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1. 发明申请

WO2007016291A3 TRANSITION STATE STRUCTURE OF 5'-METHYLTHIOADENOSINE/S-ADENOSYLHOMOCYSTEINE NUCLEOSIDASES 审中-公开
标题翻译： 5'-甲基二氢OS嗪/ S-腺苷二羟基胞嘧啶核苷酸过渡态结构
公开(公告)号：WO2007016291A3
公开(公告)日：2007-10-25
申请号：PCT/US2006029289
申请日：2006-07-26
申请人： EINSTEIN COLL MED , SCHRAMM VERN L
发明人： SCHRAMM VERN L
IPC分类号： C12N5/06 , C12N5/16 , C12N9/00
CPC分类号： C12Q1/6813
摘要： Provided are methods of designing a putative inhibitor of a 5'-methylthioadenosine/S-adenosylhomocysteine nucleosidase. The methods comprise designing a chemically stable compound that resembles the charge and geometry of the 5'-methylthioadenosine/S-adenosylhomocysteine nucleosidase transition state. Also provided are methods of inhibiting 5'-methylthioadenosine/S-adenosylhomocysteine nucleosidases using the inhibitors found by the above methods.
摘要翻译：提供设计5'-甲硫基腺苷/ S-腺苷高半胱氨酸核苷酶的推定抑制剂的方法。所述方法包括设计类似于5'-甲硫基腺苷/ S-腺苷高半胱氨酸核苷酶过渡态的电荷和几何形状的化学稳定的化合物。还提供了使用上述方法发现的抑制剂抑制5'-甲基硫代腺苷/ S-腺苷高半胱氨酸核苷酸酶的方法。

2. 发明申请

WO2010033236A2 METHODS AND COMPOSITIONS FOR TREATING BACTERIAL INFECTIONS BY INHIBITING QUORUM SENSING 审中-公开
标题翻译：通过抑制感测治疗细菌感染的方法和组合
公开(公告)号：WO2010033236A2
公开(公告)日：2010-03-25
申请号：PCT/US2009005229
申请日：2009-09-18
申请人： EINSTEIN COLL MED , SCHRAMM VERN L
发明人： SCHRAMM VERN L
IPC分类号： A61K31/519
CPC分类号： A61K31/00 , A61K31/519
摘要： The present invention provides methods for treating bacterial infections in a subject comprising administering to the subject a sub-growth inhibiting amount of a 5'-Methylthioadenosine/S-adenosyl homocysteine nucleosidase (MTAN) inhibitor. The present invention further provides pharmaceutical compositions comprising a sub-bacterial-growth inhibiting amount of a 5'-Methylthioadenosine/S-adenosyl homocysteine nucleosidase (MTAN) inhibitor and a pharmaceutically acceptable carrier.
摘要翻译：本发明提供了治疗受试者细菌感染的方法，其包括向受试者施用次生长抑制量的5'-甲硫基腺苷/ S-腺苷高半胱氨酸核苷酶（MTAN）抑制剂。本发明还提供包含亚细菌生长抑制量的5'-甲硫基腺苷/ S-腺苷高半胱氨酸核苷酶（MTAN）抑制剂和药学上可接受的载体的药物组合物。

3. 发明申请

WO2008030119A9 ACYCLIC AMINE INHIBITORS OF NUCLEOSIDE PHOSPHORYLASES AND HYDROLASES 审中-公开
标题翻译：核苷酸磷酸盐和水解物的酰胺类抑制剂
公开(公告)号：WO2008030119A9
公开(公告)日：2009-09-24
申请号：PCT/NZ2007000261
申请日：2007-09-07
申请人： IND RES LTD , EINSTEIN COLL MED , CLINCH KEITH , EVANS GARY BRIAN , FURNEAUX RICHARD HUBERT , KELLY PETER MICHAEL , SCHRAMM VERN L , TYLER PETER CHARLES , WOOLHOUSE ANTHONY DAVID , GULAB SHIVALI ASHWIN
发明人： CLINCH KEITH , EVANS GARY BRIAN , FURNEAUX RICHARD HUBERT , KELLY PETER MICHAEL , SCHRAMM VERN L , TYLER PETER CHARLES , WOOLHOUSE ANTHONY DAVID , GULAB SHIVALI ASHWIN
IPC分类号： C07D487/04 , A61K31/519 , A61P17/06 , A61P31/04 , A61P33/02 , A61P35/00 , A61P37/06
CPC分类号： C07D487/04
摘要： The invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNPs) and/or nucleoside hydrolases (NHs). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds.
摘要翻译：本发明涉及作为嘌呤核苷磷酸化酶（PNP）和/或核苷水解酶（NHs）的抑制剂的通式（I）的化合物。本发明还涉及这些化合物在治疗包括癌症，细菌感染，原生动物感染和T细胞介导的疾病的疾病和感染中的用途以及含有该化合物的药物组合物。

