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1. 发明申请

WO2006085978A3 CONJUGATES OF A CEPHALOSPORIN DERIVATIVE AND A FLUOROPHOR PRECURSOR AND RELATED COMPOUNDS AS SUBSTRATES FOR BETA-LACTAMASE GENE EXPRESSION 审中-公开
标题翻译： CEPHOROSPORIN衍生物和荧光素前体的相关化合物及相关化合物作为β-乳酸酶基因表达的基质
公开(公告)号：WO2006085978A3
公开(公告)日：2007-01-04
申请号：PCT/US2005023947
申请日：2005-06-30
申请人： UNIV CALIFORNIA , RAO JIANGHONG , TSIEN ROGER Y
发明人： RAO JIANGHONG , TSIEN ROGER Y
IPC分类号： C07D501/00 , C07D265/38 , C07D311/16 , C07D417/14 , C07D463/00 , C07D501/14 , C07D505/00 , C07F9/6561 , C12Q1/18 , C12Q1/37 , C12Q1/68
CPC分类号： C12Q1/6897 , C07D463/18 , C07D463/20 , C07D501/00 , C07D505/00 , C07F9/65613
摘要： Fluorescent substrates for beta-lactamases having the general formula shown above are provided. Z includes a fluorophore or chromophore and includes a group that may link to the lactam-containing group; R 1 and R 2 are independently selected from H, aliphatic, aromatic, alkyl, and acyl ; R 4 may be H and lower alkyl; B may be H, physiologically acceptable salts or metal, ester groups, ammonium cations, --CHR 5 OCO(CH 2 ) n CH 3 , --CHR 5 OCOC(CH 3 ) 3 , acylthiomethyl, acyloxy-alpha-benz, deltabutyrolactonyl, mehtoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, and dialkylaminocarbonyloxymethyl, in which R 5 is selected from the group consisting of H and lower alkyl; n is an interger between 0 and 10, inclusive; and A may be S, O, SO, SO 2 , or CH 2 . In embodiments, the beta-lactam ring may be cleaved by a beta-lactamase enzyme effective to free a fluorophore. Methods of assaying beta-lactamase activity and monitoring expression in systems using beta-lactamase as a reporter gene are also disclosed.
摘要翻译：提供了具有上述通式的β-内酰胺酶的荧光底物。 Z包括荧光团或发色团，并且包括可以连接到含内酰胺基团的基团; R 1和R 2独立地选自H，脂族，芳族，烷基和酰基; R 4可以是H和低级烷基; B可以是H，生理上可接受的盐或金属，酯基，铵阳离子，--CHR 5 OCO（CH 2）n CH （CH 3）3，酰基硫甲基，酰氧基-α-苯并三唑，丁内酰丁基，甲氧基羰基氧基甲基，苯基，甲基亚磺酰基甲基，β-吗啉代乙基，二烷基氨基乙基和二烷基氨基羰基氧基甲基，其中R 5选自H和低级烷基; n是0到10之间的整数，包括0和10; A可以是S，O，SO，SO 2，或CH 2。在实施方案中，β-内酰胺环可以被有效释放荧光团的β-内酰胺酶切割。还公开了使用β-内酰胺酶作为报道基因的系统中测定β-内酰胺酶活性和监测表达的方法。

