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1. 发明申请

US20130018103A1 BIFUNCTIONAL HISTONE DEACETYLASE INHIBITORS 有权
公开(公告)号：US20130018103A1
公开(公告)日：2013-01-17
申请号：US13550110
申请日：2012-07-16
申请人： James Elliot Bradner , Ralph Mazitschek , Weiping Tang , Stuart S. Schreiber
发明人： James Elliot Bradner , Ralph Mazitschek , Weiping Tang , Stuart S. Schreiber
IPC分类号： A61K31/197 , C12N5/071 , C12N9/99 , C07C259/06 , A61P35/00
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.

2. 发明授权

US08716344B2 Class- and isoform-specific HDAC inhibitors and uses thereof 有权
标题翻译：类别和异构体特异性HDAC抑制剂及其用途
公开(公告)号：US08716344B2
公开(公告)日：2014-05-06
申请号：US13389814
申请日：2010-08-11
申请人： Ralph Mazitschek , James Elliot Bradner
发明人： Ralph Mazitschek , James Elliot Bradner
IPC分类号： A61K38/05 , A61K31/495 , C12Q1/48 , A61K45/06 , C07D239/42 , C07D401/04
CPC分类号： C07C243/38 , A61K31/175 , A61K31/495 , A61K38/05 , A61K45/06 , C07D239/42 , C07D401/04 , C12Q1/48
摘要： The present invention relates to compounds of the following formula wherein R3 is a fluorescent tag. Another aspect of the invention provides an assay for determining the inhibitory effect of a test compound on an HDAC protein comprising: incubating the HDAC protein with a substrate of the above formula in the presence of a test compound; and determining the activity of the HDAC protein.
摘要翻译：本发明涉及下式的化合物，其中R3是荧光标记。本发明的另一方面提供了一种用于测定测试化合物对HDAC蛋白质的抑制作用的测定法，包括：在测试化合物存在下，将HDAC蛋白质与上式的底物一起孵育; 并测定HDAC蛋白的活性。

3. 发明申请

US20130040998A1 FLUORINATED HDAC INHIBITORS AND USES THEREOF 审中-公开
标题翻译：氟化HDAC抑制剂及其用途
公开(公告)号：US20130040998A1
公开(公告)日：2013-02-14
申请号：US13520650
申请日：2011-01-05
申请人： James Elliot Bradner , Ralph Mazitschek
发明人： James Elliot Bradner , Ralph Mazitschek
IPC分类号： A61K31/165 , A61K31/4045 , C07C239/14 , A61P35/00 , A61K31/40 , C07D213/56 , A61K31/44 , C07D209/14 , C07D207/333
CPC分类号： C07C259/06 , C07C259/10 , C07C271/28 , C07D207/323 , C07D209/14 , C07D213/75 , C07D221/14 , C07D413/12
摘要： Fluorinated deacetylase inhibitors of the general formulae (I), (II), and (III): and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and disorders associated with acetylase activity as described herein (e.g., cancer, neurodegenerative diseases, inflammatory diseases).
摘要翻译：如本文所述的通式（I），（II）和（III）的氟化脱乙酰酶抑制剂及其药学上可接受的盐可用作组蛋白脱乙酰酶或其它脱乙酰酶的抑制剂，因此可用于治疗各种与本文所述的乙酰酶活性相关的疾病和病症（例如，癌症，神经变性疾病，炎性疾病）。

4. 发明申请

US20090312363A1 BIFUNCTIONAL HISTONE DEACETYLASE INHIBITORS 有权
标题翻译：双功能脱乙酰壳多糖酶抑制剂
公开(公告)号：US20090312363A1
公开(公告)日：2009-12-17
申请号：US12279440
申请日：2007-02-14
申请人： James Elliot Bradner , Ralph Mazitschek , Tang Weiping , Stuart S. Schreiber
发明人： James Elliot Bradner , Ralph Mazitschek , Tang Weiping , Stuart S. Schreiber
IPC分类号： A61K31/4353 , C07D263/04 , A61K31/421 , C07D319/06 , A61K31/351 , C07D221/04 , C07C237/02 , A61K31/16 , C07D209/04 , A61K31/40 , C07C243/00 , C07D249/04 , A61K31/4192 , C12N9/99 , C12Q1/37
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。

