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1. 发明申请

US20120316191A1 Peripheral Opioid Receptor Antagonists and Uses Thereof 有权
标题翻译：外周阿片受体拮抗剂及其用途
公开(公告)号：US20120316191A1
公开(公告)日：2012-12-13
申请号：US13570836
申请日：2012-08-09
申请人： Nataliya Bazhina , George Joseph Donato, III , Steven R. Fabian , John Lokhnauth , Sreenivasulu Megati , Charles Melucci , Christian Ofslager , Niketa Patel , Galen Radebaugh , Syed M. Shah , Jan Szeliga , Huyi Zhang , Tianmin Zhu
发明人： Nataliya Bazhina , George Joseph Donato, III , Steven R. Fabian , John Lokhnauth , Sreenivasulu Megati , Charles Melucci , Christian Ofslager , Niketa Patel , Galen Radebaugh , Syed M. Shah , Jan Szeliga , Huyi Zhang , Tianmin Zhu
IPC分类号： A61K31/439 , A61P1/10 , A61P1/00
CPC分类号： A61K31/485 , A61J1/05 , A61K9/0019 , A61K9/0053 , A61K9/08 , A61K9/20 , A61M5/178 , C07D471/08 , C07D489/08 , Y10T436/145555
摘要： The present invention provides a compound of formula I: wherein X−, R1, and R2 are as defined herein, and compositions thereof.
摘要翻译：本发明提供式I化合物：其中X，R 1和R 2如本文所定义，及其组合物。

2. 发明申请

US20130011929A1 PERIPHERAL OPIOID RECEPTOR ANTAGONISTS AND USES THEREOF 有权
公开(公告)号：US20130011929A1
公开(公告)日：2013-01-10
申请号：US13546500
申请日：2012-07-11
申请人： Nataliya Bazhina , George Joseph Donato, III , Steven R. Fabian , John Lokhnauth , Sreenivasulu Megati , Charles Melucci , Christian Ofslager , Niketa Patel , Galen Radebaugh , Syed M. Shah , Jan Szeliga , Huyi Zhang , Tianmin Zhu
发明人： Nataliya Bazhina , George Joseph Donato, III , Steven R. Fabian , John Lokhnauth , Sreenivasulu Megati , Charles Melucci , Christian Ofslager , Niketa Patel , Galen Radebaugh , Syed M. Shah , Jan Szeliga , Huyi Zhang , Tianmin Zhu
IPC分类号： C07D221/28 , G01N30/02 , G01N33/00
CPC分类号： A61K31/485 , A61J1/05 , A61K9/0019 , A61K9/0053 , A61K9/08 , A61K9/20 , A61M5/178 , C07D471/08 , C07D489/08 , Y10T436/145555
摘要： The present invention provides a compound of formula I: wherein X−, R1, and R2 are as defined herein, and compositions thereof.

3. 发明申请

US20100120813A1 PERIPHERAL OPIOID RECEPTOR ANTAGONISTS AND USES THEREOF 有权
标题翻译：外周血糖受体拮抗剂及其用途
公开(公告)号：US20100120813A1
公开(公告)日：2010-05-13
申请号：US12570891
申请日：2009-09-30
申请人： Nataliya Bazhina , George Joseph Donato, III , Steven R. Fabian , John Lokhnauth , Sreenivasulu Megati , Charles Melucci , Christian Ofslager , Niketa Patel , Galen Radebaugh , Syed M. Shah , Jan Szeliga , Huyi Zhang , Tianmin Zhu
发明人： Nataliya Bazhina , George Joseph Donato, III , Steven R. Fabian , John Lokhnauth , Sreenivasulu Megati , Charles Melucci , Christian Ofslager , Niketa Patel , Galen Radebaugh , Syed M. Shah , Jan Szeliga , Huyi Zhang , Tianmin Zhu
IPC分类号： A61K31/485 , C07D211/06 , C07D489/02 , A61P1/10 , G01N33/00
CPC分类号： A61K31/485 , A61J1/05 , A61K9/0019 , A61K9/0053 , A61K9/08 , A61K9/20 , A61M5/178 , C07D471/08 , C07D489/08 , Y10T436/145555
摘要： The present invention provides a compound of formula I: wherein X−, R1, and R2 are as defined herein, and compositions thereof.
摘要翻译：本发明提供式I化合物：其中X，R 1和R 2如本文所定义，及其组合物。