4. 发明申请

WO2008105796A3 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：WO2008105796A3
公开(公告)日：2009-02-12
申请号：PCT/US2007015145
申请日：2007-06-28
申请人： EINSTEIN COLL MED , SCHRAMM VERN L , RODAY SETU
发明人： SCHRAMM VERN L , RODAY SETU
IPC分类号： C12Q1/68 , C12Q1/34
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。

5. 发明申请

WO2010053498A3 METHODS FOR DETECTING RICIN AND RELATED COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：检测蓖麻毒素及相关化合物的方法及其用途
公开(公告)号：WO2010053498A3
公开(公告)日：2010-07-08
申请号：PCT/US2009004075
申请日：2009-07-14
申请人： EINSTEIN COLL MED , SCHRAMM VERN L
发明人： SCHRAMM VERN L
IPC分类号： C12Q1/48 , C12Q1/66
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化合物的存在的方法，所述蓖麻毒素和化合物催化从核酸或其他生物材料释放腺嘌呤并筛选这些化合物的抑制剂。

6. 发明申请

WO2005023203A3 TRANSITION STATE ANALOG INHIBITORS OF RICIN A-CHAIN 审中-公开
标题翻译： RICIN A链的过渡状态模拟抑制剂
公开(公告)号：WO2005023203A3
公开(公告)日：2007-08-30
申请号：PCT/US2004029491
申请日：2004-09-09
申请人： EINSTEIN COLL MED , IND RES LTD , SCHRAMM VERN L , FURNEAUX RICHARD H , TYLER PETER C , EVANS GARY B
发明人： SCHRAMM VERN L , FURNEAUX RICHARD H , TYLER PETER C , EVANS GARY B
IPC分类号： C07H21/04 , A61K20060101 , C07H19/00 , C12Q1/68
CPC分类号： C12N15/11 , C12N2310/13 , C12N2310/323 , C12N2310/333 , C12N2310/53
摘要： Improved transition state analog inhibitors of ricin toxin-A are provided. Methods of using those inhibitors to inhibit ricin toxin-A and to prevent the toxic effects of ricin toxin-A in a mammal are also provided.
摘要翻译：提供了改进的蓖麻毒素-A的过渡态类似物抑制剂。还提供了使用这些抑制剂抑制蓖麻毒素-A并防止蓖麻毒素-A在哺乳动物中的毒性作用的方法。

7. 发明申请

WO0061783A3 PROCESS FOR PREPARING INHIBITORS OF NUCLEOSIDE METABOLISM 审中-公开
标题翻译：制备核苷酸代谢抑制剂的方法
公开(公告)号：WO0061783A3
公开(公告)日：2001-02-08
申请号：PCT/NZ0000048
申请日：2000-04-07
申请人： IND RES LTD , EINSTEIN COLL MED , FURNEAUX RICHARD HUBERT , TYLER PETER CHARLES , SCHRAMM VERN L
发明人： FURNEAUX RICHARD HUBERT , TYLER PETER CHARLES , SCHRAMM VERN L
IPC分类号： A61K31/519 , A61P31/00 , A61P43/00 , C07D207/34 , C07D207/40 , C07D207/416 , C07D487/04 , C07D491/056 , C07F7/18 , C07H19/14
CPC分类号： C07D207/416 , C07D487/04 , C07H19/14 , Y02P20/55
摘要： A process of preparing a compound of formula (I), wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H, halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and Z is selected from OH, hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof, which comprises reacting a compound of formula (II) with an anion produced by abstraction of the bromine or iodine atom from a compound of formula (XIX), to form a compound of formula (XX). The compound of formula (XX) is N- and O-deprotected to obtain the compound of formula (I).
摘要翻译：制备式（I）化合物的方法，其中B选自OH，NH 2，NHR，H或卤素; D选自OH，NH 2，NHR，H，卤素或SCH 3; R是任选取代的烷基，芳烷基或芳基; Z选自OH，氢，卤素，羟基，SQ或OQ，Q是任选取代的烷基，芳烷基或芳基; 或其互变异构体; 或其药学上可接受的盐; 或其酯; 其包括使式（II）的化合物与通过从式（XIX）的化合物中提取溴或碘原子产生的阴离子反应形成式（XX）的化合物。式（XX）的化合物是N-和O-去保护的，得到式（I）的化合物。

