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1. 发明申请

WO2007017762A3 PHOSPHONATED FLUOROQUINOLONES, ANTIBACTERIAL ANALOGS THEREOF, AND METHODS FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS 审中-公开
标题翻译：磷酸荧光素，其抗菌类型及其预防和治疗骨和关节感染的方法
公开(公告)号：WO2007017762A3
公开(公告)日：2007-07-26
申请号：PCT/IB2006002922
申请日：2006-04-21
申请人： TARGANTA THERAPEUTICS INC , DELORME DANIEL , HOUGHTON TOM , KANG TING , TANAKA KELLY , LAFONTAINE YANICK , DIETRICH EVELYNE , RAFI FAR ADEL
发明人： DELORME DANIEL , HOUGHTON TOM , KANG TING , TANAKA KELLY , LAFONTAINE YANICK , DIETRICH EVELYNE , RAFI FAR ADEL
IPC分类号： C07D401/04 , A61K31/395 , A61K31/4709 , A61K31/496 , A61K31/65 , A61K31/675 , A61P31/04 , C07D401/14 , C07D405/14 , C07D471/04
CPC分类号： C07F9/65586 , C07F9/65583 , C07F9/6561
摘要： The present invention relates to phosphonated fluoroquinolones such as moxifloxacm, gatifloxacm and ciprofloxacin, antibacterial analogs thereof, and methods of using such compounds The disclosed compounds represent prodrugs of fluoroquinolones wherein a phosphonated group is tethered to a fluoroquinolone antibiotic via a cleavable linker These compounds are useful as antibiotics for prevention and/or treatment of bone and joint infections, especially for the prevention and/or treatment of osteomyelitis
摘要翻译：本发明涉及磷酸化氟喹诺酮类，例如莫西沙星，加替沙星和环丙沙星，其抗菌类似物，以及使用这些化合物的方法本发明公开的化合物代表氟喹诺酮类药物的前药，其中膦酸化基团通过可切割接头连接到氟喹诺酮抗生素上。这些化合物是有用的作为用于预防和/或治疗骨和关节感染的抗生素，特别是用于预防和/或治疗骨髓炎

2. 发明申请

WO2011019839A2 GLYCOPEPTIDE AND LIPOGLYCOPEPTIDE ANTIBIOTICS WITH IMPROVED SOLUBILITY 审中-公开
标题翻译：具有改善溶解性的糖肽类和脂类肽类抗生素
公开(公告)号：WO2011019839A2
公开(公告)日：2011-02-17
申请号：PCT/US2010/045201
申请日：2010-08-11
申请人： RAFAI FAR, Adel , TANAKA, Kelly , DIETRICH, Evelyne , REDDY, Ranga , KANG, Ting , THE MEDICINES COMPANY
发明人： RAFAI FAR, Adel , TANAKA, Kelly , DIETRICH, Evelyne , REDDY, Ranga , KANG, Ting
IPC分类号： C07K5/12 , C07K7/06 , A61K38/12 , A61K38/14 , A61P31/04
CPC分类号： C07K9/008 , A61K38/12 , A61K38/14 , A61K45/06 , A61K47/48038 , A61K47/48046 , A61K47/48215 , A61K47/542 , A61K47/543 , A61K47/60 , A61K2300/00
摘要： The invention relates to derivatives of glycopeptide and lipoglycopeptide antibiotics possessing an altered ionization state with respect to the parent glycopeptide or lipoglycopeptide antibiotic, and having the ability to be regenerated as the parent glycopeptide or lipoglycopeptide antibiotic under physiological conditions. These compounds are useful as antibiotics for the prevention and/or the treatment of bacterial infections.
摘要翻译：本发明涉及具有相对于母体糖肽或脂糖肽抗生素改变的离子化状态并且具有在生理条件下作为母体糖肽或脂糖肽抗生素再生的能力的糖肽和脂糖肽抗生素的衍生物。这些化合物可用作预防和/或治疗细菌感染的抗生素。

