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1. 发明授权

US10227332B2 T-type calcium channel modulator and uses thereof 有权
公开(公告)号：US10227332B2
公开(公告)日：2019-03-12
申请号：US15518473
申请日：2015-10-15
申请人： UTI Limited Partnership , University of Montana
发明人： Gerald Werner Zamponi , Philippe Diaz
IPC分类号： C07D209/88 , C07D403/12 , C07D401/12
摘要： The present invention provides T-type calcium channel modulators and methods for producing and using the same. In some embodiments, compounds of the invention are of the formula: where R1 is selected from the group consisting of alkyl, alkenyl, polyether, alkoxy and cycloalkyl; X is selected from the group consisting of methylene, —C(═O)—[NR4]a—, —C(═S)—, and —S(═O)b; R2 is selected from the group consisting of heterocycloalkyl and heteroaryl; R3 is selected from the group consisting of alkyl, alkenyl, polyether, alkoxy, cycloalkyl, —NR5R6, —C(═O)NR5R6, —C(═O)ORa (where Ra is alkyl, typically C1-C8 alkyl, often C2-C6 alkyl, and in one particular embodiment Ra is tert-butyl), and —SO2NR5R6; R4 is hydrogen, alkyl, or a nitrogen protecting group; each of R5 and R6 are independently selected from the group consisting of hydrogen and alkyl; a is 0 or 1; b is 1 or 2; n=1 to 3; and m=0 to 1.

2. 发明申请

US20170197996A1 Cholinesterase Inhibitors 审中-公开
公开(公告)号：US20170197996A1
公开(公告)日：2017-07-13
申请号：US15258356
申请日：2016-09-07
申请人： Charles M. Thompson , John M. Gerdes , Syed K. Ahmed , Yamina Belabassi
发明人： Charles M. Thompson , John M. Gerdes , Syed K. Ahmed , Yamina Belabassi
IPC分类号： C07F9/40 , C07F9/38 , A61K51/04
CPC分类号： C07F9/4071 , A61K51/0489 , C07B59/004 , C07F9/38 , C07F9/4021
摘要： The invention provides compounds that inhibit cholinesterases, such as acetylcholinesterase and butyrylcholinesterase. Such compounds are useful to prevent or treat exposure of a patient (e.g., a human) to an organophosphoric nerve agent (e.g., sarin and VX) or to treat a patient suffering from a neurodegenerative disorder such as Alzheimer's Disease or Lewy Body Dementia. The compounds are further useful as diagnostic tools for use in medical or research radiography (e.g., positron emission tomography) when synthesized with a radionuclide (e.g., [18F]. Synthetic schemes to produce such compounds are also provided.

3. 发明授权

US09499472B2 Aspartylamide inhibitors of excitatory amino acid transporters 有权
标题翻译：兴奋性氨基酸转运蛋白的天冬氨酰胺抑制剂
公开(公告)号：US09499472B2
公开(公告)日：2016-11-22
申请号：US14382508
申请日：2013-03-05
申请人： THE UNIVERSITY OF MONTANA
发明人： John M. Gerdes , Richard J. Bridges , Syed K. Ahmed , Sarjubhai Patel
IPC分类号： A61K51/00 , A61M36/14 , C07C69/635 , C07C237/04 , C07B59/00 , A61K51/04 , C07C67/317 , C07F7/22
CPC分类号： C07C69/635 , A61K51/04 , C07B59/001 , C07B2200/05 , C07C67/317 , C07C237/04 , C07C2603/18 , C07F7/2208
摘要： The compounds of the invention are inhibitors of excitatory amino acid transporters (EAAT) that penetrate the blood-brain barrier to access the central nervous system. The compounds of the invention follow the structural formula: or a salt, ester or prodrug thereof, wherein X is a halogen, such as fluorine, or a radionuclide, such as fluorine-18. The compounds and methods described herein can be used for the treatment of, e.g., neurodegenerative disorders (e.g., amyotrophic lateral sclerosis), ischemia, spinal cord injury, and traumatic brain injury in a patient (e.g., a human). The invention further provides compounds and methods for the synthesis and use of radiographic tracers to diagnose and follow the progression of such disorders.

4. 发明授权

US09315624B2 Hydroxypolyamide gel forming agents 有权
公开(公告)号：US09315624B2
公开(公告)日：2016-04-19
申请号：US14107297
申请日：2013-12-16
申请人： THE UNIVERSITY OF MONTANA
发明人： Donald E. Kiely , Tyler N. Smith
IPC分类号： C08G69/26 , C08G69/28 , C08J3/075 , A01N25/04 , A61K47/34 , C05G3/00 , C08K3/22 , C08K3/26 , C08K3/28 , C08K3/32 , C08K5/05 , C08K5/21 , C08K5/41 , C08L5/00 , C08L77/06 , C08L89/00
CPC分类号： C08G69/28 , A01N25/04 , A61K47/34 , C05B7/00 , C05C5/02 , C05C9/00 , C05G3/0064 , C05G3/0076 , C08G69/26 , C08G69/265 , C08J3/075 , C08J2377/06 , C08K3/22 , C08K3/26 , C08K3/28 , C08K3/32 , C08K5/05 , C08K5/21 , C08K5/41 , C08K2003/324 , C08L5/00 , C08L77/06 , C08L89/00 , C08L2201/54 , C08L2201/56 , C08L2203/02
摘要： Hydroxypolyamides, hydroxypolyamide products, and post-hydroxypolyamides are disclosed as gel forming agents. Hydroxypolyamides and post-hydroxypolyamides are prepared from known methods. Hydroxypolyamide products are produced from a modified polymerization procedure which utilizes strong base for deprotonation of ammonium salts from the esterification of stoichiometrically equivalent polyacid:polyamine salts. The hydroxypolyamide products are capable of gel formation at lower concentrations than hydroxypolyamides and post-hydroxypolyamides from the known methods of preparation, and are therefore superior gel forming agents.

