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1. 发明授权

US08754237B2 Bifunctional histone deacetylase inhibitors 有权
标题翻译：双功能组蛋白脱乙酰酶抑制剂
公开(公告)号：US08754237B2
公开(公告)日：2014-06-17
申请号：US13550110
申请日：2012-07-16
申请人： James Elliot Bradner , Ralph Mazitschek , Weiping Tang , Stuart L. Schreiber
发明人： James Elliot Bradner , Ralph Mazitschek , Weiping Tang , Stuart L. Schreiber
IPC分类号： A61K31/24 , C07C229/02
CPC分类号： A61K31/19 , A61K31/44 , A61K47/55 , C07C259/06 , C07D249/04 , C07D249/06 , C07D413/12
摘要： In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
摘要翻译：鉴于需要开发新的治疗剂及其有效的合成方法，本发明提供用于抑制组蛋白脱乙酰酶的新型双功能，三官能或多功能化合物及其药学上可接受的盐和衍生物。本发明还提供了治疗由组蛋白脱乙酰酶活性（例如增殖性疾病，癌症，炎性疾病，原生动物感染，脱发等）调节的病症的方法，包括向有需要的受试者施用治疗有效量的本发明化合物。本发明还提供了制备本发明化合物的方法。

2. 发明申请

US20130261023A1 SMALL MOLECULE PRINTING 审中-公开
公开(公告)号：US20130261023A1
公开(公告)日：2013-10-03
申请号：US13648667
申请日：2012-10-10
申请人： David W. Barnes , Angela N. Koehler , James Elliot Bradner , Ralph Mazitschek , Stuart L. Schreiber
发明人： David W. Barnes , Angela N. Koehler , James Elliot Bradner , Ralph Mazitschek , Stuart L. Schreiber
IPC分类号： G01N33/68
CPC分类号： G01N33/6803 , B01J19/0046 , B01J2219/00527 , B01J2219/00605 , B01J2219/00626 , B01J2219/00659 , B01J2219/0072 , B01J2219/0074 , C40B30/04 , C40B40/04 , C40B80/00 , G01N33/50 , G01N33/53 , G01N33/543 , G01N33/54353 , G01N33/547 , G01N33/552 , G01N33/553
摘要： The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support using isocyanate or isothiocyanate chemistry, wherein the density of the array of compounds is at least 1000 spots per cm2. In general, these inventive arrays are generated by: (1) providing a solid support, wherein said solid support is functionalized with an isocyanate or isothiocyanate moiety capable of interacting with a desired chemical compound to form a covalent attachment; (2) providing one or more solutions of one or more types of compounds to be attached to the solid support; (3) delivering said one or more types of compounds to the solid support; and (4) catalyzing the attachment of the compound to the solid support, whereby an array is formed and the array of compounds has a density of at least 1000 spots per cm2. In another aspect, the present invention provides methods for utilizing these arrays to identify small molecule partners for biological macromolecules of interest.

3. 发明申请

US20130331455A1 DEACETYLASE INHIBITORS AND USES THEREOF 有权
标题翻译：脱乙酰酶抑制剂及其用途
公开(公告)号：US20130331455A1
公开(公告)日：2013-12-12
申请号：US13861519
申请日：2013-04-12
申请人： Weiping Tang , James Elliot Bradner , Stuart L. Schreiber
发明人： Weiping Tang , James Elliot Bradner , Stuart L. Schreiber
IPC分类号： C07C259/06
CPC分类号： C07C259/06 , C07C251/86
摘要： The present invention provides novel compounds of formula (I) and pharmaceutical compositions thereof. The inventive compounds are useful as deacetylase inhibitors (e.g., histone deacetylase inhibitors) and may be useful in the treatment of proliferative diseases such as cancer. In particular, the inventive compounds are HDAC6 inhibitors. The invention also provide synthetic methods for preparing the inventive compounds.
摘要翻译：本发明提供新的式（I）化合物及其药物组合物。本发明化合物可用作脱乙酰酶抑制剂（例如组蛋白脱乙酰酶抑制剂），并且可用于治疗增殖性疾病如癌症。特别地，本发明化合物是HDAC6抑制剂。本发明还提供了制备本发明化合物的合成方法。

