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51 条记录 (耗时 0.036 秒)

    Intermediate cefdinir salts
    22.
    发明授权
    Intermediate cefdinir salts 失效
    中间头孢地尼盐

    公开(公告)号：US07405294B2

    公开(公告)日：2008-07-29

    申请号：US10529649

    申请日：2003-09-26

    申请人： Giovanni Pozzi ,  Patricio Martin Gomez ,  Marco Alpegiani ,  Walter Cabri

    发明人： Giovanni Pozzi ,  Patricio Martin Gomez ,  Marco Alpegiani ,  Walter Cabri

    IPC分类号： C07D501/22 ,  C07D501/04

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： Disclosed are salts of the general formula (I) wherein R1, R2 and B are defined in the description. These salts are useful intermediates for the preparation of cefdinir. Also, disclosed are processes for the preparation thereof from the compounds of the general formula (II) and (III). Further, disclosed is a method of producing cefdinir from the salts of the general formula (I) including the steps of removing protecting groups.

    摘要翻译： 公开了通式（I）的盐，其中R 1，R 2和B在说明书中定义。 这些盐是制备头孢地尼的有用中间体。 还公开了由通式（II）和（III）的化合物制备方法。 此外，公开了从通式（I）的盐生产头孢地尼的方法，包括除去保护基的步骤。

    Penem derivatives
    24.
    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。

    Penem derivatives
    25.
    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。

    Matrix metalloproteinase inhibitors
    29.
    发明授权
    Matrix metalloproteinase inhibitors 失效
    基质金属蛋白酶抑制剂

    公开(公告)号：US06482827B1

    公开(公告)日：2002-11-19

    申请号：US09147798

    申请日：1999-03-10

    申请人： Marco Alpegiani ,  Pierluigi Bissolino ,  Francesca Abrate ,  Ettore Perrone ,  Riccardo Corigli ,  Daniela Jabes

    发明人： Marco Alpegiani ,  Pierluigi Bissolino ,  Francesca Abrate ,  Ettore Perrone ,  Riccardo Corigli ,  Daniela Jabes

    IPC分类号： A61K3116

    CPC分类号： C07D213/74 ,  C07B2200/07 ,  C07C259/06 ,  C07C2601/08 ,  C07C2601/14 ,  C07D233/32 ,  C07D295/185 ,  C07D317/68 ,  C07D405/12

    摘要： A compound, which is an amine derivative of formula (I) wherein W is —CNHOH or —COOH: R1 and R2 are each hydrogen or an organic residue, R3 is an organic group, Q is a secondary or tertiary acyclic or cyclic amido group, and the pharmaceutically acceptable salts, solvates and hydrates thereof, are inhibitors of matrix metalloproteinases (MMPs) and of the release of tumor necrosis factor-alpha (TNF) from cells. They are therefore useful in the prevention, control and treatment of diseases in which MMPs or TNF are involved, especially tumoral and inflammatory diseases. Processes for their preparation and pharmaceutical compositions containing them are also described.

    摘要翻译： 作为式（I）的胺衍生物的化合物，其中W为-CNHOH或-COOH：R 1和R 2各自为氢或有机残基，R 3为有机基团，Q为仲或叔无环或环状酰氨基 及其药学上可接受的盐，溶剂化物和水合物，是基质金属蛋白酶（MMPs）的抑制剂和从细胞释放肿瘤坏死因子-α（TNF）的抑制剂。 因此，它们可用于预防，控制和治疗涉及MMP或TNF的疾病，特别是肿瘤和炎性疾病。 还描述了其制备方法和含有它们的药物组合物。