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91. 发明授权

US08461190B2 Process for the purification of rufinamide 有权
标题翻译： Rufinamide净化方法
公开(公告)号：US08461190B2
公开(公告)日：2013-06-11
申请号：US13451651
申请日：2012-04-20
申请人： Pietro Allegrini , Dario Pastorello , Gabriele Razzetti
发明人： Pietro Allegrini , Dario Pastorello , Gabriele Razzetti
IPC分类号： A61K31/41 , C07D249/00
CPC分类号： C07D249/04
摘要： A process for purifying Rufinamide, comprising: a) providing a dispersion of crude 1-[(2,6-difluorophenyl)methyl]-1H-1,2,3-triazole-4-carboxamide in a solvent mixture containing at least a carboxylic acid, and dissolving it; b) slowly cooling the solution to precipitate Rufinamide crystalline form A; and c) recovering the solid.
摘要翻译：一种用于纯化Rufinamide的方法，包括：a）提供粗制的1 - [（2,6-二氟苯基）甲基] -1H-1,2,3-三唑-4-甲酰胺在含有至少一种羧酸酸，并溶解; b）缓慢冷却溶液以沉淀Ruformamide结晶形式A; 和c）回收固体。

92. 发明授权

US08404730B2 3-substituted propanamine compounds 有权
标题翻译： 3-取代丙胺化合物
公开(公告)号：US08404730B2
公开(公告)日：2013-03-26
申请号：US13276804
申请日：2011-10-19
申请人： Chun-Eung Park , Kyung-Hyun Min , Yong-Je Shin , Yu-Jin Shin , Hae-Jeong Yoon , Won Kim , Eun-Ju Ryu , Coo-Min Chung , Hui-Ho Kim
发明人： Chun-Eung Park , Kyung-Hyun Min , Yong-Je Shin , Yu-Jin Shin , Hae-Jeong Yoon , Won Kim , Eun-Ju Ryu , Coo-Min Chung , Hui-Ho Kim
IPC分类号： A61K31/41 , C07D257/04
CPC分类号： A61K31/41 , A61K31/4192 , A61K31/4709 , A61K31/4725 , C07D249/04 , C07D257/04 , C07D401/06 , C07D405/06 , C07D409/06
摘要： Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof are disclosed. Pharmaceutical compositions containing the subject compounds are also disclosed. The subject compounds are useful for the treatment of diseases of the central nervous system, such as depression, anxiety and pain disorders.
摘要翻译：公开了由以下结构式（I）表示的外消旋或对映异构体富集的3-取代的丙胺化合物或其药学上可接受的盐。还公开了含有本发明化合物的药物组合物。本发明化合物可用于治疗中枢神经系统的疾病，例如抑郁症，焦虑症和疼痛障碍。

93. 发明申请

US20120296085A1 CHEMILUMINESCENT DYES AND DYE-STAINED PARTICLES 审中-公开
标题翻译： CHEMILUMINESCENT DYES和DYE-STAINED PARTICLES
公开(公告)号：US20120296085A1
公开(公告)日：2012-11-22
申请号：US13522296
申请日：2010-06-01
申请人： Bradley Smith
发明人： Bradley Smith
IPC分类号： C09B5/00 , B01J19/12
CPC分类号： C09K11/06 , C07D249/04 , C07D257/10 , C07D273/00 , C09K2211/1011 , C09K2211/1014 , C09K2211/1059
摘要： Chemiluminescent compounds that can be activated by reaction with chemical or photochemical sources of singlet oxygen are provided. At certain temperatures, such as from approximately 15 to 60° C., the compounds slowly return to their deactivated state by emitting visible and/or infrared light that is observable with various types of light detectors. Suitable conjugates of these compounds, or small particles containing these compounds, may be used for chemiluminescence imaging and sensing technologies. In particular, embodiments provide optical molecular imaging using novel squaraine rotaxane endoperoxides (SREPs) and squaraine catenane endoperoxides (SCEPs), interlocked fluorescent and chemiluminescent dye molecules that have a squaraine chromophore encapsulated inside a macrocycle endoperoxide. The dyes may be stored at low temperature, such as below 0° C., but, upon warming above 15° C., such as to body temperature, they undergo a unimolecular cycloreversion reaction that releases singlet oxygen and emits visible or near-infrared light that can pass through living tissue. The chemiluminescent signal is detectable with inherently high contrast because there is negligible background emission.
摘要翻译：提供了可以通过与单线态氧化学或光化学源反应而被活化的化学发光化合物。在某些温度，例如约15至60℃，化合物通过发射可用和各种类型的光检测器可观察到的可见光和/或红外光，缓慢地回到其失活状态。这些化合物或含有这些化合物的小颗粒的合适的缀合物可用于化学发光成像和感测技术。具体地，实施方案提供使用新型方酸酯轮烷内酯过氧化物（SREP）和方酸核苷正丁烯内过氧化物（SCEP）的光学分子成像，具有封装在大环内酯过氧化物内的方形荧光和化学发光染料分子。染料可以在低于0℃的低温下储存，但是当温度高于15℃，例如体温时，它们进行单分子旋转反应，其释放单线态氧并发射可见光或近红外能通过活组织的光。化学发光信号可以用固有的高对比度检测，因为可忽略的背景辐射。

