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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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3.发明申请SUBSTITUTED TETRAZOL-1-YL-PHENOXYMETHYL-THIAZOL-2-YL-PIPERIDINYL-PYRIMIDINE SALTS 有权取代的四氮唑-1-基-L-苯氧基甲基 - 噻唑-2-基-L-哌啶子基吡啶盐公开(公告)号：US20110152270A1
公开(公告)日：2011-06-23
申请号：US12886470
申请日：2010-09-20
申请人： Jiangao Song , Charles A. McWherter , Fang Ma , Mark Andres , Igor Ivanisevic , Ekaterina Albert , Patricia Andres
发明人： Jiangao Song , Charles A. McWherter , Fang Ma , Mark Andres , Igor Ivanisevic , Ekaterina Albert , Patricia Andres
IPC分类号： A61K31/506 , C07D417/14 , A61K31/4985 , A61P3/00 , A61P3/10 , A61P3/08 , A61P3/06
CPC分类号： C07D417/14 , A61K31/506 , A61K45/06 , C07B2200/13 , C07D513/14
摘要： Crystalline salts of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine, compositions thereof, methods for their preparation, and methods for their use are disclosed.
摘要翻译： 5-乙基-2- {4- [4-（4-四唑-1-基 - 苯氧基甲基） - 噻唑-2-基] - 哌啶-1-基} - 嘧啶的结晶盐，其组合物，其制备方法 ，并公开了其使用方法。
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4.发明申请SUBSTITUTED TETRAZOL-1-YL-PHENOXYMETHYL-THIAZOL-2-YL-PIPERIDINYL-PYRIMIDINE SALTS 有权取代的四氮唑-1-基-L-苯氧基甲基 - 噻唑-2-基-L-哌啶子基吡啶盐公开(公告)号：US20140038971A1
公开(公告)日：2014-02-06
申请号：US13853000
申请日：2013-03-28
申请人： Jiangao SONG , Charles A. McWherter , Fang Ma , Mark Andres , Igor Ivanisevic , Ekaterina Albert , Patricia Andres
发明人： Jiangao SONG , Charles A. McWherter , Fang Ma , Mark Andres , Igor Ivanisevic , Ekaterina Albert , Patricia Andres
IPC分类号： C07D417/14 , A61K31/506 , A61K45/06
CPC分类号： C07D417/14 , A61K31/506 , A61K45/06 , C07B2200/13 , C07D513/14
摘要： Crystalline salts of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine, compositions thereof, methods for their preparation, and methods for their use are disclosed.
摘要翻译： 5-乙基-2- {4- [4-（4-四唑-1-基 - 苯氧基甲基） - 噻唑-2-基] - 哌啶-1-基} - 嘧啶的结晶盐，其组合物，其制备方法 ，并公开了其使用方法。
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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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![POLYMORPHS OF BENZOATE SALT OF 2-[[6-[(3r)-3-AMINO-1- PIPERIDINYL]-3,4-DIHYDRO-3- METHYL-2,4-DIOXO-1(2H)-PYRIMIDINYL]METHYL]-BENZONITRILE AND METHODS OF USE THEREFORE](/abs-image/US/2009/12/10/US20090306379A1/abs.jpg.150x150.jpg)
6.发明申请POLYMORPHS OF BENZOATE SALT OF 2-[[6-[(3r)-3-AMINO-1- PIPERIDINYL]-3,4-DIHYDRO-3- METHYL-2,4-DIOXO-1(2H)-PYRIMIDINYL]METHYL]-BENZONITRILE AND METHODS OF USE THEREFORE 失效2 - [[6 - [（3r）-3-氨基-1-哌啶基] -3,4-二氢-3-甲基-2,4-二氧代-1（2H） - 嘧啶]亚甲基]苯甲酸盐的聚合物] - 苯并噻唑及其使用方法公开(公告)号：US20090306379A1
公开(公告)日：2009-12-10
申请号：US12536377
申请日：2009-08-05
申请人： Mark Andres , Keith Lorimer
发明人： Mark Andres , Keith Lorimer
IPC分类号： C07D239/553
CPC分类号： A61K31/513 , C07D401/04
摘要： Compositions comprising Compound I, wherein the Compound I is present in one or more polymorphic forms. Also provided are kits and articles of manufacture with compositions comprising one or more polymorphs of Compound I, and methods of using the compositions to treat various diseases.
