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公开(公告)号:US20050009869A1
公开(公告)日:2005-01-13
申请号:US10844037
申请日:2004-09-16
申请人: Everett Pesci , Barbara Iglewski , Jared Milbank , James Pearson , Andrew Kende , Everett Greenberg
发明人: Everett Pesci , Barbara Iglewski , Jared Milbank , James Pearson , Andrew Kende , Everett Greenberg
IPC分类号: C07D215/22 , C07D215/233 , C12N1/20 , C12P17/12 , C12Q1/02 , C12Q1/04 , C07D215/16 , C07D311/74 , C07D335/06
CPC分类号: C07D215/233 , C12N1/20 , C12P17/12 , C12Q1/025 , C12Q1/045
摘要: Novel bacterial quinolone signal molecules and, more particularly, pseudomonas quinolone signal (“PQS”) molecules, e.g., 2-heptyl-3-hydroxy-4-quinolone, and analogs and derivatives thereof are described. Therapeutic compositions containing the molecules, and therapeutic methods, methods of for regulating gene expression, methods for identifying modulators of the autoinducer molecules, and methods of modulating quorum sensing signalling in bacteria using the compounds of the invention are also described.
摘要翻译: 描述了新的细菌喹诺酮信号分子,更特别地,假单胞菌喹诺酮信号(“PQS”)分子,例如2-庚基-3-羟基-4-喹诺酮及其类似物和衍生物。 还描述了含有分子的治疗组合物,治疗方法,调节基因表达的方法,用于鉴定自身诱导剂分子的调节剂的方法,以及使用本发明的化合物调节细菌群体感应信号传导的方法。
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公开(公告)号:US20070231839A1
公开(公告)日:2007-10-04
申请号:US11220224
申请日:2005-09-06
申请人: Andrew Kende , Barbara Iglewski , Roger Smith , Richard Phipps , James Pearson
发明人: Andrew Kende , Barbara Iglewski , Roger Smith , Richard Phipps , James Pearson
IPC分类号: G01N33/554 , G01N33/569 , C07K16/12 , C07K16/46
CPC分类号: C07D207/273 , A61K39/385 , A61K2039/505 , A61K2039/6081 , C07D263/26 , C07D307/33 , C07D333/36 , C07K16/1203 , C07K16/1214 , G01N33/56911 , Y10S435/975 , Y10S436/80 , Y10S436/804 , Y10S530/806 , Y10S530/808
摘要: The present invention relates to an immunogenic conjugate comprising a carrier molecule coupled to an autoinducer of a Gram negative bacteria The immunogenic conjugate, when combined with a pharmaceutically acceptable carrier, forms a suitable vaccine for mammals to prevent infection by the Gram negative bacteria The immunogenic conjugate is also used to raise and subsequently isolate antibodies or binding portions thereof which are capable of recognizing and binding to the autoinducer. The antibodies or binding portions thereof are utilized in a method of treating infections, a method of inhibiting autoinducer activity, and in diagnostic assays which detect the presence of autoinducers or autoinducer antagonists in fluid or tissue samples. TABLE OF CONTENTS Page 1. FIELD OF THE INVENTION1 2. BACKGROUND OF THE INVENTION1 3. SUMMARY OF THE INVENTION4 4. BRIEF DESCRIPTION OF THE DRAWINGS7 5. DETAILED DESCRIPTION OF THE INVENTION7 5.1 Isolation and Synthesis of Homoserine Lactones7 5.2 Bacterial Autoinducer Conjugation to a Carrier17 5.3 Generation of Antibodies to BAI Immunogenic conjugates19 5.4 Therapeutic Uses of Immunogenic conjugates22 or Antibodies Thereto 5.4.1 Administration and Formulation22 5.4.2 Effective Dose25 5.5 Diagnostic Methods27 6. EXAMPLE: SYNTHESIS32 Preparation of Compound C32 Preparation of Compound D32 Preparation of Compound 532 Preparation of Compound 633 Preparation of Compound 733 Preparation of Compound 833 Preparation of Compound 1034 Preparation of Compound 1134 Preparation of Compound 1335 Preparation of Compound 1235 Preparation of Compound 1435 Preparation of Compound 1536 Preparation of Compound 1736 Preparation of Compound 2137 Preparation of Compound 2237 Preparation of Compound 2438 Preparation of Compound 2538 Preparation of Compound 2738 Preparation of Compound 2939 7. EXAMPLE: PRODUCTION OF BAI ANTIBODIES39 7.1 PAI'S Role In Virulence39 7.2 Anti-PAI Polyclonal Antibodies40 7.3 Neutralization of PAI With Antibodies40
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