94. 发明申请

US20120289704A1 ANTI-CANCER COMPOUNDS, SYNTHESIS THEREOF, AND METHODS OF USING SAME 有权
标题翻译：抗癌化合物，其合成方法及使用方法
公开(公告)号：US20120289704A1
公开(公告)日：2012-11-15
申请号：US13551464
申请日：2012-07-17
申请人： Marvin J. Miller , Garrett C. Moraski , Jonathan Stefely
发明人： Marvin J. Miller , Garrett C. Moraski , Jonathan Stefely
IPC分类号： C07D249/04 , C07D401/12
CPC分类号： C07D413/12 , C07D249/04 , C07D401/12
摘要： Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to anti-cancer compounds, synthesis thereof, and methods of using same. Disclosed herein are various heterocyclic compounds and methods of using the novel anti-cancer compounds to inhibit the growth of a cancer cell, for instance a leukemia, non-small cell lung, central nervous system (CNS), skin, ovarian, renal, prostate, breast, or colon cancer cell. Other embodiments include methods of treating cancer in a subject, such as using the disclosed heterocyclic anti-cancer agents.
摘要翻译：实施方案涉及化学和生物化学领域，更具体地涉及抗癌化合物，其合成及其使用方法。本文公开了各种杂环化合物和使用新的抗癌化合物抑制癌细胞例如白血病，非小细胞肺，中枢神经系统（CNS），皮肤，卵巢，肾，前列腺的生长的各种杂环化合物和方法，乳腺癌或结肠癌细胞。其它实施方案包括治疗受试者的癌症的方法，例如使用所公开的杂环抗癌药物。

95. 发明授权

US08309740B2 One-pot synthesis of fluorinated ionic liquids 有权
标题翻译：一锅合成氟化离子液体
公开(公告)号：US08309740B2
公开(公告)日：2012-11-13
申请号：US12192433
申请日：2008-08-15
申请人： Hyun Joo Lee , Dong Jin Suh , Byoung Sung Ahn , Hong Gon Kim , Chang Soo Kim , Hoon Sik Kim
发明人： Hyun Joo Lee , Dong Jin Suh , Byoung Sung Ahn , Hong Gon Kim , Chang Soo Kim , Hoon Sik Kim
IPC分类号： C07D207/02 , C07D211/04 , C07D213/06 , C07D233/06 , C07D233/56 , C07D237/06 , C07D239/24 , C07D241/04 , C07D249/02 , C07D251/56 , C07D253/06 , C07D295/02
CPC分类号： C07D207/06 , C07C209/60 , C07D213/20 , C07D233/06 , C07D233/56 , C07D233/64 , C07D237/08 , C07D239/26 , C07D249/04 , C07D251/14 , C07D253/065 , C07D295/067
摘要： The present invention relates to a method for one-pot synthesis of ionic liquid with fluoroalkyl group, more particularly to a method for one-pot synthesis of ionic liquid with fluoroalkyl group represented by the following Chemical Formula 1 by adding and reacting a nitrogen-containing compound, a Brønsted acid of the formula YH and a fluoroolefin compound of the formula CFR1═CR2R3 in a single reactor: wherein represents a nitrogen-containing compound; Y− represents an anion of the Brønsted acid; and R1, R2 and R3, which may be same or different, represent hydrogen, fluorine, C1-C10 alkyl or C1-C10 fluoroalkyl having from 1 to 23 fluorine atoms.
摘要翻译：本发明涉及一种用氟烷基进行一锅合成离子液体的方法，更具体地说，涉及一种通过以下化学式1代表的具有氟代烷基的一锅合成离子液体的方法：将含氮化合物，式YH的布朗斯台德酸和式CFR1 = CR2R3的氟烯烃化合物在单个反应器中：其中代表含氮化合物; Y-代表布朗斯台德酸的阴离子; 可以相同或不同的R 1，R 2和R 3表示氢，氟，C 1 -C 10烷基或具有1至23个氟原子的C 1 -C 10氟代烷基。