2. 发明申请

WO02068678A2 BETA-LACTAMASE SUBSTRATES HAVING PHENOLIC ETHERS 审中-公开
标题翻译：具有酚醛树脂的BETA-LACTAMASE底物
公开(公告)号：WO02068678A2
公开(公告)日：2002-09-06
申请号：PCT/US0200769
申请日：2002-01-11
申请人： UNIV CALIFORNIA , TSIEN ROGER Y , RAO JIANGHONG
发明人： TSIEN ROGER Y , RAO JIANGHONG
IPC分类号： C07D463/00 , C07D501/00 , C07D501/14 , C07D501/24 , C07D501/28 , C07D501/30 , C07D501/34 , C07D501/36 , C07D501/40 , C07D501/42 , C07D501/46 , C07D505/00 , C07F9/6561 , C12Q1/18 , C12Q1/34 , C12Q1/37 , C12Q1/68 , C12Q
CPC分类号： C12Q1/6897 , C07D463/18 , C07D501/00 , C07D505/00 , C07F9/65613 , C12Q1/34
摘要： Provided are fluorescent substrates for β-lactamases having general formula (I), in which R is a benzyl, 2-thienylmethyl, or cyanomethyl group; R' is selected from the group consisting of H, physiologically acceptable salts or metal, ester groups, ammonium cations, --CHR2OCO(CH2)nCH3, --CHR2OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benzyl, deltabutyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, β-morpholinoethyl, dialkylaminoethyl, and dislkylaminocarbonyloxymethyl, in which R2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO2 and CH2; and Z is a donor fluorescent moiety. Also provided are methods of use of the compound of general formula (I).
摘要翻译：提供具有通式（I）的β-内酰胺酶的荧光底物，其中R是苄基，2-噻吩基甲基或氰基甲基; R'选自H，生理上可接受的盐或金属，酯基，铵阳离子，-CHR2OCO（CH2）nCH3，-CH2OCOC（CH3）3，酰基硫代甲基，酰氧基-α-苄基，脱乙酰丁酰基，甲氧羰基氧甲基，苯基，甲基亚磺酰基甲基，β-吗啉代乙基，二烷基氨基乙基和二烷基氨基羰氧基甲基，其中R2选自H和低级烷基; A选自S，O，SO，SO 2和CH 2; Z是供体荧光部分。还提供了通式（I）的化合物的使用方法。

3. 发明申请

WO2010033647A3 CYSTEINE LABELING SYSTEM AND METHOD OF USE THEREOF 审中-公开
标题翻译：半胱氨酸标签系统及其使用方法
公开(公告)号：WO2010033647A3
公开(公告)日：2010-06-03
申请号：PCT/US2009057224
申请日：2009-09-16
申请人： UNIV STANFORD , RAO JIANGHONG , REN HONGJUN
发明人： RAO JIANGHONG , REN HONGJUN
IPC分类号： C07D417/04 , A61K31/541 , C07D417/02
CPC分类号： C07D277/68 , A61K47/545 , A61K47/64
摘要： A method of use of a cysteine labeling system including: providing a 2-cyano benzothial core with a covalently-linked biomolecule X in a reaction environment; and reacting the 2-cyano benzothial core to an N-terminal cystenine.
摘要翻译：一种使用半胱氨酸标记系统的方法，包括：在反应环境中用共价连接的生物分子X提供2-氰基苯并噻唑核心; 并使2-氰基苯并噻唑核心与N-末端半胱氨酸反应。

4. 发明申请

WO2008049036A2 ENZYME DETECTION SYSTEM WITH CAGED SUBSTRATES 审中-公开
标题翻译：带有基底的酶检测系统
公开(公告)号：WO2008049036A2
公开(公告)日：2008-04-24
申请号：PCT/US2007081697
申请日：2007-10-17
申请人： ZYMERA INC , SOBEK DANIEL , RAO JIANGHONG
发明人： SOBEK DANIEL , RAO JIANGHONG
CPC分类号： C12Q1/34
摘要： An enzyme detection system (600) including forming a caged substrate (104); releasing an uncaged substrate (108) by cleaving a caging molecule (302) from the caged substrate (104); and emitting a light emission (118) from a Bioluminescence Resonance Energy Transfer luminescent nanocrystal conjugate (500) reacting with the uncaged substrate (108).
摘要翻译：一种酶检测系统（600），包括形成笼状基底（104）; 通过从笼形基底（104）切割笼状分子（302）来释放未起始的底物（108）; 以及从与所述未起始衬底（108）反应的生物发光共振能量转移发光纳米晶体共轭物（500）发射发光（118）。

5. 发明申请

WO2008049039A2 ASSAY SYSTEM FOR ADENOSINE TRIPHOSPHATE AND CREATINE KINASE 审中-公开
标题翻译：腺苷三磷酸和发酵激酶的测定系统
公开(公告)号：WO2008049039A2
公开(公告)日：2008-04-24
申请号：PCT/US2007081702
申请日：2007-10-17
申请人： ZYMERA INC , SOBEK DANIEL , RAO JIANGHONG
发明人： SOBEK DANIEL , RAO JIANGHONG
CPC分类号： G01N33/587 , G01N33/542 , G01N33/5735 , G01N2333/9123
摘要： An assay system (700) including providing a luminescent nanocrystal (500); combining a solution (606) having an adenosine triphosphate molecule (100); and displaying a light emission (418) by the luminescent nanocrystal (500) and the solution (606) combined.
摘要翻译：一种测定系统（700），包括提供发光纳米晶体（500）; 组合具有三磷酸腺苷分子（100）的溶液（606）; 以及通过所述发光纳米晶体（500）和所述溶液（606）显示出发光（418）。

