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公开(公告)号：US20070270397A1
公开(公告)日：2007-11-22
申请号：US10577239
申请日：2004-10-27
申请人： Simon Bates , Igor Ivanisevic , Barbara Stahly
发明人： Simon Bates , Igor Ivanisevic , Barbara Stahly
IPC分类号： A01N43/00
CPC分类号： G01N23/207
摘要： Crystalline solid forms may be characterized by their unit cell parameters through a process known as indexing. An embodiment of the invention searches for the unit cell parameters of a crystalline solid form using a Monte-Carlo algorithm that incorporates certain rules to reduce search space. Another embodiment refines the results of the search to identify the correct unit cell parameters of the crystalline solid form. These methods may be automated, conveniently requiring little interaction from the user. The indexing method of the invention may be applied, for example, to distinguish between different crystalline solid forms of a substance.
摘要翻译： 结晶固体形式可以通过称为分度的方法通过其单元电池参数来表征。 本发明的实施例使用包含某些规则以减少搜索空间的蒙特卡罗算法搜索结晶固体形式的晶胞参数。 另一个实施方案提炼出结晶固体形式的正确的晶胞参数的搜索结果。 这些方法可以是自动的，方便地要求用户几乎没有交互。 本发明的分度方法可以用于例如区分物质的不同结晶固体形式。
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2.发明申请Analysis and Screening of Solid Forms Using the Atomic Pair Distribution Function 审中-公开使用原子对分布函数分析和筛选固体形式公开(公告)号：US20070243620A1
公开(公告)日：2007-10-18
申请号：US10590204
申请日：2005-02-24
申请人： Simon Bates , Igor Ivanisevic
发明人： Simon Bates , Igor Ivanisevic
CPC分类号： G01N23/207
摘要： A method that comprises providing a PDF trace of a first sample of a substance, providing a PDF trace of a second sample of the substance, and comparing the PDF traces to determine whether the substance of the first sample and the substance of the second sample have the same or different solid forms. This embodiment may be used, for example, to distinguish one solid form of a compound from another, to screen for new solid forms of a compound, or to determine whether a disordered crystalline compound has the same solid form as another crystalline sample of the compound.
摘要翻译： 一种方法，其包括提供物质的第一样品的PDF踪迹，提供所述物质的第二样品的PDF踪迹，以及比较所述PDF踪迹以确定所述第一样品的物质和所述第二样品的物质是否具有 相同或不同的固体形式。 该实施方案可用于例如将化合物的一种固体形式与另一种固体形式区分开，以筛选化合物的新固体形式，或者确定无序结晶化合物是否与化合物的另一结晶样品具有相同的固体形式 。
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公开(公告)号：US07715527B2
公开(公告)日：2010-05-11
申请号：US11935965
申请日：2007-11-06
IPC分类号： G01N23/20
CPC分类号： G01N23/2055
摘要： A method of analyzing patterns. The method comprises: receiving a first diffraction pattern; receiving a second diffraction pattern; receiving a third diffraction pattern; determining a similarity between the first and second diffraction patterns; determining a similarity between the first and third diffraction pattern; determining a similarity between the second and third diffraction pattern; and performing hierarchical cluster analysis on the first and second diffraction pattern based on the determined similarity.
摘要翻译： 分析模式的方法。 该方法包括：接收第一衍射图; 接收第二衍射图案; 接收第三衍射图; 确定所述第一和第二衍射图案之间的相似度; 确定第一和第三衍射图案之间的相似度; 确定第二和第三衍射图案之间的相似度; 以及基于所确定的相似度对所述第一和第二衍射图案执行层次聚类分析。
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公开(公告)号：US07372941B2
公开(公告)日：2008-05-13
申请号：US10635113
申请日：2003-08-06
IPC分类号： G01N23/20
CPC分类号： G01N23/2055
摘要： A method of analyzing patterns. The method comprises: receiving a first diffraction pattern; receiving a second diffraction pattern; receiving a third diffraction pattern; determining a similarity between the first and second diffraction patterns; determining a similarity between the first and third diffraction pattern; determining a similarity between the second and third diffraction pattern; and performing hierarchical cluster analysis on the first and second diffraction pattern based on the determined similarity.
摘要翻译： 分析模式的方法。 该方法包括：接收第一衍射图; 接收第二衍射图案; 接收第三衍射图; 确定所述第一和第二衍射图案之间的相似度; 确定第一和第三衍射图案之间的相似度; 确定第二和第三衍射图案之间的相似度; 以及基于所确定的相似度对所述第一和第二衍射图案执行层次聚类分析。
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公开(公告)号：US08410127B2
公开(公告)日：2013-04-02
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： 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.
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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：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：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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