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1. 发明申请

WO2021226330A1 AGENTS TO PREVENT TISSUE DAMAGE FROM CLOSTRIDIUM DIFFICILE INFECTIONS BY INHIBITION OF THE GUT-DAMAGING BACTERIAL TOXINS TCDA AND TCDB 审中-公开
公开(公告)号：WO2021226330A1
公开(公告)日：2021-11-11
申请号：PCT/US2021/031072
申请日：2021-05-06
申请人： ALBERT EINSTEIN COLLEGE OF MEDICINE , VICTORIA LINK LIMITED
发明人： SCHRAMM, Vern, L. , PAPARELLA, Ashleigh, S. , TYLER, Peter, Charles
IPC分类号： A61K31/4164 , A61K31/4709 , A61K31/65
摘要： Methods for treating or preventing diseases and conditions associated with Clostridium difficile infection are provided. The methods effectively inhibit bacterial pathogens induced UDP-glucose hydrolysis activity with minimized damage to host tissue.

2. 发明申请

WO2012074912A1 METHODS, ASSAYS AND COMPOUNDS FOR TREATING BACTERIAL INFECTIONS BY INHIBITING METHYLTHIOINOSINE PHOSPHORYLASE 审中-公开
标题翻译：通过抑制甲硫氨酸磷酸酶处理细菌感染的方法，测定和化合物
公开(公告)号：WO2012074912A1
公开(公告)日：2012-06-07
申请号：PCT/US2011/062208
申请日：2011-11-28
申请人： ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , INDUSTRIAL RESEARCH LIMITED , SCHRAMM, Vern, L. , CLINCH, Keith , TYLER, Peter, Charles , EVANS, Gary, Brian , FURNEAUX, Richard, Hubert
发明人： SCHRAMM, Vern, L. , CLINCH, Keith , TYLER, Peter, Charles , EVANS, Gary, Brian , FURNEAUX, Richard, Hubert
IPC分类号： A61K31/7076 , A61K31/41
CPC分类号： C07D487/04 , A61K31/00 , A61K31/519 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7076 , A61K31/708 , A61K45/06 , C12Q1/48
摘要： The present invention discloses methods for treating bacterial infections in a subject comprising administering to the subject a sub-growth inhibiting amount of a 5'- methylthioinosine phosphorylase (MTIP) inhibitor, as well as assays for identifying such inhibitors, and compounds and pharmaceutical compositions comprising the inhibitors.
摘要翻译：本发明公开了用于治疗受试者细菌感染的方法，包括向受试者施用次生抑制量的5'-甲硫基肌苷磷酸化酶（MTIP）抑制剂，以及用于鉴定这些抑制剂的测定法，以及包含抑制剂。

3. 发明申请

WO2005026131A1 TRANSITION STATE STRUCTURE AND INHIBITORS OF THYMIDINE PHOSPHORYLASES 审中-公开
标题翻译：过氧化物磷酸转移态结构和抑制剂
公开(公告)号：WO2005026131A1
公开(公告)日：2005-03-24
申请号：PCT/US2004/028703
申请日：2004-09-03
申请人： ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , INDUSTRIAL RESEARCH LIMITED , SCHRAMM, Vern, L. , BIRCK, Matthew, R. , TYLER, Peter, C. , FURNEAUX, Richard, H. , EVANS, Gary, B.
发明人： SCHRAMM, Vern, L. , BIRCK, Matthew, R. , TYLER, Peter, C. , FURNEAUX, Richard, H. , EVANS, Gary, B.
IPC分类号： C07D239/52
CPC分类号： C07D277/56 , A61K31/427 , A61K31/506 , C07D401/06 , C07D403/06 , C07D417/04 , C07D417/06 , C07F9/65122 , C07F9/6536 , C07F9/65586 , C12Q1/48 , G01N2333/91142
摘要： The transition state structure of thymidine phosphorylase is provided as a blueprint for design of transition state inhibitors. Several thymidine phosphorylase inhibitors that resemble the charge and geometry of the thymidine phosphorylase transition state are provided. Also provided are methods of inhibiting a thymidine phosphorylase, methods of treating cancer, and methods of inhibiting angiogenesis which utilize the thymidine phosphorylase transition state inhibitors.
摘要翻译：提供胸苷磷酸化酶的过渡态结构作为设计过渡状态抑制剂的蓝图。提供了类似于胸苷磷酸化酶转变状态的电荷和几何形状的几种胸苷磷酸化酶抑制剂。还提供了抑制胸苷磷酸化酶的方法，治疗癌症的方法，以及利用胸苷磷酸化酶过渡状态抑制剂抑制血管发生的方法。

