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1. 发明授权

US09725410B2 N-hydroxylsulfonamide derivatives as new physiologically useful nitroxyl donors 有权
公开(公告)号：US09725410B2
公开(公告)日：2017-08-08
申请号：US15286145
申请日：2016-10-05
申请人： Cardioxyl Pharmaceuticals, Inc. , The Johns Hopkins University
发明人： John P. Toscano , Frederick Arthur Brookfield , Andrew D. Cohen , Stephen Martin Courtney , Lisa Marie Frost , Vincent Jacob Kalish
IPC分类号： C07C311/00 , C07C317/00 , C07C323/00 , C07D213/74 , C07D231/00 , C07D261/00 , A61K31/00 , C07C311/48 , C07D261/10 , C07D263/58 , C07D285/125 , C07D295/096 , C07D307/82 , C07D333/62 , C07C317/14 , C07C323/67 , C07D309/12 , C07D317/14 , C07D231/18 , C07D333/34
CPC分类号： C07C311/48 , C07C317/14 , C07C323/67 , C07D213/74 , C07D231/18 , C07D261/10 , C07D263/58 , C07D285/125 , C07D295/096 , C07D307/82 , C07D309/12 , C07D317/14 , C07D333/34 , C07D333/62
摘要： The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.

2. 发明授权

US09365471B2 Substituted phenylsulfur trifluoride and other like fluorinating agents 有权
公开(公告)号：US09365471B2
公开(公告)日：2016-06-14
申请号：US14213494
申请日：2014-03-14
申请人： UBE INDUSTRIES, LTD.
发明人： Teruo Umemoto
IPC分类号： C07C315/00 , C07C319/00 , C07C317/00 , C07C331/00 , C07C381/00 , C07C321/00 , C07C323/00 , C09B49/00 , C09B59/00 , C07C17/18 , C07B39/00 , C07C319/14 , C07C319/20 , C07C323/19 , C07C17/093 , C07C17/16 , C07C17/361 , C07C45/65 , C07C51/60
CPC分类号： C07C17/18 , C07B39/00 , C07C17/093 , C07C17/16 , C07C17/361 , C07C45/65 , C07C51/60 , C07C319/14 , C07C319/20 , C07C323/19 , C07C381/00 , C07C2601/14 , C07C19/08 , C07C22/08 , C07C23/10 , C07C323/03 , C07C63/10 , C07C63/04
摘要： Novel substituted phenylsulfur trifluorides that act as fluorinating agents are disclosed. Also disclosed are methods for their preparation and methods for their use in introducing one or more fluorine atoms into target substrate compounds. Finally, various intermediate compounds for use in preparing substituted phenylsulfur trifluorides are provided.

3. 发明授权

US09024073B2 Thio compounds and preparing method of the same 有权
标题翻译：硫化合物及其制备方法相同
公开(公告)号：US09024073B2
公开(公告)日：2015-05-05
申请号：US13394730
申请日：2010-08-31
申请人： Hyung Jae Lee , Chang Kyo Shin , Jin Eok Kim
发明人： Hyung Jae Lee , Chang Kyo Shin , Jin Eok Kim
IPC分类号： C07C319/00 , C07C321/00 , C07C323/00 , C07C381/00 , C08K5/375 , C07C323/16 , C08G8/30 , C08L61/18
CPC分类号： C08K5/375 , C07C323/16 , C07C2603/68 , C08G8/30 , C08L61/18 , C08L21/00
摘要： Provided are novel thio compounds and a method for preparing the same. More particularly, there is provided a novel thio compound prepared by reacting an alkylation product of p-cresol and dicyclopentadiene with mercaptan and paraformaldehyde. Unlike existing antioxidants such as 2,6-di-t-butyl-4-methylphenol (BHT) being harmful to the human body due to the high volatility, the novel thio compounds of the present invention, which have the low volatility because of their high molecular weight, give no harm to the human body. Further, with excellent performances, they are suitable to replace the existing antioxidants.
摘要翻译：提供新的硫代化合物及其制备方法。更具体地，提供了通过使对甲酚和二环戊二烯的烷基化产物与硫醇和多聚甲醛反应制备的新的硫代化合物。与由于挥发性高而对人体有害的2,6-二叔丁基-4-甲基苯酚（BHT）的现有抗氧化剂不同，本发明的新型硫代化合物由于它们的挥发性低而具有低挥发性高分子量，对人体无害。此外，具有优异的性能，它们适合替代现有的抗氧化剂。

