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21. 发明公开

EP3271021A2 TAT-INDUCED CRISPR/ENDONUCLEASE-BASED GENE EDITING 审中-公开
标题翻译： TAT诱导的基于CRISPR /内切核酸酶的基因编辑
公开(公告)号：EP3271021A2
公开(公告)日：2018-01-24
申请号：EP16769422.3
申请日：2016-03-18
申请人： Temple University Of The Commonwealth System Of Higher Education
发明人： KHALILI, Kamel
IPC分类号： A61P31/12 , A61P31/18 , C12N9/22 , C12N15/63 , C12N15/49
CPC分类号： C12N15/111 , A61K45/06 , A61K48/005 , A61K48/0075 , C12N7/00 , C12N9/22 , C12N15/11 , C12N15/1132 , C12N15/86 , C12N2310/20 , C12N2310/3519 , C12N2320/30 , C12N2740/16062 , C12N2800/107 , C12N2800/22 , C12N2830/00 , C12N2830/30 , C12N2830/60
摘要： Compositions and methods are provided for Tat-inducible expression of a CRISPR-associated endonuclease by a truncated HIV LTR promoter containing at least a core region and a TAR region of a HIV LTR promoter. The compositions may be used as a therapeutic treatment for the treatment and/or prevention of HIV.

22. 发明公开

EP3243513A1 USE OF THE RNASE INHIBITOR RNPA-3000 FOR TREATING STAPHYLOCOCCUS INFECTIONS 有权转让
标题翻译： RNA酶抑制剂RNPA-3000在治疗金黄色葡萄球菌感染中的应用
公开(公告)号：EP3243513A1
公开(公告)日：2017-11-15
申请号：EP17171427.2
申请日：2012-01-26
申请人： University of Rochester , Board of Regents of the University of Nebraska , Temple University - Of The Commonwealth System of Higher Education
发明人： DUNMAN, Paul M. , OLSON, Patrick D. , CHILDERS, Wayne
IPC分类号： A61K31/427 , A61K45/06
CPC分类号： A61K31/427 , A61K31/341 , A61K31/402 , A61K45/06 , C07D207/337 , C07D307/56 , C07D307/68 , C07D405/06 , C07D417/06 , C12Q1/44 , G01N2333/922 , G01N2500/04 , G01N2500/10 , A61K2300/00
摘要： Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease.
摘要翻译：本文描述了细菌核糖核酸酶（例如RnpA）的小分子抑制剂及其合成和使用方法。使用这些化合物的方法包括治疗和预防微生物感染和抑制细菌核糖核酸酶。

23. 发明公开

EP3212183A1 SYNERGISTIC COMPOSITIONS FOR TREATING MICROBIAL INFECTIONS 有权
标题翻译：用于治疗微生物感染的协同组合物
公开(公告)号：EP3212183A1
公开(公告)日：2017-09-06
申请号：EP15854238.1
申请日：2015-10-30
申请人： University of Rochester , Temple University Of The Commonwealth System Of Higher Education
发明人： DUNMAN, Paul M. , CHILDERS, Wayne
IPC分类号： A61K31/341 , A61K45/06 , C07D417/06
CPC分类号： A61K31/341 , A61K9/0043 , A61K9/06 , A61K31/17 , A61K31/343 , A61K31/351 , A61K31/381 , A61K31/4045 , A61K31/415 , A61K31/4184 , A61K31/44 , A61K31/4409 , A61K31/443 , A61K31/47 , A61K31/497 , A61K45/06 , A61K47/10 , A61K2300/00
摘要： Synergistic pharmaceutical compositions including an RNase P inhibitor and a tRNA synthetase inhibitor are provided, as well as methods for their use in treating infections. Also provided herein are methods of using the compositions to inhibit a bacterial tRNA synthetase in a cell and to decolonize bacteria on a surface.
摘要翻译：提供了包括RNA酶P抑制剂和tRNA合成酶抑制剂的协同药物组合物，以及它们用于治疗感染的方法。本文还提供了使用组合物抑制细胞中的细菌tRNA合成酶并使表面上的细菌去乳化的方法。

