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    Carbapenem derivatives having antibiotic activity, their preparation and their use
    2.
    发明授权
    Carbapenem derivatives having antibiotic activity, their preparation and their use 失效
    具有抗生素活性的碳青霉烯类衍生物及其制备及其应用

    公开(公告)号：US5420119A

    公开(公告)日：1995-05-30

    申请号：US143996

    申请日：1993-10-27

    Applicant: Isao Kawamoto ,  Masao Miyauchi ,  Eiji Nakayama ,  Rokuro Endo ,  Satoshi Ohya ,  Yukio Utsui

    Inventor： Isao Kawamoto ,  Masao Miyauchi ,  Eiji Nakayama ,  Rokuro Endo ,  Satoshi Ohya ,  Yukio Utsui

    IPC: C07D487/04 ,  A61K31/40 ,  A61K31/435 ,  A61K31/44 ,  A61K31/495 ,  A61K31/55 ,  C07D477/00 ,  C07D477/10 ,  C07D477/12 ,  C07D477/20 ,  A01N43/00 ,  A61K31/395

    CPC classification number: C07D477/20

    Abstract: Carbapenem compounds of formula (I): ##STR1## [in which: A is a fully saturated heterocyclic group, of which at least one ring atom is nitrogen; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or a negative ion; Q is: (i) --B--N.sup.+ R.sup.8 R.sup.9 R.sup.10, where R.sup.8, R.sup.9 and R.sup.10 are alkenyl, alkynyl or optionally substituted alkyl, and B is alkylene or alkylidene; (ii) a heterocyclic group of which one ring atom is a >N.sup.+ R.sup.11 R.sup.12, where R.sup.11 and R.sup.12 are alkenyl, alkynyl or optionally substituted alkyl; (iii) alkyl substituted by a heterocyclic group as defined in (ii) above; or (iv) alkyl substituted by an aromatic heterocyclic group, of which one ring atom is ##STR2## or R.sup.2 and Q, and the nitrogen to which they are attached, form a group of formula (II): ##STR3## where m and n are 1, 2 or 3; R.sup.6 is optionally substituted alkyl; and R.sup.7 is alkenyl, alkynyl or optionally substituted alkyl] and pharmaceutically acceptable salts and esters thereof have valuable antibacterial activity with enhanced resistance to dehydropeptidase I and .beta.-lactamase. Methods of preparing and using the compounds are also provided.

    Abstract translation: （I）的碳青霉烯化合物：其中：A是完全饱和的杂环基团，其中至少一个环原子是氮; R1是氢或甲基; R2是氢或烷基; R3是氢或负离子; Q为：（i）-B-N + R8R9R10，其中R8，R9和R10为烯基，炔基或任选取代的烷基，B为亚烷基或亚烷基; （ii）一个环原子是> N + R11R12的杂环基，其中R11和R12是烯基，炔基或任选取代的烷基; （iii）被上述（ii）中定义的杂环基取代的烷基; 或（iv）被芳族杂环基取代的烷基，其中一个环原子是R 1和R 2和Q，并且与它们相连的氮形成式（II）的基团： 其中m和n为1,2或3; R6是任选取代的烷基; 并且R 7是烯基，炔基或任选取代的烷基]及其药学上可接受的盐和酯具有有利于抗脱水肽酶I和β-内酰胺酶的抗菌活性。 还提供了制备和使用化合物的方法。

    Antibacterial carbapenem compounds
    4.
    发明授权
    Antibacterial carbapenem compounds 失效
    抗菌碳青霉烯类化合物

    公开(公告)号：US4464299A

    公开(公告)日：1984-08-07

    申请号：US370260

    申请日：1982-04-20

    Applicant: Shoichiro Uyeo

    Inventor： Shoichiro Uyeo

    IPC: C07D405/04 ,  A61K31/395 ,  A61K31/397 ,  A61P17/00 ,  A61P31/00 ,  A61P31/04 ,  C07D205/08 ,  C07D477/00 ,  C07D477/10 ,  C07F7/08 ,  C07F9/535 ,  C07F9/54 ,  A61K31/40

    CPC classification number: C07D477/10 ,  C07D205/08

    Abstract: Antibacterial carbapenem compounds represented by the general formula ##STR1## wherein X is hydrogen or alkyl, A is hydrogen or alkyl, R is hydrogen or a monovalent substituent and COB is carboxy, its pharmaceutically acceptable ester or its alkali metal salt are prepared from the suitably substituted monocyclic 2-azetidinone by a Wittig cyclization or carbene-insertion cyclization to give Compounds(I) or by cleaving the dioxolane ring of above Compounds(I) with a strong base e.g. DEN or DBU to give above Compounds(II). Some other alterations of COB, R and side chain structure are also disclosed.

    Abstract translation: 其中X为氢或烷基，A为氢或烷基，R为氢或一价取代基，COB为羧基，其药学上可接受的酯或其碱金属盐为抗菌碳青霉烯类化合物 通过Wittig环化或卡宾插入环化由适当取代的单环2-氮杂环丁酮制备，得到化合物（I）或通过用强碱例如化合物（I）裂解上述化合物（I）的二氧戊环 DEN或DBU，得到上述化合物（II）。 还公开了COB，R和侧链结构的一些其它改变。

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