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1. 发明申请

WO2007137255A3 BACTERIAL THIOREDOXIN REDUCTASE INHIBITORS AND METHODS FOR USE THEREOF 审中-公开
公开(公告)号：WO2007137255A3
公开(公告)日：2007-11-29
申请号：PCT/US2007/069455
申请日：2007-05-22
申请人： THIOREDOXIN SYSTEMS AB , THYOGEN PHARMACEUTICALS, INC. , HOLMGREN, Arne , LU, Jun , VLAMIS-GARDIKAS, Alexios , ZHAO, Rong , KANDASAMY, K. , ENGMAN, Lars , ENGSTRAND, Lars , HOFFNER, Sven
发明人： HOLMGREN, Arne , LU, Jun , VLAMIS-GARDIKAS, Alexios , ZHAO, Rong , KANDASAMY, K. , ENGMAN, Lars , ENGSTRAND, Lars , HOFFNER, Sven
IPC分类号： A61K31/555 , A61K31/385 , A61K31/38
摘要： The mechanism of action of Ebselen differentiates between bacterial and mammalian thioredoxin reductase (TrxR). It displays fast oxidation of mammalian Trx and via the NADPH-TrxR catalyzed turnover of ebselen selenol with hydrogen peroxide, and therefore are mammalian antioxidants. Ebselen, and its diselenide, are strong competitive inhibitors of E.coli TrxR with K i of 0.14 µM and 0.46 µM, respectively. E.coli mutants lacking glutathione reductase or glutathione were much more sensitive to inhibition by ebselen. Since either glutaredoxin or thioredoxin systems are electron donors to ribonucleotide reductase, ebselen targets primarily glutathione and glutaredoxin-negative bacteria, a class which includes major pathogens. Ebselen, and similar compounds are therefore useful as antibacterial agents, even for multiresistant strains. Two major pathogenic bacteria, which previously had not been known to be sensitive to ebselen, Mycobacterium tuberculosis (tuberculosis) and Helicobacter pylori (stomach ulcer and cancer), were shown to be excellent targets. Helicobacter pylori was also sensitive to ebsulfur.

2. 发明申请

WO2011039381A1 ANTIOXIDANTS FOR USE IN THERAPY 审中-公开
标题翻译：用于治疗的抗氧化剂
公开(公告)号：WO2011039381A1
公开(公告)日：2011-04-07
申请号：PCT/EP2010/064767
申请日：2010-10-04
申请人： KAROLINSKA INSTITUTET INNOVATIONS AB , ENGMAN, Lars , JOHANSSON, Henrik Alexander
发明人： ENGMAN, Lars , JOHANSSON, Henrik Alexander
IPC分类号： A61K33/04 , A61P29/00 , A61P35/00 , A61P25/28
CPC分类号： A61K33/04 , A61K31/095
摘要： Compounds based on the followining structures: wherein each of R1, R2, R3 and R4 is independently selected from: hydrogen, alkyl, and substituted alkyl; and each of R5, R6 and R7 is independently selected from: hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, N,N-dialkylamino, substituted N,N-dialkylamino, N-monoalkylamino, substituted N-monoalkylamino, and electron-donating substituents are useful in the treatment of disorders or conditions caused by or involving free radical-mediated or oxidative tissue damage.
摘要翻译：基于以下结构的化合物：其中R 1，R 2，R 3和R 4各自独立地选自：氢，烷基和取代的烷基; R5，R6和R7各自独立地选自氢，烷基，取代的烷基，烷氧基，取代的烷氧基，N，N-二烷基氨基，取代的N，N-二烷基氨基，N-单烷基氨基，取代的N-单烷基氨基，给药取代基可用于治疗由自由基介导的或氧化组织损伤引起的或涉及自由基介导的或氧化性组织损伤引起的疾病或病症。

