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1. 发明申请

US20140018287A1 BRIDGE-HELIX CAP: TARGET AND METHOD FOR INHIBITION OF BACTERIAL RNA POLYMERASE 有权
标题翻译： BRIDGE-HELIX CAP：用于抑制细菌RNA聚合酶的靶和方法
公开(公告)号：US20140018287A1
公开(公告)日：2014-01-16
申请号：US14006035
申请日：2012-03-19
申请人： Richard H. Ebright , David Degen , Katherine Y. Ebright
发明人： Richard H. Ebright , David Degen , Katherine Y. Ebright
IPC分类号： A61K38/12 , A61K45/06 , A61K31/155 , G01N33/68 , A61K31/395
CPC分类号： A61K38/15 , A61K31/15 , A61K31/155 , A61K31/343 , A61K31/395 , A61K31/496 , A61K38/12 , A61K45/06 , C07D498/08 , C12Q1/18 , G01N33/68 , G01N2333/91275 , Y02A50/473 , A61K2300/00
摘要： It has been discovered that the Sal target represents a new and promising target for antibacterial drug discovery. The Sal target is distinct from the rifamycin target and from the CBR703 target. This indicates that antibacterial compounds that function through the Sal target should exhibit no, or minimal, cross-resistance with rifamycins and CBR703. This further implies that it should be possible to co-administer antibacterial compounds that function through the Sal target together with a rifamycin, together with CBR703, or together with both a rifamycin and CBR703, in order to achieve additive or synergistic antibacterial effects and in order to suppress or eliminate the emergence of resistance.
摘要翻译：已经发现，Sal靶标是抗菌药物发现的新的有希望的靶标。 Sal靶标与利福霉素靶标和CBR703靶标不同。这表明通过Sal靶标起作用的抗菌化合物应该与利福霉素和CBR703不表现出或最小的交叉抗性。这进一步意味着应该可以共同施用通过Sal靶与利培酮一起发挥作用的抗菌化合物与CBR703，或者与利福霉素和CBR703一起共同施用，以获得添加或协同的抗菌作用抑制或消除抵抗的出现。

2. 发明申请

US20100311074A1 SWITCH-REGION: TARGET AND METHOD FOR INHIBITION OF BACTERIAL RNA POLYMERASE 失效
标题翻译：开关区：用于抑制细菌RNA聚合酶的靶和方法
公开(公告)号：US20100311074A1
公开(公告)日：2010-12-09
申请号：US12612787
申请日：2009-11-05
申请人： RICHARD H. EBRIGHT
发明人： RICHARD H. EBRIGHT
IPC分类号： G01N33/53
CPC分类号： G01N33/566 , C07K2299/00 , C12N9/1247 , C12Q1/48 , G01N33/569 , G01N33/573 , G01N2333/9125 , G01N2500/00
摘要： The invention provides a target and methods for specific binding and inhibition of RNA polymerase from bacterial species. The invention provides methods for identifying agents that bind to a bacterial RNA polymerase, and that inhibit an activity of a bacterial RNA polymerase, through interactions with a bacterial RNA polymerase homologous switch-region amino-acid sequence. Said methods comprise preparing a reaction solution comprising the compound to be tested and an entity containing a bacterial RNAP homologous switch-region amino-acid sequence, and detecting binding or inhibition. The invention has applications in control of bacterial gene expression, control of bacterial viability, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.
摘要翻译：本发明提供了从细菌种类特异性结合和抑制RNA聚合酶的靶标和方法。本发明提供了通过与细菌RNA聚合酶同源转换区氨基酸序列的相互作用来鉴定结合细菌RNA聚合酶并且抑制细菌RNA聚合酶活性的试剂的方法。所述方法包括制备包含待测试化合物和含有细菌RNAP同源转换区氨基酸序列的实体的反应溶液，并检测结合或抑制。本发明可用于控制细菌基因表达，控制细菌活力，控制细菌生长，抗菌化学和抗菌治疗。

