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11. 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。

12. 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。

13. 发明授权

US6140318A 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：US6140318A
公开(公告)日：2000-10-31
申请号：US168622
申请日：1998-10-08
申请人： Lovji D. Cama , Robert R. Wilkening , Ronald W. Ratcliffe , Kenneth J. Wildonger , Wanying Sun
发明人： Lovji D. Cama , Robert R. Wilkening , Ronald W. Ratcliffe , Kenneth J. Wildonger , Wanying Sun
IPC分类号： A61P31/06 , C07D487/04 , A61K31/395 , A01N43/60 , C07D413/00 , C07D487/00
CPC分类号： C07D487/04
摘要： Compounds of formula I are disclosed. ##STR1## as well as pharmaceutically acceptable salts thereof. The naphthosultam is substituted with various substituent groups including at least one cationic group -A-Q-L-B.The carbapenems of the invention are effective against susceptible bacterial organisms, including methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and methicillin resistant coagulase negative Staphylococci (MRCNS).
摘要翻译：公开了式I化合物。以及其药学上可接受的盐。萘磺叠胺被包括至少一个阳离子基团-A-Q-L-B的各种取代基取代。本发明的碳青霉烯类药物对抗敏感细菌生物有效，包括耐甲氧西林金黄色葡萄球菌（MRSA），耐甲氧西林葡萄球菌（MRSE）和耐甲氧西林凝固酶阴性葡萄球菌（MRCNS）。

14. 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）。

15. 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。

16. 发明授权

US4783453A 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：US4783453A
公开(公告)日：1988-11-08
申请号：US97348
申请日：1987-09-08
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 , C07D487/04 , A61K31/40
CPC分类号： C07D477/22 , C07F9/65611 , 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-碳代萘二甲酸-2-烯-3-羧酸I，其中通用的2-氮杂基团包括叠氮基，酰氨基，氨基，烷基氨基，二烷基氨基，三唑基，三唑基，氮丙啶基及其药学上可接受的盐，可用作抗生素的酯，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。

17. 发明授权

US4739048A Process for the preparation of thienamycin and intermediates 失效
标题翻译：噻吩霉素和中间体的制备方法
公开(公告)号：US4739048A
公开(公告)日：1988-04-19
申请号：US754493
申请日：1985-07-12
申请人： Burton G. Christensen , Ronald W. Ratcliffe , Thomas N. Salzmann
发明人： Burton G. Christensen , Ronald W. Ratcliffe , Thomas N. Salzmann
IPC分类号： C07D205/08 , C07D477/04 , C07F7/10 , C07D487/04 , A61K31/40
CPC分类号： C07D205/08 , C07D477/04 , C07F7/10
摘要： Disclosed is a process for the total synthesis of thienamycin from L-aspartic acid via intermediate III: ##STR1##
摘要翻译：公开了一种通过中间体III从L-天冬氨酸全合成噻吩霉素的方法：其中R = H，封闭基团或盐阳离子

18. 发明授权

US4729993A Carbapenems and 1-methylcarbapenems having an externally alkylated mono- or bicyclic 2-quaternary heteroarylalkyl substituent 失效
标题翻译：具有外部烷基化单 - 或双环2-季杂芳基烷基取代基的碳青霉烯和1-甲基碳青霉烯
公开(公告)号：US4729993A
公开(公告)日：1988-03-08
申请号：US681179
申请日：1984-12-13
申请人： Burton G. Christensen , Ronald W. Ratcliffe , James V. Heck , Thomas N. Salzmann , David H. Shih
发明人： Burton G. Christensen , Ronald W. Ratcliffe , James V. Heck , Thomas N. Salzmann , David H. Shih
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61K31/44 , A61K31/495 , A61K31/53 , A61P31/04 , C07D477/14 , C07F7/18 , C07F9/6558 , C07D499/00 , A61K31/425
CPC分类号： C07D477/14 , C07F7/186 , C07F9/65583
摘要： Carbapenems having the formula: ##STR1## wherein ##STR2## is mono- or bicyclic quaternary heteroaryl, their preparation and antibiotic use are disclosed.
摘要翻译：具有以下分子式的碳青霉烯类似物：其中其中是单环或双环季铵杂芳基，其制备和抗生素使用。