5. 发明授权

US09293949B2 Electric power grid signal processing methods, oscillatory mode estimation methods and mode shape estimation methods 有权
标题翻译：电网信号处理方法，振荡模式估计方法和模态形状估计方法
公开(公告)号：US09293949B2
公开(公告)日：2016-03-22
申请号：US13367276
申请日：2012-02-06
申请人： Dan Trudnowski , John Pierre
发明人： Dan Trudnowski , John Pierre
IPC分类号： H02J13/00 , G01R19/25
CPC分类号： H02J13/0006 , G01R19/2513 , Y02E60/728 , Y04S10/265
摘要： Electric power grid monitoring methods and apparatus are described. According to one aspect, an electric power grid signal processing method includes accessing a plurality of signals which are individually indicative of a characteristic of electromechanical energy within an electric power grid, using the plurality of signals, generating a composite signal, and analyzing the composite signal to provide information regarding an oscillatory mode within the electric power system.
摘要翻译：描述了电网监测方法和装置。根据一个方面，一种电力电网信号处理方法包括：使用所述多个信号来访问单独指示电力网内的机电能的特性的多个信号，生成复合信号，以及分析复合信号提供关于电力系统内的振荡模式的信息。

6. 发明授权

US09162959B2 Method of oxidation using nitric acid 有权
标题翻译：使用硝酸的氧化方法
公开(公告)号：US09162959B2
公开(公告)日：2015-10-20
申请号：US14150633
申请日：2014-01-08
申请人： The University of Montana
发明人： Donald E. Kiely , Kirk R. Hash, Sr.
IPC分类号： C07C51/00 , C07C51/27
CPC分类号： C07C51/27 , C07C51/00 , C07C59/285
摘要： A controlled nitric acid process employing oxygen and nitric acid as co-oxidants is used to oxidize organic compounds subject to nitric acid oxidation, to their corresponding carboxylic acids. Oxidation of some carbohydrates by this process can produce one or more of their corresponding acid forms. The process is carried out at moderate temperatures, typically in the range of 20° C. to 45° C. in a closed reactor, with oxygen gas being introduced into the reaction chamber as needed in order to sustain the reaction. Computer controlled reactors allow for careful and reproducible control of reaction parameters. Nitric acid can be recovered by a distillation/evaporation process, or by diffusion dialysis, the aqueous solution made basic with inorganic hydroxide, and the residual inorganic nitrate removed using a filtration (nanofiltration) device. The method eliminates issues of thermal control of the oxidation, release of nitrogen into the atmosphere, and post-reaction difficulties in the removal of nitric acid and inorganic nitrates.
摘要翻译：使用使用氧和硝酸作为辅助氧化剂的受控硝酸方法将经受硝酸氧化的有机化合物氧化成其相应的羧酸。通过该方法氧化一些碳水化合物可以产生一种或多种相应的酸形式。该方法在中等温度下进行，通常在封闭反应器中在20℃至45℃的范围内，根据需要将氧气引入反应室，以维持反应。计算机控制的反应器允许仔细和可重复地控制反应参数。硝酸可以通过蒸馏/蒸发过程或通过扩散透析回收，水溶液用无机氢氧化物制成碱性，并且使用过滤（纳滤）装置除去残留的无机硝酸盐。该方法消除了氧化的热控制，氮气释放到大气中的问题，以及去除硝酸和无机硝酸盐的后反应困难。

7. 发明授权

US08895607B2 Inhibitors of the amino acid transporters ASCT1 and ASCT2 有权
标题翻译：氨基酸转运蛋白ASCT1和ASCT2的抑制剂
公开(公告)号：US08895607B2
公开(公告)日：2014-11-25
申请号：US13549779
申请日：2012-07-16
申请人： Michael P. Kavanaugh , Brent Lyda , Nicholas R. Natale , Stephanie Lynn Martinelli
发明人： Christopher Sean Esslinger , Michael P. Kavanaugh , Brent Lyda , Nicholas R. Natale
IPC分类号： A61K31/40 , C07D207/12
CPC分类号： C07D207/12 , C07D207/16
摘要： The present invention relates to a compound of Formula (I) or (II) or a salt thereof, wherein R is described herein. The compounds are novel hydroxy-proline analog inhibitors of the ASCT1 and ASCT2 neutral amino acid transporters.
摘要翻译：本发明涉及式（I）或（II）化合物或其盐，其中R如本文所述。该化合物是ASCT1和ASCT2中性氨基酸转运蛋白的新型羟基 - 脯氨酸类似物抑制剂。