3. 发明申请

US20100047780A1 TARGET AND METHOD FOR INHIBITION OF BACTERIAL RNA POLYMERASE 有权
标题翻译：用于抑制细菌RNA聚合酶的靶和方法
公开(公告)号：US20100047780A1
公开(公告)日：2010-02-25
申请号：US12257801
申请日：2008-10-24
申请人： Richard H. Ebright
发明人： Richard H. Ebright
IPC分类号： C07K14/32 , C07K14/245 , G01N33/53 , C12Q1/68
CPC分类号： G01N33/533 , C07K14/245 , G01N33/502 , G01N33/569 , G01N2500/00
摘要： Target and method for inhibition of bacterial RNA polymerase disclosed are targets and methods for specific binding and inhibition of RNAP from bacterial species.
摘要翻译：公开的抑制细菌RNA聚合酶的靶标和方法是从细菌物种特异性结合和抑制RNAP的靶标和方法。

4. 发明授权

US07381572B2 Reagents and procedures for multi-label high-specificity labeling 有权
标题翻译：多标签高特异性标记的试剂和程序
公开(公告)号：US07381572B2
公开(公告)日：2008-06-03
申请号：US11256900
申请日：2005-10-24
申请人： Richard H. Ebright , Yon W. Ebright
发明人： Richard H. Ebright , Yon W. Ebright
IPC分类号： G01N33/533 , G01N21/76 , G01N21/00 , G01N33/53 , C07K1/13 , C07D209/04
CPC分类号： G01N33/542 , C07K5/0827 , C07K5/1013 , C07K7/06 , C07K7/08 , G01N33/58 , G01N33/582 , Y10S435/968 , Y10S436/80 , Y10S436/805
摘要： A detectable complex and methods for use thereof are provided herein. The detectable complex includes: at least one target material; a first peptide tag bound to the at least one target material; and a second peptide tag bound to the at least one target material. The complex further includes a first conjugate having a detectable group and two pendant phenylarsine moieties comprising a first tag binding group; wherein the first conjugate preferentially associates with the first peptide tag; and a second conjugate having a detectable group and two pendant phenylarsine moieties comprising a second tag binding group; wherein the second conjugate preferentially associates with the second peptide tag. The mean distance and/or mean angle between the pendant phenylarsine moieties in the first conjugate is different from the mean distance and/or mean angle between the pendant phenylarsine moieties in the second conjugate. Further provided herein are useful peptide tag combinations, target materials or sets of target materials including these peptide tag combinations, and nucleic acids or nucleic acid sets encoding these compositions.
摘要翻译：本文提供可检测的复合物及其使用方法。可检测的复合物包括：至少一种靶材料; 与所述至少一种靶材料结合的第一肽标签; 和与所述至少一种靶材料结合的第二肽标签。所述复合物还包括具有可检测基团的第一缀合物和包含第一标签结合基团的两个侧链胂基部分; 其中所述第一缀合物优先与所述第一肽标签缔合; 和具有可检测基团的第二缀合物和包含第二标签结合基团的两个侧链胂基部分; 其中所述第二缀合物优先与所述第二肽标签相关联。第一共轭物中的侧基胂基部分之间的平均距离和/或平均角度不同于第二共轭物中的侧基胂基部分之间的平均距离和/或平均角度。本文进一步提供了有用的肽标签组合，靶标材料或包含这些肽标签组合的靶物质组以及编码这些组合物的核酸或核酸组。

5. 发明授权

US09133155B2 Antibacterial agents: high-potency myxopyronin derivatives 有权
标题翻译：抗菌剂：高效的myxopyronin衍生物
公开(公告)号：US09133155B2
公开(公告)日：2015-09-15
申请号：US13822935
申请日：2011-09-16
申请人： Richard H. Ebright , Yon W. Ebright
发明人： Richard H. Ebright , Yon W. Ebright
IPC分类号： A61K31/35 , C07D309/38 , A61K9/00 , A61K31/366 , A61K47/18 , A61K47/44 , C07D309/22 , A01N47/12 , C12N9/99
CPC分类号： C07D309/38 , A01N47/12 , A61K9/0019 , A61K31/366 , A61K47/18 , A61K47/44 , C07D309/22 , C12N9/99 , Y02A50/473
摘要： The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Ya, Yb, R1, R2, and G are as described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as inhibitors of bacterial RNA polymerase and as antibacterial agents.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐，其中Ya，Yb，R 1，R 2和G如说明书中所述，以及包含式（I）化合物的组合物。该化合物可用作细菌RNA聚合酶和抗菌剂的抑制剂。