4. 发明授权

US08440716B2 Deacetylase inhibitors and uses thereof 有权
标题翻译：脱乙酰酶抑制剂及其用途
公开(公告)号：US08440716B2
公开(公告)日：2013-05-14
申请号：US13055241
申请日：2009-07-22
申请人： Weiping Tang , James Elliot Bradner , Stuart L. Schreiber
发明人： Weiping Tang , James Elliot Bradner , Stuart L. Schreiber
IPC分类号： A61K31/24 , A61K31/195 , A61K31/165 , C07C229/02 , C07C251/00 , C07C233/88
CPC分类号： C07C259/06 , C07C251/86
摘要： The present invention provides novel compounds of formula (I) and pharmaceutical compositions thereof. The inventive compounds are useful as deacetylase inhibitors (e.g., histone deacetylase inhibitors) and may be useful in the treatment of proliferative diseases such as cancer. In particular, the inventive compounds are HDAC6 inhibitors. The invention also provide synthetic methods for preparing the inventive compounds.
摘要翻译：本发明提供新的式（I）化合物及其药物组合物。本发明化合物可用作脱乙酰酶抑制剂（例如组蛋白脱乙酰酶抑制剂），并且可用于治疗增殖性疾病如癌症。特别地，本发明化合物是HDAC6抑制剂。本发明还提供了制备本发明化合物的合成方法。

5. 发明申请

US20110172303A1 DEACETYLASE INHIBITORS AND USES THEREOF 有权
标题翻译：脱乙酰酶抑制剂及其用途
公开(公告)号：US20110172303A1
公开(公告)日：2011-07-14
申请号：US13055241
申请日：2009-07-22
申请人： Weiping Tang , James Elliot Bradner , Stuart L. Schreiber
发明人： Weiping Tang , James Elliot Bradner , Stuart L. Schreiber
IPC分类号： A61K31/24 , C12N9/99 , A61K31/195 , A61K31/165 , C07C229/02 , C07C251/00 , C07C233/88
CPC分类号： C07C259/06 , C07C251/86
摘要： The present invention provides novel compounds of formula (I) and pharmaceutical compositions thereof. The inventive compounds are useful as deacetylase inhibitors (e.g., histone deacetylase inhibitors) and may be useful in the treatment of proliferative diseases such as cancer. In particular, the inventive compounds are HDAC6 inhibitors. The invention also provide synthetic methods for preparing the inventive compounds.
摘要翻译：本发明提供新的式（I）化合物及其药物组合物。本发明化合物可用作脱乙酰酶抑制剂（例如组蛋白脱乙酰酶抑制剂），并且可用于治疗增殖性疾病如癌症。特别地，本发明化合物是HDAC6抑制剂。本发明还提供了制备本发明化合物的合成方法。

6. 发明授权

US08999289B2 Treatment of protein degradation disorders 有权
标题翻译：治疗蛋白质降解障碍
公开(公告)号：US08999289B2
公开(公告)日：2015-04-07
申请号：US11386959
申请日：2006-03-22
申请人： Kenneth C. Anderson , James E. Bradner , Edward Franklin Greenberg , Teru Hideshima , Nicholas Paul Kwiatkowski , Ralph Mazitschek , Stuart L. Schreiber , Jared Shaw , Stephen J. Haggarty
发明人： Kenneth C. Anderson , James E. Bradner , Edward Franklin Greenberg , Teru Hideshima , Nicholas Paul Kwiatkowski , Ralph Mazitschek , Stuart L. Schreiber , Jared Shaw , Stephen J. Haggarty
IPC分类号： A61K51/00 , A61K31/357 , A61K31/35 , A61K31/4965 , A61K31/69 , A61K45/06 , A61K49/00 , G01N33/50 , A61K38/50
CPC分类号： A61K38/05 , A61K31/35 , A61K31/357 , A61K31/422 , A61K31/4965 , A61K31/69 , A61K38/50 , A61K45/06 , A61K49/0008 , G01N33/5011 , A61K2300/00
摘要： The invention relates to methods of treating protein degradation disorders, such cellular proliferative disorders (e.g., cancer) and protein deposition disorders (e.g., neurodegenerative disorders). The invention provides methods and pharmaceutical compositions for treating these diseases using aggresome inhibitors or combinations of aggresome inhibitors and proteasome inhibitors. The invention further relates to methods and pharmaceutical compositions for treating multiple myeloma. New HDAC/TDAC inhibitors and aggresome inhibitors are also provided as well as synthetic methodologies for preparing these compounds.
摘要翻译：本发明涉及治疗蛋白质降解病症，细胞增殖性疾病（例如癌症）和蛋白质沉积病症（例如神经变性疾病）的方法。本发明提供了使用聚集抑制剂或聚集抑制剂和蛋白酶体抑制剂的组合来治疗这些疾病的方法和药物组合物。本发明还涉及用于治疗多发性骨髓瘤的方法和药物组合物。还提供了新的HDAC / TDAC抑制剂和聚集抑制剂以及用于制备这些化合物的合成方法。

