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    Penem derivatives
    1.
    发明授权
    Penem derivatives 失效
    Penem衍生物

    公开(公告)号：US4863914A

    公开(公告)日：1989-09-05

    申请号：US849387

    申请日：1986-04-08

    申请人： Ettore Perrone ,  Marco Alpegiani ,  Angelo Bedeschi ,  Franco Zarini ,  Giovanni Franceschi ,  Costantino D. Bruna

    发明人： Ettore Perrone ,  Marco Alpegiani ,  Angelo Bedeschi ,  Franco Zarini ,  Giovanni Franceschi ,  Costantino D. Bruna

    IPC分类号： C07D519/06 ,  A61K31/425 ,  A61K31/43 ,  A61K31/431 ,  A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61P31/04 ,  C07D499/00 ,  C07D499/04 ,  C07D499/06 ,  C07D499/861 ,  C07D499/88 ,  C07D499/897 ,  C07D519/00

    CPC分类号： C07D499/88

    摘要： Compounds of formula ##STR1## wherein R is hydrogen atom or C.sub.1 -C.sub.4 alkyl group optionally substituted from halogen atom or hydroxy group optionally protected, A is a Z, Z--O--C--O-- or Z--C)-- residue, wherein Z is phenylene, naphthylene, heterocyclediyl, C.sub.1 -C.sub.7 alkylene, C.sub.2 -C.sub.4 alkenylene, alkynylene, ##STR2## C.sub.3 -C.sub.8 cycloalkylene, aralkylene radical optionally substituted, and O.sup.(+) represents a group +NR.sub.1 R.sub.2 R.sub.3, wherein R.sub.1, R.sub.2 and R.sub.3 are each either:(i) a optionally substituted alkyl, aralkyl or aryl radical or(ii) R.sub.1 is as defined above under (i) and R.sub.2 and R.sub.3, taken together, represent an optionally substituted or fused heterocyclic radical, or(iii) R.sub.1, R.sub.2 and R.sub.3, taken together, represent an optionally substituted azonia-bicyclo or tricyclo radical, or(iv) R.sub.1, R.sub.2 and R.sub.3, taken together, represent an optionally substituted or fused pyridinium, pyrazinium, pyrazolium or pyridazinium radical, and the pharmaceutically or veterinarily acceptable salts thereof, are disclosed.A method of preparation is also provided. The compounds show high antibacterial activity.

    摘要翻译： 其中R是氢原子或任选被卤素原子或羟基取代的任选被保护的C 1 -C 4烷基的化合物，A是Z，ZOCO-或ZC）残基，其中Z是亚苯基，亚萘基，杂环基， C 1 -C 7亚烷基，C 2 -C 4亚烯基，亚炔基，C 3 -C 8亚环烷基，任选取代的亚芳基，O（+）表示基团+ NR 1 R 2 R 3，其中R 1，R 2和R 3各自为：（ⅰ） 任选取代的烷基，芳烷基或芳基，或（ii）R 1如（i）中所定义，R 2和R 3一起表示任选取代或稠合的杂环基，或（iii）R 1，R 2和R 3一起 代表任选取代的亚氮基 - 双环或三环基团，或（iv）R 1，R 2和R 3一起表示任选取代或稠合的吡啶鎓，吡嗪鎓，吡唑鎓或哒嗪鎓基，其药学或兽医学上可接受的盐是 披露 还提供了一种制备方法。 该化合物显示出高抗菌活性。

    Penem derivatives
    2.
    发明授权
    Penem derivatives 失效
    Penem衍生物

    公开(公告)号：US4837215A

    公开(公告)日：1989-06-06

    申请号：US849388

    申请日：1986-04-08

    申请人： Ettore Perrone ,  Marco Alpegiani ,  Angelo Bedeschi ,  Franco Zarini ,  Giovanni Franceschi ,  Costantino D. Bruna

    发明人： Ettore Perrone ,  Marco Alpegiani ,  Angelo Bedeschi ,  Franco Zarini ,  Giovanni Franceschi ,  Costantino D. Bruna

    IPC分类号： C07D519/06 ,  A61K31/425 ,  A61K31/43 ,  A61K31/435 ,  A61K31/44 ,  A61K31/535 ,  A61P31/04 ,  C07D499/00 ,  C07D499/88 ,  C07D499/897