4. 发明申请

WO2002059084A3 INHIBITORS OF ADP-RIBOSYL TRANSFERASES, CYCLASES, AND HYDROLASES, AND USES THEREOF 审中-公开
公开(公告)号：WO2002059084A3
公开(公告)日：2002-08-01
申请号：PCT/US2002/000371
申请日：2002-01-04
申请人： ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY
发明人： SAUVÉ, Anthony, A. , SCHRAMM, Vern, L.
IPC分类号： A01N43/04
摘要： The present invention provides pharmaceutical compositions for inhibiting and treating diseases associated with ADP-ribosyl transferase, ADP-ribosyl cyclase, or ADP-ribosyl hydrolase.

5. 发明申请

WO2017106259A1 NUCLEAR RECEPTOR SET DOMAIN CONTAINING PROTEIN 2 TRANSITION STATE AND USES THEREOF 审中-公开
标题翻译：核受体组含有蛋白2转换状态的域及其用途
公开(公告)号：WO2017106259A1
公开(公告)日：2017-06-22
申请号：PCT/US2016/066514
申请日：2016-12-14
申请人： ALBERT EINSTEIN COLLEGE OF MEDICINE, INC.
发明人： SCHRAMM, Vern, L. , POULIN, Myles, B.
IPC分类号： G06F19/12 , G06F17/30 , G06F19/24 , G01N33/574
CPC分类号： G06F19/16 , A61K38/00 , G01N2500/00
摘要： Methods and systems for obtaining inhibitors of Nuclear receptor SET Domain containing protein 2 (NSD2) are disclosed where the methods involve designing compounds that resemble the NSD2 transition state.
摘要翻译：公开了用于获得含有核受体SET结构域的蛋白质2（NSD2）抑制剂的方法和系统，其中所述方法涉及设计类似于NSD2过渡态的化合物。

6. 发明申请

WO2013126370A1 HIV-1 PROTEASE TRANSITION STATE AND USES THEREOF 审中-公开
标题翻译： HIV-1蛋白过渡状态及其用途
公开(公告)号：WO2013126370A1
公开(公告)日：2013-08-29
申请号：PCT/US2013/026802
申请日：2013-02-20
申请人： ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY
发明人： SCHRAMM, Vern, L. , KIPP, David, Randal , HIRSCHI, Jennifer, S.
IPC分类号： A01N43/36
CPC分类号： A61K31/40 , G01N33/56983
摘要： Methods and systems for obtaining inhibitors of human immunodeficiency virus- 1 (HIV-1) protease are disclosed where the methods involve designing compounds that resemble the HIV-1 protease transition state.
摘要翻译：公开了获得人免疫缺陷病毒-1（HIV-1）蛋白酶抑制剂的方法和系统，其中所述方法涉及设计类似于HIV-1蛋白酶转变状态的化合物。

7. 发明申请

WO2010053498A2 METHODS FOR DETECTING RICIN AND RELATED COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：检测赖氨酸及相关化合物的方法和用途
公开(公告)号：WO2010053498A2
公开(公告)日：2010-05-14
申请号：PCT/US2009/004075
申请日：2009-07-14
申请人： ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , SCHRAMM, Vern, L.
发明人： SCHRAMM, Vern, L.
IPC分类号： C12Q1/68
CPC分类号： C12Q1/48
摘要： The present invention is directed to methods for detecting the presence of ricin and compounds that catalyze the release of adenine from nucleic acids or other biological materials and for screening for inhibitors of such compounds.
摘要翻译：本发明涉及用于检测蓖麻毒素和催化从核酸或其他生物材料中释放腺嘌呤并筛选这些化合物的抑制剂的化合物的存在的方法。

