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1. 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。

2. 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。

3. 发明申请

WO2008079028A1 AZETIDINE ANALOGUES OF NUCLEOSIDASE AND PHOSPHORYLASE INHIBITORS 审中-公开
标题翻译：核苷酸酶和磷酸酶抑制剂的AZETIDINE ANALOGUES
公开(公告)号：WO2008079028A1
公开(公告)日：2008-07-03
申请号：PCT/NZ2007/000387
申请日：2007-12-21
申请人： INDUSTRIAL RESEARCH LIMITED , ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , EVANS, Gary Brian , FURNEAUX, Richard Hubert , GREATREX, Ben William , SCHRAMM, Vern L. , TYLER, Peter Charles
发明人： EVANS, Gary Brian , FURNEAUX, Richard Hubert , GREATREX, Ben William , SCHRAMM, Vern L. , TYLER, Peter Charles
IPC分类号： C07D403/14 , C07D401/02 , C07D401/04 , C07D401/06 , C07D405/14
CPC分类号： C07D471/04
摘要： Azetidine analogues of nucleosidase and nucleoside phosphorylase inhibitors having the general formula (I), the use of these compounds as pharmaceuticals, pharmaceutical compositions containing the compounds, methods of treating certain diseases using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds wherein W and X are each independently selected from hydrogen, CH 2 OH, CH 2 OQ and CH 2 SQ; Y and Z are each independently selected from hydrogen, halogen, CH 2 OH, CH 2 OQ, CH 2 SQ, SQ, OQ and Q; Q is an alkyl, aralkyl or aryl group each of which may be optionally substituted with one or more substituents selected from hydroxy, halogen, methoxy, amino, or carboxy; R 1 is a radical of the formula (II) or R 1 is a radical of the formula (III) A is selected from N, CH and CR 2 , where R 2 is selected from halogen, alkyl, aralkyl, aryl, OH, NH 2 , NHR 3 , NR 3 R 4 and SR 5 , where R 3 , R 4 and R 5 are each alkyl, aralkyl or aryl groups optionally substituted with hydroxy or halogen, and where R 2 is optionally substituted with hydroxy or halogen when R 2 is alkyl, aralkyl or aryl; B is selected from hydroxy, NH 2 , NHR 6 , SH, hydrogen and halogen, where R 6 is an alkyl, aralkyl or aryl group optionally substituted with hydroxy or halogen; D is selected from hydroxy, NH 2 , NHR 7 , hydrogen, halogen and SCH 3 , where R 7 is an alkyl, aralkyl or aryl group optionally substituted with hydroxy or halogen; E is selected from N and CH; G is a C 1-4 saturated or unsaturated alkyl group optionally substituted with hydroxy or halogen, or G is absent; or a tautomer thereof, or a pharmaceutically acceptable salt thereof, or an ester thereof, or a prodrug thereof.
摘要翻译：具有通式（I）的核苷酸的氮杂环丁烷类似物和具有通式（I）的核苷磷酸化酶抑制剂，这些化合物作为药物的用途，含有该化合物的药物组合物，使用该化合物治疗某些疾病的方法，制备该化合物的方法和用于其中W和X各自独立地选自氢，CH 2 OH，CH 2 OQ和CH 2 SQ的化合物的制备; Y和Z各自独立地选自氢，卤素，CH 2 OH，CH 2 OQ，CH 2 SQ，SQ，OQ和Q ; Q是烷基，芳烷基或芳基，其各自可以任选被一个或多个选自羟基，卤素，甲氧基，氨基或羧基的取代基取代; R 1是式（II）的基团或R 1是式（III）的基团，A选自N，CH和CR 2 其中R 2选自卤素，烷基，芳烷基，芳基，OH，NH 2，NHR 3，NR 3，其中R 3，R 4，R 4和R 4独立地为氢，任何被羟基或卤素任选取代的烷基，芳烷基或芳基，其中R 2任选地被羟基或卤素取代时，R 2，是烷基，芳烷基或芳基; B选自羟基，NH 2，NHR 6，SH，氢和卤素，其中R 6是烷基，芳烷基或芳基任选被羟基或卤素取代; D选自羟基，NH 2，NHR 7，氢，卤素和SCH 3，其中R 7，是任选被羟基或卤素取代的烷基，芳烷基或芳基; E选自N和CH; G是任选被羟基或卤素取代的C 1-4 - 饱和或不饱和烷基，或G不存在; 或其互变异构体，或其药学上可接受的盐或其酯，或其前药。

