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1. 发明授权

US09309508B2 Boronic and borinic acid compound as inhibitors of sulfenic acid-containing proteins 有权
标题翻译：硼酸和硼酸化合物作为含亚磺酸蛋白质的抑制剂
公开(公告)号：US09309508B2
公开(公告)日：2016-04-12
申请号：US14576613
申请日：2014-12-19
申请人： Stephen Benkovic , Chunyu Liu , John W. Tomsho
发明人： Stephen Benkovic , Chunyu Liu , John W. Tomsho
IPC分类号： C12N9/99 , C12N9/88
CPC分类号： C12N9/99 , C12N9/88 , C12Y402/01084
摘要： A boronic or borinic acid compound is used to inhibit the activity of a sulfenic acid-containing protein. Thus, a biologically-active sulfenic acid-containing protein is contacted with an activity-inhibiting effective amount of a boronic or borinic acid compound of Formula I or a salt, hydrate or solvate thereof, whose components are disclosed within, and that contact is maintained for a time sufficient to inhibit the biological activity of the protein.
摘要翻译：使用硼酸或硼酸化合物抑制含亚磺酸的蛋白质的活性。因此，含有生物活性的含亚磺酸的蛋白质与活性抑制有效量的式I的硼酸或硼酸化合物或其盐，水合物或溶剂合物接触，其组分在其中公开，并且保持接触足以抑制蛋白质的生物活性。

2. 发明申请

US20060035270A1 Unique recognition sequences and methods of use thereof in protein analysis 审中-公开
标题翻译：蛋白质分析中独特的识别序列及其使用方法
公开(公告)号：US20060035270A1
公开(公告)日：2006-02-16
申请号：US11249847
申请日：2005-10-13
申请人： Frank Lee , Xun Meng , John Chan , Shengsheng Zhang , Stephen Benkovic
发明人： Frank Lee , Xun Meng , John Chan , Shengsheng Zhang , Stephen Benkovic
IPC分类号： C12Q1/68 , G01N33/53 , G06F19/00
CPC分类号： C40B30/04 , B82Y5/00 , B82Y10/00 , B82Y30/00 , C12Q1/48 , G01N33/68 , G01N33/6803 , G01N33/6842 , G01N33/6851 , Y02A90/26
摘要： Disclosed are methods for reliably detecting the presence of proteins in a sample by the use of capture agents that recognize and interact with recognition sequences uniquely characteristic of a set of proteins in the sample. Arrays comprising these capture agents are also provided.
摘要翻译：公开的是通过使用识别和与样品中一组蛋白质唯一特征的识别序列相互作用的捕获剂来可靠地检测样品中蛋白质的存在的方法。还提供了包含这些捕获剂的阵列。

3. 发明申请

US20050054644A1 Hydrolytically-resistant boron-containing therapeutics and methods of use 有权
标题翻译：耐水解硼含量治疗剂及使用方法
公开(公告)号：US20050054644A1
公开(公告)日：2005-03-10
申请号：US10868268
申请日：2004-06-15
申请人： Ving Lee , Jacob Plattner , Stephen Benkovic , Stephen Baker , Kirk Maples , Carolyn Bellinger-Kawahara , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio Sauro
发明人： Ving Lee , Jacob Plattner , Stephen Benkovic , Stephen Baker , Kirk Maples , Carolyn Bellinger-Kawahara , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio Sauro
IPC分类号： A61K20060101 , A61K31/498 , A61K31/53 , A61K31/69 , C07D471/02 , C07D487/02 , C07F5/02
CPC分类号： C07F5/025
摘要： Compositions and methods of use of borole derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
摘要翻译：公开了用于治疗由细菌或病毒引起的疾病的治疗剂的硼烷衍生物，包括苯并恶唑，苯并唑并苯并噻唑的组合物和方法，以及合成所述试剂及其组合物的方法。

4. 发明申请

US20080293675A1 ANTIBIOTICS CONTAINING BORINIC ACID COMPLEXES AND METHODS OF USE 有权
标题翻译：含有硼酸复合物的抗生素及其使用方法
公开(公告)号：US20080293675A1
公开(公告)日：2008-11-27
申请号：US11971693
申请日：2008-01-09
申请人： Ving Lee , Stephen Benkovic , Stephen Baker , Kirk Maples , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio Sauro , Chetan Pandit , Zhuoyi Su , Zhixiang Yang
发明人： Ving Lee , Stephen Benkovic , Stephen Baker , Kirk Maples , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio Sauro , Chetan Pandit , Zhuoyi Su , Zhixiang Yang
IPC分类号： A61K31/69 , C07F5/02 , A01N55/08
CPC分类号： C07F5/025
摘要： The structure and preparation of antibiotics incorporating borinic acid complexes are disclosed, especially hydroxyquinoline, imidazole and picolinic acid derivatives, along with compositions of these antibiotics and methods of using the antibiotics and compositions as bactericidal and fungicidal agents as well as therapeutic agents for the treatment of diseases caused by bacteria and fungi.
摘要翻译：公开了包含硼酸络合物的抗生素的结构和制备，特别是羟基喹啉，咪唑和吡啶甲酸衍生物，以及这些抗生素的组合物以及使用抗生素和组合物作为杀菌和杀真菌剂的方法以及用于治疗细菌和真菌引起的疾病。