    CPC分类号： C07D499/00

    摘要： Compounds of the following formula I ##STR1## wherein X represents a sulphur or an oxygen atom,R is hydrogen or a C.sub.1 -C.sub.4 alkyl group either unsubstituted or substituted by one or more substituents chosen from a free or protected hydroxy group and halogen atom;A is a Z, Z--O--CO-- or --Z--CO-- residue, whereinZ represents(a) an optionally substituted phenylene or naphthylene group,(b) an optionally substituted heterocyclediyl radical wherein the hetero ring is mono or bicyclic, saturated or unsaturated containing at least one heteroatom selected from the group of oxygen, sulphur and nitrogen;(c) an optionally substituted linear or branched C.sub.1 -C.sub.7 alkylene radical;(d) a C.sub.2 -C.sub.4 alkenylene or alkynylene group or a group of formula ##STR2## (e) an optionally substituted C.sub.3 -C.sub.8 cycloalkylene ring; (f) an aralkylene radical of the formula ##STR3## wherein n is 1, 2 or 3; andQ.sup.(+) represents a +NR.sub.1 R.sub.2 R.sub.3 group, wherein(i) R.sub.1, R.sub.2, R.sub.3, are each independently an optionally substituted alkyl, aralkyl or aryl radical; or p1 (ii) R.sub.1 is as defined above under (i) and R.sub.2, R.sub.3 taken together with the nitrogen atom represent an optionally substituted heterocyclic or fused heterocyclic radical; or(iii) R.sub.1, R.sub.2, R.sub.3, taken together with the nitrogen atom, represent an optionally substituted azoniabicyclo or azoniatricyclo radical; or(iv) R.sub.1, R.sub.2, R.sub.3, taken together with nitrogen atom, represent an optionally substituted pyridinium, pirazinium, pyrazolium, or pyridazinium radical, such radicals being optionally fused with one phenyl ring or with a 5-7 membered, saturated or unsaturated cycloaliphatic or heterocyclic ring,or a pharmaceutically or veterinarily acceptable salt thereof having high antibacterial activity.

    摘要翻译： 下式I的化合物其中X表示硫或氧原子，R是氢或未被取代或被一个或多个选自游离或保护的羟基的取代基取代的C 1 -C 4烷基， 卤素原子; A是Z，ZO-CO-或-Z-CO-残基，其中Z表示（a）任选取代的亚苯基或亚萘基，（b）任选取代的杂环二基，其中杂环是单或双环，饱和或 不饱和的含有至少一个选自氧，硫和氮的杂原子; （c）任选取代的直链或支链C 1 -C 7亚烷基; （d）C 2 -C 4亚链烯基或亚炔基或式（A）的基团：（e）任选取代的C 3 -C 8亚环烷基环; （f）下式的芳亚烷基：其中n为1,2或3; 并且Q（+）表示+ NR 1 R 2 R 3基团，其中（i）R 1，R 2，R 3各自独立地为任选取代的烷基，芳烷基或芳基; 或p1（ii）R1如上文（i）和（R2）中所定义，R3与氮原子一起表示任选取代的杂环或稠合杂环基; 或（iii）与氮原子一起的R 1，R 2，R 3代表任选取代的二氮杂双环或氮杂三环基; 或（iv）R 1，R 2，R 3与氮原子一起代表任选取代的吡啶鎓，吡嗪鎓，吡唑鎓或哒嗪鎓基团，该基团任选地与一个苯环或与5-7元饱和或不饱和的 脂环族或杂环，或其具有高抗菌活性的药学上或兽医学上可接受的盐。

    Penem derivatives
    3.
    发明授权
    Penem derivatives 失效
    Penem衍生物

    公开(公告)号：US4713378A

    公开(公告)日：1987-12-15

    申请号：US747829

    申请日：1985-06-24

    申请人： Ettore Perrone ,  Marco Alpegiani ,  Franco Zarini ,  Costantino D. Bruna ,  Giovanni Franceschi

    发明人： Ettore Perrone ,  Marco Alpegiani ,  Franco Zarini ,  Costantino D. Bruna ,  Giovanni Franceschi

    IPC分类号： C07D513/04 ,  A61K31/425 ,  A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/04 ,  C07D499/06 ,  C07D499/88 ,  C07D499/897 ,  C07D519/00 ,  C07D519/06

    CPC分类号： C07D499/88

    摘要： There are provided compounds of formula ##STR1## wherein R is hydrogen atom or C.sub.1 -C.sub.3 alkyl group optionally substituted from halogen atom or hydroxy group optionally protected, and Q.sup.(+) represents a group ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are each either: (i) optionally substituted alkyl, aralkyl or aryl radical or(ii) R.sub.1 is as defined above under (i) and R.sub.2, R.sub.3, taken together, represent an optionally substituted or fused heterocyclic radical or(iii) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted azonia-bicyclo or tricyclo radical or(iv) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted fused pyridinium radical or(v) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted pyrazimium, pyrazolium or pyridazinium radical, and the pharmaceutically or veterinarily acceptable salts thereof.A method of preparation is also provided.The compounds show high antibacterial activity.