6. 发明申请

WO2011152883A3 USE OF BACTERIAL BETA-LACTAMASE FOR IN VITRO DIAGNOSTICS AND IN VIVO IMAGING, DIAGNOSTICS AND THERAPEUTICS 审中-公开
标题翻译：用于体外诊断和体内成像，诊断和治疗的细菌β-乳糖酶的使用
公开(公告)号：WO2011152883A3
公开(公告)日：2012-03-29
申请号：PCT/US2011001018
申请日：2011-06-03
申请人： TEXAS A & M UNIV SYS , UNIV LELAND STANFORD JUNIOR , CIRILLO JEFFREY D , SACHETTINI JAMES C , RAO JIANGHONG , XIE HEXIN
发明人： CIRILLO JEFFREY D , SACHETTINI JAMES C , RAO JIANGHONG , XIE HEXIN
IPC分类号： C12Q1/34 , C12Q1/04 , C12R1/32 , G01N33/15 , G01N33/52
CPC分类号： A61K49/0013 , A61K49/0021 , A61K49/0028 , A61K49/0032 , A61K49/0041 , A61K49/0052 , C12Q1/04 , C12Q1/34 , G01N2333/986
摘要： Provided herein are methods for detecting, quantifying, differentiating, diagnosing and imaging pathogenic bacteria or condition associated therewith using substrates for bacterial enzymes. Fluorescent, luminescent or colorimetric signals emitted by substrates or enzyme products in the presence of the bacteria are compared to controls to detect and locate the pathogenic bacteria. Provided is a method for screening therapeutic agents to treat the pathophysiological conditions by measuring a signal emitted from the substrates or products in the presence and absence of the potential therapeutic agent and a diagnostic method for detecting a mycobacterial infection in a subject by contacting biological samples with a substrate and imaging for signals emitted from a mycobacterial beta-lactamase product. Also provided are fluorogenic substrates or substrates comprising a colored dye or a chemical reagent effective to induce a color or pH change.
摘要翻译：本文提供了用于细菌酶底物检测，定量，鉴别，诊断和成像病原菌或与其相关的病症的方法。在细菌存在下由底物或酶产物发射的荧光，发光或比色信号与对照相比较以检测和定位病原菌。本发明提供了一种用于筛选治疗剂以治疗病理生理状况的方法，该方法是通过在存在和不存在潜在治疗剂的情况下测量从底物或产物发出的信号，以及用于通过使生物样品与生物样品接触来检测受试者中的分枝杆菌感染的诊断方法底物和成像从分枝杆菌β-内酰胺酶产物发射的信号。还提供了含有色素或有效诱导颜色或pH变化的化学试剂的荧光底物或底物。

7. 发明申请

WO2010033738A3 ACTIVATABLE BIOLUMINESCENT PROBE SYSTEM AND METHOD OF USE THEREOF 审中-公开
标题翻译：可激活的生物发光探测系统及其使用方法
公开(公告)号：WO2010033738A3
公开(公告)日：2010-07-22
申请号：PCT/US2009057368
申请日：2009-09-17
申请人： UNIV STANFORD , RAO JIANGHONG , XIA ZUYONG
发明人： RAO JIANGHONG , XIA ZUYONG
IPC分类号： G01N33/52 , G01N33/68
CPC分类号： G01N33/542
摘要： A method of use of an activatable bioluminescent probe system includes: providing a bioluminescent protein and a quencher in a reaction environment; modifying a ligand between the quencher and the bioluminescent protein using a ligand interacting molecule; adding a bioluminescence initiating molecule to the reaction environment; and measuring light originating from the interaction between the bioluminescent protein and the bioluminescence initiating molecule.
摘要翻译：使用可激活的生物发光探针系统的方法包括：在反应环境中提供生物发光蛋白和猝灭剂; 使用配体相互作用分子修饰猝灭剂和生物发光蛋白质之间的配体; 在反应环境中加入生物发光引发分子; 并测量源自生物发光蛋白和生物发光起始分子之间相互作用的光。

