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1. 发明申请

WO2011143497A1 AMINOGLYCOSIDE DERIVATIVES 审中-公开
标题翻译：氨基胆甾醇衍生物
公开(公告)号：WO2011143497A1
公开(公告)日：2011-11-17
申请号：PCT/US2011/036344
申请日：2011-05-12
申请人： REMPEX PHARMACEUTICALS, INC. , GLINKA, Tomasz, W. , RODNY, Olga
发明人： GLINKA, Tomasz, W. , RODNY, Olga
IPC分类号： C07H15/234 , A61P31/00 , C07H15/236 , A61K31/7036 , A61P31/04
CPC分类号： C07H15/236
摘要： The present invention relates to antimicrobial and antibiotic aminoglycoside derivatives. The compounds of the present application have the following chemical structures. The invention also relates to compositions, methods of preparation and methods of treatment of bacterial infections using the above aminoglycoside derivative.
摘要翻译：本发明涉及抗微生物和抗生素氨基糖苷衍生物。本申请的化合物具有以下化学结构。本发明还涉及使用上述氨基糖苷衍生物的组合物，制备方法和治疗细菌感染的方法。

2. 发明申请

WO2007079010A2 CARBONATES OF FENICOL ANTIBIOTICS 审中-公开
标题翻译：芬诺抗菌素的碳酸盐
公开(公告)号：WO2007079010A2
公开(公告)日：2007-07-12
申请号：PCT/US2006048929
申请日：2006-12-20
申请人： SCHERING PLOUGH LTD , GLINKA TOMASZ W , SCHUSTER DALE EDWARD , CELLY CHANDER SHEKHER , SIMMONS ROBERT D , ZHANG JASON
发明人： GLINKA TOMASZ W , SCHUSTER DALE EDWARD , CELLY CHANDER SHEKHER , SIMMONS ROBERT D , ZHANG JASON
IPC分类号： C07C233/18 , A61K31/16 , C07C317/32 , C07D213/40
CPC分类号： C07C317/32 , A61K31/222 , A61K31/265 , A61K31/42 , A61K31/433 , A61K31/44 , A61K45/06 , C07B2200/07 , C07C233/18 , C07C2601/02 , C07C2601/14 , C07D213/40 , C07D213/84 , A61K2300/00
摘要： Novel fenicol compounds having useful properties as antibiotic prodrugs, are provided, together with methods of making and using these new compounds.
摘要翻译：提供了具有作为抗生素前药的有用性质的新型芬西醇化合物，以及制备和使用这些新化合物的方法。

3. 发明申请

WO2007079010A3 CARBONATES OF FENICOL ANTIBIOTICS 审中-公开
公开(公告)号：WO2007079010A3
公开(公告)日：2007-07-12
申请号：PCT/US2006/048929
申请日：2006-12-20
申请人： SCHERING-PLOUGH LTD. , GLINKA, Tomasz, W. , SHUSTER, Dale, Edward , CELLY, Chander, Shekher , SIMMONS, Robert, D. , ZHANG, Jason
发明人： GLINKA, Tomasz, W. , SHUSTER, Dale, Edward , CELLY, Chander, Shekher , SIMMONS, Robert, D. , ZHANG, Jason
IPC分类号： C07C233/18 , C07C317/32 , C07D213/40 , A61K31/16 , A61P31/04
摘要： The invention relates to carbonate derivatives of fenicol compounds of formulae I and II, wherein the variables are as defined in the claims, having useful properties as antibiotic prodrugs, together with methods of making and using these compounds.

4. 发明申请

WO2008076259A1 WATER-SOLUBLE PRODRUGS OF FLORFENICOL AND ITS ANALOGS 审中-公开
标题翻译：佛罗里达水溶性物质及其类似物
公开(公告)号：WO2008076259A1
公开(公告)日：2008-06-26
申请号：PCT/US2007/025326
申请日：2007-12-11
申请人： SCHERING-PLOUGH LTD. , GLINKA, Tomasz, W. , ZHANG, Jason
发明人： GLINKA, Tomasz, W. , ZHANG, Jason
IPC分类号： C07C233/16 , C07C237/06 , C07D233/54 , A61K31/16 , A61K31/4166 , A61P31/04
CPC分类号： C07D233/60 , C07C317/32 , C07D233/54 , C07K5/06191
摘要： The present invention discloses certain novel prodrugs of florfenicol and/or of florfenicol analogs, including prodrugs of salts pharmaceutically acceptable salts of florfenicol and its analogs, including nitrogen-containing esters of the secondary alcohol group of florfenicol and of its analogs, and pharmaceutically acceptable salts thereof, compositions containing them, and methods of administering them to subjects. In particular embodiments the prodrugs are sufficiently water-soluble to serve the functions needed of a water-soluble prodrug of florfenicol or of a water-soluble prodrug of a florfenicol analog. A certain subclass of the compounds also possesses the hydrolytic stability needed to maintain the prodrug in solution in the subject's system until appropriate conditions exist when the prodrug can hydrolyze, releasing florfenicol or the florfenicol analog in question.
摘要翻译：本发明公开了氟苯尼考和/或氟苯尼考类似物的某些新型前药，包括氟代苯尼醇及其类似物的药学上可接受的盐的前药，包括氟苯尼考及其类似物的仲醇基的含氮酯和其可药用盐含有它们的组合物，以及将它们给予受试者的方法。在具体实施方案中，前药具有足够的水溶性，以用于氟苯尼考或氟苯尼考类似物的水溶性前药的水溶性前药所需的功能。化合物的某一亚类也具有将前体药物保持在受试者系统的溶液中所需的水解稳定性，直到前药可以水解，释放所讨论的氟苯尼考或氟苯尼考类似物时才有适当的条件。