3. 发明申请

WO2009144253A1 COMPOUNDS COMPRISING A 3-PYRIDINOL OR 5-PYRIMIDINOL RING HAVING AN ORGANOSELENO OR ORGANOTELLURO SUBSTITUENT FOR USE AS ANTIOXIDANTS 审中-公开
标题翻译：包含具有作为抗氧化剂的有机锗或有机替代物的3-吡啶醇或5-吡啶二胺环的化合物
公开(公告)号：WO2009144253A1
公开(公告)日：2009-12-03
申请号：PCT/EP2009/056468
申请日：2009-05-27
申请人： KAROLINSKA INSTITUTET INNOVATIONS AB , ENGMAN, Lars
发明人： ENGMAN, Lars
IPC分类号： A61K31/44 , A61K31/505 , C07D213/60 , C09K15/32 , A61P39/06
CPC分类号： A61K31/44 , A61K31/505 , C07D213/65 , C07D239/34 , C09K15/328
摘要： Compounds comprising a 3-pyridinol or 5-pyrimidinol ring carrying an organoseleno- or organotelluro- substituent on the pyridine or pyrimidine ring, exhibit useful antioxidant properties. The compounds may for example be in accordance with the following formula (I) as defined herein. Catalytic chain-breaking and hydroperoxide decomposing antioxidant properties are also disclosed. Furthermore the compounds may be used in combination with a reducing agent. The compounds are useful for the stabilization of man-made and natural materials, or for the prevention or treatment of disorders caused by or involving free radical-mediated or oxidative tissue damage.
摘要翻译：包含在吡啶或嘧啶环上携带有机硒或有机基芴取代基的3-吡啶醇或5-嘧啶环的化合物表现出有用的抗氧化性质。化合物可以例如根据如本文所定义的下式（I）。还公开了催化断链和氢过氧化物分解抗氧化性能。此外，化合物可以与还原剂组合使用。这些化合物可用于稳定人造和天然材料，或用于预防或治疗由自由基介导的或氧化组织损伤引起的疾病或引起的疾病。

4. 发明申请

WO2003052026A1 AN ANTIOXIDANT COMPOSITION 审中-公开
标题翻译：抗氧化剂组合物
公开(公告)号：WO2003052026A1
公开(公告)日：2003-06-26
申请号：PCT/SE2002/002037
申请日：2002-11-07
申请人： POLYINOVA AB , ERIKSSON, Petter , ENGMAN, Lars
发明人： ERIKSSON, Petter , ENGMAN, Lars
IPC分类号： C09K15/32
CPC分类号： C08K5/36 , C09K15/328 , C10M141/12 , C10M2207/026 , C10M2207/04 , C10M2207/289 , C10M2215/06 , C10M2219/06 , C10M2219/085 , C10M2219/102 , C10N2210/06
摘要： An antioxidant composition as a stabilising agent for polymer, elastomer, grease, lubricant and oil compounds, wherein the antioxidant composition comprises an organic tellurium compound and at least one reducing agent. A polymer, elastomer, grease, lubricant or oil compound stabilised against oxidation, comprising an organic tellurium compound and at least one reducing agent as an antioxidant composition. Method of stabilising polymer, elastomer, grease, lubricant or oil compounds against oxidation, comprising the step of adding an organic tellurim compound and at least one reducing agent as an antioxidant composition to the polymer, elastomer, grease, lubricant or oil compounds to formulating them. Use of an organic tellurium compound and at least one reducing agent as an antioxidant composition in polymer, elastomer, grease, lubricant and oil compounds.
摘要翻译：作为聚合物，弹性体，润滑脂，润滑剂和油性化合物的稳定剂的抗氧化剂组合物，其中所述抗氧化剂组合物包含有机碲化合物和至少一种还原剂。稳定抗氧化的聚合物，弹性体，润滑脂，润滑剂或油性化合物，包含有机碲化合物和至少一种还原剂作为抗氧化剂组合物。稳定聚合物，弹性体，油脂，润滑剂或油性化合物抗氧化的方法，包括将有机碲化合物和至少一种还原剂作为抗氧化剂组合物加入到聚合物，弹性体，油脂，润滑剂或油性化合物中以配制它们的步骤。在聚合物，弹性体，油脂，润滑剂和油性化合物中使用有机碲化合物和至少一种还原剂作为抗氧化剂组合物。

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