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1. 发明申请

WO2007089310A1 BIPARTITE INHIBITORS OF BACTERIAL RNA POLYMERASE 审中-公开
标题翻译：细菌RNA聚合酶的双重抑制剂
公开(公告)号：WO2007089310A1
公开(公告)日：2007-08-09
申请号：PCT/US2006/043152
申请日：2006-11-04
申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY , EBRIGHT, Richard, H. , WANG, Dongye
发明人： EBRIGHT, Richard, H. , WANG, Dongye
IPC分类号： C07D513/00 , C07D321/00 , A61K31/335
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：XaY，其中X是与细菌RNA聚合酶的Rif口结合的部分，Y是结合细菌RNA聚合酶的次级通道的部分，和是一个链接器。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。

2. 发明申请

WO2003107010A1 REAGENTS AND PROCEDURES FOR HIGH-SPECIFICITY LABELING 审中-公开
标题翻译：高特异性标签的试剂和程序
公开(公告)号：WO2003107010A1
公开(公告)日：2003-12-24
申请号：PCT/US2003/018792
申请日：2003-06-13
申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
发明人： EBRIGHT, Richard, H. , EBRIGHT, Yon, W.
IPC分类号： G01N33/68
CPC分类号： C07F9/78 , C07F9/706 , C07F9/806 , 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) Rl or R2, are each independently O-, S-, OR 3 or SR 3 with the provision that if either Rl or R2 is absent, the other remaining group is =0 or =S; or Rl 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)CH20H, or (CH2)y- 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)„ "SO3, wherein n" is 1 or 2.
摘要翻译：具有根据一般结构式（I）的两个侧链胂基部分的分子和互变异构体，酸和其盐，其中：（i）R 1或R 2各自独立地为O，S-，OR 3或SR 3，其中规定如果R1或R2不存在，另一个剩余的基团为= 0或= S; 或者R 1和R 2与砷原子一起形成根据通式（II），（III），（IV）或（V）之一的环，其中R 3是H，CH（OH）CH 2 OH，或（CH2）y-Y，其中q为1-4，Y为H，OH，NH2，SH，COOH，OAc，CONH2或CN，Z表示包含2-4个单键或双键碳原子的烃链可以进一步被氢，甲基，乙基，1-丙基，2-丙基，甲氧基，羟基，氨基，羧基，磺基，氧代，硫代，卤代（氟，氯，溴或氟）中的一个或多个取代，和（CH 2）“”SO 3，其中n“为1或2。

3. 发明申请

WO2019173507A1 ANTIBACTERIAL AGENTS : ARYLALKYLCARBOXAMIDO PHLOROGLUCINOLS 审中-公开
公开(公告)号：WO2019173507A1
公开(公告)日：2019-09-12
申请号：PCT/US2019/021004
申请日：2019-03-06
申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY , EBRIGHT, Richard, H. , EBRIGHT, Yon, W. , FREUNDLICH, Joel, S. , GALLARDO-MACIAS, Ricardo , LI, Shao-Gang
发明人： EBRIGHT, Richard, H. , EBRIGHT, Yon, W. , FREUNDLICH, Joel, S. , GALLARDO-MACIAS, Ricardo , LI, Shao-Gang
IPC分类号： C07D239/34 , C07C237/48 , C07D295/155 , C07D213/56 , C07D213/65 , A61K31/505 , A61K31/4409 , A61K31/5375 , A61K31/4406 , A61K31/4402 , A61K31/166 , A61P31/04 , A61P31/02
摘要： The invention provides compounds of formula (I) or (II) and tautomers and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula (I) or (II) or a tautomer or salt thereof, methods of making a compound of formula (I) or (II) or a tautomer or salt thereof, and methods of using a compound of formula (I) or (II) or a tautomer or salt thereof as, e.g., inhibitors of bacterial RNA polymerase or as antibacterial agents.

4. 发明申请

WO2008121154A2 NUCLEIC ACID SEQUENCES FOR BIOSYNTHESIS OF NON -MCCJ25-RELATED LARIAT PEPTIDES 审中-公开
标题翻译：用于生产非-MCCJ25相关大肠杆菌肽的核酸序列
公开(公告)号：WO2008121154A2
公开(公告)日：2008-10-09
申请号：PCT/US2007/079032
申请日：2007-09-20
申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY , EBRIGHT, Richard, H. , SEVERINOV, Konstantin
发明人： EBRIGHT, Richard, H. , SEVERINOV, Konstantin
IPC分类号： A61K38/16
CPC分类号： C07K14/36 , A61K38/00 , Y02A50/473
摘要： A nucleic acid sequence is provided, encoding at least one of a precursor of a lariat peptide, a processing factor of a lariat peptide, and an export factor of a lariat peptide, wherein the lariat peptide is a non-MccJ25 lariat peptide according to general structural formula (I) Also provided are biosynthesis systems useful for the synthesis of peptides according to formula (I), and methods of detecting and identifying nucleic acid sequences encoding the disclosed proteins.
摘要翻译：提供了一种核酸序列，其编码梭菌肽的前体，梭菌肽的加工因子和梭菌肽的出口因子中的至少一种，其中所述系列肽是根据一般的非MccJ25菌根肽结构式（I）还提供了可用于合成根据式（I）的肽的生物合成系统，以及检测和鉴定编码所公开的蛋白质的核酸序列的方法。

