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1. 发明申请

WO2004041209A2 TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：转录因子调节化合物及其使用方法
公开(公告)号：WO2004041209A2
公开(公告)日：2004-05-21
申请号：PCT/US2003/035205
申请日：2003-11-03
申请人： PARATEK PHARMACEUTICALS, INC. , LEVY, Stuart, B. , ALEKSHUN, Michael, N. , PODLOGAR, Brent, L. , OHEMENG, Kwasi , VERMA, Atul, K. , WARCHOL, Tadeusz , BHATIA, Beena , BOWSER, Todd , GRIER, Mark
发明人： LEVY, Stuart, B. , ALEKSHUN, Michael, N. , PODLOGAR, Brent, L. , OHEMENG, Kwasi , VERMA, Atul, K. , WARCHOL, Tadeusz , BHATIA, Beena , BOWSER, Todd , GRIER, Mark
IPC分类号： A61K
CPC分类号： C07D235/06 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/495 , A61K31/50 , A61K31/535 , A61K31/55 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/18 , C07D267/16 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D487/04 , C07D491/04 , Y02A50/401 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483
摘要： Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.
摘要翻译：提供了可用作降低微生物的抗性，毒力或生长的抗感染药物的取代的苯并咪唑化合物。制备和使用取代的苯并咪唑化合物的方法，以及其药物制剂，例如降低抗生素抗性和抑制生物膜。

2. 发明申请

WO2004001058A2 TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：转录因子调节化合物及其使用方法
公开(公告)号：WO2004001058A2
公开(公告)日：2003-12-31
申请号：PCT/US2002/014255
申请日：2002-05-06
申请人： PARATEK PHARMACEUTICALS, INC. , LEVY, Stuart, B. , ALEKSHUN, Micheal, N. , PODLOGAR, Brent , OHEMENG, Kwasi , VERMA, Atul , WARCHOL, Tadeusz , BHATIA, Beena
发明人： LEVY, Stuart, B. , ALEKSHUN, Micheal, N. , PODLOGAR, Brent , OHEMENG, Kwasi , VERMA, Atul , WARCHOL, Tadeusz , BHATIA, Beena
IPC分类号： C12Q
CPC分类号： A61K31/47 , A61K31/40 , A61K31/407 , A61K31/415 , A61K31/4745 , A61K31/505 , A61K31/555 , Y02A50/401 , Y02A50/47 , Y02A50/471 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483 , Y02A50/52
摘要： Methods for identifying compound useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. In one embodiment, the method comprises contacting a microbial cell comprising: 1) a selectable marker under the control of a transcription factor responsive element and 2) a transcription factor, with a compound under conditions which allow interaction of the compound with the microbial cell; and measuring the ability of the compound to affect the growth or survival of the microbial cell as an indication of whether the test compound modulates the activity of a transcription factor.
摘要翻译：提供用于鉴定可用作降低微生物的抗性，毒力或生长的抗感染剂的化合物的方法。在一个实施方案中，所述方法包括使微生物细胞接触，所述微生物细胞包含：1）在转录因子反应元件控制下的选择性标记和2）允许化合物与微生物细胞相互作用的条件下的化合物与转录因子的接触; 并测量化合物影响微生物细胞的生长或存活的能力，作为测试化合物是否调节转录因子的活性的指示。

3. 发明申请

WO0107030A3 COMPOSITIONS AN INHIBITOR OF AN ACCRAB-LIKE EFFLUX PUMP FOR REDUCUNG MICROBIAL RESISTANCE TO DRUGS 审中-公开
标题翻译：组合物用于减少对药物的微生物耐药性的类似ACCRAB的止血泵的抑制剂
公开(公告)号：WO0107030A3
公开(公告)日：2002-11-14
申请号：PCT/US0020014
申请日：2000-07-21
申请人： TUFTS COLLEGE , OETHINGER MARGRET , LEVY STUART B
发明人： OETHINGER MARGRET , LEVY STUART B
IPC分类号： G01N33/50 , A61K31/00 , A61K31/085 , A61K31/496 , A61K45/06 , A61P31/00 , A61P31/04 , A61P43/00 , C12Q1/02 , G01N33/15 , C12Q1/18
CPC分类号： C12Q1/689 , A61K31/085 , A61K31/09 , A61K31/47 , A61K31/496 , A61K45/06 , C12Q1/18 , C12Q2600/136 , C12Q2600/156 , C12Q2600/158 , A61K2300/00
摘要： The instant methods and compositions represent an advance in controlling drug resistance in microbes. AcrAB-like efflux pumps have been found to control resistance to drugs, even in highly resistant microbes. Accordingly, methods of treating infection, methods of screening for inhibitors of AcrAB-like efflux pumps, and methods of enhancing antimicrobial activity of drugs are provided. Pharmaceutical composition comprising an inhibitor of an AcrAB-like efflux pump and an antimicrobial agent are also provided.
摘要翻译：本方法和组合物代表了控制微生物耐药性的进展。已经发现AcrAB样外排泵控制对药物的抵抗力，即使在高度耐药的微生物中也是如此。因此，提供了治疗感染的方法，筛选AcrAB样外排泵的抑制剂的方法以及增强药物的抗微生物活性的方法。还提供了包含AcrAB样外排泵和抗微生物剂的抑制剂的药物组合物。