96. 发明授权

US08258170B2 Inhibitors of plasma kallikrein 有权
标题翻译：血浆激肽释放酶抑制剂
公开(公告)号：US08258170B2
公开(公告)日：2012-09-04
申请号：US13154410
申请日：2011-06-06
申请人： Sukanto Sinha , Tamie Jo Chilcote
发明人： Sukanto Sinha , Tamie Jo Chilcote
IPC分类号： A61K31/415 , C07D231/14
CPC分类号： C07D207/34 , C07D209/42 , C07D231/14 , C07D249/04 , C07D307/68 , C07D333/38 , C07D333/68 , C07D401/06
摘要： The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.
摘要翻译：本发明提供抑制血浆激肽释放酶（PK）的活性的化合物以及在PK依赖性疾病或病症例如纤维蛋白溶解处理之后或之后预防和治疗凝血酶形成的方法。

97. 发明申请

US20120186449A1 PREPARATION OF METAL-TRIAZOLATE FRAMEWORKS 有权
标题翻译：金属三叶酸框架的制备
公开(公告)号：US20120186449A1
公开(公告)日：2012-07-26
申请号：US13354574
申请日：2012-01-20
申请人： Omar M. Yaghi , Fernando J. Uribe-Romo , Felipe Gandara-Barragan , David K. Britt
发明人： Omar M. Yaghi , Fernando J. Uribe-Romo , Felipe Gandara-Barragan , David K. Britt
IPC分类号： C07F3/02 , C07F15/02 , B01D53/04 , C07F1/08 , C07F3/06 , C07F3/08 , C07F13/00 , C07F15/06
CPC分类号： C07F1/005 , B01D2253/204 , B01J20/226 , C07D249/04 , C07F3/003 , C07F13/005 , C07F15/025 , C07F15/045 , Y02C10/08 , Y02C20/10
摘要： The disclosure provides for novel metal-triazolate frameworks, methods of use thereof, and devices comprising the frameworks thereof.
摘要翻译：本公开提供了新的金属 - 三唑酸酯骨架，其使用方法和包含其框架的装置。

98. 发明授权

US08222423B2 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：US08222423B2
公开(公告)日：2012-07-17
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： C07D249/00 , C07C303/00
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.
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。