4. 发明授权

US08779003B2 Method and composition for prolonging analgesic effect of local anesthetic 失效
标题翻译：延长局部麻醉止痛效果的方法和组成
公开(公告)号：US08779003B2
公开(公告)日：2014-07-15
申请号：US13340330
申请日：2011-12-29
申请人： Yu-Chun Hung
发明人： Yu-Chun Hung
IPC分类号： A01N37/18 , A61K31/165 , A61K31/16 , A01N35/00 , A61K31/11 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00 , C07C321/00 , C07C323/00 , C07C381/00 , C07C47/00
CPC分类号： A61K31/11 , A61K31/167 , A61K31/381 , A61K31/445 , A61K31/4545 , A61K31/47 , A61K45/06 , A61K2300/00
摘要： Disclosed herein is a method for prolonging analgesic effect of a membrane permeable local anesthetic in a subject in need thereof. The method uses cinnamaldehyde as an adjuvant which, when administered prior to or simultaneously with the administration of a local anesthetic, prolongs the analgesic effect of the local anesthetic. Also disclosed herein is a method for providing analgesic effect in a subject in need thereof. The method uses cinnamaldehyde as an analgesic compound which, when administered alone to the subject in an analgesically effective amount, provides the analgesic effect.
摘要翻译：本文公开了一种延长可渗透局部麻醉剂在有需要的受试者中的镇痛作用的方法。该方法使用肉桂醛作为佐剂，当在施用局部麻醉剂之前或同时施用时，其延长局部麻醉剂的镇痛作用。本文还公开了一种在有需要的受试者中提供止痛效果的方法。该方法使用肉桂醛作为止痛化合物，当以镇痛有效量单独给予受试者时，其提供镇痛作用。

5. 发明授权

US08673980B2 Closthioamides, compositions, and methods for treating bacterial or fungal infections or cancer 有权
标题翻译： Closthioamides，组合物和治疗细菌或真菌感染或癌症的方法
公开(公告)号：US08673980B2
公开(公告)日：2014-03-18
申请号：US13504990
申请日：2010-11-02
申请人： Swantje Behnken , Hans-Martin Dahse , Christian Hertweck , Keishi Ishida , Thorger Lincke , Martin Roth , Florian Kloss
发明人： Swantje Behnken , Hans-Martin Dahse , Christian Hertweck , Keishi Ishida , Thorger Lincke , Martin Roth , Florian Kloss
IPC分类号： A01N37/18 , A61K31/16 , C07C327/00 , C07C321/00 , C07C323/00 , C07C325/00 , C07C335/00 , C07C381/00 , C07C255/00
CPC分类号： C07C327/48
摘要： This invention relates to the field of biologically active compounds and specifically to closthioamides, pharmaceutical compositions comprising these compounds, and their use as antibiotic, antifungal, and/or cytotoxic agent.
摘要翻译：本发明涉及生物活性化合物领域，特别是涉及氯二甲酰胺，包含这些化合物的药物组合物及其作为抗生素，抗真菌剂和/或细胞毒性剂的用途。