4. 发明申请

WO2004064728A3 USE OF SPECIFIC TETRACYCLINE COMPOUNDS IN THERAPY 审中-公开
标题翻译：特异性四环素化合物在治疗中的应用
公开(公告)号：WO2004064728A3
公开(公告)日：2004-12-16
申请号：PCT/US2004001036
申请日：2004-01-16
申请人： PARATEK PHARM INNC , LEVY STUART B , DRAPER MICHAEL , NELSON MARK L , JONES GRAHAM
发明人： LEVY STUART B , DRAPER MICHAEL , NELSON MARK L , JONES GRAHAM
IPC分类号： A61K31/65 , A61P29/02
CPC分类号： A61K31/65
摘要： Methods and compounds for treating diseases with tetracycline compounds having a target therapeutic activity are described.
摘要翻译：描述了用具有目标治疗活性的四环素化合物治疗疾病的方法和化合物。

5. 发明申请

WO2004064728A2 TETRACYCLINE COMPOUNDS HAVING TARGET THERAPEUTIC ACTIVITIES 审中-公开
标题翻译：具有目标治疗活性的四环素化合物
公开(公告)号：WO2004064728A2
公开(公告)日：2004-08-05
申请号：PCT/US2004/001036
申请日：2004-01-16
申请人： PARATEK PHARMACEUTICALS, INC. , LEVY, Stuart, B. , DRAPER, Michael , NELSON, Mark, L. , JONES, Graham
发明人： LEVY, Stuart, B. , DRAPER, Michael , NELSON, Mark, L. , JONES, Graham
IPC分类号： A61K
CPC分类号： A61K31/65 , Y02A50/411
摘要： Methods and compounds for treating diseases with tetracycline compounds having a target therapeutic activity are described.
摘要翻译：描述了用具有目标治疗活性的四环素化合物治疗疾病的方法和化合物。

6. 发明申请

WO2009005551A3 TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2009005551A3
公开(公告)日：2009-01-08
申请号：PCT/US2008/004090
申请日：2008-03-27
申请人： PARATEK PHARMACEUTICALS, INC. , ALEKSHUN, Michael N. , BARTLETT, Victoria , DRAPER, Michael , GARRITY-RYAN, Lynne , GAY, Raina , GRIER, Mark , KIM, Oak, K. , LEVY, Stuart, B.
发明人： ALEKSHUN, Michael N. , BARTLETT, Victoria , DRAPER, Michael , GARRITY-RYAN, Lynne , GAY, Raina , GRIER, Mark , KIM, Oak, K. , LEVY, Stuart, B.
IPC分类号： A61K31/4184 , A61K31/437 , A61K31/52 , A61P11/00 , A61P13/02 , A61P17/02 , A61P27/02 , A61P31/04 , A61P31/12 , A61P43/00
摘要： Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of using substituted benzimidazole compounds, in, e.g., reducing virulence and infectivity, inhibiting biofilms and treating bacterial infections.

7. 发明申请

WO2009005551A2 TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：转录因子调节化合物及其使用方法
公开(公告)号：WO2009005551A2
公开(公告)日：2009-01-08
申请号：PCT/US2008004090
申请日：2008-03-27
申请人： PARATEK PHARM INNC , GARRITY-RYAN LYNNE , GRIER MARK , KIM OAK K , LEVY STUART B
发明人： GARRITY-RYAN LYNNE , GRIER MARK , KIM OAK K , LEVY STUART B
CPC分类号： A61K31/4184 , A61K31/437 , A61K31/52
摘要： Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of using substituted benzimidazole compounds, in, e.g., reducing virulence and infectivity, inhibiting biofilms and treating bacterial infections.
摘要翻译：提供了可用作降低微生物的抗性，毒力或生长的抗感染药物的取代的苯并咪唑化合物。使用取代的苯并咪唑化合物的方法，例如降低毒力和感染性，抑制生物膜和治疗细菌感染。

