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    3-Oxo-6-oxa-2-azatricyclo 5.4.2. unadecene-4-carboxylate
    52.
    发明授权
    3-Oxo-6-oxa-2-azatricyclo 5.4.2. unadecene-4-carboxylate 失效
    3-氧代-6-氧杂-2-氮杂三环5.4.2。 十九碳烯-4-羧酸酯

    公开(公告)号：US4415584A

    公开(公告)日：1983-11-15

    申请号：US006436

    申请日：1979-01-25

    Applicant: Eric Hunt

    Inventor： Eric Hunt

    IPC: A61K31/42 ,  A61P31/04 ,  C07D503/00 ,  C07D498/04

    CPC classification number: C07D503/00

    Abstract: Compounds of the formula (II): ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms, CO.sub.2 R.sub.2 is a carboxyl group, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable esterified carboxyl group, are useful for their .beta.-lactamase inhibitory activity and to synergize the antibacterial activity of penicillins and cephalosporin.

    Abstract translation: 式（II）的化合物：其中R 1为氢或1至4个碳原子的烷基，CO 2 R 2为羧基，其药学上可接受的盐或药学上可接受的酯化羧基，可用于它们 β-内酰胺酶抑制活性，并协同青霉素和头孢菌素的抗菌活性。

    Methylaminodeoxy-clavulanic acid derivatives, their production and use
    55.
    发明授权
    Methylaminodeoxy-clavulanic acid derivatives, their production and use 失效
    甲基氨基脱氧 - 克拉维酸衍生物，其生产和使用

    公开(公告)号：US4303665A

    公开(公告)日：1981-12-01

    申请号：US79557

    申请日：1979-09-27

    Applicant: John B. Harbridge

    Inventor： John B. Harbridge

    IPC: C07D307/52 ,  C07D503/00 ,  C07D498/04 ,  A61K31/42

    CPC classification number: C07D503/00 ,  C07D307/52

    Abstract: Compounds of the formula (II): ##STR1## wherein X is sulphur or oxygen and R is hydrogen or alkyl of 1 to 3 carbon atoms, are useful for their antibacterial, .beta.-lactamase inhibitory activity and synergistic activity when combined with a penicillin or cephalosporin.

    Abstract translation: 式（II）化合物：其中X为硫或氧，R为氢或1至3个碳原子的烷基，可用于其抗菌，β-内酰胺酶抑制活性和协同活性，当与 青霉素或头孢菌素。

    Antibacterial agents
    58.
    发明授权
    Antibacterial agents 失效
    抗菌剂

    公开(公告)号：US4258050A

    公开(公告)日：1981-03-24

    申请号：US900541

    申请日：1978-04-27

    Applicant: John B. Harbridge

    Inventor： John B. Harbridge

    IPC: A61K31/42 ,  A61P31/04 ,  C07D503/00 ,  C07D498/04 ,  C07D413/06

    CPC classification number: C07D503/00

    Abstract: Compounds of the formula (II): ##STR1## wherein A is a group such that CO.sub.2 A is carboxylic acid, a non-toxic salt thereof or non-toxic ester thereof; R.sub.1 is COR.sub.4 or OR.sub.5 wherein R.sub.4 is lower alkyl, lower alkenyl, lower alkyl aryl or aryl and R.sub.5 is CO.sub.2 R.sub.6, COR.sub.6 or SO.sub.2 R.sub.6 wherein R.sub.6 is lower alkyl, lower alkenyl, lower alkyl aryl or aryl; and R.sub.2 is COR.sub.8 wherein R.sub.8 is lower alkyl, lower alkenyl, lower alkyl aryl or aryl; when R.sub.1 is COR.sub.4 and R.sub.2 is COR.sub.8, R.sub.4 and R.sub.8 are joined so that the N(COR.sub.4) COR.sub.8 moiety is a 5-,6-, or 7-membered heterocyclic ring or said ring to which is fused a phenyl ring unsubstituted or substituted by one or two lower alkyl, lower alkoxyl, fluorine or chlorine; when R.sub.1 is OR.sub.5 and R.sub.2 is COR.sub.8, R.sub.5 and R.sub.8 are joined so that the N(OR.sub.5) COR.sub.8 moiety is a 5-, 6-, or 7-membered heterocyclic ring, are useful for their antibacterial activity and as synergists for penicillins and cephalosporins.

    Abstract translation: 式（II）的化合物：其中A是使得CO 2 A是羧酸的基团，其无毒盐或其无毒酯; R1是COR4或OR5，其中R4是低级烷基，低级烯基，低级烷基芳基或芳基，R5是CO2R6，COR6或SO2R6，其中R6是低级烷基，低级烯基，低级烷基芳基或芳基; R2是COR8，其中R8是低级烷基，低级烯基，低级烷基芳基或芳基; 当R 1为COR 4且R 2为COR 8时，R 4和R 8连接，使得N（COR 4）COR 8部分为5-，6-或7-元杂环，或所述环与未被取代或取代的苯环稠合 一个或两个低级烷基，低级烷氧基，氟或氯; 当R 1为OR 5且R 2为COR 8时，R 5和R 8连接，使得N（OR 5）COR 8部分为5-，6-或7-元杂环，可用于其抗菌活性，并用作青霉素和 头孢菌素

    Clavulanic acid ethers
    59.
    发明授权
    Clavulanic acid ethers 失效
    克拉维酸醚

    公开(公告)号：US4228174A

    公开(公告)日：1980-10-14

    申请号：US8421

    申请日：1979-02-01

    Applicant: Roger J. Ponsford ,  Thomas T. Howarth

    Inventor： Roger J. Ponsford ,  Thomas T. Howarth

    IPC: A61K31/42 ,  A61P31/04 ,  C07D503/00 ,  C07D498/04

    CPC classification number: C07D503/00

    Abstract: The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R is an inert organic group of up to 18 carbon atoms and are able to inhibit the action of various bacterial .beta.-lactamases. Thus when a compound of the formula (II) or its salt or ester is used together with a penicillin or cephalosporin, the effectiveness of that penicillin or cephalosporin can be considerably enhanced. These novel synergysts can be prepared by etherification of an ester of clavulanic acid followed if desired by de-esterification. The novel synergysts also possess antibacterial activity.

    Abstract translation: 式（II）的化合物：其中R是具有至多18个碳原子的惰性有机基团并能够抑制各种细菌β-内酰胺酶的作用的盐和酯。 因此，当将式（II）化合物或其盐或酯与青霉素或头孢菌素一起使用时，可以显着提高该青霉素或头孢菌素的有效性。 如果需要，通过脱酯化可以通过使克拉维酸的酯化来制备这些新颖的增效剂。 新型增效剂也具有抗菌活性。

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