5. 发明申请

WO2007106472A2 NON-MCCJ25-RELATED LARIAT-PEPTIDE INHIBITORS OF BACTERIAL RNA POLYMERASE 审中-公开
标题翻译：非MCCJ25相关的细菌RNA聚合酶抑制剂
公开(公告)号：WO2007106472A2
公开(公告)日：2007-09-20
申请号：PCT/US2007/006282
申请日：2007-03-13
申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY , EBRIGHT, Richard, H. , MUKHOPADHYAY, Jayanta , SEVERINOV, Konstantin , SEMENOVA, Ekaterina
发明人： EBRIGHT, Richard, H. , MUKHOPADHYAY, Jayanta , SEVERINOV, Konstantin , SEMENOVA, Ekaterina
IPC分类号： C07K14/195 , C12N9/12 , C12Q1/18
CPC分类号： C12Q1/48 , C07K14/4703 , G01N2333/9125
摘要： The invention provides a method of inhibiting a bacterial RNA polymerase, using a compound according to general structural formula (I): wherein X is an amino acid residue containing a backbone nitrogen atom, Y is an amino acid residue containing a side-chain carboxyl group, α is a peptide segment of from about 5 to about 8 amino acid residues, β is a peptide segment of from about 6 to about 15 amino acid residues, there is an amide bond between the backbone nitrogen atom of X and the side-chain carboxyl of Y, and wherein the amino acid sequence of the compound has less than 25% identity with the amino acid sequence of microcin J25 (MccJ25). The method disclosed herein is useful for inhibition of Gram-negative bacterial RNA polymerase, Gram-positive bacterial RNA polymerase, and Thermus-Deinococcus RNA polymerase. The invention has applications in control of bacterial RNA polymerase activity, control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.
摘要翻译：本发明提供使用根据通式（I）的化合物抑制细菌RNA聚合酶的方法：其中X是含有主链氮原子的氨基酸残基，Y是含有侧链羧基的氨基酸残基 a是约5至约8个氨基酸残基的肽段，β是约6至约15个氨基酸残基的肽段，X的主链氮原子和侧链之间存在酰胺键 Y的羧基，并且其中该化合物的氨基酸序列与microcin J25（MccJ25）的氨基酸序列具有小于25％的同一性。本文公开的方法可用于抑制革兰氏阴性细菌RNA聚合酶，革兰氏阳性细菌RNA聚合酶和Thermus-Deinococcus RNA聚合酶。本发明可用于控制细菌RNA聚合酶活性，控制细菌基因表达，控制细菌生长，抗菌化学和抗菌治疗。

6. 发明申请

WO2012129173A1 BRIDGE-HELIX CAP: TARGET AND METHOD FOR INHIBITION OF BACTERIAL RNA POLYMERASE 审中-公开
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：WO2012129173A1
公开(公告)日：2012-09-27
申请号：PCT/US2012/029679
申请日：2012-03-19
申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY , EBRIGHT, Richard, H. , DEGEN, David , EBRIGHT, Katherine, Y.
发明人： EBRIGHT, Richard, H. , DEGEN, David , EBRIGHT, Katherine, Y.
IPC分类号： C12N9/99 , C12N9/12
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。

7. 发明申请

WO2012033846A1 ARYLPROPIONYL-TRIKETONE ANTIBACTERIAL AGENTS 审中-公开
标题翻译： ARYLPROPIONYL-TRIKETONE抗菌剂
公开(公告)号：WO2012033846A1
公开(公告)日：2012-03-15
申请号：PCT/US2011/050708
申请日：2011-09-07
申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY , EBRIGHT, Richard, H. , SHEN, Juan
发明人： EBRIGHT, Richard, H. , SHEN, Juan
IPC分类号： A61K31/12 , A61K31/045
CPC分类号： C07C49/723 , C07C49/747 , C07C49/753 , C07C2601/16
摘要： The invention provides a compound of formula (I): or a salt thereof, wherein R 1 -R 5 have any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as RNA polymerase inhibitors and antibacterial agents.
摘要翻译：本发明提供式（I）化合物或其盐，其中R 1 -R 5具有说明书中描述的任何值，以及包含式（I）化合物的组合物。该化合物可用作RNA聚合酶抑制剂和抗菌剂。