5. 发明申请

US20050227933A1 Treatment of bacterial induced diseases using DNA methyl transferase inhibitors 审中-公开
标题翻译：使用DNA甲基转移酶抑制剂治疗细菌诱导的疾病
公开(公告)号：US20050227933A1
公开(公告)日：2005-10-13
申请号：US10615703
申请日：2003-07-09
申请人： Stephen Benkovic , Lucy Shapiro , Rachel Wright , Craig Stephens , Lyn Kahng , Anthony Berdis , Irene Lee
发明人： Stephen Benkovic , Lucy Shapiro , Rachel Wright , Craig Stephens , Lyn Kahng , Anthony Berdis , Irene Lee
IPC分类号： A61K48/00 , C07F5/02
CPC分类号： C07F5/025
摘要： Methods for treating and/or preventing disease conditions caused or induced or aggravated by microbes, especially bacteria, by inhibiting DNA methyltransferase activity, such as by administering to an animal a DNA methyltransferase inhibitor, are disclosed, along with methods of reducing or ablating virulence in bacteria by inhibiting DNA methyltransferase activity.
摘要翻译：通过抑制DNA甲基转移酶活性，例如通过向动物施用DNA甲基转移酶抑制剂来治疗和/或预防由微生物，特别是细菌引起或加剧的疾病状况的方法，以及降低或消除毒性的方法细菌通过抑制DNA甲基转移酶活性。

6. 发明申请

US20050080048A1 Methods for the preparation of alkyl diaryl borinates and complexed diarylboronic acids 有权
标题翻译：制备烷基二芳基硼酸盐和络合的二芳基硼酸的方法
公开(公告)号：US20050080048A1
公开(公告)日：2005-04-14
申请号：US10501755
申请日：2003-01-09
申请人： Ali Tavassoli , Stephen Benkovic
发明人： Ali Tavassoli , Stephen Benkovic
IPC分类号： C07F5/02 , A61K31/69
CPC分类号： C07F5/02 , C07F5/025
摘要： The present invention provides methods for preparing complexed diaryl boronic acids from alkyl diarylborinates.
摘要翻译：本发明提供了从烷基二芳基硼酸盐制备络合的二芳基硼酸的方法。

7. 发明申请

US20050070503A1 Antibiotics containing borinic acid complexes and methods of use 有权
标题翻译：含有硼酸配合物的抗生素及其使用方法
公开(公告)号：US20050070503A1
公开(公告)日：2005-03-31
申请号：US10867465
申请日：2004-06-14
申请人： Ving Lee , Stephen Benkovic , Stephen Baker , Kirk Maples , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio Sauro , Chetan Pandit , Zhuoyi Su , Zhixiang Yang
发明人： Ving Lee , Stephen Benkovic , Stephen Baker , Kirk Maples , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio Sauro , Chetan Pandit , Zhuoyi Su , Zhixiang Yang
IPC分类号： A61K31/69 , C07F5/02 , C07F5/04
CPC分类号： C07F5/025
摘要： The structure and preparation of antibiotics incorporating borinic acid complexes are disclosed, especially hydroxyquinoline, imidazole and picolinic acid derivatives, along with compositions of these antibiotics and methods of using the antibiotics and compositions as bactericidal and fungicidal agents as well as therapeutic agents for the treatment of diseases caused by bacteria and fungi.
摘要翻译：公开了包含硼酸络合物的抗生素的结构和制备，特别是羟基喹啉，咪唑和吡啶甲酸衍生物，以及这些抗生素的组合物以及使用抗生素和组合物作为杀菌和杀真菌剂的方法以及用于治疗细菌和真菌引起的疾病。

8. 发明授权

US4900674A Antibody combining sites that exhibit amide or ester synthase activity 失效
标题翻译：表现出酰胺或酯合成酶活性的抗体结合位点
公开(公告)号：US4900674A
公开(公告)日：1990-02-13
申请号：US55177
申请日：1987-05-28
申请人： Stephen Benkovic , Richard A. Lerner , Alfonso Tramontano , Andrew D. Napper
发明人： Stephen Benkovic , Richard A. Lerner , Alfonso Tramontano , Andrew D. Napper
IPC分类号： C12N9/00
CPC分类号： C12N9/0002
摘要： A phosphorous-containing analog-ligand having a conformation that substantially corresponds to the conformation of an amide- or ester-forming transition state is used to induce production of receptor molecules whose antibody combining sites have amide or ester synthase catalytic activity when reacted with a ligand containing (i) a carbonyl carbon atom and (ii) an amine or alcohol group that are structurally capable of forming a preselected carboxylic amide or ester bond.
摘要翻译：具有基本上对应于形成酰胺或酯形成过渡态的构象的构象的含磷类似物配体被用于诱导当与配体反应时其抗体结合位点具有酰胺或酯合成酶催化活性的受体分子的产生含有（i）羰基碳原子和（ii）结构上能够形成预选择的羧酰胺或酯键的胺或醇基团。

