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1.发明申请Inhibitors of GSK-3 and crystal structures of GSK-3beta protein and protein complexes 失效GSK-3的抑制剂和GSK-3β蛋白和蛋白质复合物的晶体结构公开(公告)号：US20080262205A1
公开(公告)日：2008-10-23
申请号：US12079917
申请日：2008-03-28
CPC分类号： C07D487/04 , C07K2299/00 , C12N9/1205 , G06F19/16
摘要： The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3β or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3β protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3β protein or GSK-3β protein complexes.
摘要翻译： 本发明涉及GSK-3抑制剂及其制备方法。 本发明还提供包含抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病如糖尿病和阿尔茨海默氏病的方法。 此外，本发明涉及包含GSK-3β或其同源物的结合口袋的分子或分子复合物。 本发明涉及一种计算机，包括用这种结合口袋的结构坐标编码的数据存储介质。 本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 本发明涉及使用结构坐标来筛选和设计结合GSK-3β蛋白或其同系物的化合物的方法。 本发明还涉及可结晶组合物和包含GSK-3β蛋白或GSK-3β蛋白复合物的晶体。
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2.发明授权Inhibitors of GSK-3 and crystal structures of GSK-3β protein and protein complexes 有权GSK-3的抑制剂和GSK-3＆bgr的晶体结构; 蛋白质和蛋白质复合物公开(公告)号：US07883881B2
公开(公告)日：2011-02-08
申请号：US12652152
申请日：2010-01-05
CPC分类号： C07D487/04 , C07K2299/00 , C12N9/1205 , G06F19/16
摘要： The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3β or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3β protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3β protein or GSK-3β protein complexes.
摘要翻译： 本发明涉及GSK-3抑制剂及其制备方法。 本发明还提供包含抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病如糖尿病和阿尔茨海默氏病的方法。 此外，本发明涉及包含GSK-3和bgr的结合口袋的分子或分子复合物。 或其同系物。 本发明涉及一种计算机，包括用这种结合口袋的结构坐标编码的数据存储介质。 本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 本发明涉及使用结构坐标筛选和设计结合GSK-3和bgr的化合物的方法; 蛋白质或其同系物。 本发明还涉及可结晶组合物和包含GSK-3和bgr的晶体; 蛋白质或GSK-3＆bgr; 蛋白复合物。
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3.发明申请INHIBITORS OF GSK-3 AND CRYSTAL STRUCTURES OF GSK-3BETA PROTEIN AND PROTEIN COMPLEXES 有权GSK-3和GSK-3BETA蛋白和蛋白复合物的晶体结构的抑制剂公开(公告)号：US20100227814A1
公开(公告)日：2010-09-09
申请号：US12652152
申请日：2010-01-05
CPC分类号： C07D487/04 , C07K2299/00 , C12N9/1205 , G06F19/16
摘要： The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3β or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3β protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3β protein or GSK-3β protein complexes.
摘要翻译： 本发明涉及GSK-3抑制剂及其制备方法。 本发明还提供包含抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病如糖尿病和阿尔茨海默氏病的方法。 此外，本发明涉及包含GSK-3和bgr的结合口袋的分子或分子复合物。 或其同系物。 本发明涉及一种计算机，包括用这种结合口袋的结构坐标编码的数据存储介质。 本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 本发明涉及使用结构坐标筛选和设计结合GSK-3和bgr的化合物的方法; 蛋白质或其同系物。 本发明还涉及可结晶组合物和包含GSK-3和bgr的晶体; 蛋白质或GSK-3＆bgr; 蛋白复合物。
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4.发明授权Inhibitors of GSK-3 and crystal structures of GSK-3β protein and protein complexes 失效GSK-3的抑制剂和GSK-3＆bgr的晶体结构; 蛋白质和蛋白质复合物公开(公告)号：US07666647B2
公开(公告)日：2010-02-23
申请号：US12079917
申请日：2008-03-28
CPC分类号： C07D487/04 , C07K2299/00 , C12N9/1205 , G06F19/16
摘要： The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3β or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3β protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3β protein or GSK-3β protein complexes.
摘要翻译： 本发明涉及GSK-3抑制剂及其制备方法。 本发明还提供包含抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病如糖尿病和阿尔茨海默氏病的方法。 此外，本发明涉及包含GSK-3和bgr的结合口袋的分子或分子复合物。 或其同系物。 本发明涉及一种计算机，包括用这种结合口袋的结构坐标编码的数据存储介质。 本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 本发明涉及使用结构坐标筛选和设计结合GSK-3和bgr的化合物的方法; 蛋白质或其同系物。 本发明还涉及可结晶组合物和包含GSK-3和bgr的晶体; 蛋白质或GSK-3＆bgr; 蛋白复合物。
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公开(公告)号：US06916798B2
公开(公告)日：2005-07-12
申请号：US10212471
申请日：2002-08-02
申请人： Jeremy Green , Michael J. Arnost , Albert Pierce
发明人： Jeremy Green , Michael J. Arnost , Albert Pierce
IPC分类号： A61P3/10 , A61P17/06 , A61P19/02 , A61P25/18 , A61P25/28 , A61P31/18 , A61P31/22 , A61P35/00 , A61P43/00 , C07D231/20 , C07D231/46 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/4152 , A61K31/655 , C07D231/08 , C07D401/02
CPC分类号： C07D401/12 , C07D231/20 , C07D231/46 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. The invention also relates to methods for inhibiting Aurora-2 activity and for treating or preventing Aurora-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I. The invention also relates to methods for inhibiting cyclin-dependent kinase-2 activity and for treating or preventing inhibiting cyclin-dependent kinase-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I.