8. 发明申请

WO1993008806A1 REDUCING TETRACYCLINE RESISTANCE IN LIVING CELLS 审中-公开
标题翻译：降低生活细胞中的四环素抗性
公开(公告)号：WO1993008806A1
公开(公告)日：1993-05-13
申请号：PCT/US1992008965
申请日：1992-10-16
申请人： TRUSTEES OF TUFTS COLLEGE , LEVY, Stuart, B.
发明人： TRUSTEES OF TUFTS COLLEGE
IPC分类号： A61K31/65
CPC分类号： C07D295/13 , A61K31/65 , C07C237/26 , C07C323/29 , C07C2601/08 , A61K2300/00
摘要： The present invention provides an improved methodology by which therapeutically to overcome resistance to tetracycline in living cells including bacteria, parasites, fungi, and rickettsiae. The methodology employs a blocking agent such as C5 ester derivatives, or 6-deoxy 13-(substituted mercapto) derivatives of tetracycline, in combination with other tetracycline-type antibiotics as a synergistic combination of compositions to be administered simultaneously, sequentially or concurrently. In another embodiment, certain novel compositions are provided which may be administered along against, for example, a sensitive or resistant strain of gram positive bacteria such as S. aureus and E. faecalis. The concomitantly administered compositions effectively overcome the tetracycline resistant mechanisms present such that the cell is effectively converted from a tetracycline-resistant state to a tetracycline-sensitive state.
摘要翻译：本发明提供了一种改进的方法，其通过其治疗来克服包括细菌，寄生虫，真菌和立克次体在内的活细胞中对四环素的抗性。该方法采用封闭剂如C5酯衍生物或四环素的6-脱氧13-（取代的巯基）衍生物与其他四环素型抗生素组合，作为同时，顺序或同时施用的组合物的协同组合。在另一个实施方案中，提供某些新的组合物，其可以与例如革兰氏阳性细菌如金黄色葡萄球菌和粪肠球菌的敏感或抗性菌株相对地施用。伴随施用的组合物有效克服存在的四环素抗性机制，使得细胞有效地从四环素抗性状态转变为四环素敏感状态。

9. 发明申请

WO2010124097A3 TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2010124097A3
公开(公告)日：2010-10-28
申请号：PCT/US2010/032063
申请日：2010-04-22
申请人： PARATEK PHARMACEUTICALS, INC. , ALEKSHUN, Michael, K. , BARTLETT, Victoria , DRAPER, Michael , GARRITY-RYAN, Lynne , GAY, Raina , GRIER, Mark , KIM, Oak, K. , LEVY, Stuart, B.
发明人： ALEKSHUN, Michael, K. , BARTLETT, Victoria , DRAPER, Michael , GARRITY-RYAN, Lynne , GAY, Raina , GRIER, Mark , KIM, Oak, K. , LEVY, Stuart, B.
IPC分类号： C07D403/04 , C07D235/04 , A61K31/416 , A61P31/10
摘要： Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of using substituted benzimidazole compounds, in, e.g., reducing virulence and infectivity, inhibiting biofilms and treating bacterial infections, are also provided.

10. 发明申请

WO2010124097A2 TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：转录因子调节化合物及其使用方法
公开(公告)号：WO2010124097A2
公开(公告)日：2010-10-28
申请号：PCT/US2010032063
申请日：2010-04-22
申请人： PARATEK PHARM INNC , ALEKSHUN MICHAEL K , BARTLETT VICTORIA , DRAPER MICHAEL , GARRITY-RYAN LYNNE , GAY RAINA , GRIER MARK , KIM OAK K , LEVY STUART B
发明人： ALEKSHUN MICHAEL K , BARTLETT VICTORIA , DRAPER MICHAEL , GARRITY-RYAN LYNNE , GAY RAINA , GRIER MARK , KIM OAK K , LEVY STUART B
IPC分类号： C07D403/04 , A61K31/416 , A61P31/10 , C07D235/04
CPC分类号： C07D235/18 , A61K31/416 , A61K45/06 , C07D235/22 , C07D401/12 , C07D401/14 , C07D403/12 , A61K2300/00
摘要： Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of using substituted benzimidazole compounds, in, e.g., reducing virulence and infectivity, inhibiting biofilms and treating bacterial infections, are also provided.
摘要翻译：提供了可用作降低微生物的抗性，毒力或生长的抗感染药物的取代的苯并咪唑化合物。还提供了使用取代的苯并咪唑化合物的方法，例如降低毒力和感染性，抑制生物膜和治疗细菌感染。

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