9. 发明申请

US20160324160A1 SYNERGISTIC BENZOXABOROLE-CONTAINING ANTI-FUNGICIDAL COMPOSITION 有权
标题翻译：合成含苯甲酸的抗真菌组合物
公开(公告)号：US20160324160A1
公开(公告)日：2016-11-10
申请号：US15093331
申请日：2016-04-07
申请人： Stephen Benkovic , Chunyu Liu
发明人： Stephen Benkovic , Chunyu Liu
IPC分类号： A01N55/08 , A01N25/08 , A01N25/02
CPC分类号： A01N55/08 , A01N25/02 , A01N25/08 , A01N61/00 , A61K31/69 , A01N2300/00
摘要： An anti-fungal composition for the control of one or more target fungi (or a similar heterotrophic, hyphae-producing organism) that infect plant materials and are (is) separately controllable by a benzoxaborole and an anti-fungal compound of a preselected FRAC Target Site Code is disclosed, as is a method of its use. A composition contains a diluent medium having dissolved or dispersed therein a synergistic effective amount of each of a first and a second anti-fungal compound. The first anti-fungal compound is a benzoxaborole of Formula I. The second anti-fungal compound is other than a benzoxaborole and is known to control said one or more target species of fungus when utilized as the sole anti-fungal compound at a concentration greater than the synergistic effective amount and has a preselected FRAC Target Site Code of B, C, D, E, G, H, or M.
摘要翻译：用于控制感染植物材料的一种或多种目标真菌（或类似的异养，菌丝产生生物体）的抗真菌组合物，其可分别由预选的FRAC靶标的苯并恶唑和抗真菌化合物控制公开了现场代码，以及其使用方法。组合物含有溶解或分散有协同有效量的第一和第二抗真菌化合物的稀释介质。第一种抗真菌化合物是式I的苯并恶唑。第二种抗真菌化合物是除苯并恶唑之外的化合物，当用作唯一的抗真菌化合物时，已知可以控制所述一种或多种目标物种的真菌浓度具有协同有效量，并具有B，C，D，E，G，H或M的预先选定的FRAC目标位点代码。

10. 发明申请

US20070207502A1 CYCLIC PEPTIDES 有权
标题翻译：循环肽
公开(公告)号：US20070207502A1
公开(公告)日：2007-09-06
申请号：US11670112
申请日：2007-02-01
申请人： Stephen Benkovic , Charles Scott , Ernesto Abel-Santos
发明人： Stephen Benkovic , Charles Scott , Ernesto Abel-Santos
IPC分类号： C40B30/06 , C40B40/08 , C40B40/10 , C07K14/005 , C07K14/47 , C07K14/195
CPC分类号： C12N15/10 , C07K7/52 , C07K7/64 , C12N15/1055 , G01N2500/00
摘要： Methods of producing cyclic peptides and splicing intermediates of peptides in a looped conformation are disclosed. The methods utilize the trans-splicing ability of split inteins to catalyze cyclization of peptides from a precursor peptide having a target peptide interposed between two portions of a split intein. The interaction of the two portions of the split intein creates a catalytically-active intein and also forces the target peptide into a loop configuration that stabilizes the ester isomer of the amino acid at the junction between one of the intein portions and the target peptide. A heteroatom from the other intein portion then reacts with the ester to form a cyclic ester intermediate. The active intein catalyzes the formation of an aminosuccinimide that liberates a cyclized form of the target peptide, which spontaneously rearranges to form the thermodynamically favored backbone cyclic peptide product. Also disclosed are nucleic acid molecules, polypeptides, methods for making cyclic peptides, methods of making libraries, and methods of screening peptides.
摘要翻译：公开了以循环构象形成肽的环肽和剪接中间体的方法。所述方法利用分裂内蛋白的转拼能力来催化来自前导肽的肽的环化，所述肽的前导肽插入分裂的内含肽的两部分之间。分裂内含肽的两部分的相互作用产生催化活性内含肽，并且还将目标肽强制成使得在内含肽部分和目标肽之间的连接处稳定氨基酸的酯异构体的环构型。来自另一个内含肽部分的杂原子然后与酯反应以形成环状酯中间体。活性内含肽催化氨基琥珀酰亚胺的形成，其释放环化形式的靶肽，其自发重排以形成热力学上有利的主链环肽产物。还公开了核酸分子，多肽，制备环肽的方法，制备文库的方法和筛选肽的方法。

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