6. 发明授权

US08455552B2 Composition comprising S-allylmercapto-N-acetylcysteine (ASSNAC) for up-regulation of cellular glutathione level 有权
标题翻译：包含用于上调细胞谷胱甘肽水平的S-烯丙基巯基-N-乙酰半胱氨酸（ASSNAC）的组合物
公开(公告)号：US08455552B2
公开(公告)日：2013-06-04
申请号：US12597956
申请日：2008-05-01
申请人： Naphtali Savion , David Mirelman , Aharon Rabinkov , Alex Khenkin
发明人： Naphtali Savion , David Mirelman , Aharon Rabinkov , Alex Khenkin
IPC分类号： A01N41/12 , A61K31/105 , C07C321/00 , C07C323/00 , C07C381/00
CPC分类号： A61K31/198
摘要： The present invention relates to S-allylmercapto-N-acetylcysteine (ASSNAC) and its pharmaceutically acceptable salts and solvates, which are useful for up-regulation of cellular glutathione levels and expression of phase II detoxifying enzymes. The invention further provides methods of use thereof in the prevention, alleviation or treatment of oxidative stress induced by reactive oxygen species (ROS).
摘要翻译：本发明涉及S-烯丙基巯基-N-乙酰半胱氨酸（ASSNAC）及其药学上可接受的盐和溶剂化物，其可用于上调细胞谷胱甘肽水平和II期解毒酶的表达。本发明还提供了用于预防，减轻或治疗由活性氧（ROS）引起的氧化应激的方法。

7. 发明授权

US08338643B2 Reagent for introduction of protein or gene 有权
标题翻译：用于引入蛋白质或基因的试剂
公开(公告)号：US08338643B2
公开(公告)日：2012-12-25
申请号：US12312648
申请日：2007-11-26
申请人： Shinji Takeoka , Naoya Takeda , Hitoshi Kurumizaka , Isao Sakane , Namiko Ikegaya , Yosuke Obata , Syunsuke Saito
发明人： Shinji Takeoka , Naoya Takeda , Hitoshi Kurumizaka , Isao Sakane , Namiko Ikegaya , Yosuke Obata , Syunsuke Saito
IPC分类号： C07C251/00 , C07C233/00 , C07C253/00 , C07C237/00 , C07C239/00 , C07C321/00 , C07C323/00 , C07C381/00
CPC分类号： C07C237/22 , C07C237/08 , C07C237/12 , C07K5/021 , C07K5/06086 , C07K5/0815
摘要： The present invention provides a reagent for introducing a protein or gene into a cell. The reagent of the present invention is, for example, a reagent for introducing a protein or gene into a cell, which comprises a composition comprising a cationic amino acid type lipid represented by the following formula (I)-1: (wherein in formula (I)-1: L is a single bond, —CONH—, or —S—S—; M1 is —(CH2)k— or —(CH2CH2O)k— (wherein k is an integer between 0 and 14); and m1 and m2 are each independently an integer between 11 and 21 (in this regard, when providing a reagent for introducing a gene into a cell, the case where both m1 and m2 are 15 is excluded)).
摘要翻译：本发明提供了将蛋白质或基因导入细胞的试剂。本发明的试剂是例如将蛋白质或基因导入细胞的试剂，其包含含有下式（I）-1表示的阳离子型氨基酸型脂质的组合物（式中，式 I）-1：L是单键，-CONH-或-S-S-; M 1是 - （CH 2）k - 或 - （CH 2 CH 2 O）k-（其中k是0和14之间的整数）;和 m1和m2各自独立地为11-21之间的整数（在这方面，当提供用于将基因导入细胞的试剂时，m1和m2均为15的情况除外））。