3. 发明申请

WO2010019511A3 PHOSPHONATED RIFAMYCINS AND USES THEREOF FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS 审中-公开
标题翻译：膦酸化利福霉素及其用于预防和治疗骨和关节感染的用途
公开(公告)号：WO2010019511A3
公开(公告)日：2010-06-24
申请号：PCT/US2009053295
申请日：2009-08-10
申请人： DIETRICH EVELYNE , REDDY RANGA , TANAKA KELLY , KANG TING , LAFONTAINE YANICK , RAFAI FAR ADEL , TARGANTA THERAPEUTICS CORP
发明人： DIETRICH EVELYNE , REDDY RANGA , TANAKA KELLY , KANG TING , LAFONTAINE YANICK , RAFAI FAR ADEL
IPC分类号： C07F9/6561 , A61K31/5383 , A61K31/675 , A61P19/00 , A61P31/04
CPC分类号： C07F9/6561 , A61K31/675 , A61K47/548
摘要： The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
摘要翻译：本发明涉及膦酸化利福霉素，以及制备和使用这些化合物的方法。这些化合物可用作预防和/或治疗骨和关节感染的抗生素，特别是用于预防和/或治疗骨髓炎。

4. 发明申请

WO2008077241A1 PHOSPHONATED GLYCOPEPTIDE AND LIPOGLYCOPEPTIDE ANTIBIOTICS AND USES THEREOF FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS 审中-公开
标题翻译：磷酸化糖蛋白和脂蛋白抗体及其用于预防和治疗骨和关节感染的用途
公开(公告)号：WO2008077241A1
公开(公告)日：2008-07-03
申请号：PCT/CA2007/002288
申请日：2007-12-21
申请人： TARGANTA THERAPEUTICS, INC. , TANAKA, Kelly , RAFAI FAR, Adel , CIBLAT, Stéphane , DIETRICH, Evelyne
发明人： TANAKA, Kelly , RAFAI FAR, Adel , CIBLAT, Stéphane , DIETRICH, Evelyne
IPC分类号： C07K9/00 , A61K38/08 , A61K38/14 , A61P19/08 , A61P31/04 , C07K7/06 , C07F9/38 , A61K31/663
CPC分类号： C07K9/008 , A61K38/00 , C07F9/6561
摘要： The present invention is directed to antimicrobial compounds which have an affinity for binding bones. More particularly, the invention is directed to phosphonated derivatives of glycopeptide or lipoglycopeptide antibiotics. These compounds are useful as antibiotics for the prevention or treatment of bone and joint infections, especially for the prevention and treatment of osteomyelitis.
摘要翻译：本发明涉及对结合骨的亲和力的抗微生物化合物。更具体地，本发明涉及糖肽或脂多糖抗生素的膦酸化衍生物。这些化合物可用作预防或治疗骨和关节感染的抗生素，特别是用于预防和治疗骨髓炎。

5. 发明申请

WO2012083453A1 AGRICULTURAL COMPOSITION COMPRISING PH SENSITIVE AGRICULTURAL CHEMICALS AND ORGANIC PH BUFFER 审中-公开
标题翻译：含敏感性农业化学品和有机PH缓冲剂的农业组合物
公开(公告)号：WO2012083453A1
公开(公告)日：2012-06-28
申请号：PCT/CA2011/050791
申请日：2011-12-21
申请人： NUTRIAG LTD. , TANAKA, Kelly S. E. , BLOOMBERG, Martin David
发明人： TANAKA, Kelly S. E. , BLOOMBERG, Martin David
IPC分类号： A01N25/00 , G01N31/22 , C09B11/04
CPC分类号： A01N25/02 , A01N25/22
摘要： The invention provides a composition in concentrated form ("the concentrate") for dilution with water in the preparation of an agricultural composition for application to crops, soil or animals, comprising a carbohydrate-based pH modifying agent and a pH indicator. The agricultural composition comprises an agricultural chemical whose agricultural activity varies with the pH of the water. The proportions of the pH indicator and the pH modifying agent in the concentrate are selected so that when the concentrate is diluted with an appropriate amount of water, the pH indicator indicates visually by colouration of the composition, whether or not the pH of the water is suitable for acceptable agricultural activity of the chemical. The invention also provides a process for preparing the agricultural composition by mixing the concentrate with water, and adding the agricultural chemical to the composition, if it is not already present in the concentrate.
摘要翻译：本发明提供了一种浓缩形式的组合物（“浓缩物”），用于在制备用于施用于作物，土壤或动物的农业组合物中用水稀释，其包含基于碳水化合物的pH调节剂和pH指示剂。农业组合物包括农业活动随着水的pH而变化的农药。选择浓缩物中的pH指示剂和pH调节剂的比例，使得当浓缩物用适量的水稀释时，pH指示剂通过组合物着色指示，无论水的pH是否为适合化学品的可接受的农业活动。本发明还提供了一种通过将浓缩物与水混合并将农药添加到组合物中（如果它还没有存在于浓缩物中）来制备农业组合物的方法。

