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    6-(1-hydroxyethyl)-2-carbamimidoyl-pen-2-em-3-carboxylic acids
    1.
    发明授权
    6-(1-hydroxyethyl)-2-carbamimidoyl-pen-2-em-3-carboxylic acids 失效
    6-（1-羟基乙基）-2-氨甲脒基 - 二氧戊环-3-羧酸

    公开(公告)号：US4650794A

    公开(公告)日：1987-03-17

    申请号：US373088

    申请日：1982-04-29

    申请人： Burton G. Christensen ,  Frank P. DiNinno ,  William J. Leanza ,  Ronald W. Ratcliffe

    发明人： Burton G. Christensen ,  Frank P. DiNinno ,  William J. Leanza ,  Ronald W. Ratcliffe

    IPC分类号： C07D499/88 ,  C07D499/00 ,  A61K31/425

    CPC分类号： C07D499/88

    摘要： Disclosed are 6-(1-hydroxyethyl)-2-carbamimidoyl-pen-2-em-3-carboxylic acids (I) having the representative structure: ##STR1## wherein: A is a direct, single bond connecting the indicated S and C atoms, or A is a cyclic or acyclic connecting group selected, inter alia, from alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl; R.sup.1 and R.sup.2, which define the carbamimidoyl function, are, inter alia, independently selected from hydrogen, alkyl, aryl, alkoxy, amino; additionally, said carbamimidoyl is characterized by cyclic structures achieved by the joinder of the two nitrogen atoms via their substituents and by their joinder to connecting group A; additionally, "carbamimidiums" are disclosed by quaternization of one of the nitrogen atoms of said carbamimidoyl. Such compounds as well as 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 such compounds and compositions when an antibiotic effect is indicated.

    摘要翻译： 公开了具有以下代表性结构的6-（1-羟基乙基）-2-氨基甲脒基 - 二-2-甲基-3-羧酸（I）：其中：A是连接所指示的S和 C原子或A是环状或无环连接基团，特别是选自烷基，环烷基，芳基，杂芳基，杂烷基; 定义氨基甲酰基官能团的R 1和R 2尤其独立地选自氢，烷基，芳基，烷氧基，氨基; 另外，所述的氨基甲脒基的特征在于通过两个氮原子通过它们的取代基并通过它们与连接基团A的连接而实现的环状结构; 此外，“氨基甲酰胺”通过所述氨甲脒基的氮原子之一的季铵化来公开。 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，包括当指出抗生素效应时施用这些化合物和组合物。

    6-substituted-2-carbaminidoyl-pen-2-em-3-carboxylic acids
    2.
    发明授权
    6-substituted-2-carbaminidoyl-pen-2-em-3-carboxylic acids 失效
    6-取代-2-氨基甲酰基 - 二氧戊环-3-羧酸

    公开(公告)号：US4748162A

    公开(公告)日：1988-05-31

    申请号：US605338

    申请日：1984-04-30

    申请人： William J. Leanza ,  Burton G. Christensen ,  Frank P. DiNinno ,  Ronald W. Ratcliffe

    发明人： William J. Leanza ,  Burton G. Christensen ,  Frank P. DiNinno ,  Ronald W. Ratcliffe

    IPC分类号： C07D499/88 ,  C07D499/00 ,  A61K31/425

    CPC分类号： C07D499/88

    摘要： Disclosed are 6-substituted-2-carbamimidoyl-pen-2-em-3-carboxylic acids (I) having the representative structure: ##STR1## wherein R.sup.6, and R.sup.7 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkoxyl, halo, OH, COOH, alkenyl, aryl and aralkyl; A is a direct, single bond connecting the indicated S and C atoms, or A is a cyclic or acyclic connecting group selected, inter alia, from alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl; R.sup.1 and R.sup.2, which define the carbamimidoyl function, are, inter alia, independently selected from hydrogen, alkyl, aryl; additionally, said carbamimidoyl is characterized by cyclic structures achieved by the joinder of the two nitrogen atoms via their substituents and by their joinder to connecting group A; additionally, "carbamimidiums" are disclosed by quarternization of one of the nitrogen atoms of said carbamimidoyl. Such compounds as well as 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 such compounds and compositions when an antibiotic effect is indicated.