摘要翻译： 本发明涉及可用作GSK-3抑制剂的式I化合物。 本发明还涉及使用式I化合物或包含式I化合物的药物组合物抑制GSK-3活性的方法。 本发明还提供了利用这些化合物和药物组合物治疗和预防各种疾病如糖尿病和阿尔茨海默病的方法。 本发明还涉及使用式I化合物或包含式I化合物的药物组合物抑制Aurora-2活性和治疗或预防Aurora-2介导的疾病的方法。本发明还涉及抑制细胞周期蛋白依赖性激酶 - 2活性，以及使用式I化合物或包含式I化合物的药物组合物治疗或预防抑制细胞周期蛋白依赖性激酶-2介导的疾病。
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公开(公告)号：US07452873B2
公开(公告)日：2008-11-18
申请号：US11145356
申请日：2005-06-03
申请人： Jeremy Green , Michael J. Arnost , Albert Pierce
发明人： Jeremy Green , Michael J. Arnost , Albert Pierce
IPC分类号： C07D231/20 , C07D401/04 , C07D401/12 , A61K31/4152 , A61K31/4155 , A61K31/655
CPC分类号： C07D401/12 , C07D231/20 , C07D231/46 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. The invention also relates to methods for inhibiting Aurora-2 activity and for treating or preventing Aurora-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I. The invention also relates to methods for inhibiting cyclin-dependent kinase-2 activity and for treating or preventing inhibiting cyclin-dependent kinase-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I.
摘要翻译： 本发明涉及可用作GSK-3抑制剂的式I化合物。 本发明还涉及使用式I化合物或包含式I化合物的药物组合物抑制GSK-3活性的方法。 本发明还提供了利用这些化合物和药物组合物治疗和预防各种疾病如糖尿病和阿尔茨海默病的方法。 本发明还涉及使用式I化合物或包含式I化合物的药物组合物抑制Aurora-2活性和治疗或预防Aurora-2介导的疾病的方法。本发明还涉及抑制细胞周期蛋白依赖性激酶 - 2活性，以及使用式I化合物或包含式I化合物的药物组合物治疗或预防抑制细胞周期蛋白依赖性激酶-2介导的疾病。
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公开(公告)号：US07390808B2
公开(公告)日：2008-06-24
申请号：US10135255
申请日：2002-04-29
申请人： Jeremy Green , Michael J. Arnost
发明人： Jeremy Green , Michael J. Arnost
IPC分类号： C07D487/04 , A61K31/5025
CPC分类号： C07D487/04 , C07K2299/00 , C12N9/1205 , G06F19/16
摘要： The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3β or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3β protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3β protein or GSK-3β protein complexes.
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公开(公告)号：US20050261268A1
公开(公告)日：2005-11-24
申请号：US10914051
申请日：2004-08-06
申请人： Michael J. Arnost , Guy W. Bemis , Robert J. Davies , Cornelia J. Forster , Ronald Grey , Mark W. Ledeboer , Brian Ledford , Craig Marhefka , David Messersmith , Albert C. Pierce , Francesco Salituro , Jian Wang
发明人： Michael J. Arnost , Guy W. Bemis , Robert J. Davies , Cornelia J. Forster , Ronald Grey , Mark W. Ledeboer , Brian Ledford , Craig Marhefka , David Messersmith , Albert C. Pierce , Francesco Salituro , Jian Wang
IPC分类号： A61P35/00 , C07D249/14 , C07D401/04 , C07D401/14 , C07D403/04 , A61K31/545 , A61K31/4196 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , C07D501/14 , C07D43/02
CPC分类号： C07D401/04 , C07D249/14 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/04
摘要： The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds and methods of using the compositions in the treatment of various disorders.
摘要翻译： 本发明涉及蛋白激酶抑制剂。 本发明还提供包含本发明化合物的药物组合物，制备化合物的方法和使用该组合物治疗各种疾病的方法。
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公开(公告)号：US5316887A
公开(公告)日：1994-05-31
申请号：US923843
申请日：1992-07-31
CPC分类号： G03C8/10 , Y10S430/165
摘要： There are disclosed color-providing compounds comprising two or more cyclic 1,3 sulfur-nitrogen groups and two or more color-providing moieties, i.e., complete dyes or dye intermediates, capable of releasing the color-forming moieties upon cleavage in the presence of silver ions or a soluble silver complex. The color-providing compounds are useful as image-forming materials in color photographic processes.
摘要翻译： 公开了提供包含两个或多个环状1,3-硫 - 氮基团和两个或更多个提供颜色的部分的提供颜色的化合物，即完全染料或染料中间体，其能够在存在下裂解时释放成色部分 银离子或可溶性银络合物。 着色化合物可用作彩色照相法中的成像材料。
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公开(公告)号：US4886744A
公开(公告)日：1989-12-12
申请号：US850123
申请日：1986-04-10
申请人： Michael J. Arnost , Shai Inbar , Frank A. Meneghini , Paul S. Palumbo , Stephen G. Stroud , Charles M. Zepp
发明人： Michael J. Arnost , Shai Inbar , Frank A. Meneghini , Paul S. Palumbo , Stephen G. Stroud , Charles M. Zepp
IPC分类号： C07D309/34 , C07D311/58 , G01N33/533
CPC分类号： C07D309/34 , C07D311/58 , G01N33/533 , Y10S436/80
摘要： Fluorescent compounds which are conjugates of a biologically active moiety and an arylidene dye moiety. The compounds have a large Stokes shift and are useful in applications such as biological diagnostic elements.
摘要翻译： 作为生物活性部分和亚芳基染料部分的缀合物的荧光化合物。 这些化合物具有大的斯托克斯位移，并且在诸如生物诊断元件的应用中是有用的。
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