4. 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。

5. 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。

6. 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。

7. 发明申请

WO2011008110A1 3-HYDROXYPYRROLIDINE INHIBITORS OF 5'-METHYLTHIOADENOSINE PHOSPHORYLASE AND NUCLEOSIDASE 审中-公开
标题翻译： 5'-甲氧基苯并噻唑啉磷酸酶和核苷酸酶的3-羟基吡咯烷酮抑制剂
公开(公告)号：WO2011008110A1
公开(公告)日：2011-01-20
申请号：PCT/NZ2010/000148
申请日：2010-07-16
申请人： ALBERT EINSTEIN COLLEGE OF YESHIVA UNIVERSITY , INDUSTRIAL RESEARCH LIMITED , EVANS, Gary Brian , LONGSHAW, Alistair Ian , SCHRAMM, Vern L. , TYLER, Peter, Charles
发明人： EVANS, Gary Brian , LONGSHAW, Alistair Ian , SCHRAMM, Vern L. , TYLER, Peter, Charles
IPC分类号： C07D487/04 , A61P31/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention relates to 3-hydroxypyrrolidine compounds of the general formula (I) which are inhibitors of 5'-methylthioadenosine phosphorylase or 5'-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5'-methylthioadenosine phosphorylase or 5'-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds.
摘要翻译：本发明涉及作为5'-甲硫基腺苷磷酸化酶或5'-甲硫基腺苷核苷酶抑制剂的通式（I）的3-羟基吡咯烷化合物。本发明还涉及这些化合物在治疗期望抑制5'-甲硫基腺苷磷酸化酶或包括癌症的5'-甲基硫代腺苷核苷酸酶的疾病或病症的用途，以及含有该化合物的药物组合物。

8. 发明申请

WO2008030119A1 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：WO2008030119A1
公开(公告)日：2008-03-13
申请号：PCT/NZ2007/000261
申请日：2007-09-07
申请人： INDUSTRIAL RESEARCH LIMITED , ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , CLINCH, Keith , EVANS, Gary Brian , FURNEAUX, Richard Hubert , KELLY, Peter Michael , SCHRAMM, Vern L. , TYLER, Peter Charles , WOOLHOUSE, Anthony David
发明人： CLINCH, Keith , EVANS, Gary Brian , FURNEAUX, Richard Hubert , KELLY, Peter Michael , SCHRAMM, Vern L. , TYLER, Peter Charles , WOOLHOUSE, Anthony David
IPC分类号： C07D487/04 , A61P31/04 , A61P37/06 , A61K31/519 , A61P33/02 , A61P17/06 , A61P35/00
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。

9. 发明申请

WO2007097648A1 METHODS OF TREATING DISEASES USING INHIBITORS OF NUCLEOSIDE PHOSPHORYLASES AND NUCLEOSIDASES 审中-公开
标题翻译：使用核苷酸磷酸酶和核苷酸抑制剂治疗疾病的方法
公开(公告)号：WO2007097648A1
公开(公告)日：2007-08-30
申请号：PCT/NZ2007/000038
申请日：2007-02-23
申请人： INDUSTRIAL RESEARCH LIMITED , ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY , FURNEAUX, Richard Hubert , TYLER, Peter Charles , EVANS, Gary Brian , SCHRAMM, Vern L.
发明人： FURNEAUX, Richard Hubert , TYLER, Peter Charles , EVANS, Gary Brian , SCHRAMM, Vern L.
IPC分类号： A61K31/519 , A61K31/7042 , A61P35/00
CPC分类号： A61K31/519 , A61K31/7042
摘要： The invention relates to treating a disease or condition in which it is desirable to inhibit 5'-methylthioadenosine phosphorylase (MTAP) and/or 5'-methylthioadenosine nucleosidase (MTAN). The invention particularly relates to the co-administration of 5'-methylthioadenosine (MTA), or a prodrug of MTA, with one or more MTAP/MTAN inhibitors. Included among the diseases treatable are prostate cancer and head and neck cancer.
摘要翻译：本发明涉及治疗期望抑制5'-甲硫基腺苷磷酸化酶（MTAP）和/或5'-甲基硫代腺苷核苷酸酶（MTAN）的疾病或病症。本发明特别涉及5-methylthioadenosine（MTA）或MTA前药与一种或多种MTAP / MTAN抑制剂的共同给药。可治疗的疾病包括前列腺癌和头颈癌。

10. 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。

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