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公开(公告)号：US08435780B2
公开(公告)日：2013-05-07
申请号：US13324036
申请日：2011-12-13
CPC分类号： C07H21/04 , A01K2217/05 , C12N9/16 , C12N9/78 , C12N9/80 , C12P21/00 , C12Q1/34 , G01N33/6875
摘要： The invention provides histone deacetylase class II nucleic acids and polypeptides, methods and reagents for their use, and related compounds including small molecule libraries containing class II histone deacetylase inhibitors.
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公开(公告)号：US20120094862A1
公开(公告)日：2012-04-19
申请号：US13324036
申请日：2011-12-13
IPC分类号： C40B30/04 , G01N33/573 , C12Q1/34 , C12N9/78 , C12N9/96
CPC分类号： C07H21/04 , A01K2217/05 , C12N9/16 , C12N9/78 , C12N9/80 , C12P21/00 , C12Q1/34 , G01N33/6875
摘要： The invention provides histone deacetylase class II nucleic acids and polypeptides, methods and reagents for their use, and related compounds including small molecule libraries containing class II histone deacetylase inhibitors.
摘要翻译： 本发明提供组蛋白脱乙酰酶II类核酸和多肽，其用途的方法和试剂，以及包含含有II类组蛋白脱乙酰酶抑制剂的小分子文库的相关化合物。
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公开(公告)号：US07250504B2
公开(公告)日：2007-07-31
申请号：US10964313
申请日：2004-10-13
IPC分类号： C07H21/04 , C12N1/19 , C12N1/21 , C12N5/14 , C12N5/18 , C12N5/22 , C12N15/63 , C12N9/14 , C12N9/18
CPC分类号： C07H21/04 , A01K2217/05 , C12N9/16 , C12N9/78 , C12N9/80 , C12P21/00 , C12Q1/34 , G01N33/6875
摘要： The invention provides histone deacetylase class II nucleic acids and polypeptides, methods and reagents for their use, and related compounds including small molecule libraries containing class II histone deacetylase inhibitors.
摘要翻译： 本发明提供组蛋白脱乙酰酶II类核酸和多肽，其用途的方法和试剂，以及包含含有II类组蛋白脱乙酰酶抑制剂的小分子文库的相关化合物。
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4.发明授权Nucleic acids encoding class II human histone deacetylases, and uses related thereto 有权编码II类人组蛋白脱乙酰酶的核酸及其相关用途公开(公告)号：US08076116B2
公开(公告)日：2011-12-13
申请号：US12370390
申请日：2009-02-12
CPC分类号： C07H21/04 , A01K2217/05 , C12N9/16 , C12N9/78 , C12N9/80 , C12P21/00 , C12Q1/34 , G01N33/6875
摘要： The invention provides histone deacetylase class II nucleic acids and polypeptides, methods and reagents for their use, and related compounds including small molecule libraries containing class II histone deacetylase inhibitors.
摘要翻译： 本发明提供组蛋白脱乙酰酶II类核酸和多肽，其用途的方法和试剂，以及包含含有II类组蛋白脱乙酰酶抑制剂的小分子文库的相关化合物。
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公开(公告)号：US20090305384A1
公开(公告)日：2009-12-10
申请号：US12370390
申请日：2009-02-12
CPC分类号： C07H21/04 , A01K2217/05 , C12N9/16 , C12N9/78 , C12N9/80 , C12P21/00 , C12Q1/34 , G01N33/6875
摘要： The invention provides histone deacetylase class II nucleic acids and polypeptides, methods and reagents for their use, and related compounds including small molecule libraries containing class II histone deacetylase inhibitors.
摘要翻译： 本发明提供组蛋白脱乙酰酶II类核酸和多肽，其用途的方法和试剂，以及包含含有II类组蛋白脱乙酰酶抑制剂的小分子文库的相关化合物。
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公开(公告)号：US20090036318A1
公开(公告)日：2009-02-05
申请号：US11831303
申请日：2007-07-31
CPC分类号： C07H21/04 , A01K2217/05 , C12N9/16 , C12N9/78 , C12N9/80 , C12P21/00 , C12Q1/34 , G01N33/6875
摘要： The invention provides histone deacetylase class II nucleic acids and polypeptides, methods and reagents for their use, and related compounds including small molecule libraries containing class II histone deacetylase inhibitors.
摘要翻译： 本发明提供组蛋白脱乙酰酶II类核酸和多肽，其用途的方法和试剂，以及包含含有II类组蛋白脱乙酰酶抑制剂的小分子文库的相关化合物。
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公开(公告)号：US20080269245A1
公开(公告)日：2008-10-30
申请号：US11879466
申请日：2007-07-17
申请人： Stuart L. Schreiber , Scott M. Sternson , Jason C. Wong , Christina M. Grozinger , Stephen J. Haggarty , Kathryn M. Koeller
发明人： Stuart L. Schreiber , Scott M. Sternson , Jason C. Wong , Christina M. Grozinger , Stephen J. Haggarty , Kathryn M. Koeller
IPC分类号： A61K31/496 , C12N5/00 , A61K31/357 , A61K31/422
CPC分类号： C07D319/06 , C07D405/06 , C07D405/12 , C07D413/12 , C07D417/12 , C07D491/10
摘要： In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1, R2, R3, n, X and Y are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. The present invention further provides compounds capable of inhibiting histone deacetylatase activity and methods for treating disorders regulated by histone deacetylase activity (e.g., cancer and protozoal infections) comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof. The present invention additionally provides methods for modulating the glucose-sensitive subset of genes downstream of Ure2p. The present invention also provides methods for preparing compounds of the invention.