8. 发明申请

WO03045907A2 SIR2 PRODUCTS AND ACTIVITIES 审中-公开
标题翻译： SIR2产品和活动
公开(公告)号：WO03045907A2
公开(公告)日：2003-06-05
申请号：PCT/US0237364
申请日：2002-11-21
申请人： EINSTEIN COLL MED
发明人： SCHRAMM VERN L , BOEKE JEF D , SUAVE ANTHONY , CELIC IVANA
IPC分类号： C12Q1/48 , A61P35/00 , C07H19/04 , C07H19/20 , C07H19/207 , C12N9/10 , C12N9/99 , C12P19/32 , C12P21/02 , C07D
CPC分类号： C12N9/1077 , C07H19/04 , C07H19/20 , C12N9/99 , C12P19/32
摘要： A novel compound, 2'/3'-O-acetyl-ADP-ribose, is provided. The compound is a mixture of the 2' and 3' regioisomers of 0-acetyl-ADP ribose, and is formed nonenzymatically from 2'-O-acetyl-ADP-ribose, which is the newly discovered product of the reaction of Sir2 enzymes with acetylated peptides and NAD . Analogs of 2'/3'-O-acetyl-ADP-ribose are also provided. Additionally, methods of preparing 2'/3'-O-acetyl-ADP-ribose, methods of determining whether a test compound is an inhibitor of a Sir2 enzyme, methods of detecting Sir2 activity in a composition, methods of deacetylating an acetylated peptide, and methods of inhibiting the deacetylation of an acetylated peptide are provided. Prodrugs of 2'/3'-O-acetyl-ADP-ribose are also provided.
摘要翻译：提供了一种新化合物，2'/ 3'-O-乙酰-ADP-核糖。该化合物是O-乙酰基-ADP核糖的2'和3'区域异构体的混合物，并且是由2'-O-乙酰基-ADP-核糖非酶形成的，它是Sir2酶与新发现的Sir2酶反应产物乙酰化肽和NAD +。还提供了2'/ 3'-O-乙酰-ADP-核糖的类似物。另外，制备2'/ 3'-O-乙酰-ADP-核糖的方法，确定测试化合物是否是Sir2酶抑制剂的方法，检测组合物中Sir2活性的方法，乙酰化肽脱乙酰化的方法，和抑制乙酰化肽的脱乙酰化的方法。还提供了2'/ 3'-O-乙酰-ADP-核糖的前体药物。

9. 发明申请

WO02059084A2 INHIBITORS OF ADP-RIBOSYL TRANSFERASES, CYCLASES, AND HYDROLASES, AND USES THEREOF 审中-公开
标题翻译： ADP-RIBOSYL转移，CYCLASES和HYDROLASES的抑制剂及其用途
公开(公告)号：WO02059084A2
公开(公告)日：2002-08-01
申请号：PCT/US0200371
申请日：2002-01-04
申请人： EINSTEIN COLL MED
发明人： SAUVE ANTHONY A , SCHRAMM VERN L
IPC分类号： C07D307/20 , C07D405/04 , C07H19/04 , C07H19/10 , C07H19/20 , C07D
CPC分类号： C07D405/04 , C07D307/20 , C07H19/04 , C07H19/10 , C07H19/20
摘要： The present invention provides compounds having formula (A) wherein A is chosen from a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group; both B and C are hydrogen, or either B or C is a halogen, amino, or thiol group and the other of B or C is hydrogen; and D is a primary alcohol, a hydrogen, or an oxygen, nitrogen, carbon, or sulfur linked to phosphate, a phosphoryl group, a pyrophosphoryl group, or adenosine monophosphate through a phosphodiester or carbon-, nitrogen-, or sulfur- substituted phosphodiester bridge, or to adenosine diphosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substitutes pyrophosphodiester bridge. The present invention also provides pharmaceutical compositions containing the above compounds, methods of using the above compounds as pharmaceuticals, and processes for preparing the above compounds. Also provided are methods for inhibiting an ADP-ribosyl transferase, ADP-ribosyl cyclase, or ADP-ribosyl hydrolase enzyme, and methods for treating a disease or condition associated with an ADP-ribosyl transferase, ADP-ribosyl cyclase, or ADP-ribosyl hydrolase enzyme in a subject in need of treatment thereof.
摘要翻译：本发明提供具有式（A）的化合物，其中A选自氮，氧或硫连接的芳基，烷基，环状或杂环基; B和C都是氢，或者B或C是卤素，氨基或硫醇基，B或C中的另一个是氢; 并且D是通过磷酸二酯或碳，氮或硫取代的磷酸二酯与磷酸酯，磷酰基，焦磷酰基或单一磷酸腺苷连接的伯醇，氢或氧，氮，碳或硫。桥接或通过磷酸二酯或碳 - ，氮或硫取代的焦磷酸二酯桥接二磷酸腺苷。本发明还提供含有上述化合物的药物组合物，使用上述化合物作为药物的方法，以及制备上述化合物的方法。还提供了抑制ADP-核糖基转移酶，ADP-核糖基环化酶或ADP-核糖基水解酶的方法，以及用于治疗与ADP-核糖基转移酶，ADP-核糖基环化酶或ADP-核糖基水解酶相关的疾病或病症的方法酶在需要治疗的受试者中。

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