6. 发明申请

WO2011019839A3 GLYCOPEPTIDE AND LIPOGLYCOPEPTIDE ANTIBIOTICS WITH IMPROVED SOLUBILITY 审中-公开
标题翻译：具有改善溶解性的糖苷类和脂蛋白抗体
公开(公告)号：WO2011019839A3
公开(公告)日：2011-06-23
申请号：PCT/US2010045201
申请日：2010-08-11
申请人： RAFAI FAR ADEL , TANAKA KELLY , DIETRICH EVELYNE , REDDY RANGA , KANG TING , MEDICINES CO
发明人： RAFAI FAR ADEL , TANAKA KELLY , DIETRICH EVELYNE , REDDY RANGA , KANG TING
IPC分类号： C07K5/12 , A61K38/12 , A61K38/14 , A61P31/04 , C07K7/06
CPC分类号： C07K9/008 , A61K38/12 , A61K38/14 , A61K45/06 , A61K47/48038 , A61K47/48046 , A61K47/48215 , A61K47/542 , A61K47/543 , A61K47/60 , A61K2300/00
摘要： The invention relates to derivatives of glycopeptide and lipoglycopeptide antibiotics possessing an altered ionization state with respect to the parent glycopeptide or lipoglycopeptide antibiotic, and having the ability to be regenerated as the parent glycopeptide or lipoglycopeptide antibiotic under physiological conditions. These compounds are useful as antibiotics for the prevention and/or the treatment of bacterial infections.
摘要翻译：本发明涉及相对于母体糖肽或脂多糖抗生素具有改变的电离状态的糖肽和脂多糖抗生素的衍生物，并且具有在生理条件下作为母体糖肽或脂多糖抗生素再生的能力。这些化合物可用作预防和/或治疗细菌感染的抗生素。

7. 发明申请

WO2010019511A2 PHOSPHONATED RIFAMYCINS AND USES THEREOF FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS 审中-公开
标题翻译：磷酸缓冲溶液及其用于预防和治疗骨和关节感染的用途
公开(公告)号：WO2010019511A2
公开(公告)日：2010-02-18
申请号：PCT/US2009/053295
申请日：2009-08-10
申请人： DIETRICH, Evelyne , REDDY, Ranga , TANAKA, Kelly , KANG, Ting , LAFONTAINE, Yanick , RAFAI FAR, Adel , TARGANTA THERAPEUTICS CORP.
发明人： DIETRICH, Evelyne , REDDY, Ranga , TANAKA, Kelly , KANG, Ting , LAFONTAINE, Yanick , RAFAI FAR, Adel
IPC分类号： C07F9/6561 , A61K31/675 , A61K31/5383 , A61P19/00 , A61P31/04
CPC分类号： C07F9/6561 , A61K31/675 , A61K47/548
摘要： The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
摘要翻译：本发明涉及膦酸化的利福霉素，以及制备和使用这些化合物的方法。这些化合物可用作抗生素用于预防和/或治疗骨和关节感染，特别是用于预防和/或治疗骨髓炎。