8. 发明授权

US08334410B2 Method for producing 3-mercaptoaniline compound 有权
标题翻译： 3-巯基苯胺化合物的制备方法
公开(公告)号：US08334410B2
公开(公告)日：2012-12-18
申请号：US12743389
申请日：2008-11-28
申请人： Kentaro Kawazoe
发明人： Kentaro Kawazoe
IPC分类号： C07C209/00 , C07C323/00 , C07C317/00
CPC分类号： C07C319/02 , C07C303/22 , C07C309/86 , C07C323/34
摘要： A method for producing a 3-mercaptoaniline compound, which is a known intermediate for a 3-(1H-1,2,4-triazol-1-yl)phenylsulfide derivative, useful as a pesticide, and a method for producing a compound which can be used as a starting material in producing the 3-mercaptoaniline compound are disclosed. In one embodiment the nitro group and the chlorosulfonyl group of a 3-nitrobenzenesulfonyl chloride compound represented by general formula (1): are reduced in the presence of an acid catalyst to produce a compound of general formula (2): In the above general formulas (1) and (2), R represents an alkyl group or a cyclic alkyl group, and X represents a halogen atom.
摘要翻译：作为可用作农药的3-（1H-1,2,4-三唑-1-基）苯硫醚衍生物的已知中间体的3-巯基苯胺化合物的制造方法及其制造方法可以用作生产3-巯基苯胺化合物的原料。在一个实施方案中，通式（1）表示的3-硝基苯磺酰氯化合物的硝基和氯磺酰基在酸催化剂的存在下还原，得到通式（2）的化合物：在上述通式（1）和（2）中，R表示烷基或环状烷基，X表示卤素原子。

9. 发明授权

US08193386B2 Crystalline form of (S)-1-phenylethylammonium (R)-diphenylmethanesulphinyl-acetate 失效
标题翻译：（S）-1-苯基乙基铵（R） - 二苯基甲酰亚氨基乙酸酯的结晶形式
公开(公告)号：US08193386B2
公开(公告)日：2012-06-05
申请号：US12264502
申请日：2008-11-04
申请人： Giuseppe Barreca , Pietro Allegrini , Gabriele Razzetti
发明人： Giuseppe Barreca , Pietro Allegrini , Gabriele Razzetti
IPC分类号： C07C323/00 , C07C231/00
CPC分类号： C07C317/44 , C07C315/04
摘要： Novel crystalline hydrate form of (S)-1-phenylethylammonium (R)-diphenyl-methanesulphinyl-acetate and its use in a process for the preparation of (R)-benzhydrylsulphinylacetamide.
摘要翻译：（S）-1-苯基乙基铵（R） - 二苯基 - 甲基亚磺酰基 - 乙酸酯的新型结晶水合物形式及其在制备（R） - 二苯甲基亚磺酰基乙酰胺的方法中的用途。

10. 发明授权

US08163956B2 Inhibitors of GLYT1 transporters 有权
标题翻译： GLYT1转运蛋白的抑制剂
公开(公告)号：US08163956B2
公开(公告)日：2012-04-24
申请号：US11922074
申请日：2006-06-13
申请人： Wesley Peter Blackaby , Ian Thomas Huscroft , Linda Elizabeth Keown , Richard Thomas Lewis , Piotr Antoni Raubo , Leslie Joseph Street , Christopher George Thomson , Joanne Thomson
发明人： Wesley Peter Blackaby , Ian Thomas Huscroft , Linda Elizabeth Keown , Richard Thomas Lewis , Piotr Antoni Raubo , Leslie Joseph Street , Christopher George Thomson , Joanne Thomson
IPC分类号： C07C303/00 , C07C233/00 , C07C237/00 , C07C323/00 , A61K31/16 , A61K31/165
CPC分类号： C07D249/04 , C07C317/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/08 , C07D207/09 , C07D211/26 , C07D211/28 , C07D211/60 , C07D213/40 , C07D249/12 , C07D295/067 , C07D309/04 , C07D401/12
摘要： A compound of the formula (I): wherein R1, R2, R3, R4, Ar, A, n and m are defined herein, is disclosed as a GlyT1 inhibitor; pharmaceutical compositions containing the compound of the formula (I) are also disclosed as are their use in medicine, for example in the treatment of schizophrenia.
摘要翻译：公开了式（I）化合物：其中R 1，R 2，R 3，R 4，Ar，A，n和m如本文所定义，被公开为GlyT1抑制剂; 还公开了含有式（I）化合物的药物组合物，它们在医学中的用途，例如在精神分裂症的治疗中。

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