton Skylar Wolfe
IPC分类号： C07J7/00 , A61K31/56 , A61P35/04
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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