    摘要翻译： 提供式IMA的化合物，其中R是氢原子或任选被卤素原子或任选被保护的羟基取代的C 1 -C 3烷基，Q（+）代表基团，其中R 1，R 2和R 3各自是 （i）任选取代的烷基，芳烷基或芳基，或（ii）R 1如（i）中所定义，R 2，R 3一起表示任选取代或稠合的杂环基，或（iii）R 1，R 2， R 3一起代表任选取代的亚氮基 - 双环或三环基或（iv）R 1，R 2，R 3一起代表任选取代的稠合吡啶鎓基或（ⅴ）R 1，R 2，R 3一起代表 任选取代的吡嗪鎓，吡唑鎓或哒嗪基，以及其药学或兽医学上可接受的盐。 还提供了一种制备方法。 该化合物显示出高抗菌活性。

    Penem derivatives
    4.
    发明授权
    Penem derivatives 失效
    Penem衍生物

    公开(公告)号：US4886793A

    公开(公告)日：1989-12-12

    申请号：US022247

    申请日：1987-03-05

    申请人： Ettore Perrone ,  Marco Alpegiani ,  Angelo Bedeschi ,  Franco Zarini ,  Costantino Della Bruna ,  Giovanni Franceschi

    发明人： Ettore Perrone ,  Marco Alpegiani ,  Angelo Bedeschi ,  Franco Zarini ,  Costantino Della Bruna ,  Giovanni Franceschi

    IPC分类号： C07D237/00 ,  A61K31/43 ,  A61K31/431 ,  A61K31/435 ,  A61K31/495 ,  A61K31/50 ,  A61K31/505 ,  A61K31/53 ,  A61P31/04 ,  C07D499/04 ,  C07D499/06 ,  C07D499/861 ,  C07D499/88 ,  C07D499/897 ,  C07D519/00 ,  C07D519/06

    CPC分类号： C07D499/88

    摘要： There are provided compounds of formula I: ##STR1## wherein R.sup.1 is hydrogen or a C.sub.1 -C.sub.4 alkyl group either unsubstituted or substituted by one or more substituents chosen from a free or protected hydroxy or halogen atom;R.sup.2 is a free or esterified carboxy group or carboxylate anion;R.sup.3 and R.sup.4 are each independently hydrogen or organic group,X is --O--, ##STR2## --S--, Q is either(a") free or protected hydroxy, or(b") a C.sub.1 -C.sub.1 acyloxy, or(c") carbamoyloxy OCONH.sub.2, or(d") an optionally substituted heterocyclylthio group, or(e") an optionally substituted imido group, or(f") an optionally substituted quaternary ammonium group or(g") a halogen atom,A and the pharmaceutically or veterinarily acceptable salts thereof. There are provided also methods for preparing compounds of formula I. The compounds of formula I are useful as antibacterial agents.

    摘要翻译： 提供式I化合物：其中R 1是氢或未被取代或被一个或多个选自游离的或保护的羟基或卤原子的取代基取代的C 1 -C 4烷基; R2是游离或酯化的羧基或羧酸根阴离子; R 3和R 4各自独立地为氢或有机基团，X为-O-，Q为（a“）或保护的羟基，或（b”）a C1 -C 1酰氧基或（C“）氨基甲酰氧基OCONH 2，或（d”）任选取代的杂环硫基，或（e“）任选取代的亚氨基，或（f”）任选取代的季铵基团或 （g“）卤素原子，A及其药学上或兽医学上可接受的盐。 还提供了制备式I化合物的方法。式I化合物可用作抗菌剂。

    Process for penems
    8.
    发明授权
    Process for penems 失效
    青春期的过程

    公开(公告)号：US5416208A

    公开(公告)日：1995-05-16

    申请号：US199963

    申请日：1994-02-22

    申请人： Ettore Perrone ,  Marco Alpegiani ,  Franco Zarini ,  Giuseppe Mazzini ,  Giovanni Franceschi

    发明人： Ettore Perrone ,  Marco Alpegiani ,  Franco Zarini ,  Giuseppe Mazzini ,  Giovanni Franceschi

    IPC分类号： C07D317/40 ,  C07D499/88 ,  A61K31/425 ,  C07D499/00

    CPC分类号： C07D317/40 ,  C07D499/88 ,  Y02P20/55

    摘要： Antibacterial penems of formula (I), where R represents a hydrogen atom or a hydroxy protecting group, are prepared by reacting a .beta.-lactam of formula (II) with an oxalyl halide in an inert solvent in the presence of an organic or inorganic base or an acid scavenger to produce a compound of formula (III), wherein X is a halogen atom, treating the resultant compound of formula (III) with a 1,3-dioxolen-2-one of formula (IV), wherein Y is a hydroxy group, in the presence of molecular sieves or an organic or inorganic base to produce a compound of formula (V), and cyclizing the compound of formula (V) in the presence of a trialkylphosphite to provide the penems of formula (I).

    摘要翻译： 通过在有机或无机碱的存在下，在惰性溶剂中使式（II）的β-内酰胺与草酰卤反应来制备式（I）的抗菌青霉烯，其中R表示氢原子或羟基保护基 或酸清除剂，以制备其中X为卤素原子的式（III）化合物，用式（IV）的1,3-二氧戊环-2-酮处理所得的式（III）化合物，其中Y为 在分子筛或有机或无机碱存在下制备式（V）化合物的羟基，并且在亚烷基三烷基膦存在下使式（Ⅴ）化合物环化以提供式（I）的pen） 。