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    Poly 4-aminopyrrole-2-carboxyamide derivatives, and pharmaceutical compositions which contain them
    2.
    发明授权
    Poly 4-aminopyrrole-2-carboxyamide derivatives, and pharmaceutical compositions which contain them 失效
    聚4-氨基吡咯-2-甲酰胺衍生物和含有它们的药物组合物

    公开(公告)号：US5472976A

    公开(公告)日：1995-12-05

    申请号：US109932

    申请日：1993-08-06

    申请人： Fabio Animati ,  Federico Arcamone ,  Giuseppe Giannini ,  Paolo Lombardi

    发明人： Fabio Animati ,  Federico Arcamone ,  Giuseppe Giannini ,  Paolo Lombardi

    IPC分类号： A61K31/40 ,  A61P31/12 ,  A61P35/00 ,  C07D207/34 ,  C07D207/30

    CPC分类号： C07D207/34

    摘要： This invention relates to polyaminopyrrolecarboxyamide derivatives of general formula (I) and their pharmaceutically acceptable salts, in which A represents a chemical bond or an aromatic or heteroaromatic radical, and:if A is a chemical bond, R is hydrogen, alkyl, dialkylaminoalkyl, alkenyl, cycloalkyl, arylalkyl, arylalkenyl, haloalkyl, or an aromatic or heteroaromatic radical;whereas if A is an aromatic or heteroaromatic radical, R is nitro, amino or formylamino;n is 0 or a whole number between 1 and 4;Z is an alkylene or aromatic radical. ##STR1##

    摘要翻译： 本发明涉及通式（I）的聚氨基吡咯酰胺酰胺衍生物及其药学上可接受的盐，其中A表示化学键或芳族或杂芳族基团，以及：如果A是化学键，则R是氢，烷基，二烷基氨基烷基，烯基 ，环烷基，芳基烷基，芳基烯基，卤代烷基或芳族或杂芳族基团; 而如果A是芳族或杂芳族基团，则R是硝基，氨基或甲酰氨基; n为0或1〜4之间的整数; Z是亚烷基或芳族基团。 （1）+ TR

    Total synthesis of 7-oxo-4-thia-1-azabicyclo-[3,2,0]-heptane-2-carboxyl derivatives useful as .beta.-lactamase inhibitors and antibacterial agents
    5.
    发明授权
    Total synthesis of 7-oxo-4-thia-1-azabicyclo-[3,2,0]-heptane-2-carboxyl derivatives useful as .beta.-lactamase inhibitors and antibacterial agents 失效
    可用作β-内酰胺酶抑制剂和抗菌剂的7-氧代-4-硫杂-1-氮杂双环[3,2,0] - 庚烷-2-羧基衍生物的全合成

    公开(公告)号：US4269771A

    公开(公告)日：1981-05-26

    申请号：US93603

    申请日：1979-11-13

    申请人： Paolo Lombardi ,  Giovanni Franceschi ,  Federico Arcamone

    发明人： Paolo Lombardi ,  Giovanni Franceschi ,  Federico Arcamone

    IPC分类号： C07D499/897 ,  A61K31/43 ,  A61P31/04 ,  C07D205/09 ,  C07D499/00 ,  C07D499/06 ,  C07D499/86 ,  C07D499/87 ,  C07D499/88 ,  C07F9/568

    CPC分类号： C07F9/5683 ,  C07C323/00 ,  C07D205/09 ,  C07D499/88

    摘要： A process is disclosed for the preparation of compounds of formula I: ##STR1## wherein R is hydrogen, lower alkyl, trichloroethyl, benzyl, p-nitrobenzyl, acetoxymethyl, pivaloyloxymethyl, phthalidyl, or a --CH(CH.sub.3)OCOOEt group;R.sup.1 is --CH.sub.2 OH, --CHO, --CH.sub.2 SH, --CH.sub.2 NH.sub.2, --CH.sub.2 OCOR.sup.2, --COOR.sup.2, --CH.sub.2 NHCOR.sup.2, --CH.sub.2 OR.sup.3, or --CH.sub.2 SR.sup.4 where R.sup.2 is a lower alkyl, aryl or a heterocyclic ring, R.sup.3 is a lower alkyl, benzyl, or trityl, and R.sup.4 is a five- or six-member heterocyclic ring containing one or more heteroatoms,which comprises reacting a 4-acetoxy azetidinone with a .beta.-thioketoester to form a mixture, reacting said mixture with thionyl chloride followed by reaction with a phosphine and a base, ozonolyzing and heating to obtain the compounds of formula I.

    摘要翻译： 公开了制备式I化合物的方法：其中R是氢，低级烷基，三氯乙基，苄基，对硝基苄基，乙酰氧基甲基，新戊酰氧基甲基，邻苯二甲酰基或-CH（CH 3）OCOOEt基团; R1是-CH2OH，-CHO，-CH2SH，-CH2NH2，-CH2OCOR2，-COOR2，-CH2NHCOR2，-CH2OR3或-CH2SR4，其中R2是低级烷基，芳基或杂环，R3是低级烷基，苄基， 或三苯甲基，R4是含有一个或多个杂原子的五元或六元杂环，其包括使4-乙酰氧基氮杂环丁酮与β-硫代酮反应形成混合物，使所述混合物与亚硫酰氯反应，然后与 膦和碱，进行臭氧分解和加热，得到式I化合物。