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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。
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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。
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公开(公告)号:US06919333B2
公开(公告)日:2005-07-19
申请号:US10665227
申请日:2003-09-17
申请人: Richard H. Ebright , Yon W. Ebright
发明人: Richard H. Ebright , Yon W. Ebright
IPC分类号: C12Q1/68 , G01N33/533 , A61K31/352 , A61K31/538 , C07D265/28 , C07D407/06 , C07F19/00
CPC分类号: G01N33/533 , C12Q1/6825 , C12Q2563/113
摘要: A molecule for labeling a target material is provided including two transition-metal chelates and a detectable group. The molecule has the general structural formula (I): wherein: (a) Y and Y′ are each a transition metal, (b) R1 and R1′ are each independently CH(COO−), CH(COOH), or absent; (c) R2 and R2′ are linkers each having a length of from about 3.0 to about 20 Å; and (d) X is a detectable group. The linkers may be linear or branched, may contain aromatic moieties, and may optionally be further substituted. Methods of using the molecules of the invention as probes in detecting and analyzing target materials as well as kits including the molecule of the invention are also provided.
摘要翻译: 提供了用于标记靶材料的分子,包括两个过渡金属螯合物和可检测的基团。 该分子具有通式结构式(I):其中:(a)Y和Y'各自为过渡金属,(b)R 1和R 1'为 各自独立地为CH(COO - ),CH(COOH)或不存在; (c)R 2和R 2'是各自具有约3.0至约20的长度的接头; 和(d)X是可检测的基团。 接头可以是直链或支链的,可以含有芳族部分,并且可以任选被进一步取代。 还提供了使用本发明分子作为检测和分析靶材料的探针以及包括本发明分子的试剂盒的方法。
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公开(公告)号:US20130237595A1
公开(公告)日:2013-09-12
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: C07D309/38 , 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。
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公开(公告)号:US07371745B2
公开(公告)日:2008-05-13
申请号:US10946786
申请日:2004-09-21
申请人: Richard H. Ebright , Yon W. Ebright
发明人: Richard H. Ebright , Yon W. Ebright
IPC分类号: A61K31/352 , A61K31/538 , C07D265/28 , C07D407/06
CPC分类号: G01N33/533 , C07D209/14 , C12Q1/6825 , C12Q2563/113
摘要: A molecule for labeling a target material is provided including two transition-metal chelates and a detectable group. The molecule has the general structural formula (I): wherein: (a) Y and Y′ are each a transition metal, (b) R1 and R1′ are each independently CH(COO−), CH(COOH), or absent; (c) R2 and R2′ are linkers each having a length of from about 3.0 to about 20 Å; and (d) X is a detectable group. The linkers may be linear or branched, may contain aromatic moieties, and may optionally be further substituted. Methods of using the molecules of the invention as probes in detecting and analyzing target materials as well as kits including the molecule of the invention are also provided.
摘要翻译: 提供了用于标记靶材料的分子,包括两个过渡金属螯合物和可检测的基团。 该分子具有通式结构式(I):其中:(a)Y和Y'各自为过渡金属,(b)R 1和R 1'为 各自独立地为CH(COO - ),CH(COOH)或不存在; (c)R 2和R 2'是各自具有约3.0至约20的长度的接头; 和(d)X是可检测的基团。 接头可以是直链或支链的,可以含有芳族部分,并且可以任选被进一步取代。 还提供了使用本发明的分子作为检测和分析靶材料的探针的方法以及包括本发明的分子的试剂盒。
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公开(公告)号:US07282373B2
公开(公告)日:2007-10-16
申请号:US11257292
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: C07K7/08 , C07K5/0821 , C07K5/0827 , C07K5/1013 , C07K7/06 , C07K14/001 , G01N33/542 , Y10S435/968 , Y10S436/80 , Y10S436/805
摘要: A self-assembled relay probe for detecting a target material is provided including: a first peptide tag bound to the target material; and a first fluorescent conjugate including a first fluorochrome and a first tag binding group; wherein the first fluorescent conjugate selectively associates with the first tag. The probe further includes a second peptide tag bound to the target material; and a second fluorescent conjugate including a second fluorochrome having a longer wavelength and distinct excitation and emission maxima from the first fluorochrome and a second tag binding group. Upon exposure to the target material, the first and second fluorescent conjugates independently associate with the first and second peptide tags, respectively, so as to be a distance apart represented by about 0.1 times R0 to about 2 times R0, such that upon excitation of the first fluorescent conjugate, fluorescence resonance energy transfer results in excitation of the second fluorescent conjugate, yielding detectable emission from the second fluorescent conjugate.
摘要翻译: 提供了一种用于检测靶材料的自组装继电器探针,包括:与目标材料结合的第一肽标签; 和包含第一荧光染料和第一标签结合基团的第一荧光缀合物; 其中所述第一荧光共轭物选择性地与所述第一标签相关联。 所述探针还包括与靶材料结合的第二肽标签; 以及包含第二荧光染料的第二荧光缀合物,其具有来自第一荧光染料和第二标签结合基团的具有较长波长和不同激发和发射最大值的第二荧光染料。 在暴露于目标材料时,第一和第二荧光共轭物分别独立地与第一和第二肽标签相关联,以便间隔距离表示为约0.1倍R 0至约2倍 使得在激发第一荧光共轭物时,荧光共振能量转移导致第二荧光偶联物的激发,产生来自第二荧光缀合物的可检测的发射。
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公开(公告)号:US07141655B2
公开(公告)日:2006-11-28
申请号:US10461224
申请日:2003-06-13
申请人: Richard H. Ebright , Yon W. Ebright
发明人: Richard H. Ebright , Yon W. Ebright
IPC分类号: C07K1/13 , G01N21/64 , C07D209/10 , C07D263/54 , C07D277/62
CPC分类号: C07F9/78 , C07F9/70 , C07F9/80 , G01N33/533 , G01N33/582 , Y10S436/80
摘要: A molecule with two pendant phenylarsine moieties according to the general structural Formula (I) and tautomers, acids, and salts thereof: wherein: (i) R1 or R2, are each independently O−, S−, OR3 or SR3 with the provision that if either R1 or R2 is absent, the other remaining group is ═O or ═S; or R1 and R2, together with the arsenic atom, form a ring according to one of the general structural Formulae (II), (III), (IV), or (V): wherein R3 is H, CH(OH)CH2OH, or (CH2)q—Y, with q being 1–4 and Y being H, OH, NH2, SH, COOH, OAc, CONH2 or CN, and Z represents a hydrocarbon chain comprising 2–4 singly or doubly bonded carbon atoms each of which may be further substituted with one or more of hydrogen, methyl, ethyl, 1-propyl, 2-propyl, methoxy, hydroxy, amino, carboxy, sulfo, oxo, thio, halo (fluoro, chloro, bromo, or fluoro) and (CH2)n″SO3, wherein n″ is 1 or 2; (ii) R4, R5, R6 and R7 are each independently H, F, OR3, R3, OAc, NH2, N(C1–C4 alkyl)2, R1; or R4 with R5, or R6 together with R7, or both, form a ring; (iii) R8 is a linear or branched optionally substituted spacer having a minimum length of approximately 1.5 and a maximum length of approximately 15 Ångstroms; and (iv) X is a detectable group. Methods of using the bis-phenylarsine molecule also are provided.
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