7. 发明申请

US20090221433A1 SMALL MOLECULE PRINTING 审中-公开
标题翻译：小分子印刷
公开(公告)号：US20090221433A1
公开(公告)日：2009-09-03
申请号：US12159481
申请日：2007-01-03
申请人： David W. Barnes , Angela N. Koehler , James E. Bradner , Ralph Mazitschek , Stuart L. Schreiber
发明人： David W. Barnes , Angela N. Koehler , James E. Bradner , Ralph Mazitschek , Stuart L. Schreiber
IPC分类号： C40B30/04 , C40B40/04 , C40B50/12
CPC分类号： G01N33/6803 , B01J19/0046 , B01J2219/00527 , B01J2219/00605 , B01J2219/00626 , B01J2219/00659 , B01J2219/0072 , B01J2219/0074 , C40B30/04 , C40B40/04 , C40B80/00 , G01N33/50 , G01N33/53 , G01N33/543 , G01N33/54353 , G01N33/547 , G01N33/552 , G01N33/553
摘要： The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support using isocyanate or isothiocyanate chemistry, wherein the density of the array of compounds is at least 1000 spots per cm2. In general, these inventive arrays are generated by: (1) providing a solid support, wherein said solid support is functionalized with an isocyanate or isothiocyanate moiety capable of interacting with a desired chemical compound to form a covalent attachment; (2) providing one or more solutions of one or more types of compounds to be attached to the solid support; (3) delivering said one or more types of compounds to the solid support; and (4) catalyzing the attachment of the compound to the solid support, whereby an array is formed and the array of compounds has a density of at least 1000 spots per cm2. In another aspect, the present invention provides methods for utilizing these arrays to identify small molecule partners for biological macromolecules of interest.
摘要翻译：本发明提供了有助于鉴定能够与感兴趣的生物大分子相互作用的化合物的组合物和方法。在一个方面，提供了一种组合物，其包含使用异氰酸酯或异硫氰酸酯化学连接到固体支持物上的一种或多种类型化学化合物的阵列，其中化合物阵列的密度为每cm 2至少1000个点。通常，这些本发明的阵列通过以下方式产生：（1）提供固体支持物，其中所述固体支持物用能够与所需化学化合物相互作用以形成共价连接的异氰酸酯或异硫氰酸酯部分官能化; （2）提供待连接到固体支持物上的一种或多种类型化合物的一种或多种溶液; （3）将所述一种或多种类型的化合物递送至固体支持物; 和（4）催化化合物与固体支持物的连接，由此形成阵列，并且化合物阵列的密度至少为1000个点/ cm2。在另一方面，本发明提供了利用这些阵列鉴定感兴趣的生物大分子的小分子伴侣的方法。