99. 发明申请

US20120122918A1 ANTIBACTERIAL AGENTS 有权
标题翻译：抗菌剂
公开(公告)号：US20120122918A1
公开(公告)日：2012-05-17
申请号：US13304748
申请日：2011-11-28
申请人： David Ryall BROWN , Ian COLLINS , Lloyd George CZAPLEWSKI , David John HAYDON
发明人： David Ryall BROWN , Ian COLLINS , Lloyd George CZAPLEWSKI , David John HAYDON
IPC分类号： A61K31/437 , A61K31/166 , C07D215/14 , A61K31/47 , C07C235/84 , A61K31/216 , C07D333/24 , A61K31/381 , C07D307/54 , A61K31/341 , C07C309/73 , A61K31/255 , C07C255/44 , A61K31/277 , C07D213/81 , A61K31/44 , C07D319/20 , A61K31/357 , C07D513/04 , A61P31/04 , C07D277/64 , C07D277/30 , A61K31/428 , A61K31/426 , A01P1/00 , A01N43/78 , A01N43/90 , A01N43/32 , A01N43/40 , A01N37/34 , A01N41/04 , A01N43/08 , A01N43/10 , A01N37/44 , A01N43/42 , A01N37/18 , C07C235/46
CPC分类号： C07C235/46 , A01N37/40 , A01N41/04 , A01N43/08 , A01N43/10 , A01N43/40 , A01N43/42 , A01N43/76 , A01N43/78 , A01N43/82 , A01N43/90 , A61K31/166 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/381 , A61K31/4025 , A61K31/4155 , A61K31/4178 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/423 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/44 , A61K31/4422 , A61K31/4523 , A61K31/4709 , C07C255/16 , C07C309/73 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07D213/30 , C07D213/81 , C07D215/12 , C07D215/14 , C07D231/12 , C07D233/64 , C07D249/04 , C07D261/08 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/24 , C07D277/32 , C07D277/64 , C07D307/42 , C07D307/56 , C07D319/20 , C07D333/06 , C07D333/12 , C07D333/16 , C07D333/56 , C07D413/04 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D498/04 , C07D513/04
摘要： Compounds of formula (1) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ═C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)-Q.
摘要翻译：式（1）化合物具有抗菌活性：其中R表示氢或1,2或3个任选的取代基; W为═C（R1） - ; R1是氢，R2是氢，甲基或氟; 或R 1和R 2一起为-CH 2 - ， - CH 2 CH 2，-O-，或者在任一取向为-O-CH 2 - 或-OCH 2 CH 2 - ; 并且R 3是式 - （Alk 1）m - （Z）p-（Alk 2）-Q的基团。

100. 发明申请

US20120100358A1 METHOD FOR PREPARING MOLECULARLY IMPRINTED POLYMERS (MIP) THROUGH RADICAL POLYMERISATION 有权
标题翻译：通过光学聚合法制备分子内嵌聚合物（MIP）的方法
公开(公告)号：US20120100358A1
公开(公告)日：2012-04-26
申请号：US13062608
申请日：2009-09-01
申请人： Karsten Haupt , Arnaud Cutivet , Jeanne Bernadette Tse Sum Bui , Pinar Cakir
发明人： Karsten Haupt , Arnaud Cutivet , Jeanne Bernadette Tse Sum Bui , Pinar Cakir
IPC分类号： B32B3/00 , C08F222/14 , C08F2/48 , C08F2/50 , B32B3/26 , C09D135/02 , C07C333/00 , C07D249/04 , B32B5/16 , C08F2/04 , C08F2/06
CPC分类号： B01J20/268 , B01J20/26 , C07C333/20 , C07D249/04 , C08F2/38 , C08F2/48 , C08F2/50 , C08F8/14 , C08F8/30 , C08F8/34 , C08F222/1006 , C08F2810/20 , Y10T428/249953 , Y10T428/2982
摘要： The invention relates to a method for preparing molecular imprint polymers (MIP) by radical polymerisation that uses at least one primer including at least two chemical functions capable of forming reactive radicals, thereby providing a locally high radical concentration for priming the polymerisation on or about the imprint entity or molecule. The invention also relates to molecular imprint polymers (MIP) that can be obtained by the method of the invention, and to the use thereof in the production of biomimetic biosensors, biomimetic biochips, chemical sensors, specific adsorption separation devices, as a coating, particularly for releasing active ingredients.
摘要翻译：本发明涉及一种通过自由基聚合制备分子印迹聚合物（MIP）的方法，该方法使用至少一种引物，其包含至少两种能够形成反应性基团的化学官能团，由此提供局部高自由基浓度，以引发聚合反应印记实体或分子。本发明还涉及可通过本发明的方法获得的分子印迹聚合物（MIP）及其在生物仿生生物传感器，仿生生物芯片，化学传感器，特定吸附分离装置中的用途，作为涂层，特别是用于释放活性成分。

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