8. 发明申请

WO2005029075A1 BIS-TRANSITION-METAL-CHELATE PROBES 审中-公开
标题翻译：双相过渡金属探针探针
公开(公告)号：WO2005029075A1
公开(公告)日：2005-03-31
申请号：PCT/US2004/030449
申请日：2004-09-17
申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY , EBRIGHT, Richard, H. , EBRIGHT, Yon, W.
发明人： EBRIGHT, Richard, H. , EBRIGHT, Yon, W.
IPC分类号： G01N33/532
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) R' and R 1 ' are each independently CH(COO - ), CH(COOH), or absent; (c) R 2 and R 2 ' are linkers each having a length of from about 3.0 to about 20 A; 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（I）：其中：（a）Y和Y'各自为过渡金属，（b）R'和R'各自独立地为CH（COO - ），CH（ COOH），或不存在; （c）R 2和R 2'各自具有约3.0至约20A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。

9. 发明申请

WO2015120320A1 ANTIBACTERIAL AGENTS: N(ALPHA)-AROYL-N-ARYL-PHENYLALANINAMIDES 审中-公开
标题翻译：抗菌剂：N（ALPHA） - 氨基-N-芳基 - 苯丙氨酸
公开(公告)号：WO2015120320A1
公开(公告)日：2015-08-13
申请号：PCT/US2015/014899
申请日：2015-02-06
申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY , EBRIGHT, Richard, H. , EBRIGHT, Yon, W. , MANDAL, Soma , WILDE, Richard , LI, Shengjian
发明人： EBRIGHT, Richard, H. , EBRIGHT, Yon, W. , MANDAL, Soma , WILDE, Richard , LI, Shengjian
IPC分类号： A61K31/16 , A01N37/18 , A01N37/46 , A61P31/04
CPC分类号： C07C233/88 , A01N37/22 , A01N37/24 , A01N43/10 , A01N43/30 , A01N43/32 , A01N43/36 , A01N43/38 , A01N43/40 , A01N43/48 , A01N43/50 , A01N43/52 , A01N43/56 , A01N43/60 , A01N43/62 , A01N43/647 , A01N43/653 , A01N43/713 , A01N43/78 , A01N43/84 , A01N43/90 , A61K31/167 , A61K31/341 , A61K31/4402 , A61K31/4409 , C07C237/20 , C07C2602/08 , C07C2602/10 , C07D207/14 , C07D209/08 , C07D209/40 , C07D209/42 , C07D211/58 , C07D213/75 , C07D213/81 , C07D213/82 , C07D215/38 , C07D215/40 , C07D217/22 , C07D231/56 , C07D235/06 , C07D237/30 , C07D241/04 , C07D249/06 , C07D249/08 , C07D249/18 , C07D257/04 , C07D265/30 , C07D277/62 , C07D295/135 , C07D295/155 , C07D295/185 , C07D295/205 , C07D307/82 , C07D317/66 , C07D319/18 , C07D333/38 , C07D333/54 , C07D333/66 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04
摘要： The invention provides compounds having activity as bacterial RNA polymerase inhibitors and antibacterial agents, as well as compositions comprising the compounds and methods for their use. Specifically, phenylalanineamide and tyrosinamide compounds are disclosed that have inhibitory activity toward mycobacterium tuberculosis RNA polymerase. Use of these compounds in the treatment o prevention of M. tuberculosis infections in a mammal, is disclosed.
摘要翻译：本发明提供具有作为细菌RNA聚合酶抑制剂和抗菌剂的活性的化合物，以及包含这些化合物的组合物及其使用方法。具体地，公开了对结核分枝杆菌RNA聚合酶具有抑制活性的苯丙氨酸酰胺和酪氨酰胺化合物。公开了这些化合物在预防哺乳动物结核分枝杆菌感染的治疗中的用途。

10. 发明申请

WO2012033815A1 ARYLPROPIONYL-ALPHA-PYRONE ANTIBACTERIAL AGENTS 审中-公开
标题翻译：抗坏血酸抗坏血酸抗菌药物
公开(公告)号：WO2012033815A1
公开(公告)日：2012-03-15
申请号：PCT/US2011/050660
申请日：2011-09-07
申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY , EBRIGHT, Richard, H.
发明人： EBRIGHT, Richard, H.
IPC分类号： C07D309/38 , A61K31/351
CPC分类号： C07D309/38 , A61K31/351 , C07D309/36 , Y02A50/473
摘要： The invention provides a compound of formula (I): or a salt thereof, wherein R 1 -R 4 have any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as antibacterial agents.
摘要翻译：本发明提供式（I）化合物或其盐，其中R 1 -R 4具有说明书中所述的任何值，以及包含式（I）化合物的组合物。这些化合物可用作抗菌剂。

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