24. 发明授权

EP1689706B1 ALPHA, BETA-UNSATURATED SULFOXIDES FOR TREATING PROLIFERATIVE DISORDERS 有权转让
标题翻译： ALPHA，BETA-UNGESÄTTIGTESULFOXIDE ZUR BEHANDLUNG VON PROLIFAATIVEN ERKRANKUNGEN
公开(公告)号：EP1689706B1
公开(公告)日：2017-01-11
申请号：EP04816944.5
申请日：2004-11-08
申请人： Temple University - Of The Commonwealth System of Higher Education , Onconova Therapeutics, Inc.
发明人： REDDY, Premkumar, E. , REDDY, Ramana, M., V. , BELL, Stanley, C.
IPC分类号： C07C317/10 , A61K31/10 , C07D333/18 , C07C317/18 , C07C317/28 , C07C317/44 , C07D207/333 , C07D277/26 , C07D213/34 , C07D307/38
CPC分类号： C07C317/44 , C07C317/10 , C07C317/18 , C07C317/28 , C07D207/333 , C07D213/34 , C07D277/26 , C07D307/38 , C07D333/18

26. 发明公开

EP2667872A2 SMALL MOLECULE RNASE INHIBITORS AND METHODS OF USE 有权
标题翻译：小分子RNA酶抑制剂及使用方法
公开(公告)号：EP2667872A2
公开(公告)日：2013-12-04
申请号：EP12738820.5
申请日：2012-01-26
申请人： University of Rochester , Board of Regents of the University of Nebraska , Temple University - Of The Commonwealth System of Higher Education
发明人： DUNMAN, Paul M. , OLSON, Patrick D. , CHILDERS, Wayne
IPC分类号： A61K31/497 , C07D403/00
CPC分类号： A61K31/427 , A61K31/341 , A61K31/402 , A61K45/06 , C07D207/337 , C07D307/56 , C07D307/68 , C07D405/06 , C07D417/06 , C12Q1/44 , G01N2333/922 , G01N2500/04 , G01N2500/10 , A61K2300/00
摘要： Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease.
摘要翻译：本文描述了细菌核糖核酸酶（例如RnpA）的小分子抑制剂及其合成和使用方法。使用这些化合物的方法包括治疗和预防微生物感染和抑制细菌核糖核酸酶。

27. 发明授权

EP1539675B1 ARYL AND HETEROARYL PROPENE AMIDES, DERIVATIVES THEREOF AND THERAPEUTIC USES THEREOF 有权
标题翻译：芳和HETEROARYLPROPENAMIDE，及其衍生物和治疗它们的应用
公开(公告)号：EP1539675B1
公开(公告)日：2013-11-06
申请号：EP03796317.0
申请日：2003-08-28
申请人： Temple University - Of The Commonwealth System of Higher Education
发明人： REDDY, M., V., Ramana , REDDY, E., Premkumar
IPC分类号： C07C233/09 , C07C229/00 , A61K31/165 , A61K31/195
CPC分类号： C07C233/44 , C07C235/38 , C07C237/20 , C07C255/57

28. 发明公开

EP2359819A1 Substituted styryl benzylsulfones for treating proliferative disorders 审中-公开
标题翻译：取代基苯乙烯基苄基砜zur Behandlung von Proliferationskrankheiten
公开(公告)号：EP2359819A1
公开(公告)日：2011-08-24
申请号：EP10178360.3
申请日：2001-04-13
申请人： Temple University - Of The Commonwealth System of Higher Education
发明人： Reddy, E. Premkumar , Reddy, M.V. Ramana
IPC分类号： A61K31/10 , A61K31/19 , A61K31/216
CPC分类号： C07C323/52 , C07C317/10 , C07C317/18 , C07C317/44 , C07C323/60 , C07F9/12
摘要： Styryl benzylsulfones of formula I are useful as ant-proliferative agents, including, for example, anticancer agents. In formula I:

(a) (i) R 1 , R 2 , R 4 and R 5 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl;
(ii) R 3 is hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl, provided at least three of R 1 , R 2 , R 3 , R 4 and R 5 are other than hydrogen; and
(iii) R 6 , R 7 , R 8 , R 9 and R 10 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl;

or
(b) (i) R 6 , R 8 and R 10 are halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl, and R 7 and R 9 are hydrogen; and
(ii) R 1 , R 2 , R 3 , R 4 and R 5 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy), or trifluoromethyl;

or
(c) (i) at least four of R 6 , R 7 , R 8 , R 9 and R 10 are halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl, and the remainder of R 6 , R 7 , R 8 , R 9 and R 10 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl; and
(ii) R 1 , R 2 , R 3 , R 4 and R 5 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy), or trifluoromethyl;

or a pharmaceutically acceptable salt thereof.
摘要翻译：式I的苯乙烯基苄基砜可用作抗增殖剂，包括例如抗癌剂。在式I中：（a）（i）R 1，R 2，R 4和R 5是氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基，羧基，羟基，膦酸根，氨基，氨磺酰基，乙酰氧基，二甲基氨基（C 2 -C 6烷氧基）或三氟甲基; （ⅱ）R 3为氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，氰基，羧基，羟基，膦酸基，氨基，氨基磺酰基，乙酰氧基，二甲基氨基（C 2 -C 6烷氧基）或三氟甲基， 1，R 2，R 3，R 4和R 5不同于氢; 和（iii）R 6，R 7，R 8，R 9和R 10是氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基，羧基，羟基，膦酰基，氨基，氨基磺酰基，乙酰氧基，（C 2 -C 6烷氧基）或三氟甲基; 或（b）（i）R 6，R 8和R 10是卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基，羧基，羟基，膦酰基，氨基，氨基磺酰基，乙酰氧基，二甲基氨基）或三氟甲基，R 7和R 9为氢; 和（ii）R 1，R 2，R 3，R 4和R 5是氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基，羧基，羟基，膦酰基，氨基，氨基磺酰基，乙酰氧基，（C 2 -C 6烷氧基）或三氟甲基; 或（c）（i）R 6，R 7，R 8，R 9和R 10中的至少四个为卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基，羧基，羟基，膦酸根，氨基，亚磺酰基，乙酰氧基，二甲基氨基（C 2 -C 6烷氧基）或三氟甲基，R 6，R 7，R 8，R 9和R 10的其余部分为氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基，羧基，羟基，膦酰基，氨基，氨基磺酰基，乙酰氧基，二甲基氨基（C 2 -C 6烷氧基）或三氟甲基; 和（ii）R 1，R 2，R 3，R 4和R 5是氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基，羧基，羟基，膦酰基，氨基，氨基磺酰基，乙酰氧基，（C 2 -C 6烷氧基）或三氟甲基; 或其药学上可接受的盐。

29. 发明授权

EP1370253B8 USE OF ALPHA, BETA UNSATURATED ARYL SULFONES FOR PROTECTING CELLS AND TISSUES FROM IONIZING RADIATION TOXICITY 有权
标题翻译： ALPHA，BETA不饱和芳砜的用于细胞毒性ON离子辐射保护与组织USE
公开(公告)号：EP1370253B8
公开(公告)日：2008-11-26
申请号：EP02733811.0
申请日：2002-02-28
申请人： Temple University - of the Commonwealth System of Higher Education , Onconova Therapeutics, Inc
发明人： REDDY, Premkumar, E. , REDDY, Ramana, M.V. , COSENZA, Stephen, C. , HELSON, Lawrence
IPC分类号： A61K31/10 , A61K31/277 , A61K31/4409 , A61K31/426 , A61K31/40 , A61P39/00
CPC分类号： A61K31/435 , A61K31/10 , A61K31/275 , A61K31/35 , A61K31/40 , A61K31/425 , A61K41/00 , A61K2300/00

30. 发明授权

EP1370253B1 USE OF ALPHA, BETA UNSATURATED ARYL SULFONES FOR PROTECTING CELLS AND TISSUES FROM IONIZING RADIATION TOXICITY 有权
标题翻译： ALPHA，BETA不饱和芳砜的用于细胞毒性ON离子辐射保护与组织USE
公开(公告)号：EP1370253B1
公开(公告)日：2008-09-03
申请号：EP02733811.0
申请日：2002-02-28
申请人： Temple University of the Commonwealth System of Higher Education , Onconova Therapeutics, Inc
发明人： REDDY, Premkumar, E. , REDDY, Ramana, M.V. , COSENZA, Stephen, C. , HELSON, Lawrence
IPC分类号： A61K31/10 , A61K31/277 , A61K31/4409 , A61K31/426 , A61K31/40 , A61P39/00
CPC分类号： A61K31/435 , A61K31/10 , A61K31/275 , A61K31/35 , A61K31/40 , A61K31/425 , A61K41/00 , A61K2300/00

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