8. 发明授权

US08507274B2 Compositions and methods for promoting the generation of definitive endoderm 有权
标题翻译：用于促进确定性内胚层的产生的组成和方法
公开(公告)号：US08507274B2
公开(公告)日：2013-08-13
申请号：US12679406
申请日：2010-02-05
申请人： Douglas A. Melton , Malgorzata Borowiak , Rene Maehr , Shuibing Chen , Weiping Tang , Julia L. Fox , Stuart L. Schreiber
发明人： Douglas A. Melton , Malgorzata Borowiak , Rene Maehr , Shuibing Chen , Weiping Tang , Julia L. Fox , Stuart L. Schreiber
IPC分类号： C12N5/00 , C12N5/02 , C07C61/06 , C07C61/16 , C07C405/00
CPC分类号： C12N5/0678 , C12N5/0603 , C12N5/0606 , C12N2501/999 , C12N2506/02 , C12N2506/03
摘要： Certain embodiments disclosed herein are directed to a method of producing endoderm cells, such as definitive endoderm cells by exposing stem cells such as embryonic stem cells or induced pluripotent stem (iPS) cells to an effective amount of at least one compound described herein to differentiate the stem cells into the endoderm cells such as definitive endoderm cells. Differentated endoderm cells produced by the methods disclosed herein can be differentiated into pancreatic epithelium, and other endoderm derivatives such as thymus, liver, stomach, intestine and lung. Another aspect of the present invention relates to a method of producing pancreatic progenitor cells, such as Pdx1-positive pancreatic progenitor cells by exposing endoderm cells, such as definitive endoderm cells to an effective amount of at least one compound described herein to differentiate the definitive endoderm cells into Pdx1-positive pancreatic progenitor cells. Kits and compositions comprising Pdx1-positive pancreatic progenitor produced using the methods are also described.
摘要翻译：本文公开的某些实施例涉及通过将干细胞如胚胎干细胞或诱导的多能干（iPS）细胞暴露于有效量的本文所述的至少一种化合物来分化本发明的内胚层细胞，例如定形内胚层细胞，干细胞进入内胚层细胞，如定形内胚层细胞。通过本文公开的方法产生的分化的内胚层细胞可以分化成胰腺上皮和其它内胚层衍生物如胸腺，肝，胃，肠和肺。本发明的另一方面涉及通过将内胚层细胞如定形内胚层细胞暴露于有效量的至少一种本文所述的化合物来分化定形内胚层来产生胰腺祖细胞如Pdx1阳性胰腺祖细胞的方法细胞进入Pdx1阳性胰腺祖细胞。还描述了使用该方法制备的包含Pdx1阳性胰腺祖细胞的组合物和组合物。

9. 发明申请

US20120039909A1 EPIGENETIC MECHANISMS RE-ESTABLISH ACCESS TO LONG-TERM MEMORY AFTER NEURONAL LOSS 审中-公开
标题翻译：神经机制在神经损失后重新获得长期记忆
公开(公告)号：US20120039909A1
公开(公告)日：2012-02-16
申请号：US13279636
申请日：2011-10-24
申请人： Li-Huei Tsai , Andre Fischer , Stephen Haggarty , Weiping Tang , Stuart L. Schreiber
发明人： Li-Huei Tsai , Andre Fischer , Stephen Haggarty , Weiping Tang , Stuart L. Schreiber
IPC分类号： A61K31/167 , A61K31/404 , A61K31/166 , A61K31/353 , A61K48/00 , A61P25/00 , A61K39/395 , A61K31/7068 , A61K31/19 , A61K31/4406 , A61P25/28 , A61K31/4192 , A61K31/7088
CPC分类号： A61K31/164 , A61K31/19 , A61K31/215 , A61K31/404 , A61K31/4192 , A61K31/7052 , A61K31/7068
摘要： The invention relates to methods and products for enhancing and improving recovery of lost memories. In particular the methods are accomplished through the increase of histone acetylation.
摘要翻译：本发明涉及用于增强和改善丢失记忆恢复的方法和产品。特别是通过增加组蛋白乙酰化来实现这些方法。

10. 发明授权

US08088951B2 Epigenetic mechanisms re-establish access to long-term memory after neuronal loss 有权
标题翻译：神经元损失后，表观遗传学机制重新获得长期记忆
公开(公告)号：US08088951B2
公开(公告)日：2012-01-03
申请号：US11998834
申请日：2007-11-30
申请人： Li-Huei Tsai , Andre Fischer , Stephen Haggarty , Weiping Tang , Stuart L. Schreiber
发明人： Li-Huei Tsai , Andre Fischer , Stephen Haggarty , Weiping Tang , Stuart L. Schreiber
IPC分类号： C07C233/00
CPC分类号： A61K31/164 , A61K31/19 , A61K31/215 , A61K31/404 , A61K31/4192 , A61K31/7052 , A61K31/7068
摘要： The invention relates to methods and products for enhancing and improving recovery of lost memories. In particular the methods are accomplished through the increase of histone acetylation.
摘要翻译：本发明涉及用于增强和改善丢失记忆恢复的方法和产品。特别是通过增加组蛋白乙酰化来实现这些方法。

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