6. 发明申请

US20150031640A1 ANTIBACTERIAL AGENTS: COMBINATION OF A RIFAMYCIN AND A SWITCH REGION INHIBITOR 有权
标题翻译：抗生素代谢物：联合利福平和开关区抑制剂的组合
公开(公告)号：US20150031640A1
公开(公告)日：2015-01-29
申请号：US14376789
申请日：2013-02-05
申请人： Richard H. Ebright
发明人： Richard H. Ebright
IPC分类号： A61K31/496 , A61K31/7048 , A61K31/366
CPC分类号： A61K31/496 , A61K31/366 , A61K31/395 , A61K31/70 , A61K31/7048 , Y02A50/473 , A61K2300/00
摘要： It has been determined that co-administration of a rifamycin and a switch-region inhibitor 1) results in synergistic antibacterial effects, enabling efficacy at low, subtoxic doses, and/or 2) results in a low spontaneous resistance frequency, enabling treatment of high-titer infections without treatment failure due to spontaneous resistance. Accordingly, certain embodiments provide composition comprising a rifamycin and a switch region inhibitor, as well as methods of use thereof.
摘要翻译：已经确定，利福霉素和开关区抑制剂1）的共同给药导致协同的抗菌作用，使得在低，亚毒性剂量下有效，和/或2）导致低自发电阻频率，使得能够治疗高由于自发阻力而无治疗失败的分级感染。因此，某些实施方案提供包含利福霉素和开关区抑制剂的组合物，以及其使用方法。

7. 发明授权

US08372839B2 Bipartite inhibitors of bacterial RNA polymerase 有权
标题翻译：细菌RNA聚合酶的双分子抑制剂
公开(公告)号：US08372839B2
公开(公告)日：2013-02-12
申请号：US12084018
申请日：2006-11-04
申请人： Richard H. Ebright , Dongye Wang
发明人： Richard H. Ebright , Dongye Wang
IPC分类号： A61K31/497 , A01N43/54 , C07D239/70
CPC分类号： C07D498/08
摘要： The invention provides a compound having a structural formula (I): X-α-Y, wherein X is an moiety that binds to the Rif pocket of a bacterial RNA polymerase, Y is a moiety that binds to the secondary channel of a bacterial RNA polymerase, and α is a linker. The compound can act as an inhibitor of bacterial RNA polymerase. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.
摘要翻译：本发明提供具有结构式（I）的化合物：X-α-Y，其中X是与细菌RNA聚合酶的Rif口结合的部分，Y是与细菌RNA的第二通道结合的部分聚合酶，α是接头。该化合物可作为细菌RNA聚合酶的抑制剂。本发明可用于控制细菌基因表达，细菌生长控制，抗菌化学和抗菌治疗。

8. 发明申请

US20130030152A1 TARGET AND METHOD FOR INHIBITION OF BACTERIAL RNA POLYMERASE 有权
标题翻译：用于抑制细菌RNA聚合酶的靶和方法
公开(公告)号：US20130030152A1
公开(公告)日：2013-01-31
申请号：US13482149
申请日：2012-05-29
申请人： Richard H. Ebright
发明人： Richard H. Ebright
IPC分类号： C07K14/245
CPC分类号： G01N33/533 , C07K14/245 , G01N33/502 , G01N33/569 , G01N2500/00
摘要： Target and method for inhibition of bacterial RNA polymerase disclosed are targets and methods for specific binding and inhibition of RNAP from bacterial species.
摘要翻译：公开的抑制细菌RNA聚合酶的靶标和方法是从细菌物种特异性结合和抑制RNAP的靶标和方法。