摘要翻译： 包含化合物I的组合物，其中化合物I以一种或多种多晶型形式存在。 还提供了具有包含化合物I的一种或多种多晶型物的组合物的试剂盒和制品以及使用该组合物治疗各种疾病的方法。
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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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9.发明授权Substituted tetrazol-1-yl-phenoxymethyl-thiazol-2-yl-piperidinyl-pyrimidine salts 有权取代的四唑-1-基 - 苯氧基甲基 - 噻唑-2-基 - 哌啶基 - 嘧啶盐公开(公告)号：US08815886B2
公开(公告)日：2014-08-26
申请号：US13853000
申请日：2013-03-28
申请人： Jiangao Song , Charles A. McWherter , Fang Ma , Mark Andres , Igor Ivanisevic , Ekaterina Albert , Patricia Andres
发明人： Jiangao Song , Charles A. McWherter , Fang Ma , Mark Andres , Igor Ivanisevic , Ekaterina Albert , Patricia Andres
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D417/14 , A61K31/506 , A61K45/06 , C07B2200/13 , C07D513/14
摘要： Crystalline salts of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine, compositions thereof, methods for their preparation, and methods for their use are disclosed.
摘要翻译： 5-乙基-2- {4- [4-（4-四唑-1-基 - 苯氧基甲基） - 噻唑-2-基] - 哌啶-1-基} - 嘧啶的结晶盐，其组合物，其制备方法 ，并公开了其使用方法。
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10.发明授权Key intermediate for the preparation of Stilbenes, solid forms of Pterostilbene, and methods for making the same 有权二苯乙烯制备的主要中间体，芪二烯的固体形式及其制备方法公开(公告)号：US08524782B2
公开(公告)日：2013-09-03
申请号：US13011593
申请日：2011-01-21
申请人： Gottumukkala V. Subbaraju , Masna Mahesh , Hindupur R. Mohan , Thatipally Suresh , Igor Ivanisevic , Mark Andres , Kyle Stephens
发明人： Gottumukkala V. Subbaraju , Masna Mahesh , Hindupur R. Mohan , Thatipally Suresh , Igor Ivanisevic , Mark Andres , Kyle Stephens
IPC分类号： A01N31/14 , A61K31/075
CPC分类号： C07C37/055 , C07C41/26 , C07D309/12 , C07C39/21 , C07C43/23
摘要： The present invention provides a scalable process for the preparation of stilbenes by (i) condensing 3,5-dialkylbenzyl phosphonates with 4′-O-tetrahydropyranyl benzaldehyde to get 3,5-alkyl-4′-O-tetrahydropyranyl Stilbene and (ii) deprotecting the obtained 3,5-Dialkyl-4′-O-tetrahydropyranylstilbene to yield stilbenes. The present invention also provides a novel intermediate 3,5-Dialkyl-4′-O-tetrahydropyranyl stilbene, which is a key intermediate for the synthesis of stilbenes such as Pterostilbene and Resveratrol. The present invention also provides characteristics of various solid forms of Pterostilbene, methods for their preparation, as well as dosage forms containing the same for administration to or consumption by humans.
摘要翻译： 本发明提供了通过（i）将3,5-二烷基苄基膦酸酯与4'-O-四氢吡喃基苯甲醛缩合得到3,5-烷基-4'-O-四氢吡喃基二苯乙烯来制备二苯乙烯的可伸缩方法，和（ii） 将得到的3,5-二烷基-4'-O-四氢吡喃基芪脱保护，得到二苯乙烯。 本发明还提供了一种新型的中间体3,5-二烷基-4'-O-四氢吡喃基二苯乙烯，它是芪类和白藜芦醇合成二苯乙烯的关键中间体。 本发明还提供了各种固体形式的芪萜烯的特性，其制备方法，以及含有它们用于给予或消费人的剂型。
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