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1. 发明授权

US06294528B1 Carbapenem antibacterial compounds, compositions containing such compounds and method of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US06294528B1
公开(公告)日：2001-09-25
申请号：US09338644
申请日：1999-06-23
申请人： Timothy A. Blizzard , Robert R. Wilkening , Ronald W. Ratcliffe
发明人： Timothy A. Blizzard , Robert R. Wilkening , Ronald W. Ratcliffe
IPC分类号： C07D47714
CPC分类号： C07D477/14
摘要： Compounds of formula I: as well as pharmaceutically acceptable salts therefor and compositions useful as carbapenem antibacterial agents are disclosed.
摘要翻译：公开了式I化合物及其药学上可接受的盐和可用作碳青霉烯类抗菌剂的组合物。

2. 发明授权

US06265395B1 Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US06265395B1
公开(公告)日：2001-07-24
申请号：US09338638
申请日：1999-06-23
申请人： Timothy A. Blizzard , Ronald W. Ratcliffe
发明人： Timothy A. Blizzard , Ronald W. Ratcliffe
IPC分类号： C07D47714
CPC分类号： C07D477/14
摘要： Compounds of formula I: as well as pharmaceutically acceptable salts thereof useful as carbapenem antibacterial agents are disclosed.
摘要翻译：公开了式I化合物及其可药用盐作为碳青霉烯类抗菌剂。

3. 发明授权

US06251890B1 Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US06251890B1
公开(公告)日：2001-06-26
申请号：US09524355
申请日：2000-03-13
申请人： Timothy A. Blizzard , Ronald W. Ratcliffe , Jerry D. Morgan, II , Robert R. Wilkening
发明人： Timothy A. Blizzard , Ronald W. Ratcliffe , Jerry D. Morgan, II , Robert R. Wilkening
IPC分类号： C07D47714
CPC分类号： C07D477/14
摘要： The present invention relates to carbapenem antibacterial agents of formula I: or a pharmaceutically acceptable salt thereof, wherein: R2 represents: in formula I, in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH2 group. The naphthosultam is further substituted with various substituent groups including at least one cationic group.
摘要翻译：本发明涉及式I的碳青霉烯类抗生素或其药学上可接受的盐，其中：R2表示：在式I中，其中碳青霉烯核在2-位被通过CH2基团连接的萘磺酰胺代替。萘磺叠胺进一步被包括至少一个阳离子基团的各种取代基取代。

4. 发明授权

US6008212A Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US6008212A
公开(公告)日：1999-12-28
申请号：US168422
申请日：1998-10-08
申请人： Ronald W. Ratcliffe , Timothy A. Blizzard
发明人： Ronald W. Ratcliffe , Timothy A. Blizzard
IPC分类号： C07D477/14 , A61K31/395 , C07D487/04
CPC分类号： C07D477/14
摘要： Compounds of formula I: ##STR1## as well as pharmaceutically acceptable salts thereof are disclosed. R.sup.2 is H and R.sup.3 is C1-3 alkyl, or R.sup.2 and R.sup.3 taken in combination represent C.sub.1-3 alkylidene. Pharmaceutical compositions and methods of treatment are also included. The compounds are useful against methicillin resistant staphylococci (MRSA).
摘要翻译：公开了式I化合物及其药学上可接受的盐。 R2是H，R3是C1-3烷基，R2和R3组合表示C1-3亚烷基。还包括药物组合物和治疗方法。该化合物可用于耐甲氧西林葡萄球菌（MRSA）。

5. 发明授权

US5756725A Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US5756725A
公开(公告)日：1998-05-26
申请号：US825786
申请日：1997-04-08
申请人： Robert R. Wilkening , Ronald W. Ratcliffe , Timothy A. Blizzard
发明人： Robert R. Wilkening , Ronald W. Ratcliffe , Timothy A. Blizzard
IPC分类号： C07D20060101 , C07D477/14 , C07D519/00 , C07D521/00 , C07D487/04 , A61K31/395
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D477/14
摘要： The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH.sub.2 group. The naphthosultam is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula I: ##STR1## Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明涉及碳青霉烯类抗菌剂，其中碳青霉烯核在2-位被用CH2链连接的萘磺酰胺代替。萘磺叠胺进一步被包括至少一个阳离子基团的各种取代基取代。化合物由式I表示：还包括药物组合物和使用方法。

6. 发明授权

US5496816A Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US5496816A
公开(公告)日：1996-03-05
申请号：US359770
申请日：1994-12-20
申请人： Timothy A. Blizzard , Ronald W. Ratcliffe , Sherman T. Waddell , Sandra P. Szumiloski , Robert R. Wilkening , Kenneth J. Wildonger
发明人： Timothy A. Blizzard , Ronald W. Ratcliffe , Sherman T. Waddell , Sandra P. Szumiloski , Robert R. Wilkening , Kenneth J. Wildonger
IPC分类号： C07D477/00 , A61K31/397 , A61K31/42 , A61K31/425 , A61K31/495 , A61P31/04 , C07D477/20 , A61K31/40 , C07D487/04
CPC分类号： C07D477/20
摘要： Carbapenems of the formula: ##STR1## are disclosed as useful antibacterial agents. Pharmaceutical compositions and methods of use are also disclosed.
摘要翻译：以下公式的碳青霉烯类似物：作为有用的抗菌剂被公开。还公开了药物组合物和使用方法。