19. 发明授权

US4610823A Process for preparing substituted 2-thioxopenams and 2-substituted thiopenems 失效
标题翻译：制备取代的2-硫代戊二酸和2-取代的硫代青霉烯的方法
公开(公告)号：US4610823A
公开(公告)日：1986-09-09
申请号：US460729
申请日：1983-01-25
申请人： Frank P. DiNinno , William J. Leanza , Ronald W. Ratcliffe
发明人： Frank P. DiNinno , William J. Leanza , Ronald W. Ratcliffe
IPC分类号： C07D205/08 , A61K31/397 , A61K31/425 , A61K31/43 , A61P31/04 , C07D205/09 , C07D205/095 , C07D499/04 , C07D499/42 , C07D499/44 , C07D499/88 , C07D499/897 , C07F1/10 , C07F3/14 , C07F5/00 , C07F7/18
CPC分类号： C07D205/09 , C07D205/095 , C07D499/88 , C07F7/1804 , Y02P20/55
摘要： Disclosed is a synthesis for preparing substituted 2-thioxopenams which are useful in the synthesis of penem antibiotics 7 which may be conducted in an enantiospecific manner; said process proceeds from azetidinone 1 via the azetidinone acetic ester 2, the 4-metallothiozetidinone 3, and the 4-dithiocarbonylazetidinone 4 to the substituted 2-thioxopenam 5: ##STR1## wherein: R.sup.6 and R.sup.7 are independently selected from: hydrogen; R.sup.6 NH-- (R.sup.6 is acyl or H); substituted and unsubstituted: alkyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, and cycloalkenyl; wherein said substituents are, inter alia: halo (chloro, bromo, fluoro, iodo), hydroxyl, cyano, carboxyl, amino, and the above-recited values for R.sup.6 and R.sup.7 ; in functional terms,R.sup.2 is a group which potentially forms a stable carbonium ion, for example: trityl (--C(C.sub.6 H.sub.5).sub.3),bis(p-methoxyphenyl)methyl, ##STR2## --2,4-dimethoxybenzyl, ##STR3## 2-(diphenyl)isopropyl, ##STR4## and the like; M is a thiophilic metal such as silver, thallium, mercury, or the like;and R.sup.1 is a protecting group such as allyl, p-nitrobenzyl or a biologically removable group (pharmaceutically acceptable ester moiety), for example: pivaloyloxymethyl, pivoloyloxyethyl, ethoxycarbonyloxymethyl, phthalidyl (5-methyl-2-oxo-1,3-dioxolen-4-yl)-; and X is a methyl leaving group such as phenoxy, p-chlorophenoxy, p-nitrophenoxy, phenylthio, alkylthio, alkoxy, chloro, or the like.R.sup.8 is inter alia, substituted and unsubstituted alkyl; the final penem products 7 are known, and their various embodiments are included by this definition.
摘要翻译：公开了用于制备可以以对映体特异性方式进行的penem抗生素7的合成的用于制备取代的2-硫代青霉烯的合成物; 所述方法从氮杂环丁酮1经由氮杂环丁酮乙酸酯2，4-金属硫代环丁酮3和4-二硫代羰基氮杂环丁酮4进行到取代的2-硫青霉素5，其中：R6 和R 7独立地选自：氢; R6NH-（R6是酰基或H）; 取代和未取代的：烷基，烯基，炔基，芳基，杂环基，杂芳基，环烷基和环烯基; 其中所述取代基特别是：卤素（氯，溴，氟，碘），羟基，氰基，羧基，氨基，以及R6和R7的上述值; 在功能上，R2是潜在形成稳定的碳鎓离子的基团，例如：三苯甲基（-C（C 6 H 5）3），双（对甲氧基苯基）甲基，2,4-二甲氧基苄基， 2-（二苯基）异丙基，等等; M是硫醇类金属如银，铊，汞等; R1为保护基团，例如烯丙基，对硝基苄基或生物可除去基团（药学上可接受的酯部分），例如：新戊酰氧基甲基，桥联合氧基乙基，乙氧基羰氧基甲基，邻苯二甲酰基（5-甲基-2-氧代-1,3-二氧杂环戊烯 - 吡啶-4-基） - ; X为甲基离去基团，例如苯氧基，对氯苯氧基，对硝基苯氧基，苯硫基，烷硫基，烷氧基，氯等。 R8尤其是取代和未取代的烷基; 最终的penem产品7是已知的，并且它们的各种实施例被该定义包括。

20. 发明授权

US4530841A 6- And 6,6-disubstituted-3-substituted amino-1-azabicyclo-[3.2.0]hept-2-en-7-one-2-carboxylic acid 失效
标题翻译： 6-和6,6-二取代-3-取代的氨基-1-氮杂双环[3.2.0]庚-2-烯-7-酮-2-羧酸
公开(公告)号：US4530841A
公开(公告)日：1985-07-23
申请号：US388311
申请日：1982-06-14
申请人： Burton G. Christensen , Ronald W. Ratcliffe
发明人： Burton G. Christensen , Ronald W. Ratcliffe
IPC分类号： C07D205/08 , C07D477/22 , C07F7/10 , C07F9/6561 , A61K31/40 , C07D487/04
CPC分类号： C07F7/10 , C07D205/08 , C07D477/22 , C07F9/65611
摘要： Disclosed are 6- and 6,6-disubstituted-3-substituted amino-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acids (I): ##STR1## wherein R.sup.1 and R.sup.2 are, inter alia, independently selected from the group consisting of hydrogen, substituted and unsubstituted: alkyl, aryl, and aralkyl; and R' and R" are independently selected from the group consisting of: H, substituted and unsubstituted alkyl and aralkyl, or together form a substituted or unsubstituted cyclic group.Such compounds and their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering compounds and compositions when an antibiotic effect is indicated.
摘要翻译：公开了6-和6,6-二取代-3-取代的氨基-1-氮杂双环[3.2.0]庚-2-烯-7-酮-2-羧酸（I）：其中R1和R2是尤其是独立地选自氢，取代和未取代的：烷基，芳基和芳烷基; 并且R'和R“独立地选自：H，取代和未取代的烷基和芳烷基，或一起形成取代或未取代的环状基团。这些化合物及其药学上可接受的盐，酯和酰胺衍生物可用作抗生素。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，其中包括当指出抗生素效应时施用化合物和组合物。

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