5. 发明授权

US5838877A Noise suppression in PWM-driven DC motor 失效
公开(公告)号：US5838877A
公开(公告)日：1998-11-17
申请号：US510430
申请日：1995-08-02
申请人： James Elliot , Mohamed Abbas , John R. Suriano , Thomas W. Holmes
发明人： James Elliot , Mohamed Abbas , John R. Suriano , Thomas W. Holmes
IPC分类号： H02K11/02 , H02M1/12 , H02M1/44 , H02P7/28 , H03H1/00 , H03H7/01 , H04B15/02 , H02P5/06
CPC分类号： H02M1/44 , H02K11/02 , H02M1/12 , H02P7/28 , H03H1/0007 , H04B15/02
摘要： A system for reducing Radio Frequency Interference (RFI) produced by motors which are powered by Pulse Width Modulation (PWM). It is believed that the PWM induces radiation at the PWM frequency and harmonics. The invention shields power cables which carry the PWM pulsed current, and provides capacitive shunting of one of the cables to ground.

6. 发明申请

US20140213620A1 HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译： HISTONE脱乙酰酶抑制剂
公开(公告)号：US20140213620A1
公开(公告)日：2014-07-31
申请号：US13944320
申请日：2013-07-17
申请人： James Elliot Bradner , Ralph Mazitschek
发明人： James Elliot Bradner , Ralph Mazitschek
IPC分类号： C07D413/12 , C07C235/78 , C07D319/06
CPC分类号： A61K31/231 , A61K9/0014 , A61K31/165 , A61K31/337 , C07C235/78 , C07C259/06 , C07D319/06 , C07D413/12
摘要： In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
摘要翻译：鉴于需要开发新的治疗剂，本发明提供了新的组蛋白脱乙酰酶抑制剂。这些化合物包括酯键，使它们对酯酶的失活敏感。因此，这些化合物特别可用于治疗皮肤病。当化合物达到血流时，酯酶或具有酯酶活性的酶将化合物切割成具有大大降低的活性的生物活性片段或片段。理想地，这些降解产物表现出短的血清和/或全身半衰期并被快速消除。这些化合物及其药物组合物例如特别可用于治疗皮肤T细胞淋巴瘤，神经纤维瘤病，牛皮癣，脱发，皮肤色素沉着和皮炎。本发明还提供了制备本发明化合物及其中间体的方法。

7. 发明授权

US08720001B2 Tool for a surface treating appliance 有权
标题翻译：表面处理设备用工具
公开(公告)号：US08720001B2
公开(公告)日：2014-05-13
申请号：US11596174
申请日：2005-04-25
申请人： Stephen Benjamin Courtney , Nicholas George Byatt , James Elliot Cameron
发明人： Stephen Benjamin Courtney , Nicholas George Byatt , James Elliot Cameron
IPC分类号： A47L9/04
CPC分类号： A47L9/0416 , Y10T29/49822
摘要： A tool for a surface treating appliance, such as a vacuum cleaner, includes a housing having a suction opening. An agitator, such as a brush bar, is rotatably located in the suction opening of the housing. The interior of such a tool can get blocked due to large objects being drawn in through the suction opening, or else by threads and fibers becoming tangled in the brush bar. The brush bar may be removed through the suction opening for replacement or repair. A portion of the housing may also be removable to clear the way for the user to access a narrow opening in the neck of the tool which may be prone to blockage.
摘要翻译：用于表面处理装置的工具，例如真空吸尘器，包括具有吸入口的壳体。搅拌器，例如刷杆，可旋转地位于壳体的吸入口中。这种工具的内部由于大的物体通过吸入口被吸入而被阻塞，或者由于线和纤维缠绕在刷杆中。刷杆可以通过抽吸口移除以进行更换或修理。壳体的一部分也可以是可拆卸的，以便使用户能够进入可能易于堵塞的工具颈部中的狭窄的开口。

8. 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。

9. 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.

10. 发明授权

US08383855B2 Histone deacetylase inhibitors 有权
公开(公告)号：US08383855B2
公开(公告)日：2013-02-26
申请号：US12279398
申请日：2007-02-14
申请人： James Elliot Bradner , Ralph Mazitschek
发明人： James Elliot Bradner , Ralph Mazitschek
IPC分类号： C07C259/04 , A61K31/47 , A61K31/19
CPC分类号： A61K31/231 , A61K9/0014 , A61K31/165 , A61K31/337 , C07C235/78 , C07C259/06 , C07D319/06 , C07D413/12
摘要： In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.

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