7. 发明授权

US06291448B1 Carbapenem antibacterial compounds, compositions containing such compounds and method of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US06291448B1
公开(公告)日：2001-09-18
申请号：US09338640
申请日：1999-06-23
申请人： Timothy A. Blizzard , Robert R. Wilkening , Ronald W. Ratcliffe
发明人： Timothy A. Blizzard , Robert R. Wilkening , Ronald W. Ratcliffe
IPC分类号： C07D47714
CPC分类号： C07D477/14
摘要： Compounds of formula I: as well as pharmaceutically acceptable salts thereof useful as carbapenam antibacterial agents are disclosed wherein X is CR2R2, NR2, or O.
摘要翻译：公开了式I化合物及其可药用盐作为碳青霉烯抗菌剂，其中X为CR2R2，NR2或O.

8. 发明授权

US06346526B1 Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US06346526B1
公开(公告)日：2002-02-12
申请号：US09338646
申请日：1999-06-23
申请人： Timothy A. Blizzard , Kevin D. Dykstra , Ronald W. Ratcliffe
发明人： Timothy A. Blizzard , Kevin D. Dykstra , Ronald W. Ratcliffe
IPC分类号： C07D47714
CPC分类号： C07D477/14
摘要： Compounds of formula I: as well as pharmaceutically acceptable salts thereof useful as carbapenem antibacterial agents are disclosed wherein X is CH2 or C═O.
摘要翻译：公开了式I化合物及其可药用盐作为碳青霉烯类抗菌剂，其中X为CH 2或C = O。

9. 发明授权

US06346525B1 Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US06346525B1
公开(公告)日：2002-02-12
申请号：US09338639
申请日：1999-06-23
申请人： Timothy A. Blizzard , Ronald W. Ratcliffe , Sherman T. Waddell , Jerry D. Morgan, II
发明人： Timothy A. Blizzard , Ronald W. Ratcliffe , Sherman T. Waddell , Jerry D. Morgan, II
IPC分类号： C07D47714
CPC分类号： C07D477/14
摘要： Compounds of formula I: as well as pharmaceutically acceptable salts thereof and compositions useful as carbapenem antibacterial agents are disclosed.
摘要翻译：公开了式I化合物及其药学上可接受的盐和可用作碳青霉烯类抗菌剂的组合物。

10. 发明授权

US5140030A 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids 失效
标题翻译： 2-氮杂取代的1-碳代萘二烯-2-烯-3-羧酸
公开(公告)号：US5140030A
公开(公告)日：1992-08-18
申请号：US569257
申请日：1990-08-16
申请人： Burton G. Christensen , Ronald W. Ratcliffe , John C. Chabala
发明人： Burton G. Christensen , Ronald W. Ratcliffe , John C. Chabala
IPC分类号： C07D477/22 , C07F9/6561
CPC分类号： C07F9/65611 , C07D477/22 , Y02P20/55
摘要： Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids. I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, dialkylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of I from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: ##STR1## wherein R.sup.16 is H or CH.sub.3, preferably beta-methyl; R.sup.6, and R.sup.7 are independently hydrogen, linear, branched or cyclic C.sub.1 -C.sub.5 alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino, wherein R.sup.6 and R.sup.7 taken together can also be C.sub.2 -C.sub.4 alkylidene, similarly substituted; with the proviso that both R.sup.6 and R.sup.7 are not unsubstituted alkyl, R.sup.1 and R.sup.2 are, inter alia, hydrogen, alkyl, acyl, and can be joined to form a ring comprising 3 to 7 atoms; R.sup.a is hydrogen, a salt cation, a removable protecting group, or a pharmaceutically acceptable ester moiety.Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
摘要翻译：披露的是2-氮杂取代的1-碳代萘二烯-2-烯-3-羧酸。 I，其中通用2-氮杂基团包括可用作抗生素的叠氮基，酰氨基，氨基，烷基氨基，二烷基氨基，三唑基，三唑啉基，氮丙啶基及其药学上可接受的盐，酯，酸酐和酰胺衍生物。还公开了通过2-叠氮中心中间体III从已知的适当取代的双环酮酯II制备I的方法：其中R 16是H或CH 3，优选β- 甲基; R 6和R 7独立地是氢，直链，支链或环状的C 1 -C 5烷基，其可以被氟，羟基，保护的羟基，亚磺氧基，氨基，保护的氨基取代，其中R 6和R 7一起也可以是C 2 -C 4亚烷基，同样取代; 条件是R6和R7都不是未取代的烷基，R1和R2特别是氢，烷基，酰基，并且可以连接形成包含3至7个原子的环; Ra是氢，盐阳离子，可除去的保护基或药学上可接受的酯部分。还公开了制备这些化合物的方法; 包含这些化合物的药物组合物; 和治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。

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