8. 发明申请

WO2007138381A3 PHOSPHONATED OXAZOLIDINONES AND USES THEREOF FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS 审中-公开
标题翻译：磷酸二氢吲哚酮及其用于预防和治疗骨和关节感染的用途
公开(公告)号：WO2007138381A3
公开(公告)日：2008-04-17
申请号：PCT/IB2006004233
申请日：2006-10-13
申请人： TARGANTA THERAPEUTICS INC , DELORME DANIEL , HOUGHTON TOM , LAFONTAINE YANICK , TANAKA KELLY , DIETRICK EVELYNE , KANG TING , RAFAI FAR ADEL
发明人： DELORME DANIEL , HOUGHTON TOM , LAFONTAINE YANICK , TANAKA KELLY , DIETRICK EVELYNE , KANG TING , RAFAI FAR ADEL
IPC分类号： C07F9/38 , A61K31/496 , A61K31/663 , A61K31/675 , A61P19/08 , A61P31/00
CPC分类号： C07F9/65583
摘要： The invention relates to bisphosphonated derivatives of oxazolidmones represented by formula (I) where A is an oxazolidmone antimicrobial molecule, B is a phosphonated group and L is bond or a linker for covalently coupling B to A These derivatives are useful as antibiotics for the prevention and/or treatment of bone and joint infections, especially osteomyelitis [B- L-] n - A (I)
摘要翻译：本发明涉及由式（I）表示的恶唑烷酮的双膦酸衍生物，其中A是恶唑烷酮抗微生物分子，B是膦酸化基团，L是键或用于共价偶联B与A的连接体。这些衍生物可用作抗生素用于预防和 /或治疗骨和关节感染，特别是骨髓炎[B] - （A）

9. 发明申请

WO2007138381A2 PHOSPHONATED OXAZOLIDINONES AND USES THEREOF FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS 审中-公开
标题翻译：磷酸二氢吲哚酮及其用于预防和治疗骨和关节感染的用途
公开(公告)号：WO2007138381A2
公开(公告)日：2007-12-06
申请号：PCT/IB2006/004233
申请日：2006-10-13
申请人： TARGANTA THERAPEUTICS INC. , DELORME, Daniel , HOUGHTON, Tom , LAFONTAINE, Yanick , TANAKA, Kelly , DIETRICK, Evelyne , KANG, Ting , RAFAI FAR, Adel
发明人： DELORME, Daniel , HOUGHTON, Tom , LAFONTAINE, Yanick , TANAKA, Kelly , DIETRICK, Evelyne , KANG, Ting , RAFAI FAR, Adel
CPC分类号： C07F9/65583
摘要： The invention relates to phosphonated derivatives of oxazolidinones. These compounds are useful as antibiotics for prevention and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
摘要翻译：本发明涉及恶唑烷酮的膦酸化衍生物。这些化合物可用作预防和/或治疗骨和关节感染的抗生素，特别是用于预防和/或治疗骨髓炎。

10. 发明申请

WO2007017762A2 PHOSPHONATED FLUOROQUINOLONES, ANTIBACTERIAL ANALOGS THEREOF, AND METHODS FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS 审中-公开
标题翻译：磷酸荧光素，其抗菌模型及其预防和治疗骨和关节感染的方法
公开(公告)号：WO2007017762A2
公开(公告)日：2007-02-15
申请号：PCT/IB2006/002922
申请日：2006-04-21
申请人： TARGANTA THERAPEUTICS INC. , DELORME, Daniel , HOUGHTON, Tom , KANG, Ting , TANAKA, Kelly , LAFONTAINE, Yanick , DIETRICH, Evelyne , RAFI FAR, Adel
发明人： DELORME, Daniel , HOUGHTON, Tom , KANG, Ting , TANAKA, Kelly , LAFONTAINE, Yanick , DIETRICH, Evelyne , RAFI FAR, Adel
CPC分类号： C07F9/65586 , C07F9/65583 , C07F9/6561
摘要： The present invention relates to phosphonated fluoroquinolones, antibacterial analogs thereof, and methods of using such compounds. These compounds are useful as antibotics for prevention and/or the treatment of bone and joint infections, especially for the prevention and/or treatment of osteomyelitis.
摘要翻译：本发明涉及膦酸化氟喹诺酮类，其抗菌类似物和使用这些化合物的方法。这些化合物可用作预防和/或治疗骨和关节感染的抗生素，特别是用于预防和/或治疗骨髓炎。

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