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1. 发明申请

WO2009143509A1 SALTS AND POLYMORPHS OF A TETRACYCLINE COMPOUND 审中-公开
标题翻译：四环素化合物的盐和多元醇
公开(公告)号：WO2009143509A1
公开(公告)日：2009-11-26
申请号：PCT/US2009/045143
申请日：2009-05-26
申请人： PARATEK PHARMACEUTICALS, INC. , CVETOVICH, Raymond , WARCHOL, Tadeusz
发明人： CVETOVICH, Raymond , WARCHOL, Tadeusz
IPC分类号： A01N37/18
CPC分类号： A61K31/65 , C07B2200/13 , C07C231/12 , C07C237/26 , C07C303/32 , C07C309/30 , C07C2603/46
摘要： Crystalline forms, including salts and polymorphs, of a compound useful in the treatment of tetracycline compound-responsive states are provided herein. The crystalline compounds are useful for the treatment or prevention of conditions and disorders such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds in general.
摘要翻译：本文提供了可用于治疗四环素化合物反应状态的化合物的结晶形式，包括盐和多晶型物。结晶化合物可用于治疗或预防条件和病症，例如细菌感染和肿瘤，以及其他已知的四环素化合物的应用。

2. 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。

3. 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。

4. 发明申请

WO2009009042A1 METHODS FOR SYNTHESIZING SUBSTITUTED TETRACYCLINE COMPOUNDS 审中-公开
标题翻译：用于合成取代的四氢化合物化合物的方法
公开(公告)号：WO2009009042A1
公开(公告)日：2009-01-15
申请号：PCT/US2008/008355
申请日：2008-07-07
申请人： PARATEK PHARMACEUTICALS, INC. , SEYEDI, Farzaneh , WARCHOL, Tadeusz , GRIER, Mark
发明人： SEYEDI, Farzaneh , WARCHOL, Tadeusz , GRIER, Mark
IPC分类号： C07C237/26
CPC分类号： C07C231/12 , C07C2603/44 , C07C237/26
摘要： Methods for synthesizing a carboxaldehyde substituted tetracycline compound comprising reacting a tetracycline reactive intermediate under appropriate conditions with carbon monoxide, a palladium catalyst, a phosphine ligand, a silane and a base, such that said carboxaldehyde substituted tetracycline compound is synthesized. The palladium catalyst is chosen from PdCl2 (tBu2PhP)2 dichlorobis (di-tert-butylphenylphosphine palladium (II)] or PdCl2 (DPEPhos) [bis (diphenylphosphinophenyl) ether palladium (II) chloride]. The tetracycline reactive intermediate contains moieties selected from halogens and triflates. Methods of synthesizing a substituted tetracycline compound comprising reacting the carboxaldehyde substituted tetracycline compound under palladium catalyzed coupling conditions, hydrogenolysis conditions or reductive amination conditions.
摘要翻译：合成羧甲醛取代的四环素化合物的方法，包括在合适的条件下使四环素反应性中间体与一氧化碳，钯催化剂，膦配体，硅烷和碱反应，使得所述甲醛取代的四环素化合物合成。钯催化剂选自PdCl2（tBu2PhP）2二氯双（二叔丁基苯基膦钯（II）]或PdCl 2（DPEPhos）[双（二苯基膦基苯基）醚氯化钯（II）]，四环素反应性中间体包含选自卤素合成取代的四环素化合物的方法，包括在钯催化的偶联条件下，氢解条件或还原胺化条件下使羧醛取代的四环素化合物反应。

5. 发明申请

WO2004001058A3 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：WO2004001058A3
公开(公告)日：2005-03-03
申请号：PCT/US0214255
申请日：2002-05-06
申请人： PARATEK PHARM INNC , 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： G01N33/50 , A61K31/341 , A61K31/352 , A61K31/40 , A61K31/407 , A61K31/409 , A61K31/415 , A61K31/4184 , A61K31/4196 , A61K31/42 , A61K31/4245 , A61K31/429 , A61K31/436 , A61K31/437 , A61K31/4439 , A61K31/47 , A61K31/4709 , A61K31/4745 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/53 , A61K31/551 , A61K31/553 , A61K31/555 , A61K31/7088 , A61K45/00 , A61K47/18 , A61K47/20 , A61K47/22 , A61K47/34 , A61K48/00 , A61P1/02 , A61P9/00 , A61P11/00 , A61P13/08 , A61P17/00 , A61P19/00 , A61P27/16 , A61P29/00 , A61P31/00 , A61P31/04 , C07D235/08 , C07D235/22 , C07D243/10 , C07D253/06 , C07D261/20 , C07D307/60 , C07D311/30 , C07D401/04 , C07D403/04 , C07D405/04 , C07D413/04 , C07D471/04 , C07D487/04 , C07D487/14 , C07D491/052 , C07D498/04 , C07D498/14 , C07D513/04 , C12N15/09 , C12Q1/02 , G01N33/15 , A61K31/33 , A61K31/34 , A61K31/35 , A61K31/38 , A61K31/41 , A61K31/54 , A61K43/16 , A61K43/50
CPC分类号： A61K31/47 , A61K31/40 , A61K31/407 , A61K31/415 , A61K31/4745 , A61K31/505 , A61K31/555
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。

6. 发明申请

WO2004041209A3 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：WO2004041209A3
公开(公告)日：2004-09-30
申请号：PCT/US0335205
申请日：2003-11-03
申请人： PARATEK PHARM INNC , 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： A61K31/41 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/495 , A61K31/50 , A61K31/535 , A61K31/55 , A61P31/00 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/14 , C07D235/18 , C07D267/16 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D487/04 , C07D491/04 , C07D498/04 , C07D235/00
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
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：提供了可用作减少抗性，毒力或微生物生长的抗感染剂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及其药物制剂的方法，用于例如降低抗生素抗性和抑制生物膜。

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