摘要翻译： 鉴于需要开发新型治疗剂及其有效的合成方法，本发明提供了新的通式（I）化合物及其药学上可接受的衍生物，其中R 1，R 2， O 2，R 3，N，X和Y如本文所定义。 本发明还提供包含式（I）化合物和药学上可接受的载体的药物组合物。 本发明还提供能够抑制组蛋白去乙酰化酶活性的化合物和用于治疗由组蛋白脱乙酰酶活性调节的病症（例如，癌症和原生动物感染）的方法，包括向有需要的受试者施用治疗有效量的式（I）化合物 。 本发明另外提供了调节Ure2p下游基因的葡萄糖敏感亚群的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：US08178579B2
公开(公告)日：2012-05-15
申请号：US11879466
申请日：2007-07-17
申请人： Stuart L. Schreiber , Scott M. Sternson , Jason C. Wong , Christina M. Grozinger , Stephen J. Haggarty , Kathryn M. Koeller
发明人： Stuart L. Schreiber , Scott M. Sternson , Jason C. Wong , Christina M. Grozinger , Stephen J. Haggarty , Kathryn M. Koeller
IPC分类号： A61K31/425 , C07D317/00
CPC分类号： C07D319/06 , C07D405/06 , C07D405/12 , C07D413/12 , C07D417/12 , C07D491/10
摘要： In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1, R2, R3, n, X and Y are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. The present invention further provides compounds capable of inhibiting histone deacetylatase activity and methods for treating disorders regulated by histone deacetylase activity (e.g., cancer and protozoal infections) comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof. The present invention additionally provides methods for modulating the glucose-sensitive subset of genes downstream of Ure2p. The present invention also provides methods for preparing compounds of the invention.
摘要翻译： 鉴于需要开发新型治疗剂及其合成方法，本发明提供了新的通式（I）化合物及其药学上可接受的衍生物，其中R1，R2，R3，n，X和Y分别为 如本文所定义。 本发明还提供包含式（I）化合物和药学上可接受的载体的药物组合物。 本发明还提供能够抑制组蛋白去乙酰化酶活性的化合物和用于治疗由组蛋白脱乙酰酶活性调节的病症（例如，癌症和原生动物感染）的方法，包括向有需要的受试者施用治疗有效量的式（I）化合物 。 本发明另外提供了调节Ure2p下游基因的葡萄糖敏感亚群的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：US07244853B2
公开(公告)日：2007-07-17
申请号：US10621276
申请日：2003-07-17
申请人： Stuart L. Schreiber , Scott M. Sternson , Jason C. Wong , Christina M. Grozinger , Stephen J. Haggarty , Kathryn M. Koeller
发明人： Stuart L. Schreiber , Scott M. Sternson , Jason C. Wong , Christina M. Grozinger , Stephen J. Haggarty , Kathryn M. Koeller
IPC分类号： C07D309/00 , A01N43/02
CPC分类号： C07D319/06 , C07D405/06 , C07D405/12 , C07D413/12 , C07D417/12 , C07D491/10
摘要： In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1, R2, R3, n, X and Y are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. The present invention further provides compounds capable of inhibiting histone deacetylatase activity and methods for treating disorders regulated by histone deacetylase activity (e.g., cancer and protozoal infections) comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof. The present invention additionally provides methods for modulating the glucose-sensitive subset of genes downstream of Ure2p. The present invention also provides methods for preparing compounds of the invention.
摘要翻译： 鉴于需要开发新型治疗剂及其有效的合成方法，本发明提供了新的通式（I）化合物及其药学上可接受的衍生物，其中R 1，R 2， O 2，R 3，N，X和Y如本文所定义。 本发明还提供包含式（I）化合物和药学上可接受的载体的药物组合物。 本发明还提供能够抑制组蛋白去乙酰化酶活性的化合物和用于治疗由组蛋白脱乙酰酶活性调节的病症（例如，癌症和原生动物感染）的方法，包括向有需要的受试者施用治疗有效量的式（I）化合物 。 本发明另外提供了调节Ure2p下游基因的葡萄糖敏感亚群的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：US08329946B2
公开(公告)日：2012-12-11
申请号：US13221602
申请日：2011-08-30
IPC分类号： C07C259/04 , A61K31/19
CPC分类号： C12N9/80 , A01K2217/05 , A01K2217/075 , A61K31/00 , A61K31/165 , A61K31/407 , A61K38/00 , A61K48/00 , C07K5/126 , C07K14/4702 , C07K14/4703 , C07K2319/00 , C12N9/16
摘要： The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.
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