    摘要翻译： 公开了具有以下代表性结构的6-取代-2-氨基甲脒基 - 二-2-碳-3-羧酸（I）：其中R 6和R 7尤其独立地选自氢 烷基，烷氧基，卤素，OH，COOH，烯基，芳基和芳烷基; A是连接指示的S和C原子的直接的单键，或A是特别是选自烷基，环烷基，芳基，杂芳基，杂烷基的环状或无环连接基团; 定义氨基甲酰基官能团的R 1和R 2尤其独立地选自氢，烷基，芳基; 另外，所述的氨基甲脒基的特征在于通过两个氮原子通过它们的取代基并通过它们与连接基团A的连接而实现的环状结构; 此外，“氨基甲酰胺”是通过季铵化所述氨甲脒基的氮原子而公开的。 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，包括当指出抗生素效应时施用这些化合物和组合物。

    2-unsaturated alkylthio-pen-2-em-3-carboxylic acids
    3.
    发明授权
    2-unsaturated alkylthio-pen-2-em-3-carboxylic acids 失效
    2-不饱和烷硫基 - 笔-2-烯-3-羧酸

    公开(公告)号：US4675317A

    公开(公告)日：1987-06-23

    申请号：US460728

    申请日：1983-01-25

    申请人： Frank P. DiNinno ,  William J. Leanza ,  Ronald W. Ratcliffe ,  David A. Muthard

    发明人： Frank P. DiNinno ,  William J. Leanza ,  Ronald W. Ratcliffe ,  David A. Muthard

    IPC分类号： C07D205/09 ,  C07D205/095 ,  C07D499/88 ,  C07F7/18 ,  C07D499/00 ,  A61K31/425

    CPC分类号： C07D499/88 ,  C07D205/09 ,  C07D205/095 ,  C07F7/186

    摘要： Disclosed are 6- and 6,6-disubstituted-2-substituted thio-pen-2-em-3-carboxylic acids of the following structure: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from: hydrogen; substituted and unsubstituted: alkyl, cycloalkyl, halo, alkoxyl, alkenyl, aralkyl, aryl, heterocyclyl, heteroaryl, and heterocyclylalkyl; W is an electron withdrawing group, and, for example, is selected from: --COR.sup.5, --CN, SO.sub.2 C.sub.6 H.sub.5 ; R.sup.5 is hydrogen; substituted and unsubstituted: alkyl, aryl, aralkyl, heteroaryl, heterocyclyl, or heterocyclylalkyl; or R.sup.5 may be --OR.sup.6, --NR.sup.7 R.sup.8, and --SR.sup.9 ; wherein R.sup.6 is H; substituted and unsubstituted: alkyl, alkenyl, or a group which defines --CO.sub.2 R.sup.6 as a pharmaceutically acceptable ester wherein R.sup.6 is, for example, phthalidyl, or 5-methyl-2-oxo-1,3-dioxolen-4-ylmethyl; R.sup.7 and R.sup.8 are independently selected from: hydrogen; substituted and unsubstituted: alkyl, aralkyl, aryl, heterocyclyl, and heterocyclylalkyl; R.sup.9 is substituted and unsubstituted: alkyl, aralkyl, aryl, heterocyclyl, and heterocyclyclalkyl; R.sup.3 may also be W; n is 0 or 1; when the unsaturated moiety attached to the exocyclic sulfur atom is acetylenic, then R.sup.3 and R.sup.4 are nonexistent and W is as previously defined. Such compounds I are new and they and their pharmaceutically acceptable salt and ester derivatives are useful as antibiotics.

    摘要翻译： 公开了具有以下结构的6-和6,6-二取代-2-取代的硫代 - 笔 - 2-em-3-羧酸：其中：R1，R2，R3和R4独立地选自： 氢; 烷基，环烷基，卤素，烷氧基，烯基，芳烷基，芳基，杂环基，杂芳基和杂环基烷基; W是吸电子基团，例如，选自：-COR 5，-CN，SO 2 C 6 H 5; R5是氢; 取代和未取代的：烷基，芳基，芳烷基，杂芳基，杂环基或杂环基烷基; 或者R 5可以是-OR 6，-NR 7 R 8和-SR 9; 其中R6是H; 取代和未取代的：烷基，烯基或定义-CO 2 R 6作为药学上可接受的酯的基团，其中R 6是例如酞基或5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基甲基; R7和R8独立地选自：氢; 取代和未取代的：烷基，芳烷基，芳基，杂环基和杂环基烷基; R9是取代和未取代的：烷基，芳烷基，芳基，杂环基和杂环烷基; R3也可以是W; n为0或1; 当连接到环外硫原子上的不饱和部分是炔属时，则R3和R4不存在，W如前所定义。 这些化合物I是新的，它们及其药学上可接受的盐和酯衍生物可用作抗生素。

    Process for preparing substituted 2-thioxopenams and 2-substituted thiopenems
    4.
    发明授权
    Process for preparing substituted 2-thioxopenams and 2-substituted thiopenems 失效
    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。

    2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids
    7.
    发明授权
    2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids 失效
    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。

    2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids
    8.
    发明授权
    2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids 失效
    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。