4. 发明授权

US08455644B2 Peripheral opioid receptor antagonists and uses thereof 有权
标题翻译：外周阿片受体拮抗剂及其用途
公开(公告)号：US08455644B2
公开(公告)日：2013-06-04
申请号：US13546500
申请日：2012-07-11
申请人： Nataliya Bazhina , George Joseph Donato, III , Steven R. Fabian , John Lokhnauth , Sreenivasulu Megati , Charles Melucci , Christian Ofslager , Niketa Patel , Galen Radebaugh , Syed M. Shah , Jan Szeliga , Huyi Zhang , Tianmin Zhu
发明人： Nataliya Bazhina , George Joseph Donato, III , Steven R. Fabian , John Lokhnauth , Sreenivasulu Megati , Charles Melucci , Christian Ofslager , Niketa Patel , Galen Radebaugh , Syed M. Shah , Jan Szeliga , Huyi Zhang , Tianmin Zhu
IPC分类号： C07D221/22 , C07D489/08
CPC分类号： A61K31/485 , A61J1/05 , A61K9/0019 , A61K9/0053 , A61K9/08 , A61K9/20 , A61M5/178 , C07D471/08 , C07D489/08 , Y10T436/145555
摘要： The present invention provides a compound of formula I: wherein X−, R1, and R2 are as defined herein, and compositions thereof.
摘要翻译：本发明提供式I化合物：其中X，R 1和R 2如本文所定义，及其组合物。

5. 发明授权

US08247425B2 Peripheral opioid receptor antagonists and uses thereof 有权
标题翻译：外周阿片受体拮抗剂及其用途
公开(公告)号：US08247425B2
公开(公告)日：2012-08-21
申请号：US12570891
申请日：2009-09-30
申请人： Nataliya Bazhina , George Joseph Donato, III , Steven R. Fabian , John Lokhnauth , Sreenivasulu Megati , Charles Melucci , Christian Ofslager , Niketa Patel , Galen Radebaugh , Syed M. Shah , Jan Szeliga , Huyi Zhang , Tianmin Zhu
发明人： Nataliya Bazhina , George Joseph Donato, III , Steven R. Fabian , John Lokhnauth , Sreenivasulu Megati , Charles Melucci , Christian Ofslager , Niketa Patel , Galen Radebaugh , Syed M. Shah , Jan Szeliga , Huyi Zhang , Tianmin Zhu
IPC分类号： A61K31/485 , A61K31/4748
CPC分类号： A61K31/485 , A61J1/05 , A61K9/0019 , A61K9/0053 , A61K9/08 , A61K9/20 , A61M5/178 , C07D471/08 , C07D489/08 , Y10T436/145555
摘要： The present invention provides a compound of formula I: wherein X−, R1, and R2 are as defined herein, and compositions thereof.
摘要翻译：本发明提供式I化合物：其中X，R 1和R 2如本文所定义，及其组合物。