5. 发明申请

WO2008076256A1 WATER-SOLUBLE PRODRUGS OF CHLORAMPHENICOL, THIAMPHENICOL, AND ANALOGS THEREOF 审中-公开
标题翻译：氯化氢的可溶性原料，其他类似物及其类似物
公开(公告)号：WO2008076256A1
公开(公告)日：2008-06-26
申请号：PCT/US2007/025319
申请日：2007-12-11
申请人： SCHERING-PLOUGH LTD. , GLINKA, Tomasz, W.
发明人： GLINKA, Tomasz, W.
IPC分类号： C07C317/32 , C07D233/56 , A61K31/18 , A61P31/04 , A61P31/10
CPC分类号： C07C317/32 , C07D233/60
摘要： The present invention discloses prodrugs of chloramphenicol, thiamphenicol and their analogs, as well as pharmaceutically acceptable salts thereof, including nitrogen-containing esters of both alcohol groups. These prodrugs have the Formula (I), in which R, A a , L l , M m , X x , Y and R 3 are as defined in the claims. In certain embodiments these prodrugs are sufficiently water-soluble to serve the functions needed of a prodrug of chloramphenicol, thiamphenicol and their analogs. In one embodiment, a certain subclass of the compounds also possess the hydrolytic stability needed to maintain the prodrug in solution in the subject's system until appropriate conditions exist when the prodrug can hydrolyze, releasing the active compound in question.
摘要翻译：本发明公开了氯霉素，甲砜霉素及其类似物的前药，以及其药学上可接受的盐，包括两个醇基的含氮酯。这些前药具有式（I），其中R 1，A 2，A 1，M m，X x， SUB，Y和R 3如权利要求中所定义。在某些实施方案中，这些前药具有足够的水溶性，以满足氯霉素，甲砜霉素及其类似物前药所需的功能。在一个实施方案中，化合物的某些亚类还具有将前药保持在受试者系统溶液中所需的水解稳定性，直到当前药可水解，释放所讨论的活性化合物时，存在适当的条件。

6. 发明申请

WO2004098500A3 CARBACEPHEM ss-LACTAM ANTIBIOTICS 审中-公开
标题翻译： CARBACEPHEM ss-LACTAM抗生素
公开(公告)号：WO2004098500A3
公开(公告)日：2005-06-02
申请号：PCT/US2004013054
申请日：2004-04-27
申请人： TRINE PHARMACEUTICALS INC , GLINKA TOMASZ W , HECKER SCOTT J
发明人： GLINKA TOMASZ W , HECKER SCOTT J
IPC分类号： A61K20060101 , A61K31/4353 , A61K31/545 , A61P31/04 , C07D463/00 , C07D463/22 , C07D501/14
CPC分类号： C07K5/0827 , A61K31/4353 , C07D463/22
摘要： The present invention relates to carbacephem antibiotics and pharmaceutically acceptable salts thereof useful for the treatment of bacterial infections, in particular infections caused by methicillin-resistant Staphylococcus spp. bacteria.
摘要翻译：本发明涉及用于治疗细菌感染，特别是由耐甲氧西林葡萄球菌属引起的感染的卡巴泼姆抗生素及其药学上可接受的盐。菌。

7. 发明申请

WO2004098500A2 CARBACEPHEM ß-LACTAM ANTIBIOTICS 审中-公开
标题翻译： CARBACEPHEM ss-LACTAM抗生素
公开(公告)号：WO2004098500A2
公开(公告)日：2004-11-18
申请号：PCT/US2004/013054
申请日：2004-04-27
申请人： TRINE PHARMACEUTICALS, INC. , GLINKA, Tomasz, W. , HECKER, Scott, J.
发明人： GLINKA, Tomasz, W. , HECKER, Scott, J.
IPC分类号： A61K
CPC分类号： C07K5/0827 , A61K31/4353 , C07D463/22
摘要： The present invention relates to carbacephem antibiotics and pharmaceutically acceptable salts thereof useful for the treatment of bacterial infections, in particular infections caused by methicillin-resistant Staphylococcus spp. bacteria.
摘要翻译：本发明涉及用于治疗细菌感染，特别是由甲氧西林耐药性葡萄球菌属引起的感染的碳霉素抗生素及其药学上可接受的盐。菌。

8. 发明申请

WO0217854A3 CEPHALOSPORIN ANTIBIOTICS AND PRODRUGS THEREOF 审中-公开
标题翻译： CEPHALOSPORIN抗生素及其制剂
公开(公告)号：WO0217854A3
公开(公告)日：2002-06-13
申请号：PCT/US0126628
申请日：2001-08-23
申请人： GLINKA TOMASZ W
发明人： GLINKA TOMASZ W
IPC分类号： C07D501/59 , A61K31/546 , A61P31/04 , C07D501/00
CPC分类号： C07D501/00
摘要： The present invention relates to novel cephalosporin antibiotics, prodrugs thereof and pharmacologically acceptable salts of either, which are active against a wide spectrum of bacteria that are resistant to present clinical beta-lactam antibiotics.
摘要翻译：本发明涉及新型头孢菌素抗生素，其前药和药理学上可接受的盐，其可以对抗临床β-内酰胺抗生素的广泛细菌活性。

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