8. 发明申请

WO2007081716A3 SELF-ILLUMINATING QUANTUM DOT SYSTEMS AND METHODS OF USE THEREOF 审中-公开
标题翻译：自我照明量子点系统及其使用方法
公开(公告)号：WO2007081716A3
公开(公告)日：2008-08-07
申请号：PCT/US2007000096
申请日：2007-01-04
申请人： UNIV STANFORD , RAO JIANGHONG , LOENING ANDREAS M , GAMBHIR SANJIV S , SO MIN-KYUNG , XU CHENJIE
发明人： RAO JIANGHONG , LOENING ANDREAS M , GAMBHIR SANJIV S , SO MIN-KYUNG , XU CHENJIE
IPC分类号： G01N37/00
CPC分类号： G01N33/543 , B82Y15/00 , G01N21/763 , G01N33/588
摘要： Generally, aspects of the present disclosure are directed to conjugate systems, self-illuminating quantum dot conjugates, methods of detecting a target in a host, methods of treating a disease in a host, and the like.
摘要翻译：通常，本公开的方面涉及共轭系统，自发光量子点缀合物，检测宿主中靶标的方法，治疗宿主中疾病的方法等。

9. 发明专利

AU2002251755B2 Beta-lactamase substrates having phenolic ethers 未知
公开(公告)号：AU2002251755B2
公开(公告)日：2007-10-25
申请号：AU2002251755
申请日：2002-01-11
申请人： UNIV CALIFORNIA
发明人： TSIEN ROGER Y , RAO JIANGHONG
IPC分类号： C07D501/24 , C07D463/00 , C07D501/00 , C07D501/14 , C07D501/28 , C07D501/30 , C07D501/34 , C07D501/36 , C07D501/40 , C07D501/42 , C07D501/46 , C07D505/00 , C07F9/6561 , C12Q1/18 , C12Q1/34 , C12Q1/37 , C12Q1/68 , C12Q1/6897
摘要： Provided are fluorescent substrates for beta-lactamases having the general formula I: in which R is a benzyl, 2-thienylmethyl, or cyanomethyl group; R' is selected from the group consisting of H, physiologically acceptable salts or metal, ester groups, ammonium cations, -CHR 2 OCO(CH 2 ) n CH 3 , -CHR 2 OCOC(CH 3 ) 3 , acylthiomethyl, acyloxy-alpha-benzyl, deltabutyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, and dialkylaminocarbonyloxymethyl, in which R 2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO 2 and CH 2 ; and Z is a donor fluorescent moiety. Also provided are methods of use of the compound of general formula I.

10. 发明公开

EP1385853A4 BETA-LACTAMASE SUBSTRATES HAVING PHENOLIC ETHERS 审中-公开
标题翻译：酚醛醚β-内酰胺酶SUBSTRATES
公开(公告)号：EP1385853A4
公开(公告)日：2005-02-16
申请号：EP02720779
申请日：2002-01-11
申请人： UNIV CALIFORNIA
发明人： TSIEN ROGER Y , RAO JIANGHONG
IPC分类号： C07D463/00 , C07D501/00 , C07D501/14 , C07D501/24 , C07D501/28 , C07D501/30 , C07D501/34 , C07D501/36 , C07D501/40 , C07D501/42 , C07D501/46 , C07D505/00 , C07F9/6561 , C12Q1/18 , C12Q1/34 , C12Q1/37 , C12Q1/68
CPC分类号： C12Q1/6897 , C07D463/18 , C07D501/00 , C07D505/00 , C07F9/65613 , C12Q1/34
摘要： Provided are fluorescent substrates for β-lactamases having general formula (I), in which R is a benzyl, 2-thienylmethyl, or cyanomethyl group; R' is selected from the group consisting of H, physiologically acceptable salts or metal, ester groups, ammonium cations, --CHR2OCO(CH2)nCH3, --CHR2OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benzyl, deltabutyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, β-morpholinoethyl, dialkylaminoethyl, and dislkylaminocarbonyloxymethyl, in which R2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO2 and CH2; and Z is a donor fluorescent moiety. Also provided are methods of use of the compound of general formula (I).

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