9. 发明授权

US08114583B2 Switch-region: target and method for inhibition of bacterial RNA polymerase 失效
标题翻译：开关区：抑制细菌RNA聚合酶的靶标和方法
公开(公告)号：US08114583B2
公开(公告)日：2012-02-14
申请号：US12612787
申请日：2009-11-05
申请人： Richard H. Ebright
发明人： Richard H. Ebright
IPC分类号： C12Q1/00 , G01N33/53
CPC分类号： G01N33/566 , C07K2299/00 , C12N9/1247 , C12Q1/48 , G01N33/569 , G01N33/573 , G01N2333/9125 , G01N2500/00
摘要： A target and methods for specific binding and inhibition of RNA polymerase from bacterial species are provided, including methods for identifying agents that bind to a bacterial RNA polymerase, and that inhibit an activity of a bacterial RNA polymerase, through interactions with a bacterial RNA polymerase homologous switch-region amino-acid sequence. The methods can include preparation of a reaction solution comprising the compound to be tested and an entity containing a bacterial RNAP homologous switch-region amino-acid sequence, and detection of binding or inhibition. Applications in control of bacterial gene expression, control of bacterial viability, control of bacterial growth, antibacterial chemistry, and antibacterial therapy are also provided.
摘要翻译：提供了用于从细菌物种特异性结合和抑制RNA聚合酶的靶标和方法，包括用于鉴定结合细菌RNA聚合酶的试剂的方法，并通过与细菌RNA聚合酶同源的相互作用来抑制细菌RNA聚合酶的活性开关区氨基酸序列。所述方法可以包括制备包含待测化合物的反应溶液和含有细菌RNAP同源转换区氨基酸序列的实体以及结合或抑制的检测。还提供了控制细菌基因表达，细菌活力控制，细菌生长控制，抗菌化学和抗菌治疗的应用。

10. 发明授权

US09060970B2 Bridge-helix cap: target and method for inhibition of bacterial RNA polymerase 有权
标题翻译：桥 - 螺旋帽：抑制细菌RNA聚合酶的靶标和方法
公开(公告)号：US09060970B2
公开(公告)日：2015-06-23
申请号：US14006035
申请日：2012-03-19
申请人： Richard H. Ebright , David Degen , Katherine Y. Ebright
发明人： Richard H. Ebright , David Degen , Katherine Y. Ebright
IPC分类号： A61K45/06 , C12Q1/18 , A61K38/12 , C07D498/08 , A61K31/15 , A61K31/395 , A61K31/155 , G01N33/68
CPC分类号： A61K38/15 , A61K31/15 , A61K31/155 , A61K31/343 , A61K31/395 , A61K31/496 , A61K38/12 , A61K45/06 , C07D498/08 , C12Q1/18 , G01N33/68 , G01N2333/91275 , Y02A50/473 , A61K2300/00
摘要： It has been discovered that the Sal target represents a new and promising target for antibacterial drug discovery. The Sal target is distinct from the rifamycin target and from the CBR703 target. This indicates that antibacterial compounds that function through the Sal target should exhibit no, or minimal, cross-resistance with rifamycins and CBR703. This further implies that it should be possible to co-administer antibacterial compounds that function through the Sal target together with a rifamycin, together with CBR703, or together with both a rifamycin and CBR703, in order to achieve additive or synergistic antibacterial effects and in order to suppress or eliminate the emergence of resistance.
摘要翻译：已经发现，Sal靶标是抗菌药物发现的新的有希望的靶标。 Sal靶标与利福霉素靶标和CBR703靶标不同。这表明通过Sal靶标起作用的抗菌化合物应该与利福霉素和CBR703不表现出或最小的交叉抗性。这进一步意味着应该可以共同施用通过Sal靶与利培酮一起发挥作用的抗菌化合物与CBR703，或者与利福霉素和CBR703一起共同施用，以获得添加或协同的抗菌作用抑制或消除抵抗的出现。

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