6. 发明授权

US08420663B2 Peripheral opioid receptor antagonists and uses thereof 有权
公开(公告)号：US08420663B2
公开(公告)日：2013-04-16
申请号：US13570836
申请日：2012-08-09
申请人： Nataliya Bazhina , George Joseph Donato, III , Steven R. Fabian , John Lokhnauth , Sreenivasulu Megati , Charles K. Melucci , Christian Ofslager , Niketa Patel , Galen Radebaugh , Syed M. Shah , Jan Szeliga , Huyi Zhang , Tianmin Zhu
发明人： Nataliya Bazhina , George Joseph Donato, III , Steven R. Fabian , John Lokhnauth , Sreenivasulu Megati , Charles K. Melucci , Christian Ofslager , Niketa Patel , Galen Radebaugh , Syed M. Shah , Jan Szeliga , Huyi Zhang , Tianmin Zhu
IPC分类号： A61K31/485 , A61K31/4748
CPC分类号： A61K31/485 , A61J1/05 , A61K9/0019 , A61K9/0053 , A61K9/08 , A61K9/20 , A61M5/178 , C07D471/08 , C07D489/08 , Y10T436/145555
摘要： The present invention provides a compound of formula I: wherein X−, R1, and R2 are as defined herein, and compositions thereof.

7. 发明申请

US20050197311A1 Compositions and methods for detecting intracellular glucose and analogs thereof 有权
标题翻译：用于检测细胞内葡萄糖及其类似物的组合物和方法
公开(公告)号：US20050197311A1
公开(公告)日：2005-09-08
申请号：US11054024
申请日：2005-02-08
申请人： Denise Cooper , Niketa Patel
发明人： Denise Cooper , Niketa Patel
IPC分类号： C07H21/04 , C07K14/47 , C12N5/02 , C12N15/68 , A61K48/00 , C12Q1/68
CPC分类号： C07K14/4702 , C12N15/68 , C12N15/85 , C12N2510/00 , C12N2830/50 , C12Q1/6897 , C12Y207/11013
摘要： The subject invention pertains to nucleic acid constructs for post-transcriptional control of expression of a polynucleotide encoding a protein in a cell, wherein the constructs include a metabolite responsive instability element such as the glucose-regulated mRNA instability element. The subject invention further pertains to host cells and vectors comprising the nucleic acid constructs of the invention, as well as probes, methods, and kits for detecting metabolite responsive instability elements or mutations thereof. The present invention further concerns a reporter vector useful for detecting intracellular glucose and glucose-analogs, host cells genetically modified with the reporter vector, and methods for detecting intracellular glucose. The present invention utilizes an element that regulates messenger RNA (mRNA) stability in response to a metabolite such as glucose or a glucose analog. This glucose-regulated mRNA instability element has been mapped to the protein kinase C βII (PKCβII) mRNA that was found to decrease in the presence of elevated glucose levels. When cloned into a reporter vector, the region of PKCβII containing the mRNA instability element imparts glucose-sensitive instability to the mRNA that is transcribed, thereby down-regulating the expression of the reporter gene when glucose is elevated. The reporter vector of the present invention may be introduced into host cells, allowing detection of intracellular glucose and glucose analogs within intact, living cells in real-time and, optionally, in a high-throughput format.
摘要翻译：本发明涉及用于转录后控制编码细胞中蛋白质的多核苷酸的转录后控制的核酸构建体，其中所述构建体包括代谢物反应性不稳定性元件，例如葡萄糖调节的mRNA不稳定性元件。本发明进一步涉及包含本发明的核酸构建体的宿主细胞和载体，以及用于检测代谢物反应性不稳定性元件或其突变的探针，方法和试剂盒。本发明还涉及可用于检测细胞内葡萄糖和葡萄糖类似物的报道载体，用报告载体遗传修饰的宿主细胞和检测细胞内葡萄糖的方法。本发明利用响应于诸如葡萄糖或葡萄糖类似物的代谢物调节信使RNA（mRNA）稳定性的元件。这种葡萄糖调节的mRNA不稳定性元件已经映射到蛋白激酶CβII（PKCbetaII）mRNA，其在葡萄糖水平升高的情况下被发现降低。当克隆到报告载体中时，含有mRNA不稳定性元件的PKCbetaII区域对转录的mRNA赋予葡萄糖敏感的不稳定性，从而当葡萄糖升高时下调报告基因的表达。可以将本发明的报道载体导入宿主细胞，允许实时和任选地以高通量形式检测完整的活细胞内的细胞内葡萄糖和葡萄糖类似物。

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