8. 发明申请

WO2013112358A1 LUCIFERASE-LINKED METHODS FOR DETECTING ADENOSINE AND USES THEREOF 审中-公开
标题翻译：用于检测腺苷的连接途径的方法及其用途
公开(公告)号：WO2013112358A1
公开(公告)日：2013-08-01
申请号：PCT/US2013/022015
申请日：2013-01-18
申请人： ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY
发明人： BURGOS, Emmanuel, S. , SCHRAMM, Vern, L.
IPC分类号： C12Q1/66
CPC分类号： G01N33/582
摘要： Luciferase-linked methods for detecting adenosine and for screening for inhibitors of enzymes that produce adenosine are disclosed. The invention also provides methods for detecting the presence of Sadenosyl-L-homocysteine hydrolase (SAHH) comprising: (a) hydrolysis of S-adenosyl-Lhomocysteine (SAH) catalyzed by S-adenosyl-L-homocysteine hydrolase (SAHH) to adenosine and L-homocysteine; (b) converting adenosine to adenosine monophosphate (AMP) by adenosine kinase in the presence of a phosphate donor; (c) converting AMP to adenosine 5 '-triphosphate (ATP) by pyruvate phosphate dikinase (PPDK) in the presence of phosphoenolpyruvate (PEP) and inorganic pyrophosphate; and (d) reacting A TP with luciferin and Oz in the presence of luciferase to produce AMP and a luminescent signal, wherein the luminescent signal indicates the presence of S-adenosyl-L-homocysteine hydrolase (SAHH).
摘要翻译：公开了用于检测腺苷和筛选产生腺苷的酶抑制剂的荧光素酶连接方法。本发明还提供了用于检测Sadenosyl-L-同型半胱氨酸水解酶（SAHH）的存在的方法，其包括：（a）将S-腺苷-L-高半胱氨酸水解酶（SAHH）催化的S-腺苷 - 高半胱氨酸（SAH）水解成腺苷和 L-高半胱氨酸; （b）在磷酸盐供体存在下，通过腺苷激酶将腺苷转化为腺苷一磷酸（AMP）; （c）在磷酸烯醇丙酮酸（PEP）和无机焦磷酸盐存在下，通过丙酮酸磷酸二激酶（PPDK）将AMP转化为5'-三磷酸腺苷（ATP）; 和（d）在荧光素酶存在下使TP与荧光素和Oz反应以产生AMP和发光信号，其中发光信号表示S-腺苷-L-高半胱氨酸水解酶（SAHH）的存在。

9. 发明申请

WO2011112245A1 LUCIFERASE-LINKED ANALYSIS OF DNA-METHYLTRANSFERASE, PROTEIN METHYLTRANSFERASE AND S-ADENOSYLHOMOCYSTEIENE AND USES THEREOF 审中-公开
标题翻译： DNA甲基转移酶，蛋白质甲基转移酶和S-腺嘌呤核糖核酸的连锁分析及其用途
公开(公告)号：WO2011112245A1
公开(公告)日：2011-09-15
申请号：PCT/US2011/000430
申请日：2011-03-08
申请人： ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , SCHRAMM, Vern, L. , HEMEON, Ivan
发明人： SCHRAMM, Vern, L. , HEMEON, Ivan
IPC分类号： C12Q1/00
CPC分类号： C12Q1/48 , G01N2333/91011 , G01N2500/04
摘要： The present invention relates to methods for detecting the activity of DNA (cytosine 5)-methyltransferase, protein methyltransferase or any enzyme that forms S-adenosyl-l- homocysteine (AdoHcy) as a product, and for screening for inhibitors of DNA (cytosine 5)- methyltransferase, protein methyltransferase and any enzyme that forms S-adenosyl-l- homocysteine (AdoHcy) as a product using luciferase-linked assays that convert the S- adenosyl-l-homocysteine (AdoHcy) product to a quantifiable luminescent signal.
摘要翻译：本发明涉及用于检测DNA（胞嘧啶5） - 甲基转移酶，蛋白质甲基转移酶或形成S-腺苷-1-同型半胱氨酸（AdoHcy）作为产物的任何酶的活性的方法，并用于筛选DNA抑制剂（胞嘧啶5 ） - 甲基转移酶，蛋白质甲基转移酶和任何形成S-腺苷-1-同型半胱氨酸（AdoHcy）的酶，使用荧光素酶连接的测定法将S-腺苷-1-高半胱氨酸（AdoHcy）产物转化为可定量的发光信号。

10. 发明申请

WO2008105796A2 COMPOUNDS AND METHODS FOR DETECTING RICIN AND USES THEREOF 审中-公开
标题翻译：用于检测RICIN及其用途的化合物和方法
公开(公告)号：WO2008105796A2
公开(公告)日：2008-09-04
申请号：PCT/US2007/015145
申请日：2007-06-28
申请人： ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , SCHRAMM, Vern, L. , RODAY, Setu
发明人： SCHRAMM, Vern, L. , RODAY, Setu
IPC分类号： B32B27/38
CPC分类号： G01N33/582 , C12Q1/34 , G01N33/533
摘要： This application provides fluorescent probes, substrates, kits and methods for detecting the presence or absence of an enzyme, such as ricin, that catalyzes the release of adenine from a GAGA RNA tetraloop.
摘要翻译：本申请提供荧光探针，底物，试剂盒和方法，用于检测催化从GAGA RNA四环素中释放腺嘌呤的酶（例如蓖麻毒蛋白）的存在或不存在。

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