8. 发明授权

US08535528B1 Styrene based ion exchange resins with oxine functionalized groups 有权
标题翻译：具有氧官能团的苯乙烯基离子交换树脂
公开(公告)号：US08535528B1
公开(公告)日：2013-09-17
申请号：US12693367
申请日：2010-01-25
申请人： Paul J. Miranda , Corby G. Anderson , Edward Rosenberg
发明人： Paul J. Miranda , Corby G. Anderson , Edward Rosenberg
IPC分类号： B01D15/08
CPC分类号： B01J41/14 , B01D15/361 , B01J39/19 , C22B3/42
摘要： Oxine ligands placed on styrene base ion exchange resins selectively remove iron and gallium from acidic solutions. After loading, the oxine resin is stripped of the loaded metals and used again for further metal removal. The resins can be used for process streams, acid rock drainages, or any other iron or gallium containing solution.
摘要翻译：置于苯乙烯基离子交换树脂上的氧配体选择性地从酸性溶液中除去铁和镓。装载后，将氧化树脂除去负载的金属，并再次用于进一步的金属去除。这些树脂可以用于工艺流，酸性岩石泄放或任何其它含铁或镓的溶液中。

9. 发明授权

US08343446B2 Oxine modified silican polyamine composites for the separation of gallium from aluminum, ferric from nickel and copper from nickel 有权
标题翻译：用于从铝中分离镓的氧化改性硅烷聚胺复合物，来自镍的镍和铜的三价铁
公开(公告)号：US08343446B2
公开(公告)日：2013-01-01
申请号：US13272662
申请日：2011-10-13
申请人： Edward Rosenberg , Paul Miranda , Yuen Onn Wong
发明人： Edward Rosenberg , Paul Miranda , Yuen Onn Wong
IPC分类号： C02F1/00
CPC分类号： C08G73/0206
摘要： The oxine ligands 5-chloro-8-hydroxyquiniline and 5-sulfoxyl-8-hydroxyquinoline are covalently bound, using, for example, the Mannich reaction, to a silica gel polyamine composite made from a silanized amorphous silica xerogel and polyallylamine. The resulting modified composites, termed CB-1 (X═Cl) and SB-1 (X═SO3H), respectively, show a clear selectivity for trivalent over divalent ions and selectivity for gallium over aluminum. The compounds of the invention can be applied for the sequestration of metals, such as heavy metals, from contaminated mine tailing leachates.
摘要翻译：使用例如曼尼希反应将oxine配体5-氯-8-羟基喹啉和5-磺酰基-8-羟基喹啉与由硅烷化无定形二氧化硅干凝胶和聚烯丙基胺制成的硅胶多胺复合物共价结合。分别称为CB-1（X = Cl）和SB-1（X = SO 3 H）的所得改性复合物显示出对三价过二价离子的清晰选择性以及镓对铝的选择性。本发明的化合物可用于从受污染的矿尾矿浸出液中金属（例如重金属）的螯合。

10. 发明申请

US20070142467A1 3-alkylaryl aspartate compounds and their use for selective enhancement of synaptic transmission 审中-公开
标题翻译： 3-烷基芳基天冬氨酸化合物及其用于选择性增强突触传递的用途
公开(公告)号：US20070142467A1
公开(公告)日：2007-06-21
申请号：US11256583
申请日：2005-10-21
申请人： Christopher Esslinger , Richard Bridges , Michael Kavanaugh
发明人： Christopher Esslinger , Richard Bridges , Michael Kavanaugh
IPC分类号： A61K31/277 , A61K31/198 , C07C255/28 , C07C229/38
CPC分类号： C07C229/36
摘要： The present invention provides an L-aspartate derivative compound represented by the following structure wherein Ar represents an aromatic group; L represents a linking moiety; R represents hydrogen, alkyl, aryl, or heteroaryl; and indicates that the stereochemistry at the 3-position can be R or S. The compounds of the invention are useful for selectively inhibiting EAAT3 and for enhancing synaptic transmission. Additionally, the inventive compounds can be used to treat a patient suffering from Alzheimers disease or a neuropathy or a neurodegenerative disease in which L-glutamate transporter activity is involved in the onset of the disease.
摘要翻译：本发明提供由以下结构表示的L-天冬氨酸衍生物化合物，其中Ar表示芳族基团; L表示连接部分; R代表氢，烷基，芳基或杂芳基; “img id =”custom-character-00001“he =”1.78mm“wi =”4.91mm“file =”US20070142467A1-20070621-P00001.TIF“alt =”custom character“img-content =”character“img- format =“tif”/>表示3位的立体化学可以是R或S.本发明的化合物可用于选择性抑制EAAT3和增强突触传递。此外，本发明的化合物可用于治疗患有阿尔茨海默病或神经病变或神经变性疾病的患者，其中L-谷氨酸转运蛋白活性参与疾病发作。

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